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views from the bench masthead

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.