Drug intelligence / Profile preview

XH-30002 + afatinib

Development stage
Phase 1
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.

Other names
afatinib dimaleateAfatiinb
02

Targets

EGFR (Epidermal growth factor receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)PTPN11 (Tyrosine-protein phosphatase non-receptor type 11)

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