Drug intelligence / Profile preview

GSK5764227 + pembrolizumab

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

Overview

GSK5764227 + pembrolizumab is a **combination of an investigational antibody-drug conjugate (GSK5764227, a B7-H3-targeted ADC) and the anti-PD-1 monoclonal antibody pembrolizumab (KEYTRUDA)**. GSK5764227 is composed of a fully humanized monoclonal antibody targeting B7-H3, covalently linked via a protease-cleavable linker to a topoisomerase I inhibitor payload. It is designed to selectively target and kill B7-H3-expressing tumor cells, leveraging both direct cytotoxicity and immune modulation[2][4]. Pembrolizumab is a humanized monoclonal antibody targeting the programmed cell death protein 1 (PD-1), blocking its interaction with PD-L1 and PD-L2, thereby promoting T-cell-mediated anti-tumor responses[7]. The combination is being investigated for **advanced solid tumors and relapsed/refractory cancers**, where synergistic effects of targeted cytotoxicity and immune checkpoint blockade may enhance anti-tumor efficacy[3].

Other names
GSK-227GSK227GSK 227GSK B7-H3 ADChuman anti–B7-H3 ADCanti–B7-H3 ADCPembrolizumab
02

Targets

B7-H3PDCD1 (Programmed cell death protein 1 receptor)

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