Drug intelligence / Profile preview

CB-03-10

Development stage
Phase 1
Lead developer
Cosmo Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

CB-03-10 (cortexolone 17α-valerate-21-propionate) is a synthetic steroidal small molecule derived from cortexolone (11-deoxycortisone), an intermediate in cortisol biosynthesis. It acts as a dual antagonist of the androgen receptor (AR) and glucocorticoid receptor (GR). The drug is being developed primarily for the treatment of solid tumors, including advanced refractory cancers such as pancreatic, colon, and prostate cancer. Preclinical studies have shown that CB-03–10 inhibits tumor growth in both AR-positive prostate cancer and GR-positive triple-negative breast cancer models by antagonizing AR and GR transcriptional activities, leading to induction of apoptosis via caspase activation. Importantly, it lacks biologically relevant agonist activity at these receptors. Clinical development has reached Phase I for solid tumors and Phase II for indications such as diverticulitis, hepatic encephalopathy, and malabsorption syndromes[1][2][5][9].

Other names
cortexolone 17α-valerate-21-propionatecortexolone derivative
02

Targets

GR (Glucocorticoid receptor)AR (Adrenergic receptors)

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