|Drug class||antiplatelet drug|
|Chemical and physical data|
|Molar mass||532.45 g/mol|
|3D model (JSmol)|
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 is an experimental drug. It is classified as an antiplatelet medication. It was under investigation for use in blood clotting problems, as well as during coronary artery bypass surgery.
Regrelor is classified as a purinergic P2 receptor (P2Y12) antagonist. Other compounds in the same mechanistic class include clopidogrel and ticagrelor. It is characterized as a reversible, competitive receptor antagonist. The IC50 for antagonism of ADP-induced (P2Y12-mediated) platelet aggregation was 16 nM in vitro.
Regrelor is structurally similar to AMP, just like ticagrelor. Regrelor has 4 hydrogen bond donors and 11 acceptors. It is produced as a disodium salt. The two sodium atoms bind the negatively charged phosphate moiety in solution.
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.
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.
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