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views from the bench masthead

21/11/19

News on Vascepa

Vascepa is reported to reduce the build up of plaque in arteries, reducing cardiovascular risks.

https://www.fiercepharma.com/pharma/blockbuster-sight-amarin-s-vascepa-scores-unanimous-nod-from-fda-committee?mkt

https://www.fiercepharma.com/pharma/aha-amarin-s-vascepa-halts-progression-arterial-plaque-interim-imaging-data?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Icosapent-ethyl

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19/11/19

News on Cefiderocol

A new antibiotic for urinary tract infections, but comes with a warning.  Report can be found here:

https://www.fiercepharma.com/pharma/fda-approves-shionogi-s-antibiotic-fetroja-spooky-mortality-warning-label?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Cefiderocol

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13/11/19

News on Bardoxolone Methyl

Phase III clinical data of bardoxolone methyl, in chronic kidney disease, is discussed in the article below.

https://www.fiercebiotech.com/biotech/reata-s-kidney-med-bardoxolone-delivers-phase-3-teeing-up-fda-filing?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Bardoxolone_methyl

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12/11/19

News on Risdiplam

News of a phase III clinical trial of risdiplam, in spinal muscular atrophy, is reported.  Mode of action is reported as SMN2 splicing modifier.

https://www.fiercebiotech.com/biotech/roche-s-challenger-for-sma-market-hits-goal-phase-3?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Risdiplam

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11/11/19

News on Ninlaro (Ixazomib)

A boronic acid, proteasome inhibitor drug, used as maintenance therapy in multiple myeloma.

https://www.fiercepharma.com/pharma/takeda-scores-a-win-for-ninlaro-as-it-aims-to-pioneer-switch-maintenance-multiple-myeloma?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Ixazomib

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29/10/19

News on Gepotidacin

Outlines for phase III clinical studies on a next generation antibiotic – Gepotidacin is discussed.

https://www.fiercebiotech.com/biotech/glaxosmithkline-kickstarts-first-its-kind-late-stage-antibiotic-test?mkt

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Gepotidacin

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14/10/19

More news on Abrocitinib

Early readouts were blogged about earlier in the year. Here more detailed analysis is reported for Abrocitinib, a JAK1 inhibitor, in atopic dermatitis

https://www.fiercebiotech.com/biotech/pfizer-posts-detailed-phase-3-data-its-dupixent-rival?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/78323835

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17/9/19

News on Fosmanogepix

News of a phase II clinical study of anti-fungal fosmanogepix, is reported.

https://www.fiercebiotech.com/biotech/amplyx-boosts-pipeline-novartis-antiviral-unveils-phase-2-data-for-lead-antifungal?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Fosmanogepix

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11/9/19

News on BNP-14770

BNP-14770 is a phosphodiesterase‐4D inhibitor, under investigation in Alzheimer’s disease and fragile X syndrome, to protect patients from memory loss.

http://www.buffalo.edu/news/releases/2019/002/010.html

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/77461017

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10/9/19

News on Selpercatinib

Phase I / II clinical data is reported for Selpercatinib (LOXO-292) in non-small cell lung cancer.  The structure contains a bridged piperazine motif.  Mode of action is reported as inhibition of RET signalling.

https://www.fiercebiotech.com/biotech/lilly-s-ret-drug-nabbed-loxo-buyout-hits-68-orr-lung-cancer?mkt_

https://uk.reuters.com/article/us-lilly-cancer-lung/lillys-targeted-ret-drug-shrinks-tumors-in-lung-cancer-trial-idUKKCN1VU0L4

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Selpercatinib

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9/9/19

News on Capmatinib

Breakthrough FDA status given to Capmatinib, in MET exon14 skipping mutated non-small cell lung cancer.

https://endpts.com/novartis-late-stage-blockbuster-push-gets-major-boost-with-another-breakthrough-for-met-therapy/

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Capmatinib

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6/9/19

News on Vitrakvi (Larotrectinib)

A report on the need for genetic screening to identify which therapies will be beneficial to cancer patients, especially those whose cancers are from rare mutations e.g.1%.

https://uk.reuters.com/article/us-bayer-cancer-insight/inside-drugmakers-strategy-to-boost-cancer-medicines-with-lazarus-effect-idUKKCN1VR0EA

Structure can be found on this link:

https://en.wikipedia.org/wiki/Larotrectinib

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5/9/19

News on Neurodegenerative Diseases

New hypothesis gathering evidence, leading to new insights into 2 neurodegenerative diseases, Parkinson’s and Alzheimer’s

https://www.technologynetworks.com/neuroscience/news/parkinsons-disease-may-start-in-the-intestines-new-rat-study-conclude-323541?utm_

https://www.technologynetworks.com/proteomics/news/could-the-link-between-hunger-hormone-and-alzheimers-explain-clinical-trial-failure-323574?utm_

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29/8/19

News on Istradefylline

Istradefylline has been long approved in Japan for treating dyskinesia, a side effect of Parkinson’s disease therapies, the A2A antagonist is now approved by the FDA.

https://www.fiercepharma.com/pharma/spurned-by-fda-over-a-decade-ago-kyowa-kirin-nabs-nod-for-parkinson-s-drug?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Istradefylline

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28/8/19

News on CCR7 inhibition by Navarixin

Report on CXCR2 inhibitor Navarixin, a squaramide core structure, also inhibiting CCR7 receptor.

https://www.fiercebiotech.com/research/roche-s-search-for-cancer-metastasis-blockers-lends-unexpected-weight-to-merck-drug?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Navarixin

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23/8/19

News on Belantamab Mafodotin

Belantamab Mafodotin is an antibody-drug conjugate therapy, under investigation in multiple myeloma.  Belantamab refers to the antibody which recognises “B-cell maturation antigen” and Mafodotin is the tubulin inhibitor monomethyl auristatin F.

https://uk.reuters.com/article/us-gsk-study/gsk-builds-oncology-pipeline-as-drug-shown-to-help-myeloma-patients-idUKKCN1VD0M3

Structure of Mafodotin can be found on this link:

https://en.wikipedia.org/wiki/Monomethyl_auristatin_F

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22/8/19

News on AZD1775

Phase I clinical readout of AZD1775, a WEE inhibitor, is described in this report in pancreatic cancer.

https://www.fiercebiotech.com/research/astrazeneca-drug-heads-to-phase-2-pancreatic-cancer-after-small-trial-extends-survival?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/mk-1775

