Drug intelligence / Profile preview

MRK16

Development stage
Preclinical
Lead developer
Sanofi
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

MRK16 is a **murine monoclonal antibody** that specifically binds to P-glycoprotein (P-gp), a membrane transporter encoded by the MDR1 gene (ABCB1). P-glycoprotein mediates multidrug resistance (MDR) in tumor cells by actively pumping out chemotherapeutic agents, reducing their intracellular efficacy. MRK16 acts as a **P-glycoprotein inhibitor**; binding of MRK16 blocks the drug efflux activity, thereby sensitizing drug-resistant cancer cells to antitumor agents like vincristine and doxorubicin. MRK16 has also been conjugated to Pseudomonas exotoxin (MRK16-PE) for targeted cell killing of MDR-expressing tumors. Developed originally by Aventis (originator: Hoechst Marion Roussel, Rhône-Poulenc Rorer), MRK16 is primarily used clinically and experimentally to reverse MDR in cancer models and as a diagnostic tool for P-gp-expressing cells[6][3][5][7][8].

Other names
anti-P-glycoprotein monoclonal antibody MRK-16monoclonal antibody MRK-16MRK16-PEMRK-16-PEMRK 16-PE
02

Targets

ABCB1 (P-glycoprotein)

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