Drug intelligence / Profile preview

YL242 + pembrolizumab + 5-fluorouracil

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

Overview

YL242 + pembrolizumab + 5-fluorouracil is a combination therapy being evaluated for the treatment of advanced solid tumors. YL242 is a novel, non-internalized antibody-drug conjugate (ADC) developed by MediLink Therapeutics using the proprietary TMALIN® platform. It consists of an anti-VEGF antibody conjugated to a DNA topoisomerase I inhibitor payload (C24) via a protease-cleavable tripeptide linker. This combination pairs the anti-angiogenic and cytotoxic effects of YL242 with the immune checkpoint inhibition of pembrolizumab (a PD-1 inhibitor) and the antimetabolite activity of 5-fluorouracil. The regimen is designed to provide dual anticancer activity through both anti-angiogenesis and cytotoxicity from the extracellularly released payload in the tumor microenvironment, while simultaneously enhancing the immune response. It is currently in Phase 1/2 clinical trials for indications including non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, and gastric/gastroesophageal junction cancers.

Other names
YL242 + pembrolizumab + 5-FU
02

Targets

UNG (Uracil-DNA glycosylase)VEGFA (Vascular endothelial growth factor A)UPP1 (Uridine phosphorylase)TS (Thymidylate synthase)PDCD1 (Programmed cell death protein 1 receptor)

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