Drug intelligence / Profile preview

XH-30002 + afatinib

Development stage
Unknown
Lead developer
Xuanzhu Biopharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

XH-30002 + afatinib is an investigational combination therapy being evaluated for the treatment of locally advanced or metastatic esophageal squamous cell carcinoma (ESCC). The regimen consists of XH-30002, a small molecule allosteric inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP2), and afatinib, an irreversible covalent inhibitor of the ErbB receptor tyrosine kinase family, including EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4). SHP2 is a critical signaling node that mediates the activation of the RAS/MAPK pathway downstream of various receptor tyrosine kinases; its inhibition is intended to prevent or overcome resistance to ErbB family blockers by suppressing compensatory signaling. Afatinib is an approved therapy for certain non-small cell lung cancers. This specific combination is currently being investigated in a Phase Ib clinical study sponsored by Fujian Cancer Hospital to assess its safety and preliminary efficacy in patients with advanced ESCC.

Brand names
Gilotrif
Other names
afatinib dimaleateAfatiinbAfatiinb-Fujian Cancer Hospital-esophageal squamous cell carcinoma
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)

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