Drug intelligence / Profile preview

MRG003 + tislelizumab + capecitabine

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

Overview

MRG003 + tislelizumab + capecitabine is a combination therapy regimen being evaluated for the treatment of locally recurrent nasopharyngeal carcinoma. The regimen consists of MRG003 (becotatug vedotin), an antibody-drug conjugate (ADC) targeting the epidermal growth factor receptor (EGFR); tislelizumab, a monoclonal antibody targeting the programmed cell death protein 1 (PD-1) receptor; and capecitabine, an oral fluoropyrimidine carbamate. MRG003 delivers the microtubule-disrupting agent monomethyl auristatin E (MMAE) directly to EGFR-expressing tumor cells. Tislelizumab acts as a checkpoint inhibitor to restore T-cell anti-tumor activity. Capecitabine is converted to 5-fluorouracil in the body, where it inhibits thymidylate synthase to interfere with DNA synthesis. This specific treatment protocol, involving an induction phase followed by maintenance therapy, is currently in Phase 2 clinical trials led by Fujian Cancer Hospital.

Brand names
TevimbraXeloda
Other names
becotatug vedotin + tislelizumab + capecitabine
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)

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