Drug intelligence / Profile preview

xl888

Development stage
Phase 1
Lead developer
Exelixis
Modality
Small Molecules
Administration
Oral
01

Overview

XL888 is a fully synthetic, orally available small molecule that acts as a potent and selective ATP-competitive inhibitor of heat shock protein 90 (HSP90), a molecular chaperone involved in the regulation of multiple oncogenic proteins. Unlike natural product-based HSP90 inhibitors, XL888 was designed for improved oral bioavailability and tolerability. Preclinical studies have shown that it inhibits proliferation across various human tumor cell lines and induces degradation of key HSP90 client proteins such as BRAF, MET, and HER2. It has demonstrated substantial anti-tumor activity in xenograft models and preferential retention in tumors compared to plasma or liver. The drug was discovered by Exelixis and has been investigated primarily for the treatment of cancers driven by HSP90 client proteins, including malignant melanoma and gastrointestinal cancers[1][3][7].

Other names
Heat Shock Protein 90 Inhibitor XL888Hsp90 Inhibitor XL888Hsp-90 Inhibitor XL888Hsp 90 Inhibitor XL888
02

Targets

HSP90 (Heat shock protein 90 chaperone complex)

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