BMS-986242 / Bayer, BMS - LARVOL DELTA

Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors. (PubMed, ACS Med Chem Lett) - "We recently reported the identification of several novel heme-displacing IDO1 inhibitors, including the clinical molecules linrodostat (BMS-986205) and BMS-986242. Efforts to swap this quinoline with an alternative aromatic system led to the discovery of 2,3-disubstituted pyridines as suitable replacements. Further optimization, which included lowering ClogP in combination with strategic fluorine incorporation, led to the discovery of compound 29, a potent, selective IDO1 inhibitor with robust pharmacodynamic activity in a mouse xenograft model."

Journal • Genito-urinary Cancer • Melanoma • Oncology • Renal Cell Carcinoma • Solid Tumor

Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1. (PubMed, ACS Med Chem Lett) - "Given the substantial interest around this target for cancer immunotherapy, we sought to identify a structurally differentiated clinical candidate that performs comparably to linrodostat (BMS-986205) in terms of both in vitro potency and in vivo pharmacodynamic effect in a mouse xenograft model. On the basis of its preclinical profile, BMS-986242 was selected as a candidate for clinical development."

Journal • Preclinical • Genito-urinary Cancer • Melanoma • Oncology • Renal Cell Carcinoma • Solid Tumor • IDO1

An Investigational Immuno-Therapy Study of Experimental Medication BMS-986242 Given in Combination With Nivolumab in Patients With Advanced Cancer (clinicaltrials.gov) - P1/2; N=7; Terminated; Sponsor: Bristol-Myers Squibb; Completed ➔ Terminated; Inability to meet protocol objectives

Trial termination

An Investigational Immuno-Therapy Study of Experimental Medication BMS-986242 Given in Combination With Nivolumab in Patients With Advanced Cancer (clinicaltrials.gov) - P1/2; N=7; Completed; Sponsor: Bristol-Myers Squibb; Terminated ➔ Completed

Clinical • Combination therapy • Trial completion