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views from the bench masthead

21/9/2017
News on RNAi Patisiran

A positive readout on a RNAi drug, in a phase III clinical trial, is this the start of a new dawn in medicines?

http://www.fiercebiotech.com/biotech/alnylam-s-patisiran-hits-all-endpoints-critical-phase-3?utm_

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20/9/2017
News on Trelegy Ellipta

Trelegy Ellipta is a triple drug combination, for COPD. It is fixed dose in a single inhaler device. The 3 known drugs are: fluticasone furoate; umeclidinium [bromide] and vilanterol. Approval in US and Europe.

http://uk.reuters.com/article/us-gsk-copd-fda/glaxosmithkline-breathes-easier-as-u-s-approves-triple-lung-drug-idUKKCN1BU0UJ

Structures can be found on these links:

https://en.wikipedia.org/wiki/Umeclidinium_bromide
https://en.wikipedia.org/wiki/Fluticasone_furoate
https://en.wikipedia.org/wiki/Vilanterol

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19/9/2017
News on Lefamulin

Clinical trial outcome for Lefamulin in treating pneumonia.

http://uk.reuters.com/article/us-nabriva-study/nabrivas-pneumonia-drug-succeeds-in-late-stage-trial-shares-soar-idUKKCN1BT19V

Structure can be found on this link:

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

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5/9/2017
News on Duaklir

Duaklir is a combination of long-acting muscarinic antagonist (LAMA) aclidinium bromide and long-acting beta-agonist (LABA) formoterol fumarate.

http://uk.reuters.com/article/us-astrazeneca-duaklir-circassia-pharma/positive-lung-drug-trial-opens-path-to-u-s-market-for-circassia-idUKKCN1BI0PX

Structures can be found on these links:

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

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

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30/8/2017
News on Vabomere

Vabomere, a combination of an antibiotic Meropenem and beta lactamase inhibitor Varobactam, has been approved by the FDA for urinary tract infections.

http://uk.reuters.com/article/us-fda-medicines-idUKKCN1B92UD

Structures can be found on these links:

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

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

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29/8/2017
News on Canakinumab

The monoclonal antibody to interleukin 1 beta, Canakinumab, has shown a remarkable effect in treating heart attack patients.

http://www.telegraph.co.uk/science/2017/08/27/new-wonder-drug-hailed-biggest-breakthrough-fight-against-heart/

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24/8/2017
News on Kisqali (Ribociclib)

Kisqali, an inhibitor of cyclin D1/CDK4 and CDK6, receives approval in a tough breast cancer patient population.

http://uk.reuters.com/article/us-novartis-kisqali-idUKKCN1B40D1

Structure can be found on this link:

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

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23/8/2017
News on GLPG169

News on a phase II trial of GLPG169, in patients with idiopathic pulmonary fibrosis.

http://www.glpg.com/docs/view/598b6182b414d-en

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/90420193#section=Top

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22/8/2017
Extended patient scope for Lynparza (olaparib)

The PARP inhibitor, olaparib, has had its approved suitable patient population increased.

http://uk.reuters.com/article/us-astrazeneca-lynparza-fda-idUKKCN1AX2MY

Structure can be found on this link:

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

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18/8/2017
News on Semaglutide

A long acting GLP-1 agonist, Semaglutide, controlling blood sugar levels and weight in type II diabetes.

http://www.fiercepharma.com/marketing/novo-nordisk-s-new-semaglutide-trounces-lilly-s-trulicity-diabetes-trial?utm_

Structure can be found on this link:

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

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8/8/2017
News on Mavacamten

A small study of patients with an inherited genetic heart condition has ”impressive” results from a patient perspective. As a medicinal chemist, a nice small MW molecule.

http://www.fiercebiotech.com/biotech/myokardia-transforms-inherited-heart-disease-symptoms-mid-stage-trial?utm_

Structure can be found on this link:

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

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4/8/2017
News on Exenatide in Parkinsons Disease

