Drug intelligence / Profile preview

CGP 4832

Development stage
Preclinical
Lead developer
Novartis
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
01

Overview

CGP 4832 is a semisynthetic derivative of rifamycin S, classified as a naphthofuran compound. It was developed to enhance antibacterial activity, particularly against Gram-negative bacteria. Compared to rifampicin, CGP 4832 demonstrates significantly higher potency—up to 400 times lower minimum inhibitory concentrations (MICs) against certain Gram-negative strains. Its mechanism of action involves inhibition of DNA-dependent RNA polymerase (DNA-directed RNA polymerase), similar to other rifamycins, thereby blocking bacterial transcription. The increased efficacy is attributed not to a difference in enzyme inhibition but likely due to improved penetration into bacterial cells via specific uptake mechanisms[1][2][3][5].

02

Targets

RNAP (Bacterial dna-dependent RNA polymerase)

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