Olutasidenib: Potentially Longer Complete Remissions in AML with a Second-Generation IDH1 Inhibitor
Other articles you may be interested in
Are Drugs Becoming More Lipophilic Over Time?
Drug lipophilicity is a core property that contributes to drug solubility, permeability, metabolic disposition, and other key properties. Increasing lipophilicity can often lead to increased affinity in relevant biological assays due to the hydrophobic nature of many protein binding pockets, but this may also increase promiscuity to [...]
Targeting Post-Transcriptional RNA-Modification with a First-to-Clinic METTL3 Inhibitor: STC15
STC15 is Storm Therapeutics' first-in-class and first-to-clinic inhibitor of the post-transcriptional RNA modifier, METTL3, which progressed from HTS hit to clinical development in less than three years. METTL3 inhibitors have been previously identified, but no METTL3 inhibitors have entered clinical development until now. In this article, we explore METTL3 as a therapeutic target, highlight the discovery story of STC15, its fascinating mechanism of action, provide the latest clinical development update, and much more.
KIN-3248: Overcoming FGFR Resistance with a Next-Generation Pan-FGFR Inhibitor
KIN-3248 (Kinnate Biopharma) is a next-generation, irreversible, pan-fibroblast growth factor receptor inhibitor (FGFRi) in a first-in-human (FIH) dose-escalation study (NCT05242822) in adults with advanced tumors harboring FGFR2 and FGFR3 gene alterations. The program is an excellent case study for rational covalent drug design to address kinase mutations while maintaining sufficient PK properties for oral daily dosing in humans.
AACR Orlando 2023: New Drug Candidates
The AACR 2023 first disclosures presented in the Chemistry in Cancer Research’s “New Drugs on the Horizon” sessions are always fascinating. This article contains the structures of all of the novel small molecule first disclosures presented at AACR in the session, along with notes on their significance, and another molecule disclosed in the [...]
Another KRASG12C Inhibitor in Ph. III, Bayer’s Massive FXIa Ph. III Clinical Trial, and 21 Other Molecules in the News
In this update of small molecules in the news for February 2023, we will cover recent: - Molecules in Motion : clinical trial updates and FDA filings - Negative Readouts : halted, discontinued or altered clinical trials - Million-Dollar Molecules : recent M&A’s, IPOs, and other fundraising - Potential Approvals : recent NDA filings and [...]
