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views from the bench masthead

17/3/20

News on Osilodrostat (Isturisa)

News on a small molecule, nonsteroidal corticosteroid biosynthesis inhibitor, for the treatment of Cushings disease.

https://www.fda.gov/news-events/press-announcements/fda-approves-new-treatment-adults-cushings-disease

Structure can be found on this link:

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

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4/2/20

News on INS1007

INS1007 is an oral reversible dipeptidyl peptidase 1 (DPP1) inhibitor, formerly known as AZD7986, has shown benefit in a phase II clinical study in non-cystic fibrosis bronchiectasis patients.

https://www.fiercebiotech.com/biotech/insmed-s-inflammatory-lung-disease-drug-makes-grade-phase-2?mkt_

Structure can be found on this link:

https://medkoo.com/products/11027

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24/1/20

News on Risdiplam

This report looks to be a phase III clinical trial outcome, for Risdiplam in spinal muscular atrophy patients.

https://uk.reuters.com/article/us-roche-hldg-sma/roches-sma-drug-trial-win-bolsters-2-billion-sales-prospects-idUKKBN1ZM0N2

Structure can be found on this link:

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

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23/1/20

News on Surufatinib

A phase III clinical trial of Surufatinib, an oral angio-immuno kinase inhibitor for pancreatic cancer, was stopped at an interim analysis, as endpoints of the trial had been met.

https://www.fiercebiotech.com/biotech/chi-med-stops-pivotal-pancreatic-cancer-trial-upon-early-success?mkt_

Structure can be found on this link:

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

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13/1/20

News on Avapritinib / Ayvakit

Ayvakit has been approved by the FDA for gastrointestinal stromal tumours.  The drug is reported to be a targeted tyrosine kinase inhibitor.

https://uk.reuters.com/article/us-blueprint-fda/fda-approves-blueprints-stomach-cancer-therapy-priced-at-32000-per-month-idUKKBN1Z82LP

Structure can be found on this link:

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

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3/1/20

News on Ubrogepant / Ubrelvy

Ubrelvy is a calcitonin gene related peptide inhibitor, for oral dosing, in acute migraine.

https://www.fiercepharma.com/pharma/allergan-scores-year-end-fda-nod-for-cgrp-migraine-med-ubrelvy-plans-early-2020-launch?mkt_

Structure can be found on this link:

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

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20/12/19
News on Vosoritide

A peptide of some 4000 molecular weight, Vosoritide, is reported to show benefit in a phase III clinical study of achondroplasia.

https://www.fiercebiotech.com/biotech/biomarin-s-dwarfism-drug-clears-phase-3-poised-for-2021-launch?mkt

Structure can be found on this link:

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

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19/12/19

News on Belantamab Mafodotin

News on Belantamab Mafodotin, an anti-body drug conjugate is reported to show benefits in advanced multiple myeloma in a phase II clinical study. In anti-body drug conjugates, the antibody shields the toxic drug and only releases it at the tumour, when it interacts with a tumour specific antigen.

https://www.fiercebiotech.com/biotech/gsk-s-anti-bcma-med-shrinks-tumors-31-advanced-multiple-myeloma-patients?mkt_

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18/12/19

News on Lumasiran

News of a positive phase III clinical study on Lumasiran, a small interfering RNA (siRNA) treatment targeting primary hyperoxaluria type 1, where oxalate builds up in the kidneys, leading to kidney stones.

https://www.fiercebiotech.com/biotech/alnylam-preps-next-filing-as-rare-kidney-disease-med-aces-phase-3?mkt_

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10/12/19

News on AZD9567

First a disclaimer – this was my last project with AstraZeneca and I left the project in 2011.  AZD9567 was synthesized after my time on the project, however seeing compounds enter clinical trials and hopefully go on and become drugs is why we do medicinal chemistry.  It always give me a buzz to see compounds/projects  I have worked on make it to the human animal!

https://www.thelancet.com/journals/lanrhe/article/PIIS2665-9913(19)30103-1/fulltext

Structure can be found on this link:

https://pubchem.ncbi.nlm.nih.gov/compound/121248172

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9/12/19

News on Calquence (Acalabrutinib)

Calquence is a Bruton’s Tyrosine Kinase inhibitor used to chronic lymphocytic leukaemia.  Data discussed in newly diagnosed patients.

https://www.fiercepharma.com/pharma/ash-astrazeneca-s-calquence-posts-sky-high-survival-numbers-previously-untreated-cll?mkt_

Structure can be found on this link:

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

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26/11/19

News on Oxbryta

Reports that Oxbryta (Voxelotor) has been approved to treat sickle cell disease.  Mode of action is unclear, but appears to prevent sickling of the red blood cell.

https://uk.reuters.com/article/us-global-blood-theraprutics-fda/fda-approves-global-blood-therapeutics-sickle-cell-disease-drug-idUKKBN1XZ2E5

Structure can be found on this link:

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

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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=Topborder

Read earlier blog posts from 2018, 2017, 2016 and 2015 by clicking here.