Drug intelligence / Profile preview

disitamab vedotin + fruquintinib

Development stage
Unknown
Lead developer
RemeGen
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

Disitamab vedotin + fruquintinib is an investigational combination therapy being studied primarily in patients with HER2-expressing or HER2-amplified metastatic colorectal cancer who have progressed after at least two prior lines of treatment. Disitamab vedotin is a novel antibody-drug conjugate consisting of a humanized anti-HER2 monoclonal antibody linked to the cytotoxic agent monomethyl auristatin E (MMAE) via a cleavable linker. It targets HER2 on tumor cells, leading to internalization and release of MMAE, which disrupts microtubule formation and induces cell death. Fruquintinib is an oral small molecule inhibitor that selectively targets vascular endothelial growth factor receptors 1, 2, and 3 (VEGFR1/2/3), thereby inhibiting angiogenesis required for tumor growth. The rationale behind combining these agents is to simultaneously target tumor cell proliferation through HER2 inhibition/cytotoxicity and suppress tumor angiogenesis via VEGFR blockade[1][5][10].

Brand names
FruzaqlaElunateAidixi
Other names
disitamab vedotin (RC48)
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)ERBB2 (Erb-b2 receptor tyrosine kinase 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)TUBB (Tubulin (alpha and beta subunits))

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