Exenatide is an injectable peptide drug, which is an agonist at the glucagon-like peptide-1 receptor (GLP-1 agonist).

http://www.bbc.co.uk/news/health-40814250

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3/8/2017
News on Idhifa (Enasidenib)

Idhifa is an isocitrate dehydrogenase-2 inhibitor. The FDA release suggests a poly-pharmacology; “by blocking several enzymes that promote cell growth”. Indicated for the treatment for acute myeloid leukaemia patients, with a specific genetic mutation.

https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm569421.htm

Structure can be found on this link:

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

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1/8/2017
News on Acalabrutinib

Acalabrutinib granted “breakthrough” designation by FDA, for treating mantle cell lymphoma. The target is inhibition of Bruton tyrosine kinase (BTK).

http://uk.reuters.com/article/us-astrazeneca-cancer-blood-idUKKBN1AH38K

Structure can be found on this link:

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

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31/7/2017
News on Galantamine

Repurposing galantamine for metabolic syndrome.

http://www.fiercebiotech.com/research/targeting-inflammation-could-treat-metabolic-syndrome-s-many-symptoms?utm_

Structure can be found on this link:

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

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27/7/2017
News on Revefenacin

Revefenacin is a high molecule weight, nebulized therapy for chronic obstructive pulmonary disease (COPD).

http://www.fiercebiotech.com/biotech/theravance-copd-drug-clears-safety-study-setting-up-nda?utm_

Structure can be found on this link:

http://en.pharmacodia.com/web/drug/1_1425.html

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4/7/17
News on ALM201

ALM201 is a polypeptide of MW 2575 under evaluation in ovarian cancer, has been granted Orphan status by the FDA.

https://www.almacgroup.com/discovery-news/almac-discovery-is-granted-orphan-drug-designation-for-alm201-programme-in-ovarian-cancer/?utm_

Structure can be found on this link:

http://en.pharmacodia.com/web/drug/1_3852.html

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26/6/17
News on Tivozanib

Following a protracted clinical path, it looks like Tivozanib may get approval in kidney cancer. Its mode of action is described as a tyrosine kinase inhibitor.

http://www.fiercebiotech.com/biotech/aveo-soars-as-long-beleaguered-cancer-drug-nears-approval?utm_

Structure can be found on this link:

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

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23/6/17
News on Delafloxacin

Delafloxacin, a new antibiotic, has been approved by the FDA.

http://uk.reuters.com/article/us-melinta-antibiotic-fda-idUKKBN19A2X3

Structure can be found on this link:

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

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13/6/17
News on Canagliflozin (Invokana or Sulisent)

The drug Canagliflozin, as well as controlling type 2 diabetes, reduces heart disease problems too in these patients.

http://uk.reuters.com/article/us-johnson-johnson-diabetes-idUKKBN1932LH

Structure can be found on this link

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

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12/6/17
More News on Lynparza (olaparib)

The PARP inhibitor, olaparib, shows a positive phase III clinical trial result in Breast cancer.

http://www.fiercepharma.com/pharma/asco-astrazeneca-s-lynparza-posts-42-survival-edge-breast-cancer?utm

Structure can be found on this link:

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

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7/6/17
News on Zytiga (Abiraterone acetate) and Abiraterone

Abiraterone is covalent inhibitor of CYP17A1 inhibitor, under investigation as an adjunct to standard therapy in prostate cancer. The acetate is a prodrug of Abiraterone. Looking at the linked paper in the BBC article I believe both are Zytiga (Abiraterone acetate).

http://www.bbc.co.uk/news/health-40131381

http://www.fiercepharma.com/pharma/j-j-s-zytiga-slashes-death-risk-by-38-earlier-stage-prostate-cancer-patients?utm

Structures can be found on these links:

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

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

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6/6/17
News on ONX-0801

A proof of concept clinical trials does not get much better than this. It appears the compound is only effective for a subset of ovarian cancers with a particular mutation.

