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| Drug class | antiplatelet drug |
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| Formula | C22H25N6O8P |
| Molar mass | 532.450 g·mol−1 |
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Regrelor (also known asINS50589) is an experimentalantiplatelet drug that was under investigation byMerck Sharp and Dohme in humanclinical 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.[1] It was under investigation for use inblood clotting problems,[2] as well as duringcoronary artery bypass surgery.[3]
Regrelor is available in anintravenous formulation.[1]
Regrelor is classified as apurinergic P2 receptor (P2Y12)antagonist.[4] Other compounds in the same mechanistic class includeclopidogrel andticagrelor. It is characterized as areversible,competitive receptor antagonist.[5] TheIC50 for antagonism of ADP-induced (P2Y12-mediated) platelet aggregation was 16 nMin vitro.[3]
Regrelor'sprimary metabolite is called INS51088.[5]
Regrelor is structurally similar toAMP, just liketicagrelor.[3] Regrelor has 4hydrogen bond donors and 11 acceptors.[4] It is produced as a disodium salt.[6] The twosodium atoms bind the negatively chargedphosphate moiety in solution.[3]
Regrelor was synthesized fromadenosine diphosphate (ADP), an endogenous chemical involved inmetabolism.[7] The authors noted that the addition of a lipophilic moiety likecinnamaldehyde at the C-2' and C-3' positions, combined with ethylurea at N-6 on theadenine base, yielded regrelor.[8]
Regrelor was developed around the same time asprasugrel andcangrelor.[1] After Inspire Pharmaceuticals initially developed the drug, it was purchased by Merck Sharp and Dohme.[6]
Pre-clinical experiments inrats, dogs, andmonkeys found that the drug acted quickly to inhibit platelet aggregation, and that baseline function was restored quickly after discontinuation of treatment.[5]
In aphase 1 clinical trial sponsored by Merck Sharp and Dohme Corporation, regrelor was well tolerated in healthy volunteers.[9][5] In 2008, phase 2 trials were discontinued.[2] It is believed that further development of the drug was ceased due to safety reasons.[6] In the trial, there was an increased risk ofbleeding for patients on regrelor.[3]
