Regrelor (also known as INS50589) is an experimental antiplatelet drug that was under investigation by Merck Sharp and Dohme in human clinical trials. Although it was initially found to be well-tolerated in healthy subjects, safety concerns led to cessation of clinical trials.
Regrelor was synthesized from adenosine diphosphate (ADP), an endogenous chemical involved in metabolism. The authors noted that the addition of a lipophilic moiety like cinnamaldehyde at the C-2' and C-3' positions, combined with ethylurea at N-6 on the adenine base, yielded regrelor.
Regrelor was developed around the same time as prasugrel and cangrelor. After Inspire Pharmaceuticals initially developed the drug, it was purchased by Merck Sharp and Dohme.
Pre-clinical experiments in rats, dogs, and monkeys found that the drug acted quickly to inhibit platelet aggregation, and that baseline function was restored quickly after discontinuation of treatment.
In a phase 1 clinical trial sponsored by Merck Sharp and Dohme Corporation, regrelor was well-tolerated in healthy volunteers. In 2008, phase 2 trials were discontinued. It is believed that further development of the drug was ceased due to safety reasons. In the trial, there was an increased risk of bleeding for patients on regrelor.
^ abcdeChackalamannil, S; Rotella, D; Ward, S. "Comprehensive Medicinal Chemistry III". p. 568. Missing or empty |url= (help)
^ ab"Regrelor". pubchem.ncbi.nlm.nih.gov. National Center for Biotechnology Information. Retrieved 3 August 2017.
^ abcdJohnson, FL; Boyer, JL; Leese, PT; Crean, C; Krishnamoorthy, R; Durham, T; Fox, AW; Kellerman, DJ (2007). "Rapid and reversible modulation of platelet function in man by a novel P2Y(12) ADP-receptor antagonist, INS50589". Platelets. 18 (5): 346–56. doi:10.1080/09537100701268741. PMID17654304.