trabectedin + rifampin

Trabectedin is a synthetic alkaloid originally isolated from the marine tunicate Ecteinascidia turbinata, used as an antineoplastic agent predominantly for soft tissue sarcoma and ovarian cancer. Its mechanism includes binding to the minor groove of DNA, affecting DNA transcription and repair, and modulating the tumor microenvironment, particularly by targeting monocytes/macrophages. Rifampin is an antibiotic of the rifamycin class and a potent cytochrome P450 3A4 (CYP3A4) inducer, used primarily to treat tuberculosis and other bacterial infections by inhibiting bacterial DNA-dependent RNA polymerase. The combination of trabectedin and rifampin is **not an approved therapeutic regimen**; it is instead a clinically relevant drug-drug interaction: rifampin, as a strong CYP3A4 inducer, significantly increases the metabolic clearance of trabectedin, reducing trabectedin systemic exposure by about 31% in area under the curve (AUC) and 21–22% in maximum concentration (Cmax), potentially reducing trabectedin’s efficacy. This combination is generally advised against in clinical guidelines due to pharmacokinetic interaction leading to subtherapeutic levels of trabectedin.[1][2][3][4]

Brand names

YondelisRifadinRimactane

Other names

ET-743ET743ET 743NSC 684766NSC684766NSC-684766RP-56976RP56976RP 56976rifampicin