Drug intelligence / Profile preview

PF-06895751

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

Overview

PF-06895751 (also known as RN927) is an antibody-drug conjugate (ADC) developed by Pfizer for the treatment of advanced solid tumors. It consists of a humanized monoclonal antibody targeting Programmed Death-Ligand 1 (PD-L1) conjugated to the potent microtubule-disrupting agent monomethyl auristatin E (MMAE) via a protease-cleavable valine-citrulline linker. The ADC is designed to bind to PD-L1-expressing tumor cells, undergo internalization, and release the cytotoxic MMAE payload intracellularly, leading to cell cycle arrest and apoptosis. Beyond its direct cytotoxic effects, PF-06895751 may also function as a checkpoint inhibitor by blocking the PD-1/PD-L1 interaction, potentially enhancing the anti-tumor immune response within the tumor microenvironment.

Other names
anti-PD-L1-vcMMAEanti-PD-L-1-vcMMAEanti-PD-L 1-vcMMAEPD-L1 ADCPD-L-1 ADCPD-L 1 ADC
02

Targets

SLC22A8 (Organic anion transporter 3)OCT1 (Organic cation transporter 1)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)ABCB1 (P-glycoprotein)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)SLC47A1 (Multidrug and toxin extrusion transporter 1)ABCG2 (Breast cancer resistance protein)

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