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21/8/19

News on Lefamulin

A new antibiotic to treat bacterial pneumonia is reported

https://www.fiercepharma.com/marketing/nabriva-scores-fda-nod-for-novel-antibiotic-to-treat-bacterial-pneumonia?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Lefamulin

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20/8/19

News on Farxiga (Dapagliflozin)

News on sodium-glucose transport protein 2 (SGLT2) Inhibitor, Farxiga, in a clinical study of heart failure.

https://uk.reuters.com/article/uk-astrazeneca-farxiga-trial/astrazeneca-diabetes-drug-shows-promise-in-heart-failure-idUKKCN1VA0JP

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Dapagliflozin

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19/8/19

News on Inrebic (Fedratinib)

JAK inhibitor, Inrebic, gets the nod from the FDA for myelofibrosis.  Reading around, it has had a long and complex journey to the clinic.

https://www.fiercepharma.com/pharma/once-left-for-dead-celgene-s-jak-inhibitor-inrebic-scores-fda-nod-eve-takeover?mkt

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Fedratinib

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16/8/19

News on Rozlytrek (Entrectinib)

Rozlytrek is a selective tyrosine kinase inhibitor, which has been approved for use in any tumour where a specific mutation has occurred.

https://uk.reuters.com/article/us-roche-hldg-fda/roches-personalized-cancer-treatment-wins-fda-approval-idUKKCN1V52AW

Structure can be found on this link:

https://en.wikipedia.org/wiki/Entrectinib

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8/8/19

News on Lynparza in Prostate Cancer

Early in 2019, I blogged on news of Lynparza in pancreatic cancer.  Here is some preliminary reporting of a phase III clinical study in prostate cancer.  This demonstrates the need to ascertain which genes are altered, in any cancer and treat with a therapy for that mutation.

https://www.icr.ac.uk/news-archive/positive-clinical-trial-results-for-olaparib-in-advanced-prostate-cancer

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Olaparib#section=Top

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5/8/19

News on AMG510

Early clinical data is reported for AMG510, a KRAS inhibitor, across many cancer types.  The structure representation in the link below suggests the compound may be an atropisomer or just the active conformation.

https://www.fiercebiotech.com/biotech/amgen-s-kras-drug-hits-mark-2-additional-cancers-colorectal-and-appendiceal?mkt_

https://en.wikipedia.org/wiki/KRAS

Structure can be found on this link:

https://cen.acs.org/pharmaceuticals/drug-discovery/Amgen-unveils-KRas-inhibitor-human/97/i14

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1/8/19

News on Darolutamide

FDA approval for Darolutamide in prostate cancer is reported.  Mode of action appears to be by inhibition of the androgen receptor.

https://uk.reuters.com/article/us-bayer-orion-usa/orion-bayer-prostate-cancer-drug-gets-fda-approval-idUKKCN1UQ0OM

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Darolutamide

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30/7/19

News on Ponesimod

News of a clinical phase III trial readout of Ponesimod, a sphingosine-1-phosphate receptor, in multiple sclerosis is reported.

https://www.fiercebiotech.com/biotech/j-j-s-multiple-sclerosis-prospect-beats-sanofi-drug-phase-3?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Ponesimod

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26/6/19
News on Zejula

It is reported here that the PARP inhibitor Niraparib (trade name Zejula) is being reviewed by the FDA , as 4th line therapy for advanced ovarian, fallopian tube or primary peritoneal cancers.

https://www.fiercepharma.com/pharma/gsk-wins-fda-priority-review-for-zejula-late-stage-ovarian-cancer?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Niraparib

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18/6/19
News on the Halichondrins

This is a remarkable story of synthetic chemistry endeavour, resulting in a significant quantity of C52-halichondrin-B amine (E7130) synthesised, to enable a phase I clinical investigation to be carried out.

https://www.technologynetworks.com/drug-discovery/news/chemists-breakthrough-in-synthesis-drives-development-of-anti-cancer-agent-320742?utm_

Structures can be found on this link to the original paper which is open access:

https://www.nature.com/articles/s41598-019-45001-9

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7/6/19
News on Acalabrutinib

A late stage trial for Acalabrutinib in chronic lymphocytic leukaemia is outlined in this article.

https://uk.reuters.com/article/us-astrazeneca-cancer/astrazenecas-blood-cancer-drug-meets-main-goal-in-late-stage-trial-idUKKCN1T710V

Structure can be found on this link:

https://en.wikipedia.org/wiki/Acalabrutinib

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6/6/19
Drug Metabolism by Gut Bacteria

This article and original Nature paper, makes complete sense and surprises me that these observations have not been more widely reported before. The topic brings to the fore many questions for the medicinal chemist,  even in early stage DMPK assessments and ultimately the patient.  E.g. As to whether the gut metabolites are already accounted for, by maximum absorbed dose.  E.g. Clinical trial participants will all have different gut bacterial populations.

https://www.technologynetworks.com/drug-discovery/news/your-gut-bacteria-may-determine-how-well-you-respond-to-drugs-320199?utm_

https://www.nature.com/articles/s41586-019-1291-3

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17/5/19
News on Abrocitinib

Top line read out of a phase III clinical study, in atopic dermatitis has been announced.  A small molecule inhibitor of Janus kinase 1 (JAK1), almost fragment like in MW terms.

https://www.pfizer.com/news/press-release/press-release-detail/pfizer_announces_positive_top_line_results_from_phase_3_study_of_investigational_oral_jak1_candidate_abrocitinib_pf_04965842_in_patients_aged_12_and_older_with_moderate_to_severe_atopic_dermatitis

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/78323835

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16/5/19
News on combo Venclexta plus Gazyva

Gazyva (Obinutuzumab) is an antibody and Venclexta is a small molecule to treat chronic lymphocytic leukaemia.  Venclexta is not that small at molecular weight 868 and the molecule contains a nitro functionality, which are often avoided in current medchem.

https://uk.reuters.com/article/us-roche-hldg-venclexta/roche-fda-approves-drug-combo-venclexta-plus-gazyva-for-previously-untreated-chronic-lymphocytic-leukemia-idUKKCN1SM0EG

Structure can be found on this link:

https://en.wikipedia.org/wiki/Venetoclax

https://en.wikipedia.org/wiki/Obinutuzumab

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15/5/19
News on Relugolix

Phase III clinical data of Relugolix in uterine fibroids is discussed in this article.  As an oral drug, with a molecular weight of 623 is comment able, as we come to the 20 years since Lipinski guidelines on oral drugs were first published.  But they are just guidelines and not hard cut-offs as some have interpreted over those years.

