Drug intelligence / Profile preview

LGK974 + PDR001

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

Overview

**LGK974 + PDR001** is a combination investigational cancer therapy consisting of LGK974, a small molecule inhibitor of the enzyme *porcupine* (critical for activating Wnt signaling), and PDR001 (spartalizumab), a monoclonal antibody targeting PD-1. LGK974 inhibits Wnt signaling by blocking palmitoylation and secretion of Wnt ligands, and is intended for use in Wnt-ligand dependent cancers. PDR001 acts as an immune checkpoint inhibitor by blocking the programmed cell death protein 1 (PD-1) pathway, thereby enhancing the anti-tumor immune response. This combination has been investigated for advanced malignancies, including melanoma, lung squamous cell carcinoma, head and neck squamous cell carcinoma, esophageal squamous cell carcinoma, cervical squamous cell carcinoma, and triple-negative breast cancer, particularly in patients refractory to prior anti-PD-1 treatment[1][3][5].

Other names
LGK974 + PDR001WNT974 + spartalizumab
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)PORCN (Porcupine protein)

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