The Chemist's Playbook: Impactful Bioisosteres for Modern Drug Design
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Tackling MedChem Bias One Functional Group at a Time
Functional groups that medicinal chemists don't encounter regularly often face greater scrutiny compared to more common ones. In his Flash Talk, Gilles Ouvry challenges these biases and presents data on four uncommon functional groups that required extra convincing to gain acceptance. Here we supply a PDF download of his slides for our members.
Where Do Recent Small Molecule Clinical Candidates Come From?
Modern hit-finding technologies are incredible. Dean Brown and Jonas Bostrom at AstraZeneca have a very nice review out summarizing the hit-finding strategies for 66 clinical candidates published from 2016-2017. Some highlights include a clinical candidate from DNA-encoded libraries at GSK, the discovery of an RNA-binding drug candidate by [...]
Molecules on the Move: Reversible BTKi in MS, THR-beta Agonist in NASH, and More
This article compiles recent high-profile clinical readouts and related news with small molecules of general interest and structures where they are available. Targets and indications discussed in this article include BTK for MS, Axl, TYRO3, and Mer for oncology, HIF prolyl-hydroxylase in anemia, ET/AT in nephrology, a JAK2 inhibitor for myelofibrosis, and THR-beta in NASH. [...]
Patent Pulse: A Spotlight on Recent Highlights from Small Molecule Patents
As part of our Coffee Chat webinar series, our team (Lew Pennington, Matt Hesse, and Dennis Koester), explored Drug Hunter’s patent highlight feature and shared their favorite molecules and notable stories from recent patent filings. we present a PDF of the slide deck. Check out the recording of the talk on our Drug Hunter YouTube channel.
Olutasidenib: Potentially Longer Complete Remissions in AML with a Second-Generation IDH1 Inhibitor
Olutasidenib, discovered by Forma Therapeutics and marketed by Rigel, is an oral, brain-penetrant, selective mIDH1 inhibitor. It was granted Orphan Drug Designation and approved in December 2022 by the FDA for adults with relapsed/refractory acute myeloid leukemia. Approval was granted based on a Ph. I/II trial showing a 35% CR+CRh rate and a favorable 25.9-month median duration. This article describes the discovery and development of olutasidenib, how it is distinct from other mIDH inhibitors, and its potential in treating gliomas.