https://www.fiercebiotech.com/biotech/myovant-hits-goal-uterine-fibroid-phase-3-teeing-up-abbvie-showdown?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Relugolix

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24/4/19
News on Elafibranor

Elafibranor is a dual PPARα/δ agonist under investigation for the autoimmune disease primary biliary cholangitis.  News of FDA breakthrough status as it looks to start phase III trials.

https://www.fiercebiotech.com/biotech/genfit-bags-fda-breakthrough-tag-route-to-phase-3-pbc?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Elafibranor

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16/4/19
News on Balversa (Erdafitinib)

FDA approval for Erdafitinib in metastatic bladder cancer patients whose tumours have mutations FGFR3 or FGFR2.

https://www.fiercepharma.com/pharma/j-j-s-balversa-wins-quick-blockbuster-nod-as-first-targeted-therapy-for-bladder-cancer?mkt

Structure can be found on this link:

https://en.wikipedia.org/wiki/Erdafitinib

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5/4/19
News on Umbralisib

Phase IIb clinical readout is reported for Umbralisib, in marginal zone lymphoma.

https://www.fiercebiotech.com/biotech/aacr-tg-therapeutics-umbralisib-shrinks-tumors-52-lymphoma-patients?mkt

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/tgr-1202#section=Top

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4/4/19
News on Rubraca

Early phase II data in pancreatic cancer, is reported for Rubraca.

https://www.fiercepharma.com/pharma/aacr-clovis-follows-lynparza-s-big-pancreatic-cancer-win-phase-2-rubraca-response-data?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/rucaparib#section=Top

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3/4/19
News on Xospata (Gilteritinib)

Phase III clinical readout of Xospata in acute myeloid leukaemia, is reported.

https://www.fiercepharma.com/pharma/astellas-pads-xospata-lead-positive-aml-survival-data?mkt

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/76970819#section=Top

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2/4/19
News on Mavenclad (Cladribine)

It has taken 10 years of safety data but now the FDA has approved Mavenclad, in multiple sclerosis (MS).

https://www.fiercepharma.com/pharma/better-8-years-late-than-never-merck-kgaa-nabs-fda-nod-for-ms-drug-mavenclad?mkt

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/20279

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27/3/19
News on Mayzent (Siponimod)

Mayzent (Siponimod) has been approved by the FDA to treat relapsing multiple sclerosis. The drug contains the functional group of an O-alkyl oxime, which is unusual.

https://uk.reuters.com/article/us-fda-mayzent/novartis-gets-u-s-approval-for-new-drug-to-treat-multiple-sclerosis-idUKKCN1R8019

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/44599207#section=Top

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21/3/19
Parkinson’s Biomarkers

I recall this story from its origins. Now after 3 years, the biomarkers have been identified and results published. Now to understand what causes the biomarkers to be made and the linkage to the disease.

https://www.bbc.co.uk/news/uk-scotland-47627179

Pertinent structures can be found on these links:

https://pubchem.ncbi.nlm.nih.gov/compound/Hippuric_acid

https://pubchem.ncbi.nlm.nih.gov/compound/eicosane#section=UNII

https://pubchem.ncbi.nlm.nih.gov/compound/12533

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19/3/19
News on Eliquis

Eliquis (Apixaban) is an anticoagulant, under investigation in clinical phase IV trial, in atrial fibrillation patients.

https://www.fiercepharma.com/pharma/acc-bms-pfizer-s-eliquis-tops-warfarin-high-risk-afib-subgroup?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Apixaban

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18/3/19
News on Bempedoic Acid

A phase III clinical study readout is reported, for bempedoic acid to treat high cholesterol.

https://www.bbc.co.uk/news/health-47543985

Structure can be found on this link:

https://en.wikipedia.org/wiki/Bempedoic_acid#cite_note-2

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13/3/19
News on NBI-74788

Interim results of a phase II clinical study of NBI-74788, in congenital adrenal hyperplasia, are presented.

https://www.fiercebiotech.com/biotech/positive-phase-2-neurocrine-eyes-pivotal-trial-for-rare-disease-drug?mkt

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/nbi-42902#section=Top

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4/3/19
News on Fevipiprant

Fevipiprant is an orally administered antagonist of the DP2 or CRTh2 receptor, under investigation in asthma.

https://news.sky.com/story/new-asthma-pill-shows-promise-after-clinical-trials-by-leicester-scientists-11637136?fbclid=IwAR1TP6da-RHnfLn10LEcJiV88MaN5GJRTYCEoQ23sq0gyNuC0I68DlsaDNY

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Fevipiprant#section=Top

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1/3/19
News on Lynparza in Pancreatic Cancer

Lynparza is a PARP inhibitor already approved to treat a number of cancers. Here is a report of a study in hard to treat pancreatic cancer.

https://www.fiercepharma.com/pharma/astrazeneca-merck-s-lynparza-posts-pancreatic-cancer-win-another-parp-class-first?mkt_

https://uk.reuters.com/article/uk-astrazeneca-lynparza/astrazenecas-lynparza-meets-main-goal-in-late-stage-pancreatic-cancer-study-idUKKCN1QF0UM

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Olaparib#section=Top

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28/2/19
News on Dasatinib (Sprycel) co-admin with Anti-PD-1/L1 Therapy

This is only a preclinical report, but co-administration giving a jump in response from 10% to 90% is impressive across a range of tumours.

https://www.fiercebiotech.com/research/using-bristol-myers-popular-leukemia-drug-to-improve-anti-pd-1-cancer-immunotherapy?mkt

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Dasatinib#section=Top

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27/2/19
Insight into Diabetes using Venclexta

Preclinical report on Venclexta, in diabetic mouse model, targeting senescence beta cells.

https://www.fiercebiotech.com/biotech/abbvie-s-cancer-drug-venclexta-blocks-diabetes-mice-by-targeting-beta-cell-senescence?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/abt-199#section=Top

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22/2/19
News on Obeticholic Acid

Positive late stage clinical trial data is reported in liver fibrosis, with obeticholic acid.

https://uk.reuters.com/article/us-intercept-study/intercepts-drug-for-patients-with-liver-fibrosis-due-to-nash-meets-main-goal-idUKKCN1Q81F5

Structure can be found on this link:

https://en.wikipedia.org/wiki/Obeticholic_acid

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21/2/19
News on Darolutamide

