Drug intelligence / Profile preview

GSK1904529A

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK1904529A, also known as GSK4529, is a potent, selective, orally active, and ATP-competitive small molecule inhibitor of both the insulin-like growth factor-1 receptor (IGF-1R) and the insulin receptor (IR). It has demonstrated activity in preclinical studies, inhibiting the proliferation of various cancer cell lines and reducing tumor growth in xenograft models. Additionally, GSK1904529A has been shown to reverse MRP1-mediated multidrug resistance, suggesting a potential role in overcoming chemotherapy resistance in cancer. Preclinical research also indicates its potential in alleviating inflammation in diabetic kidney disease models.

02

Targets

IGF-1R (Insulin-like growth factor 1 receptor)ABCC1 (MRP1)INSR (Insulin receptor)

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