http://www.bbc.co.uk/news/health-40097274

Structure can be found on this link:

https://en.wikipedia.org/wiki/ONX-0801

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5/6/17
Further News on Vancomycin

As a medicinal chemist, chemical structure and understanding of interaction with the biological system are important. The article in Chemistry World gives both.

https://www.chemistryworld.com/news/modified-antibiotic-beats-superbug-resistance-/3007506.article

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31/5/17
News on Antibiotic Vancomycin

With a dire need for new antibiotics this headline looks great news. Then on reading the article, the triply changed Vancomycin has only been tested in vitro. Unfortunately I have not been able to access the PNAS article to check the facts.

http://www.bbc.co.uk/news/health-40091179

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19/5/17
News on Imfinzi (Durvalumab)

Imfinzi is an FDA-approved antibody therapy for cancer from AstraZeneca.

http://www.fiercepharma.com/pharma/az-gains-major-i-o-ground-imfinzi-lung-cancer-maintenance-stunner?utm_

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18/5/17
News on Copanlisib

Copanlisib, a PI3kinase inhibitor gets priority review from the FDA, based on phase II data, for follicular lymphoma.

http://uk.reuters.com/article/us-health-bayer-cancerdrug-idUKKCN18D0S6

Structure can be found on this link

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

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17/5/17
News on Metformin

Metformin is being reported as beneficial in a mouse model of fragile X syndrome. Metformin is a very simple molecule – molecular formula C4H11N5

http://www.fiercebiotech.com/research/diabetes-drug-metformin-shows-promise-treating-one-form-autism?utm_

Structure can be found on this link

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

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9/5/17
News on Radicava (Edaravone)

A drug to treat amyotrophic lateral sclerosis, and given FDA approval based on Japanese only clinical trial data, according to the article.

http://www.fiercepharma.com/pharma/mitsubishi-tanabe-wins-fda-backing-for-als-med-radicava?utm_

Structure can be found on this link:

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

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2/5/17
News on Rydapt (Midostaurin)

FDA approves Rydapt for acute myeloid leukaemia. Rydapt is a poly Kinase inhibitor.

http://www.fiercepharma.com/regulatory/novartis-wins-fda-nod-for-rydapt-a-new-targeted-drug-for-acute-myeloid-leukemia?utm

Structure can be found on this link:

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

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28/4/17
News on Stivarga

Stivarga, also known as Regorafenib, has been approved for use in liver cancer; adding to its previously approved cancer uses.

http://uk.reuters.com/article/us-bayer-cancer-liver-idUKKBN17T2PU

Structure can be found on this link:

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

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24/4/17
Preclinically 2 Known Drugs Halts Neurodegeneration

It is unclear from the BBC report if the 2 drugs have to be co-dosed and have a synergistic effect, or they are effective independently. The original paper is linked within, each drug looks to be efficacious alone.

http://www.bbc.co.uk/news/health-39641123

Trazodone chemical structure can be found here https://en.wikipedia.org/wiki/Trazodone

DBM (dibenzoylmethane) chemical structure can be found here

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

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21/4/17
P2X7 Antagonist in Diabetic Kidney Disease

Diabetic Kidney disease may be treatable with P2X7 antagonists.

http://www.bbc.co.uk/news/uk-scotland-edinburgh-east-fife-39642235

Original file http://www.research.ed.ac.uk/portal/files/29497460/Mullins_J_Renal_Disease_….pdf

Details of compound used https://openinnovation.astrazeneca.com/az11657312.html

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19/4/17
FDA Approvals in Q1 2017

FDA has approved 13 new drugs in the first quarter of 2017. 4 are antibody derived with the name ending ….mab.

https://www.fda.gov/Drugs/DevelopmentApprovalProcess/DrugInnovation/ucm537040.htm

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10/4/17
Low Dose Ketamine for Depression

Reports of a trial of using low doses of Ketamine to treat patients with depression.

http://www.bbc.co.uk/news/health-39501566

Structure can be found on this link

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

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5/4/17
First Deuterated Drug Deutetrabenazine