Darolutamide is under investigation in prostate cancer, news here on phase III clinical trials.

https://uk.reuters.com/article/us-bayer-orion-prostate-cancer/bayer-stresses-drugs-tolerability-in-bid-for-prostate-cancer-market-idUKKCN1Q32YV

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/odm-201

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19/2/19
News on Keytruda/Inlyta combination

Combinations seem to be the way to go in treating cancer. Here the Keytruda/Inlyta combination, in kidney cancer is reported. Keytruda is an antibody and Inlyta a small molecule.

https://uk.reuters.com/article/us-cancer-merck-co-kidney/merck-pfizer-drug-combo-extends-kidney-cancer-survival-study-idUKKCN1Q50QH

Structure of Inlyta(Axitinib) can be found on this link:

https://en.wikipedia.org/wiki/Axitinib

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21/1/19
News on Zynquista

FDA advisory panel split opinion on Zynquista (sotagliflozin), a dual inhibitor of both SGLT1 and SGLT2.

https://www.fiercepharma.com/pharma/fda-panel-split-sanofi-s-type-1-diabetes-candidate-zynquista?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/lx-4211#section=Top

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16/1/19
News on Tomivosertib (eFT508)

News of a phase II clinical study showing eFT508 works by reducing levels of PD-L1 in liver cancers with specific mutations, leading to slower tumour growth.

https://www.eurekalert.org/pub_releases/2019-01/uoc–dhd010919.php

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/118598754#section=Top

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2/1/19
News on Roxadustat

Roxadustat improves haemoglobin count in anaemic patients undergoing dialysis.

https://uk.reuters.com/article/uk-astrazeneca-trials/astrazenecas-ovarian-cancer-and-anaemia-treatments-meet-goals-in-late-stage-studies-idUKKCN1OJ0QN

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/fg-4592#section=Top

28/12/18
News on Selatogrel

Anti-blood clotting drug Selatogrel, P2Y12 receptor antagonist, has reported top line of 2 phase II clinical trials.

https://www.fiercebiotech.com/biotech/idorsia-s-selatogrel-hits-goals-phase-2-cardiovascular-trials?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/59534142#section=Top

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21/12/18
News on LX9211

News of a phase I clinical trial of LX9211, an AAK1 inhibitor.

https://www.fiercebiotech.com/biotech/lexicon-pain-drug-advances-after-clearing-early-clinical-test?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/507806#section=Top

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18/12/18
News on Tackling Malaria

An open access paper on research to tackling the malarial parasite, in the early stages in the liver. There are some interesting chemical structures too, in the publication.

http://science.sciencemag.org/content/362/6419/eaat9446

I wish all my readers a Merry Christmas

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28/11/18
News on Vitrakvi (larotrectinib)

Building on a blog from the middle of the year. Vitrakvi (larotrectinib) is now approved by FDA as a “tissue agnostic” therapy. Nice to see this move to cancer therapy targeting mutations making it to drugs.

https://www.fiercepharma.com/pharma/tissue-agnostic-cancer-drug-from-bayer-loxo-comes-high-price?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/LOXO-101_sulfate

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23/11/18
News on Daurismo (Glasdegib)

Glasdegib has been approved for use in adults who are 75 years of age or older for- acute myeloid leukemia (AML). The approval though does come with a Boxed Warning about the risk of embryo-foetal death or severe birth defects.

https://uk.reuters.com/article/us-pfizer-fda/fda-approves-new-blood-cancer-treatment-from-pfizer-idUKKCN1NQ2B9

https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm626443.htm

Structure can be found on this link:

https://en.wikipedia.org/wiki/Glasdegib

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19/11/18
News on Fexinidazole

A new treatment for sleeping sickness. A small molecule with functionality that is currently in vogue in medicines, usually!

https://www.telegraph.co.uk/news/0/new-drug-developed-uk-backing-will-revolutionise-treatment-deadly/

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Fexinidazole#section=Top

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15/11/18
News on Lasmiditan

Lasmiditan, a 5-HT1F agonist to treat migraine, from Lilly has been filed with the FDA and awaits approval decision.

https://www.fiercebiotech.com/biotech/lilly-files-for-fda-approval-migraine-drug-lasmiditan?mkt

Structure can be found on this link:

https://en.wikipedia.org/wiki/Lasmiditan

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6/11/18
News on LORBRENA (lorlatinib)

FDA has approved this new anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI), for ALK-positive metastatic non-small cell lung cancer (NSCLC).

https://www.fiercepharma.com/pharma/pfizer-snags-ok-for-xalkori-follow-up-lorbrena-its-third-cancer-approval-two-months?mkt_

https://www.businesswire.com/news/home/20181102005583/en/U.S.-FDA-Approves-LORBRENA%C2%AE-lorlatinib-Previously-Treated-ALK-Positive

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/pf-06463922#section=Top

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1/11/18
News on Upadacitinib

Phase III results of JAK inhibitor Upadacitinib are discussed in the article below.

https://uk.reuters.com/article/us-abbvie-trial/abbvie-rheumatoid-arthritis-drug-succeeds-in-late-stage-trial-idUKKCN1MX22B

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Upadacitinib#section=Top

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30/10/18
News on Cefiderocol

An antibiotic which uses bacterial active transport to get into the bacterium.

https://www.bbc.co.uk/news/health-45983320

Structure can be found on this link:

https://en.wikipedia.org/wiki/Cefiderocol

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17/10/18
News on Talazoparib

Talazoparib a new PARP inhibitor for a specific BRCA gene mutation in breast cancer has been approved by the FDA.

https://uk.reuters.com/article/us-pfizer-fda/fda-approves-pfizers-drug-for-advanced-breast-cancer-idUKKCN1MQ2AU

Structure can be found on this link:

https://en.wikipedia.org/wiki/Talazoparib

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9/10/18
News on Baloxavir Marboxil

With winter flu season approaching, this report on a phase III clinical trial is interesting, the chemical structure more so!

https://uk.reuters.com/article/us-roche-flu/flu-drug-speeds-relief-from-symptoms-in-at-risk-patients-roche-idUKKCN1ME0CM

Structure can be found on this link:

https://en.wikipedia.org/wiki/Baloxavir_marboxil

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8/10/18
News on 2 new antibiotics

2 New tetracycline antibiotics getting the go ahead by the FDA.

https://www.fiercepharma.com/marketing/2-paratek-antibiotics-win-fda-nods-one-slated-for-500m-peak-sales?mkt_

