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GSK5757810

Development stage: Unknown
Lead developer: GSK
Modality: Small Molecules
Administration: Intravenous

Overview

GSK5757810 is a cytotoxic small molecule that serves as the payload component of the antibody-drug conjugate (ADC) mocertatug rezetecan (GSK5733584). Developed by GSK, GSK5757810 is a camptothecin derivative that acts as a DNA topoisomerase I inhibitor. In the context of the ADC, it is conjugated to a monoclonal antibody via a cleavable linker; upon internalization into cancer cells, the free cytotoxin is released to induce DNA damage and cell death. It is currently being investigated in Phase 1/2 clinical trials as the warhead of mocertatug rezetecan for the treatment of advanced solid tumors and gynecologic cancers.

Other names: GSK5757810 payloadGSK-5757810 payloadGSK 5757810 payloadGSK5757810 cytotoxinGSK-5757810 cytotoxinGSK 5757810 cytotoxin

Targets

PRMT5 (Protein arginine N-methyltransferase 5)

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