Drug intelligence / Profile preview

RO46-2005

Development stage: Unknown
Lead developer: Roche
Modality: Small Molecules
Administration: Oral, Intravenous

Overview

RO46-2005 is a small-molecular-weight, synthetic, non-peptide endothelin receptor antagonist. It was one of the first compounds identified to inhibit the binding of endothelin-1 (ET-1) to both endothelin A (ETA) and endothelin B (ETB) receptors with equipotent affinity. Initially studied for its in vivo pharmacology and its influence on cardiovascular morphology in uremic rats, it demonstrated both depressor and pressor effects depending on the dose. It was also noted as the first orally active endothelin receptor antagonist, serving as a precursor in the development of later clinical candidates like bosentan.

Targets

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

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