Structures can be found on these links:

https://en.wikipedia.org/wiki/Omadacycline

https://en.wikipedia.org/wiki/Sarecycline

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5/10/18
Placebo Effect

The episode is only available to watch for October 2018 in the UK. As a medicinal chemist and someone who has taken part in clinical trials this was an interesting watch.

https://www.bbc.co.uk/programmes/b0bmblb8

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4/10/18
2018 Nobel Prize for Chemistry

Scientists Frances Arnold, George Smith and Gregory Winter won the 2018 Nobel Prize for Chemistry for research using directed evolution to produce enzymes and antibodies.

https://uk.reuters.com/article/uk-nobel-prize-chemistry/briton-and-two-americans-win-2018-nobel-chemistry-prize-idUKKCN1MD10Y

https://www.theguardian.com/science/2018/oct/03/frances-h-arnold-george-p-smith-and-gregory-p-winter-win-nobel-prize-in-chemistry

An understanding of directed evolution can be found here:

https://en.wikipedia.org/wiki/Directed_evolution

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3/10/18
News on Dacomitinib

Dacomitinib, an irreversible inhibitor of EGFR has gained FDA approval for non-small-cell lung carcinoma (NSCLC).

https://uk.reuters.com/article/us-pfizer-fda/pfizers-lung-cancer-drug-gets-fda-approval-idUKKCN1M72UW

Structure can be found on this link:

https://en.wikipedia.org/wiki/Dacomitinib

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1/10/18
News on Bardoxolone

A phase II trial readout of Bardoxolone in chronic kidney disease, shows improvements in kidney function, as indicated by estimated glomerular filtration rate.

https://www.fiercebiotech.com/biotech/reata-s-bardoxolone-hits-goals-phase-2-kidney-disease-trial?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Bardoxolone#section=Top

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28/9/18
News on Olorinab

A positive proof of concept clinical trial of Olorinab, reduces pain in Crohn’s patients.

https://www.fiercebiotech.com/biotech/arena-three-for-three-as-crohn-s-drug-meets-proof-concept-test?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/60164925#section=Top

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27/9/18
Bridged 6-membered Heterocycles & logD7.4

Medicinal chemist Derek Lowe in his blog discusses this paper https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b01148 How a methylene bridge reduces logD7.4.

This is counter intuitive when you consider adding a methyl usually adds 0.5 unit to the logD/P. Importantly logP/D prediction tools, cited in the paper, do get this observation correct.

http://blogs.sciencemag.org/pipeline/archives/2018/09/26/simple-rings-simply-wrong

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26/9/18
News on Copiktra

Copiktra, also known as Duvelisib, a dual inhibitor of PI3K-delta and PI3k-gamma has FDA approval for lymphoma.

https://www.fiercepharma.com/pharma/once-troubled-verastem-wins-fda-nod-for-abbvie-abandoned-lymphoma-drug-copiktra?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Duvelisib

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21/9/18
News on MGB-BP-3

A new antibiotic against Clostridium difficile, to commence Phase II clinical investigations.

https://www.bbc.co.uk/news/uk-scotland-scotland-business-45508036

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/23730143#section=Top

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20/9/18
News on Fasudil in Alzheimer’s

This is early research using a known drug substance in in vitro experiments. However, it shines a light on an area of research that has been well trodden without success.

https://www.independent.co.uk/news/health/alzheimers-disease-drugs-treatment-beta-amyloid-fasudil-dementia-a8545591.html

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Fasudil#section=Top

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19/9/18
News on G0775

This is a preclinical report on new broad-spectrum antibiotic, with possibly a novel mode of action.

https://www.fiercebiotech.com/research/genentech-antibiotic-shows-broad-activity-against-multidrug-resistant-bugs-mice?mkt_

Structure can be found within this article:

https://cen.acs.org/pharmaceuticals/antibiotics/Aryl-compound-attacks-Gram-negative/96/i37

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18/9/18
News on VK2809

Phase II study readout news, on VK2809, in non-alcoholic fatty liver disease (NAFLD).

https://uk.reuters.com/article/us-viking-study/viking-shares-soar-as-liver-disease-drug-succeeds-in-mid-stage-study-idUKKCN1LY1PM

Structure can be found on this link to a corporate pdf slide 8:

PDF slide 8

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14/9/18
News on Filgotinib

A positive phase III clinical readout of JAK1 inhibitor, filgotinib, in rheumatoid arthritis is reported.

https://www.fiercebiotech.com/biotech/gilead-galapagos-filgotinib-aces-first-phase-3-suggesting-it-can-compete-abbvie-s?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Filgotinib

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5/9/18
News on Fruquintinib

An oral VEGF inhibitor Fruquintinib, discovered and approved in China, for colorectal cancer.

https://uk.reuters.com/article/us-chi-med-cancer-china/boost-for-made-in-china-medicine-as-chi-med-wins-key-approval-idUKKCN1LL0NA

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Fruquintinib#section=Top

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4/9/18
News on ABX464

Positive observations on ABX464 in a phase IIa clinical study in ulcerative colitis.

https://www.fiercebiotech.com/biotech/abivax-posts-ulcerative-colitis-data-commits-to-phase-2b?mkt_

Structure can be found on this link:

https://aidsinfo.nih.gov/drugs/587/abx464/0/professional

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31/8/18
News on Doravirine

Doravirine has been approved by the FDA for treatment of HIV patients, as a standalone or fixed dose combination.

https://uk.reuters.com/article/us-merck-co-fda/fda-approves-two-new-hiv-drugs-from-merck-idUKKCN1LF2IL

https://www.businesswire.com/news/home/20180830005793/en/FDA-Approves-Merck%E2%80%99s-DELSTRIGO%E2%84%A2-doravirine-lamivudine-tenofovir

Structure can be found on this link:

https://en.wikipedia.org/wiki/Doravirine

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6/8/18
News on Acebilustat

News on a phase II clinical study of leukotriene A4 hydrolase inhibitor, acebilustat, in cystic fibrosis.

https://www.fiercebiotech.com/biotech/celtaxsys-cystic-fibrosis-drug-reduces-lung-exacerbations-phase-2-study?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Acebilustat#section=Top

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3/8/18
News on Azedra

A chemically simple, radioactive drug to treat pheochromocytoma or paraganglioma.

https://uk.reuters.com/article/us-progenics-pharm-fda/fda-approves-progenics-treatment-for-rare-adrenal-gland-tumors-idUKKBN1KK2C2

