Drug intelligence / Profile preview

AR-C124910XX

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
01

Overview

AR-C124910XX is the **major active metabolite** of ticagrelor, formed primarily by hepatic CYP3A4 and CYP3A5 enzymes through de-hydroxyethylation of ticagrelor at the cyclopentane ring[1][2][3][4][5][7][10]. Like ticagrelor, AR-C124910XX is a reversible allosteric antagonist of the **P2Y12 adenosine diphosphate (ADP) receptor** on platelets, directly inhibiting platelet activation and aggregation[1][4][7]. AR-C124910XX achieves plasma concentrations that contribute significantly to overall pharmacologic effect; it is **equipotent** to ticagrelor in inhibiting platelet activation[4][10]. Its formation, bioavailability, and exposure can be influenced by factors such as age, sex, ethnicity, renal and hepatic function, and exposure to CYP3A inducers or inhibitors[2][3][4][5].

Other names
ticagrelor metabolite
02

Targets

P2Y12 (Purinergic P2Y12 receptor)

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