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KCZ-229A

Development stage: Preclinical
Lead developer: University of Texas MD Anderson Cancer Center
Modality: Small Molecules

Overview

KCZ-229A is a novel, brain-penetrant small molecule derivative of the antifungal ketoconazole, specifically designed to target the truncated GLI1 (tGLI1) transcription factor. Unlike its parent compound, KCZ-229A does not inhibit CYP3A4, thereby avoiding common toxicities such as liver damage and adrenal insufficiency. It selectively inhibits tGLI1-positive breast cancer stem cells and suppresses the progression of breast cancer brain metastases (BCBM) in preclinical models. The drug works by binding directly to the tGLI1 protein, inducing apoptosis and reducing the CD44+/CD24- stem cell population, while demonstrating high blood-brain barrier permeability.

Other names: ketoconazole derivative KCZ-229A

Targets

GLI1

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