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/substance/12013292#section=Top

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2/8/18
Smallpox

A disease thought extinct has a new treatment, in case of bioterrorism or a natural resurrection.

https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm613496.htm

Structure can be found on this link:

https://en.wikipedia.org/wiki/Tecovirimat

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1/8/18
News on Ivosidenib (Tibsovo)

Tibsovo is approved to treat relapsed / refractory acute myeloid leukaemia patients with a particular genetic mutation.

https://www.fiercepharma.com/pharma/agios-wins-fda-nod-for-targeted-aml-drug-tibsovo?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Ivosidenib#section=Top

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31/7/18
News on Tafenoquine

A single dose treatment to treat recurring malaria, caused by the parasite plasmodium vivax.

https://bbc.in/2JKp88Y

Structure can be found on this link:

https://en.wikipedia.org/wiki/Tafenoquine

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30/7/18
News on Xtandi and Erleada

Both drugs now approved for nonmetastatic prostate cancer. From a medchem perspective it is interesting to see only 2 minor changes between the chemical structures.

https://www.fiercepharma.com/marketing/pfizer-and-astellas-xtandi-ready-to-vie-j-j-nonmetastatic-prostate-cancer?mkt_

Structures can be found on these links:

https://en.wikipedia.org/wiki/Enzalutamide

https://en.wikipedia.org/wiki/Apalutamide

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4/7/18
News on Metformin

Metformin is an established diabetes therapy and a very small molecule. Here are reports of lab research (preclinical) on its effects in idiopathic pulmonary fibrosis (IPF).

https://www.fiercebiotech.com/research/old-diabetes-drug-metformin-may-find-yet-another-role-reversing-lung-fibrosis?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/metformin#section=Top

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3/7/18
News on Luspatercept

Phase III clinical data of Luspatercept is discussed in this article.

https://www.fiercebiotech.com/acceleron-s-rare-blood-disease-drug-flies-high-phase-3?mkt_

https://en.wikipedia.org/wiki/Luspatercept

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2/7/18
News on Gemcabene

Probably a phase IIb readout of Gembacene, quite a simple looking molecule.

https://www.fiercebiotech.com/gemphire-sparkles-third-trial-win-for-lead-drug-gemcabene?mkt

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Gemcabene#section=Top

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19/6/18
Cannabis Oil

In the UK there has been a lot of coverage at present over treating epileptic patients with cluster seizures with cannabis oil – brought in from elsewhere in the world. Currently due to presence of 9-tetrahydrocannabinol(THC), this is banned in the UK and classed as a schedule 1 controlled drug. The European Medicines Agency does have a cannabis oil medicine approved, Sativex, for Multiple sclerosis use only.

https://www.bbc.co.uk/news/uk-44519058

This is a useful document in understanding the whole area.

www.emcdda.europa.eu/system/files/publications/4135/TD0217210ENN.pdf

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14/6/18
News on Baricitinib

News on a clinical trial of baricitinib, dual JAK1/2 inhibitor,, in lupus.

https://uk.reuters.com/article/us-lilly-study/lillys-lupus-treatment-succeeds-in-mid-stage-trial-idUKKBN1J92MD

Structure can be found on this link:

https://en.wikipedia.org/wiki/Baricitinib

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13/6/18
News on Lanabecestat

Trials of lanabecestat are halted as experts stated “destined to fail”. Is this the end for the beta amyloid hypothesis in Alzheimer’s Disease, as so many BACE inhibitors have failed in the clinic.

https://www.fiercebiotech.com/biotech/lilly-astrazeneca-halt-phase-3-alzheimer-s-trials-for-futility-further-denting-bace?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Lanabecestat

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8/6/18
News on Lemborexant

Reports on Leborexant, a dual orexin antagonist, in phase I & III clinical trials, in sleep disorders.

https://www.fiercebiotech.com/biotech/eisai-purdue-reveal-eye-opening-data-for-sleep-drug-lemborexant?mkt

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Lemborexant#section=Top

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7/6/18
News on Elenbecestat

News on BACE inhibitor Elenbecestat, in phase II clinical trial.

https://www.fiercebiotech.com/biotech/eisai-biogen-s-bace-drug-lowers-amyloid-levels-but-not-alzheimer-s-symptoms?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/57827330#section=Top

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6/6/18
News on a Vaccine for Glioblastoma

A patient’s dendritic cells are primed and stimulated, ex vivo with their tumour cells and then reintroduced back to the patient.

http://www.bbc.co.uk/news/health-44288503

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5/6/18
News on Filgotinib

Phase II readout of filgotinib in psoriatic arthritis is reported here.

https://www.fiercebiotech.com/biotech/gilead-galapagos-hit-goal-psoriatic-arthritis-phase-2?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Filgotinib

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4/6/18
News on Larotrectinib

Priority review granted for Larotrectinib, under investigation for a rare gene mutation and present in a number of tumours.

https://uk.reuters.com/article/us-loxo-oncology-cancer/loxo-bayer-cancer-drug-gets-priority-review-from-fda-idUKKCN1IU1C6

Structure can be found on this link:

https://en.wikipedia.org/wiki/Larotrectinib

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24/5/18
News on Bempedoic Acid

Readout on a 3rd phase III clinical trial for bempedoic acid in lowering LDL cholesterol. A simple dicarboxylic acid molecule.

https://www.fiercebiotech.com/biotech/esperion-s-ldl-med-aces-a-third-pivotal-trial?mkt

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/etc-1002#section=Top

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23/5/18
News on Lefamulin

Reports of a second positive phase III clinical study of oral antibiotic Lefamulin.

https://www.fiercebiotech.com/biotech/nabriva-lines-up-fda-filing-after-antibiotic-clears-second-pivotal-test?mkt

Structure can be found on this link:

https://en.wikipedia.org/wiki/Lefamulin

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22/5/18
The Doctor who gave up Drugs

An interesting 2nd series for those of us in pharmaceutical research “The Doctor who gave up drugs”. As scientists we observe and interpret and look to cure / improve ailments and conditions.

https://www.bbc.co.uk/programmes/b0b4nxwt

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18/5/18
News on Aimovig

An antibody drug, delivered by injection to treat migraine.

https://uk.reuters.com/article/us-amgen-migraine-fda/u-s-fda-approves-amgen-drug-for-prevention-of-migraines-idUKKCN1II344

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17/5/18
News on Neflamapimod

