Drug intelligence / Profile preview

becotatug vedotin + sacituzumab tirumotecan

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

Overview

This combination therapy involves the co-administration or comparative use of two antibody-drug conjugates (ADCs): becotatug vedotin (MRG003) and sacituzumab tirumotecan (SKB264/MK-2870). Becotatug vedotin is an EGFR-targeted ADC that delivers the microtubule-disrupting agent monomethyl auristatin E (MMAE) via a cleavable valine-citrulline linker. Sacituzumab tirumotecan is a TROP2-targeted ADC that utilizes a humanized monoclonal antibody (sacituzumab) conjugated to a novel topoisomerase I inhibitor payload (tirumotecan) through a carbonate-based linker. These agents are being evaluated in clinical trials, such as a Phase II study for recurrent or metastatic salivary gland carcinoma (NCT06414330), where they are assigned based on the expression of EGFR and TROP2 on tumor cells. The strategy aims to provide targeted cytotoxic delivery to tumors that overexpress these common epithelial markers, potentially overcoming resistance to standard therapies in head and neck cancers.

Other names
MRG003 + SKB264
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))TOP1 (DNA Topoisomerase I)TACSTD2 (Tumor-associated calcium signal transducer 2)

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