Drug intelligence / Profile preview

DX1002

Development stage
Unknown
Lead developer
Guangzhou Anhao Pharmaceutical Technology
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

DX1002 is a novel, orally bioavailable, small-molecule tubulin inhibitor that specifically targets the beta subunit of tubulin in tumor vascular endothelial cells. Its primary mechanism is to disrupt tumor vasculature, leading to destruction of blood vessels supplying tumors and subsequent tumor necrosis. Preclinical studies have demonstrated its efficacy in causing tumor vasculature destruction and necrosis in xenograft models. In clinical trials, DX1002 has shown preliminary anti-tumor activity and manageable safety profiles in patients with advanced solid tumors, including hepatocellular carcinoma (HCC) and gastric cancer. The most common treatment-related adverse events include nausea, vomiting, fatigue, increased liver enzymes (aspartate aminotransferase), albuminuria, hypoalbuminemia, and increased gamma-glutamyl transferase[1][3][4].

02

Targets

TUBB (Tubulin (alpha and beta subunits))

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