Drug intelligence / Profile preview

ASLAN001 + fluorouracil + leucovorin

Development stage
Unknown
Lead developer
ASLAN Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

ASLAN001, also known as varlitinib, is a small-molecule, adenosine triphosphate-competitive inhibitor of the tyrosine kinases epidermal growth factor receptor (EGFR/HER1), human epidermal growth factor receptor 2 (HER2), and HER4. It is designed to block signaling through these receptors, which are often dysregulated in various cancers. Fluorouracil and leucovorin are standard chemotherapeutic agents; fluorouracil is a pyrimidine analog that inhibits thymidylate synthase, disrupting DNA synthesis, while leucovorin enhances the binding of fluorouracil to its target enzyme. The combination of ASLAN001 with fluorouracil and leucovorin aims to provide synergistic antitumor activity by targeting both receptor tyrosine kinase signaling pathways and DNA synthesis in cancer cells[1][5].

Other names
varlitinib + fluorouracil + leucovorin
02

Targets

TS (Thymidylate synthase)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB3 (Erb-b2 receptor tyrosine kinase 3)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)

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