Funding to investigate Neflamapimod in Alzheimer’s disease, in a phase IIb clinical study has been secured.

https://www.fiercebiotech.com/biotech/eip-pharma-nabs-20-5m-to-push-alzheimer-s-med-through-phase-2?mkt_

Structure can be found on this link:

http://www.chemspider.com/Chemical-Structure.2302086.html

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30/4/18
News on Ubrogepant

An oral CGRP drug to treat migraine, reports of success in phase III clinical trials.

https://www.fiercebiotech.com/biotech/allergan-s-ubrogepant-aces-2nd-phase-3-migraine-trial

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Ubrogepant#section=Top

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26/4/18
News On Tavalisse

Tavalisse is a small molecule spleen tyrosine kinase inhibitor, to treat chronic immune thrombocytopenia.

https://www.fiercepharma.com/pharma/rigel-snags-first-fda-win-approval-for-autoimmune-therapy-tavalisse?mkt

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Fostamatinib#section=Top

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19/4/18
Something A Bit Different

This is a long way off commercialisation and not medchem, indeed only chemistry in a looser sense. Natural enzyme, improved in the lab through biological and molecular modelling understanding, to efficiently catabolise PET plastics.

http://www.bbc.co.uk/news/science-environment-43783631

https://uk.reuters.com/article/us-science-plastic-enzyme/plastic-eating-enzyme-holds-promise-in-fighting-pollution-scientists-idUKKBN1HN2OZ

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18/4/18
News on BLU-667

A small molecule, structure unknown, RET inhibitor, reports positive phase I clinical trial, in cancer patients.

https://www.fiercebiotech.com/biotech/blueprint-reports-promising-phase-1-data-ret-altered-tumors-aacr?mkt_

More details and structure can be found in this open access article

http://cancerdiscovery.aacrjournals.org/content/early/2018/04/12/2159-8290.CD-18-0338?utm_source=olf&utm_medium=socialatAM&utm_campaign=180338

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17/4/18
News on ATX-GD-59

A positive antibody therapy, in immune disorder Graves disease, in a phase I clinical trial.

https://www.fiercebiotech.com/biotech/apitope-preps-graves-disease-drug-for-phase-2-after-positive-trial?mkt_

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9/4/18
Classification on Tumours

I blogged on this twice in 2016, now in mainstream media.

http://www.bbc.co.uk/news/health-43659760

https://www.telegraph.co.uk/news/2018/04/07/cancer-textbook-should-rewritten-classify-cancers-type-not-start/

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4/4/2018
News on Cyramza

A successful trial in Liver cancer, for Cyramza (an antibody), is reported.

https://uk.reuters.com/article/us-lilly-study/lillys-cyramza-succeeds-in-late-stage-liver-cancer-trial-idUKKCN1HB1F8

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28/3/2018
News on Bempedoic Acid

Bempedoic acid lowers LDL cholesterol in add-on therapy

https://www.fiercebiotech.com/biotech/esperion-s-ldl-drug-flies-through-phase-2-as-add-treatment?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/etc-1002#section=Top

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21/3/2018
News on Etrasimod

Etrasimod, a sphingosine 1-phosphate receptor inhibitor, phase II data in ulcerative colitis.

https://www.fiercebiotech.com/biotech/midstage-success-prompts-arena-to-push-bowel-disease-drug-etrasimod-into-phase-3?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Etrasimod#section=Top

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20/3/2018
News on Rezafungin

Anti-fungal, Rezafungin, has a reported positive Phase II clinical study as an IV formulation. A literal heavy weight drug, at MW1226.

https://www.fiercebiotech.com/biotech/cidara-leaps-as-antifungal-drug-aces-phase-2?mkt_

Structure can be found on this link

http://www.chemspider.com/Chemical-Structure.58826030.html

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19/3/2018
News on stem Cells in MS

Multiple sclerosis (MS) is a disease where the immune system goes rogue and attacks the nerve cells. This report on how stem cell therapy could help MS patients and its costs versus conventional drugs.

http://www.bbc.co.uk/news/health-43435868

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15/3/2018
News on PRX-106 / OPRX-106

An unusual biological drug under investigation in ulcerative colitis, human tumour necrosis factor receptor II fused to an IgG1 Fc domain expressed in a plant cell. The whole plant cell is administered and protects the drug on its passage through the GI tract.

https://www.fiercebiotech.com/biotech/protalix-oral-anti-tnf-drug-hits-mark-phase-2-ulcerative-colitis-trial?mkt_

http://protalix.com/products/prx-106-oral-antitnf/

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14/3/2018
News on Xeljanz (Tofacitinib)

JAK inhibitor, Tofacitinib, could benefit patients with ulcerative colitis, according to this report.

https://uk.reuters.com/article/us-pfizer-fda/fda-panel-backs-pfizers-xeljanz-as-bowel-disease-treatment-idUKKCN1GK2TW

Structure can be found on this link:

https://en.wikipedia.org/wiki/Tofacitinib

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12/3/2018
News on Mavacamten

News on a positive phase II readout for Mavacanten in obstructive hypertrophic cardiomyopathy.

https://www.fiercebiotech.com/biotech/myokardia-delivers-midstage-trial-revs-up-for-phase-3?mkt_

Structure can be found on this link:

https://chem.nlm.nih.gov/chemidplus/rn/1642288-47-8

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9/3/2018
News on Evobrutinib

BTK inhibitor, evobrutinib, is reported to have had a positive clinical phase IIa outcome in multiple sclerosis.

https://www.fiercebiotech.com/biotech/merck-kgaa-btk-inhibitor-beats-placebo-phase-2-multiple-sclerosis-trial?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/71479709#section=Top

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7/3/2018
News on RG6042

News on an antisense drug, in a combined phase I/II clinical study, of RG6042, in Huntingdon’s Disease.

https://www.fiercebiotech.com/biotech/roche-ionis-hail-huntington-s-success-plan-pivotal-trial?mkt_

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5/3/2018
News on RPL-554

RPL-554 is a dual PDE3/PDE4 inhibitor under investigation in COPD and CF. Here are some reports of a clinical IIa study in CF patients.

https://www.fiercebiotech.com/biotech/verona-jumps-as-midphase-cystic-fibrosis-data-dial-up-hopes?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/RPL-554

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27/2/2018
Screening Oncology Drugs with Mini-tumours

