BMS-919373 / BMS - LARVOL DELTA

Discovery and chemical development of BMS-919373 – a selective IKur inhibitor for the potential treatment of atrial fibrillation (ACS-Fall 2022) - "The transition to process chemistry, the initial scale-up route, commercial route exploration, and commercial route development led to an impactful C-H direct arylation. The development and mechanistic studies of the direct arylation led to a commercial route with significant improvements in yield, cost, and number of steps."

Atrial Fibrillation • Cardiovascular

Utilizing Native Directing Groups: Synthesis of a Selective IKur Inhibitor, BMS-919373, via a Regioselective C-H Arylation. (PubMed, J Org Chem) - "The strategy of leveraging this inherent directing group allowed the synthesis of this complex heterocycle in only six steps from commodity chemicals. The scope of the C-H activation was further investigated, and the generality of the transformation across a series of bicyclic aromatic heterocycles was explored."

Journal

A Blinded Study to Evaluate Effect on Atrial Fibrillation Burden in Patients With Paroxysmal Atrial Fibrillation (clinicaltrials.gov) - P2; N=158; Terminated; Sponsor: Bristol-Myers Squibb; N=27 ➔ 158; Completed ➔ Terminated; Sponsor decision based on business reasons, unrelated to safety

Enrollment change • Trial termination