Drug intelligence / Profile preview

cavosonstat + rifampin

Development stage
Unknown
Lead developer
Vertex
Modality
Small Molecules
Administration
Oral
01

Overview

Cavosonstat + rifampin is a combination of two drugs: cavosonstat (N91115), an orally bioavailable small molecule inhibitor of S-nitrosoglutathione reductase (GSNOR) designed to promote cystic fibrosis transmembrane conductance regulator (CFTR) protein maturation and stability, and rifampin, a well-known antibiotic that acts as a bacterial RNA polymerase inhibitor. Cavosonstat was primarily developed for cystic fibrosis and tested in clinical trials for its ability to restore GSNO levels by inhibiting GSNOR, thus stabilizing CFTR function. Rifampin is commonly used for treating tuberculosis and other bacterial infections. Studies indicate that cavosonstat’s pharmacokinetics were not significantly affected by rifampin-mediated effects on metabolism and transport. Cavosonstat development for cystic fibrosis was discontinued after failing to meet efficacy endpoints in Phase 2 clinical trials[1][3][4][5].

Other names
N91115N-91115N 911153-chloro-4-(6-hydroxyquinolin-2-yl)benzoic acid
02

Targets

CFTR (Cystic fibrosis transmembrane conductance regulator)RNAP (Bacterial dna-dependent RNA polymerase)GSNOR (S-nitrosoglutathione reductase)

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