Drug intelligence / Profile preview

avatrombopag + fluconazole

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

Overview

Combination of **avatrombopag** (a small molecule thrombopoietin receptor agonist that increases platelet production by stimulating the thrombopoietin receptor, used for chronic immune thrombocytopenia and thrombocytopenia in chronic liver disease) and **fluconazole** (an azole antifungal which acts as a moderate dual inhibitor of CYP2C9 and CYP3A4/5). Coadministration leads to significantly increased exposure to avatrombopag (AUC ~2.16x, Cmax ~1.17x), requires dose adjustment and monitoring for increased platelet count due to CYP-mediated metabolic inhibition. Used clinically where both antiplatelet elevation and antifungal treatment are required, but with specific dose modification guidance.[1][2][3][4][5][6]

02

Targets

TPOR (Thrombopoietin receptor)CYP3A4 (Cytochrome P450 3A4)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)CYP51A1 (Sterol 14α-demethylase)

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