Drug intelligence / Profile preview

CACN136

Development stage
Preclinical
Lead developer
Azevan Pharmaceuticals
Modality
Small Molecules
Administration
Unknown
01

Overview

CACN136 is a synthetic **curcumin analog** designed to improve upon curcumin’s poor stability and low activity for therapeutic purposes. Preclinical studies demonstrate that CACN136 significantly **reduces atherosclerotic plaque formation** and **inhibits inflammation** and **lipid accumulation** in high-fat diet-induced ApoE−/− mice, key processes in atherosclerosis development. The drug functions by regulating **macrophage polarization**—promoting a shift from the pro-inflammatory M1 phenotype toward the anti-inflammatory M2 phenotype—and by modulating lipid metabolism through alterations of cholesterol handling and expression of related proteins such as ABCA1, CD36, and SRA1. These effects result in reduced plasma levels of inflammatory factors including IL-6 and TNF-α, and improvement in aortic pathology. Preclinical data suggests CACN136 offers **superior safety and efficacy compared to simvastatin** at equal doses, and is considered a promising new candidate for the treatment of **atherosclerosis**[1][3][5][7][9].

02

Targets

ABCA1 (ATP-binding cassette transporter A1)ABCG1 (ATP-binding cassette sub-family G member 1)ARG1 (Arginase 1)CD36 (CD36 antigen)SCARB1 (Scavenger receptor class B member 1)SRA1 (Steroid receptor RNA activator 1)NOS2 (Nitric Oxide Synthase 2)MSR1 (Amyloid beta precursor protein binding family B member 3)

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