lurbinectedin + bosentan

Lurbinectedin + bosentan is a combination of two small molecule drugs, investigated for pharmacokinetic and safety interactions in patients with advanced solid tumors. **Lurbinectedin** (marketed as Zepsyre, code name PM1183) is a selective inhibitor of oncogenic transcription, binding to the DNA minor groove and inhibiting RNA polymerase II, leading to apoptosis of cancer cells. **Bosentan** (brand name Tracleer, code name RO47-0203) is an endothelin receptor antagonist used primarily in pulmonary arterial hypertension, but in this combination it acts as a moderate inducer of CYP3A4, affecting lurbinectedin clearance. The co-administration primarily leads to an approximately 20% reduction in systemic exposure (AUC) of lurbinectedin and a 25% increase in its clearance, via enhanced hepatic metabolism induced by bosentan, but does not result in clinically significant safety or toxicity differences compared to lurbinectedin monotherapy in cancer patients[1][2].

Brand names

Zepsyre

Other names

PM1183PM-1183PM 1183RO47-0203RO-47-0203RO 47-0203