BMS-986224
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- LARVOL DELTA
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November 21, 2021
Identification of 6-Hydroxypyrimidin-4(1H)-one-3-carboxamides as Potent and Orally Active APJ Receptor Agonists.
(PubMed, ACS Med Chem Lett)
- "Recently we disclosed clinical lead BMS-986224 (1), a C3 oxadiazole pyridinone APJ receptor agonist with robust pharmacodynamic effects similar to (Pyr)apelin-13 in an acute rat pressure-volume loop model. Herein we describe the structure-activity relationship of the carboxamides as oxadiazole bioisosteres at C3 of the pyridinone core and C5 of the respective pyrimidinone core. This study led to the identification of structurally differentiated 6-hydroxypyrimidin-4(1H)-one-3-carboxamide 14a with pharmacodynamic effects comparable to those of compound 1."
Journal • Cardiovascular • Congestive Heart Failure • Heart Failure
March 06, 2021
In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure.
(PubMed, Circ Heart Fail)
- "We identify a novel, potent, and orally bioavailable nonpeptidic APJ agonist that closely recapitulates the signaling properties of (Pyr) apelin-13. We show that oral APJ agonist administration induces a sustained increase in cardiac output in the cardiac disease setting and exhibits a differentiated profile from the renin-angiotensin system inhibitor enalapril, supporting further clinical evaluation of BMS-986224 in heart failure."
Journal • Preclinical • Anesthesia • Cardiovascular • Congestive Heart Failure • Fibrosis • Heart Failure • Immunology
March 10, 2020
A Study of BMS-986224 in Healthy Subjects and Heart Failure Patients With Reduced Ejection Fraction
(clinicaltrials.gov)
- P1; N=199; Terminated; Sponsor: Bristol-Myers Squibb; Completed ➔ Terminated; Business objectives have changed
Clinical • Trial termination
November 26, 2019
A Study of BMS-986224 in Healthy Subjects and Heart Failure Patients With Reduced Ejection Fraction
(clinicaltrials.gov)
- P1; N=199; Completed; Sponsor: Bristol-Myers Squibb; Active, not recruiting ➔ Completed; Trial completion date: Oct 2019 ➔ Apr 2019
Clinical • Trial completion • Trial completion date
October 23, 2019
A Study of BMS-986224 in Healthy Subjects and Heart Failure Patients With Reduced Ejection Fraction
(clinicaltrials.gov)
- P1; N=262; Active, not recruiting; Sponsor: Bristol-Myers Squibb; Trial primary completion date: Sep 2019 ➔ Apr 2019
Clinical • Trial primary completion date
October 01, 2019
An Investigational Study to Evaluate Experimental Medication BMS-986224 in Renally Impaired Participants
(clinicaltrials.gov)
- P1; N=50; Completed; Sponsor: Bristol-Myers Squibb; Recruiting ➔ Completed
Clinical • Trial completion
August 05, 2019
A Study of BMS-986224 in Healthy Subjects and Heart Failure Patients With Reduced Ejection Fraction
(clinicaltrials.gov)
- P1; N=262; Active, not recruiting; Sponsor: Bristol-Myers Squibb; Trial completion date: May 2019 ➔ Oct 2019; Trial primary completion date: May 2019 ➔ Sep 2019
Clinical • Trial completion date • Trial primary completion date
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