Drug intelligence / Profile preview

tesetaxel + rifampin

Development stage
Preclinical
Lead developer
Odonate Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

**Tesetaxel + rifampin** is a combination of two oral small-molecule drugs: tesetaxel, an investigational taxane-class antineoplastic agent, and rifampin, a classic rifamycin antibiotic. Tesetaxel stabilizes microtubules and inhibits cell division, while rifampin acts as a potent inducer of cytochrome P450 3A4 (CYP3A4) and is primarily used as an antimicrobial. The combination does not have clinical precedent or an established therapeutic rationale but may be studied for pharmacological interaction: taxanes (including paclitaxel, docetaxel, and novel agents like tesetaxel) are metabolized by CYP3A4, and concurrent rifampin can significantly induce hepatic metabolism, potentially reducing tesetaxel exposure and efficacy. There are reports that similar combinations with taxane-structured drugs may result in altered pharmacokinetics and require careful monitoring. There are no approved, marketed combinations of tesetaxel and rifampin nor combination products containing both.

Other names
rifampicin
02

Targets

TUBB (Tubulin (alpha and beta subunits))CYP3A4 (Cytochrome P450 3A4)

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