larotinib + rifampin

**Larotinib + rifampin** is an investigational drug combination involving larotinib, a small molecule tyrosine kinase inhibitor, and rifampin, a well-established antibiotic and strong inducer of cytochrome P450 enzymes, particularly CYP3A4. Larotinib, similar to other ALK inhibitors such as lorlatinib, is being evaluated primarily for its antineoplastic activity in cancers like non-small cell lung cancer (NSCLC). Rifampin, when used concomitantly, acts as a pharmacokinetic modulator, primarily inducing hepatic enzymes (CYP3A4) and transporters, and is commonly employed in drug–drug interaction studies to model maximal enzyme induction. The combination of larotinib and rifampin is most often administered to characterize the impact of strong CYP3A induction on larotinib metabolism and safety. Clinical studies indicate that co-administration can result in severe reductions in larotinib exposure (over 75% reduction in AUC and Cmax) and a high risk of transient, severe hepatotoxicity (LFT elevations grade 2-4), with these liver effects typically reversible after discontinuation. Rifampin is not a cancer therapy but a standard antimicrobial (antitubercular); its use in this combination is for metabolic probing rather than therapeutic intent[2][1][6].

Other names

rifampicin