Drug intelligence / Profile preview

GRWD5769 + cemiplimab

Development stage
Unknown
Lead developer
Grey Wolf Therapeutics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

GRWD5769 + cemiplimab is an investigational combination therapy consisting of GRWD5769, an oral, potent, and selective first-in-class ERAP1 inhibitor developed by Grey Wolf Therapeutics, and cemiplimab, a fully human monoclonal antibody targeting programmed death receptor-1 (PD-1), marketed as Libtayo. GRWD5769 modulates the tumor immunopeptidome by inhibiting ERAP1, leading to the presentation of novel neoantigens and enhancing anti-tumor T cell responses, thereby circumventing T cell exhaustion, a key resistance mechanism in immuno-oncology[1][3][5]. Cemiplimab blocks PD-1, enhancing T cell-mediated anti-tumor activity. The combination aims to boost anti-tumor immunity beyond what either agent can achieve alone and is currently in early-phase clinical testing for advanced solid tumors[1][5].

Other names
GRWD5769 + Libtayo
02

Targets

ERAP1 (Endoplasmic reticulum aminopeptidase 1)PDCD1 (Programmed cell death protein 1 receptor)

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