Drug intelligence / Profile preview

avatrombopag + itraconazole

Development stage
Unknown
Lead developer
Sobi
Modality
Small Molecules
Administration
Oral
01

Overview

**Avatrombopag + itraconazole** is a combination of the thrombopoietin receptor agonist avatrombopag and the antifungal agent itraconazole, primarily relevant in the context of drug-drug interaction studies. Avatrombopag acts as a small-molecule agonist of the thrombopoietin receptor (c-Mpl), stimulating proliferation and differentiation of megakaryocytes, thus increasing platelet production for the treatment of thrombocytopenia in chronic liver disease and chronic immune thrombocytopenia. Itraconazole is a strong cytochrome P450 3A (CYP3A) inhibitor used in antifungal therapy. Co-administration of these agents leads to a mild increase in avatrombopag exposure (AUC and Cmax) and a corresponding mild increase in its pharmacodynamic effects on platelet count, compared to monotherapy. This combination may require adjustment in avatrombopag dose or treatment duration due to pharmacokinetic modulation by itraconazole[1][2][3][4].

Brand names
Doptelet (for avatrombopag)
Other names
avatrombopagitraconazole
02

Targets

TPOR (Thrombopoietin receptor)CYP51A1 (Sterol 14α-demethylase)CYP3A (CYP3A family)

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