Synonyms: (4S)-2-Oxoclopidogrel | compound IV-1 [EP3290423B1] [3] | compound of formula I [US2022028976]
Compound class:
Synthetic organic
Comment: Becondogrel is the INN for a platelet aggregation inhibitor (WHO proposed INN list 132, Feb 2025). It is a derivative of the irreversible P2Y12 receptor anti-platelet prodrug clopidogrel that has been modified to overcome individual differences in hepatic CYP450 enzyme activity that limit conversion of clopidogrel into its active metabolite [1-2] and conversion to an inactive carboxylic derivative by carboxylesterase 1 (CES1) [4]. Becondogrel is a prodrug that is converted to its active metabolite in vivo.
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References |
1. Cen G, Yang M, Tan S. (2022)
Crystalline form b of tetrahydrothienopyridine compound, preparation method, composition and application thereof. Patent number: US20220289761A1. Assignee: Chengdu Shibeikang Biomedical Technology Co Ltd. Priority date: 23/05/2022. Publication date: 15/09/2022. |
2. Lau WC, Gurbel PA, Watkins PB, Neer CJ, Hopp AS, Carville DG, Guyer KE, Tait AR, Bates ER. (2004)
Contribution of hepatic cytochrome P450 3A4 metabolic activity to the phenomenon of clopidogrel resistance. Circulation, 109 (2): 166-71. [PMID:14707025] |
3. Sun H, Shan J, Zhang B, Yuan F. (2021)
Optically active 2-hydroxy tetrahydrothienopyridine derivatives, preparation method and use in manufacture of medicament thereof. Patent number: EP3290423B1. Assignee: Jiangsu Vcare Pharmatech Co Ltd. Priority date: 28/01/2011. Publication date: 21/07/2021. |
4. Tang M, Mukundan M, Yang J, Charpentier N, LeCluyse EL, Black C, Yang D, Shi D, Yan B. (2006)
Antiplatelet agents aspirin and clopidogrel are hydrolyzed by distinct carboxylesterases, and clopidogrel is transesterificated in the presence of ethyl alcohol. J Pharmacol Exp Ther, 319 (3): 1467-76. [PMID:16943252] |