fostamatinib + verapamil

Fostamatinib + verapamil is a combination of two small molecule drugs evaluated clinically for pharmacokinetic drug-drug interactions. Fostamatinib is an orally active prodrug that is rapidly converted to R406, an inhibitor of spleen tyrosine kinase (SYK), a key signaling protein in immune cell activation. It is primarily metabolized by CYP3A4. Verapamil is a calcium channel blocker (phenylalkylamine class) used primarily to treat hypertension, angina, and certain arrhythmias, and is a moderate inhibitor of CYP3A4. Clinical studies demonstrated that verapamil increases the exposure of R406 (the active form of fostamatinib) by approximately 39% via CYP3A4 inhibition, raising the potential for increased effects or adverse events from fostamatinib. The combination is not a marketed fixed-dose formulation but has been studied for drug-drug interaction potential in clinical pharmacology settings, particularly by AstraZeneca[1][2][4][5].

Other names

fostamatinib disodiumfostamatinib disodium hexahydrateR788R-788R 788R406R-406R 406verapamil hydrochloride