Drug intelligence / Profile preview

tunlametinib + fruquintinib

Development stage
Preclinical
Lead developer
HUTCHMED
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of **tunlametinib**, a selective MEK inhibitor, and **fruquintinib**, a highly selective vascular endothelial growth factor receptor (VEGFR) 1/2/3 inhibitor. Both are small molecule oral drugs. - **Tunlametinib** inhibits the MEK1/2 kinases in the MAPK pathway, frequently dysregulated in cancer, leading to inhibition of tumor cell proliferation. - **Fruquintinib** inhibits angiogenesis by blocking VEGFR1, VEGFR2, and VEGFR3, disrupting tumor blood supply and exerting antitumor effects. This combination is being clinically investigated for use in certain cancers, notably metastatic colorectal cancer and potentially other solid tumors, based on the rationale that dual inhibition of tumor growth pathways and angiogenesis may yield synergistic antitumor activity[1].

Other names
HMPL-013 (fruquintinib)ELUNATE (fruquintinib, China)tunlametinib (no brand/trade name identified)
02

Targets

PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)RET (Rearranged during transfection receptor tyrosine kinase)

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