Drug intelligence / Profile preview

ASLAN001 + oxaliplatin + capecitabine

Development stage
Unknown
Lead developer
ASLAN Pharmaceuticals
Modality
Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

ASLAN001 (varlitinib) combined with oxaliplatin and capecitabine is an investigational multi-drug regimen studied for the treatment of advanced or metastatic solid tumors, particularly those with dysregulated EGFR or HER2 signaling. Varlitinib is a potent, reversible small-molecule inhibitor targeting the HER-family of receptor tyrosine kinases—specifically EGFR (HER1), HER2, and HER4. By inhibiting these receptors, varlitinib aims to block key pathways involved in tumor growth and survival. Oxaliplatin is a platinum-based chemotherapeutic agent that induces DNA crosslinking and apoptosis in cancer cells. Capecitabine is an oral prodrug converted to 5-fluorouracil (5-FU) in vivo, which inhibits thymidylate synthase and disrupts DNA synthesis. This combination has been evaluated in early-phase clinical trials for patients with metastatic solid tumors suitable for CAPOX regimens or mFOLFOX6[5][4].

Other names
varlitinib + oxaliplatin + capecitabine
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)DNAABCG2 (Breast cancer resistance protein)

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