Reports that the FDA have approved the first deuterated drug, Deutetrabenazine for Huntington’s Chorea.

http://www.medscape.com/viewarticle/878162

Structure can be found on this link

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

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20/3/17
News on Abemaciclib

Abemaciclib is a CDK4/6 inhibitor, indicated for use in breast cancer

http://www.fiercebiotech.com/biotech/lilly-gets-positive-abemaciclib-phase-3-data-plots-2017-nda?utm

Structure can be found on this link

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

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16/3/17
More News on Lynparza (olaparib)

The PARP inhibitor, olaparib, shows a positive phase III clinical trial result in ovarian cancer.

http://uk.reuters.com/article/us-astrazeneca-cancer-ovarian-idUKKBN16L2EG

Structure can be found on this link

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

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15/3/17
News on Kisqali® (ribociclib, LEE011)

Kisqali is a CDK4/6 inhibitor, indicated for use in breast cancer.

https://www.multivu.com/players/English/8021851-fda-approves-new-novartis-advanced-breast-cancer-treatment/

Structure can be found on this link

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

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14/3/17
Fluorescent Molecule

Not a new medicine, but a natural compound found in an amphibians with bioluminescence. The fluorophore is described in this news piece both as being the double bonds and the isoquinolineone.

https://www.chemistryworld.com/2500541.article

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9/3/17
News on Dupixent (Dupilumab)

Dupixent is a monoclonal antibody, under investigation in moderate-to-severe atopic dermatitis.

http://uk.reuters.com/article/uk-sanofi-regeneron-idUKKBN16B0JN

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7/3/17
News on Ublituximab

Ublituximab is a monoclonal antibody, under investigation in chronic lymphocytic leukaemia patients, in combination with Imbruvica (Ibrutinib).

Http://uk.reuters.com/article/us-tg-therapeutics-study-idUKKBN16D1EB

Chemical stricture of Ibrutinib can be found on this link

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

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3/3/17
News on Letermovir

Positive news on Letermovir, an antiviral, undergoing trials to prevent infection in bone marrow transplants.

http://www.fiercebiotech.com/biotech/merck-s-letermovir-aces-bone-marrow-transplant-study-cutting-death-rate?utm_

Structure can be found on this link

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

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1/3/17
News on CAR-T Clinical Study

News on a CAR-T study, by Kite Pharma, in non-Hodgkin lymphoma. By trial size I think this would be a phase I study.

http://www.telegraph.co.uk/science/2017/02/28/terminal-cancer-patients-complete-remission-one-gene-therapy/

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28/2/17
News on Nexvax2

A potential vaccine to protect patients of celiac disease, Nexvax2 is a combination of 3 peptides. This report is of a phase Ib trial, so early days.

http://www.fiercebiotech.com/biotech/immusant-s-celiac-disease-immunotherapy-passes-first-clinical-test?utm_

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24/2/17
News on inotuzumab ozogamicin

The 2 part name reflects the drugs constituent parts a humanized monoclonal antibody inotuzumab (to CD22), linked to a cytotoxic agent ozogamicin.

http://www.fiercebiotech.com/biotech/fda-accepts-pfizer-s-blood-cancer-candidate-for-speedy-review

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22/2/17
News on Siliq (brodalumab)

Siliq (brodalumab) is an injectable antibody to treat plaque psoriasis. The biological has been approved by the FDA, but it does come with severe side effect warnings. Hence restricted prescribing and black box warnings.

http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm541981.htm

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20/2/17
News on Lynparza (olaparib)

The PARP inhibitor, olaparib, shows a positive phase III clinical trial result in breast cancer.

https://www.astrazeneca.com/content/astraz/media-centre/press-releases/2017/lynparza-meets-primary-endpoint-in-phase-iii-trial-in-brca-mutated-metastatic-breast-cancer-17022017.html

Structure can be found on this link

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

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13/2/17
News on Eravacycline

More a “potential revenue from our new drug” piece, however we do need new antibiotics.

http://uk.reuters.com/article/us-tetraphase-outlook-ceo-idUKKBN15O157

Chemical structures can be found on this link.

