2. Academic Validation
  3. BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate

BMS-813160: A Potent CCR2 and CCR5 Dual Antagonist Selected as a Clinical Candidate

  • ACS Med Chem Lett. 2021 Oct 15;12(11):1753-1758. doi: 10.1021/acsmedchemlett.1c00373.
Robert J Cherney 1,  Prakash Anjanappa 2,  Kumaravel Selvakumar 2,  Douglas G Batt 1,  Gregory D Brown 1,  Anne V Rose 1,  Ragini Vuppugalla 1,  Jing Chen 1,  Jian Pang 1,  Songmei Xu 1,  Melissa Yarde 1,  Andrew J Tebben 1,  Venkatram Reddy Paidi 2,  Mary Ellen Cvijic 1,  Arvind Mathur 1,  Joel C Barrish 1,  Sandhya Mandlekar 1,  Qihong Zhao 1,  Percy H Carter 1
Affiliations

Affiliations

  • 1 Bristol Myers Squibb Company, Research and Early Development, Princeton, New Jersey 08540-4000, United States.
  • 2 Biocon Bristol Myers Squibb Research and Development Center, Bangalore 560099, India.
PMID: 34795864 DOI: 10.1021/acsmedchemlett.1c00373
Abstract

BMS-813160 (compound 3) was identified as a potent and selective CCR2/5 dual antagonist. Compound 3 displayed good permeability at pH = 7.4 in PAMPA experiments and demonstrated excellent human liver microsome stability. Pharmacokinetic studies established that 3 had excellent oral bioavailability and exhibited low clearance in dog and cyno. Compound 3 was also studied in the mouse thioglycollate-induced peritonitis model, which confirmed its ability to inhibit the migration of inflammatory monocytes and macrophages. As a result of this profile, compound 3 was selected as a clinical candidate.

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