Drug intelligence / Profile preview

vibetocotumab

Development stage
Unknown
Lead developer
Lepu Biopharma
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Vibetocotumab (MRG003) is an antibody-drug conjugate (ADC) targeting the epidermal growth factor receptor (EGFR). It is composed of a humanized anti-EGFR monoclonal antibody conjugated to the potent microtubule-disrupting agent monomethyl auristatin E (MMAE) via a protease-cleavable valine-citrulline (vc) linker. Upon binding to EGFR on the surface of tumor cells, the ADC is internalized through endocytosis and transported to lysosomes, where the linker is cleaved to release MMAE. The released payload then inhibits tubulin polymerization, leading to cell cycle arrest and apoptosis. Vibetocotumab is primarily being developed for the treatment of EGFR-overexpressing solid tumors, including head and neck squamous cell carcinoma (HNSCC), nasopharyngeal carcinoma (NPC), and oral squamous cell carcinoma.

Other names
vibetocotumabEGFR-ADCanti-EGFR ADC
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))

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