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

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3/2/17
Fruit can be bad for you

Lychees and Ackee fruits contain hypoglycin A, which inhibits glucose regulation. An individual can become hypoglycaemic as a consequence of eating the fruit, particularly if consumed on an empty stomach.

http://www.bbc.co.uk/news/world-asia-india-38831240

Chemical structures can be found on this link.

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

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1/2/17
News on Votubia (Everolimus)

Everolimus goes under a number of trade names, for a variety of indications, it is an mTOR inhibitor. EU medicines agency extends usage licencing, to include treatment of refractory partial-onset seizures, in patients with tuberous sclerosis complex.

http://uk.reuters.com/article/us-novartis-votubia-idUKKBN15F0H6

Chemical structures can be found on this link.

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

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30/1/17
Artificial Intelligence to Identify Skin Cancer

Artificial Intelligence (computer software) has been shown to be as accurate at identifying skin cancers from a photograph as expert dermatologist. In both cases biopsies are necessary to confirm diagnosis.

http://www.bbc.co.uk/news/health-38717928

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27/1/17
Receptor Occupancy

In designing an new medicine, you design a strong interaction with a receptor or enzyme and with that a long duration of action for once a day dosing. This article shows that LSD not only has a strong interaction with the serotonin receptor, to which it binds, but also a long residence time due to being completely encapsulated in the receptor.

https://www.chemistryworld.com/2500304.article

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26/1/17
News on Pancreatic Cancer treatment

Combination of gemcitabine and capecitabine, shows better survival than monotherapy with gemcitabine.

http://www.independent.co.uk/life-style/health-and-families/health-news/pancreatic-cancer-monumental-leap-treatment-chemotherapy-liverpool-university-a7544166.html

Chemical structures can be found on these links.

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

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

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23/1/17
News on CTP-656

CTP-656 is in the middle of a phase II clinical study, but has been granted orphan status by the FDA. Like all Concert Pharmaceutical – it is heavily deuterated.

http://www.businesswire.com/news/home/20170120005277/en/Concert-Pharmaceuticals-Receives-FDA-Orphan-Drug-Designation

Believed chemical structure on this link

https://www.pharmacodia.com/web/drug/1_3614.html

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20/1/17
News on Regorafenib

News on a phase III clinical trial of Regorafenib, in patients with hepatocellular carcinoma.

https://scienmag.com/mount-sinai-researchers-involved-in-successful-phase-3-trial-of-drug-for-liver-cancer/

Structure can be found on this link

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

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19/1/17
News on Chloroquine

Chloroquine is under investigation, in cancers, to inhibit autophagy. Autophagy is a mechanism used by some cancers to develop resistance to some chemotherapies.

https://www.sciencedaily.com/releases/2017/01/170117084050.htm

Structure can be found on this link

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

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18/1/17
News on Propranolol

Propranolol shown to treat soft tissue sarcoma and now given orphan status by the European Commission.

http://www.newswise.com/articles/common-heart-drug-repurposed-to-treat-rare-cancer-in-europe

Structure can be found on this link

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

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12/1/17
News on Tideglusib

Tideglusib shown to stimulate dental stem cells to produce dentine, when co-administered in a biodegradable matrix with glycogen synthase kinase, leading to the repair of dental cavities.

http://www.kcl.ac.uk/dentistry/newsevents/news/newsrecords/2017/January/Natural-tooth-repair-method-using-Alzheimer’s-drug-could-revolutionise-dental-treatments.aspx

Structure can be found on this link

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

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10/1/17
New Drug Approvals in 2016

Not sure if I captured all 22 new drug approvals in the blog. Fiercebiotech have curated them here.

http://www.fiercebiotech.com/special-report/new-drug-approvals-took-a-nosedive-2016-here-are-22-made-grade?utm_

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