Identifying a tumour by mutation, rather than tissue of origin, has been a step forward in treating cancer. Here a biopsy sample has been grown into mini-tumours and then incubated with various anti-cancer drugs to identify the most efficacious. Very much how we used to grow bacteria in petri dishes and then introduce impregnated discs of antibiotics to identify an efficacious drug for that pathogen.

http://www.bbc.co.uk/news/health-43154878

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23/2/2018
News on Semaglutide

A long acting GLP-1 agonist, Semaglutide, previously blogged in Aug 2017, now reports on phase III clinical trial readout.

https://www.fiercepharma.com/pharma/novo-trumpets-first-ph3-semaglutide-results-does-lilly-need-to-worry-yet?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Semaglutide

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14/2/2018
News on Antibiotics

A new class of antibiotic is reported in main stream media. Macrocyclic in nature and 4 carboxylic acids, to me it does not look like your typical “oral drug”.

http://www.bbc.co.uk/news/health-43032602

Structure can be found on this link:

https://en.wikipedia.org/wiki/Malacidin

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9/2/2018
News on MGL-3196

Information on MGL-3196, in phase II clinical trial, for heterozygous familial hypercholesterolemia (HeFH). Reports of significant reduction in LDL cholesterol.

https://www.fiercebiotech.com/biotech/madrigal-says-nash-drug-also-works-genetic-cholesterol-disorder?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/mgl-3196#section=Top

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8/2/2018
News on a Drug Combo Binimetinib and Encorafenib

A positive report on a drug combination to treat melanoma. The drugs are MEK inhibitor (Binimetinib) and BRAF inhibitor (Encorafenib).

https://www.fiercebiotech.com/biotech/array-s-encorafenib-binimetinib-beats-roche-s-zelboraf-phase-3?mkt_

Structure can be found on these links:

https://pubchem.ncbi.nlm.nih.gov/compound/10288191#section=Top

https://pubchem.ncbi.nlm.nih.gov/compound/50922675#section=Top

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7/2/2018
News on Ubrogepant

Ubrogepant is a calcitonin gene-related peptide (CGRP) type 1 receptor antagonist for migraine.

https://www.fiercebiotech.com/biotech/allergan-cgrp-drug-hits-goals-phase-3-migraine-trial?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Ubrogepant#section=Top

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1/2/2018
News on Balovaptan

Balovaptan, a vasopressin V1a receptor antagonist, is currently in phase II trials, to treat autism spectrum disorders.

https://www.fiercebiotech.com/biotech/roche-bags-breakthrough-status-for-autism-hope-balovaptan?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/RG7314

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30/1/2018
News on Revefenacin

Revefenacin, a nebulised long acting muscarinic antagonist (LAMA), has been accepted for review by the FDA, to treat COPD.

https://www.medscape.com/viewarticle/890044

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Revefenacin#section=Top

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29/1/2018
News on Lutathera

FDA approves radioactive drug, Lutathera, for gastroenteropancreatic neuroendocrine tumours.

https://uk.reuters.com/article/us-advanced-accelerator-fda/fda-clears-radioactive-drug-for-cancer-that-killed-steve-jobs-idUKKBN1FF29K

Structure can be found on these links:

https://chem.nlm.nih.gov/chemidplus/rn/437608-50-9

https://pubchem.ncbi.nlm.nih.gov/compound/121225499#section=Top

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26/1/2018
News on Ezutromid

Early readout on a phase II trial of Ezutromid in Duchenne Muscular Dystrophy. Route of administration is not given; however, vendors report oral bioavailable.

https://www.fiercebiotech.com/biotech/summit-therapeutics-unveils-encouraging-early-data-for-duchenne-drug?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Ezutromid#section=Top

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22/1/2018
Cancer Screening with a Blood Test

It is well appreciated that the earlier you can detect and treat cancer, the better the prognosis. So whilst not a new drug, this blood test to potential detect 16 mutated genes and 8 circulating proteins as indicators of cancer is exciting.

http://www.bbc.co.uk/news/health-42736764


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18/1/2018
News on Kymriah

Novartis entry in the CAR-T area is Kymriah; patients own T-cells are removed, modified and then returned to fight cancer.

https://uk.reuters.com/article/us-novartis-fda-kymriah/novartiss-kymriah-wins-speedy-reviews-in-u-s-europe-idUKKBN1F60KT

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17/1/2018
Kinases

Derek Lowe is a blog I read quite often. Here he gives his perspective on Kinases and a review article covering the whole area comprehensively (subscription required). As a medicinal chemist, you like your potential drug to be selective for your target only. You only know about selectivity when you go and look for it; and only quote selectivity over the enzymes/receptors screened.

http://blogs.sciencemag.org/pipeline/archives/2018/01/16/the-landscape-of-kinase-inhibitors

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10/1/2018
News on BGB324

Measured response to AXL inhibitor BGB324 (bemcentinib) clinical data disclosure.

https://www.fiercebiotech.com/biotech/bergenbio-s-axl-inhibitor-clears-early-efficacy-test-nsclc?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/r428#section=Top

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5/1/2018
News on EOS200271

This is an interim readout, on a phase I trial. What grabbed my interest is the small chemical structure and that it is racemic. Presumably what could be a chiral centre, racemises rapidly, negating isolation as a single enantiomer.

https://www.fiercebiotech.com/biotech/pfizer-drops-iteos-ido1-cancer-drug-due-to-lack-efficacy?mkt_

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/23063810#section=Top

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4/1/2018
New Drugs Approved by FDA in 2017

Headline figure shows more new medicines getting to patients in 2017. However, many are for small disease populations.

https://uk.reuters.com/article/us-pharmaceuticals-approvals/new-drug-approvals-hit-21-year-high-in-2017-idUKKBN1ER0P7

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3/1/2018
News on Cabometyx

Cabozantinib, a poly kinase inhibiter, now approved in renal cancers.

https://www.fiercepharma.com/regulatory/exelixis-soars-early-expanded-approval-for-kidney-cancer-drug?mkt_

Structure can be found on this link:

https://en.wikipedia.org/wiki/Cabozantinib

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2/1/2018
News on Steglatro (ertugliflozin)

Steglatro is a SGLT2 inhibitor, to treat type II diabetes, whose mode of action is to excrete excess sugars in urine.

https://www.reuters.com/article/us-merck-co-pfizer-diabetes/u-s-fda-approves-new-diabetes-drug-from-merck-and-pfizer-idUSKBN1EE2QT

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/Ertugliflozin#section=To

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Read earlier blog posts from 2017, 2016 and 2015 by clicking here.