macitentan + temozolomide

Macitentan + temozolomide is a combination therapy that pairs a dual endothelin receptor antagonist (macitentan) with an alkylating agent (temozolomide). This combination has been investigated for the treatment of glioblastoma. Preclinical studies have shown that astrocytes and brain endothelial cells can protect glioma cells from temozolomide through an endothelin-dependent signaling mechanism. Macitentan works by blocking this protective effect, thereby enhancing the efficacy of temozolomide against glioblastoma cells. In orthotopic models of human glioblastoma, including temozolomide-resistant tumors, the combination produced durable responses with 96% of treated mice showing no evidence of disease.

Brand names

OpsumitTemodarTemodal

Other names

MacitentanTemozolomidePhase 1 Dose Escalation-Actelion-glioblastomaPhase1 Dose Escalation-Actelion-glioblastomaPhase-1 Dose Escalation-Actelion-glioblastoma