Enereductases (EREDs) and ketoreductases (KREDs) are highly selective enzymes that offer greener alternatives to more traditional asymmetric hydrogenation reactions. Enzyme cascades are a powerful way to enable more environmentally friendly and cost-effective synthetic processes for the manufacture of APIs. Here we report the discovery and development of an ERED/KRED biocatalytic cascade to enable efficient installation of the two stereocenters on a cyclohexyl ring for the synthesis of BMS-986278, a potent small-molecule LPA1 antagonist. A combination of protein engineering and process development optimized the cascade, resulting in orders of magnitude improvement over the original cascade proof-of-concept, and an over four-fold reduction in PMI over the first generation non-biocatalytic campaign for synthesis of the fragment. The synthesis of BMS-986278 was honored as a co-winner of the 2023 Peter J. Dunn award for Green Chemistry & Engineering Impact in the Pharmaceutical Industry, in large part because of the sustainability improvements enabled by this enzymatic cascade.
The FDA approves remibrutinib for symptomatic dermographism, the first such therapy, extending an oral BTK inhibitor label via the Phase III RemIND trial.
The company is showcasing new development solutions and advanced digital technologies including its new OSD Express and Steriles Express solutions for drug development.
Ron Scarboro, Azurity Pharmaceuticals, explains when formulation robustness justifies added cost and which post-approval quality and supply metrics teams can track.
The winners of the CPHI Pharma Awards 2026 include a neurodegeneration platform, a track-and-trace packaging innovation, a enzymatic mRNA manufacturing technology, and a cell-free enzymatic biomanufacturing platform.
This week on PharmTech, Merck diversified its pipeline, USP emphasizes supply chain security, AI systems are examined, and speakers preview their presentations at CPHI Milan and AAPS PharmSci 360.