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 upcoming PDUFA dates
– Where Are They Now? updates on past Molecules of the Month

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Molecules in Motion 

RG6330

Roche has added RG6330 to the Ph. III B-FAST study investigating multiple therapies as single agents or in combination for non-small cell lung cancer (NSCLC, NCT03178552), adding another late-stage contender to this competitive field. The new arm will compare RG6330 monotherapy (QD) against docetaxel in second-line KRAS^G12C-mutant disease. Like approved covalent molecules sotorasib and adagrasib, the compound shuts down oncogenic signaling by locking KRAS^G12C into the inactive GDP-bound state. KRAS^G12C is a hotly pursued target that we have covered in depth previously, including articles on sotorasib (Lumakras, Amgen),  MRTX849 (Krazati, Mirati), Revolution Medicines’ RM-018, AstraZeneca’s compound 25, Novartis’s JDQ443, and Boehringer Ingelheim’s BI-0474, among others. This recent article discusses how new inhibitors could differentiate.