Drug intelligence / Profile preview

avatrombopag + rifampin

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

Overview

**Avatrombopag + rifampin** is a combination of two pharmaceutical agents: avatrombopag, an orally administered small molecule thrombopoietin receptor agonist used to treat thrombocytopenia in patients with chronic liver disease or chronic immune thrombocytopenia, and rifampin, a broad-spectrum antibiotic commonly used in the treatment of tuberculosis and as a strong inducer of certain cytochrome P450 (CYP) enzymes. Avatrombopag stimulates the thrombopoietin receptor (c-Mpl) to promote megakaryocyte proliferation and platelet production. Rifampin induces CYP3A and moderately induces CYP2C9, leading to increased clearance and reduced systemic exposure of drugs like avatrombopag that are substrates of these enzymes. When coadministered, rifampin significantly decreases avatrombopag exposure (by approximately half), which may limit avatrombopag’s effectiveness; therefore, their coadministration is generally not recommended except with careful monitoring and possible dose adjustment.

Brand names
DopteletRifadinRimactane
Other names
avatrombopag maleaterifampicin
02

Targets

TPOR (Thrombopoietin receptor)CYP3A7 (Cytochrome P450 3A7)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)PXR (Pregnane X receptor)

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