Drug intelligence / Profile preview

bosentan + dacarbazine

Development stage
Unknown
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**Bosentan + dacarbazine** is a combination therapy investigated in metastatic melanoma. **Bosentan** is a dual endothelin receptor (ET_A and ET_B) antagonist, primarily used to treat pulmonary arterial hypertension, while **dacarbazine** is an alkylating agent chemotherapy used mainly for melanoma and Hodgkin lymphoma. In a phase 2, proof-of-concept study, the combination was evaluated as first-line treatment in patients with stage IV metastatic cutaneous melanoma. The trial found that adding high-dose bosentan to standard-dose dacarbazine did not improve time to tumor progression or overall efficacy compared to dacarbazine alone. The safety profile of the combination was consistent with known profiles for each agent; anemia and thrombocytopenia were somewhat more common with the combination.

02

Targets

EDNRB (Endothelin receptor type B)DNAEDNRA (Endothelin receptor type A)

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