[Commercial Synthesis Spotlight] Improved Synthesis of a Sotorasib Key Intermediate rac-4

rac-4 is a key intermediate in the synthesis of Sotorasib (AMG 510), the first-in-class KRAS G12C inhibitor approved for the treatment of various solid tumors, including non-small cell lung cancer (NSCLC). Sotorasib contains a unique C-N atropisomer, and rac-4 must undergo classical resolution to isolate the desired M-4 atropisomer for drug substance preparation.

[New Drug Spotlight] Ensifentrine: a New Dual PDE3/4 Inhibitor Approved for COPD Treatment

Ensifentrine (trade name: Ohtuvayre) was approved by the U.S. FDA in June 2024 as a maintenance treatment for adult patients with COPD. Developed by Verona Pharma, Ensifentrine is the first inhaled PDE3/4 dual inhibitor to reach the market. Its dual mechanism offers both bronchodilatory and anti-inflammatory effects, setting it apart from traditional therapies.