Drug intelligence / Profile preview

favezelimab + pembrolizumab + enfortumab vedotin

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

Overview

**favezelimab + pembrolizumab + enfortumab vedotin** is an investigational triple combination therapy designed for advanced urothelial cancer. This regimen combines: - **Favezelimab**, a monoclonal antibody targeting lymphocyte activation gene-3 (LAG-3), inhibiting an immune checkpoint and augmenting T-cell antitumor activity. - **Pembrolizumab**, a programmed death 1 (PD-1) immune checkpoint inhibitor that blocks PD-1 and restores T-cell mediated immune responses against tumor cells. - **Enfortumab vedotin**, an antibody-drug conjugate that targets Nectin-4 (highly expressed in urothelial cancer), delivering the cytotoxic agent monomethyl auristatin E (MMAE) to tumor cells—causing microtubule disruption, cell cycle arrest, and apoptosis. Combined, this modality aims to maximize immune-mediated tumor killing, overcome resistance to single-agent checkpoint inhibitors, and deliver direct cytotoxicity[1][3][5][6]. As of now, this triplet therapy is being studied in clinical trials for patients with advanced or metastatic urothelial carcinoma, but has not yet reached regulatory approval as a combination. Most clinical data to date pertain to the doublet (pembrolizumab + enfortumab vedotin), which is approved for locally advanced and metastatic disease[1][4][5].

02

Targets

TUBB (Tubulin (alpha and beta subunits))PVRL4 (Nectin cell adhesion molecule 4)PDCD1 (Programmed cell death protein 1 receptor)

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