Drug intelligence / Profile preview

adavosertib + rifampicin

Development stage
Discontinued
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

**Adavosertib + rifampicin** is a combination of two pharmaceuticals: adavosertib, a first-in-class small molecule inhibitor of WEE1 kinase, and rifampicin, a broad-spectrum antibiotic primarily used for tuberculosis. Adavosertib selectively inhibits WEE1 kinase, disrupting the G2/M cell cycle checkpoint and inducing mitotic catastrophe in tumor cells with replication stress or TP53 mutations[1][3]. Rifampicin is a potent inducer of CYP3A4 and is sometimes co-administered in drug-drug interaction studies to assess the effect of enzyme induction on the pharmacokinetics of investigational agents. Combination use is generally for research (pharmacokinetic interaction), not for primary therapeutic indications.

02

Targets

WEE1 (WEE1 G2 checkpoint kinase)WEE2 (Wee1-like protein kinase 2)CYP3A4 (Cytochrome P450 3A4)

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