Drug intelligence / Profile preview

BLZ945 + spartalizumab

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

Overview

BLZ945 + spartalizumab is an investigational combination therapy for cancer composed of two agents: - **BLZ945 (sotuletinib):** an orally bioavailable, brain-penetrant, highly selective small molecule inhibitor of colony-stimulating factor 1 receptor (**CSF1R**). BLZ945 reduces recruitment of tumor-associated macrophages (TAMs), depletes TAM populations, alters the tumor microenvironment, and inhibits tumor growth. In animal models and early-phase clinical trials, it has been investigated especially for tumors with high TAM infiltration, such as glioblastoma multiforme (GBM) and pancreatic cancer. - **Spartalizumab (PDR001):** a humanized monoclonal IgG4 antibody targeting programmed cell death protein 1 (**PD-1**), functioning as an immune checkpoint inhibitor to enhance T-cell mediated anti-tumor immune responses. The combination aims to overcome resistance to single-agent PD-1 blockade by modulating myeloid-derived suppression and concurrently unleashing T-cell activity. Clinical trials focused on advanced or refractory solid tumors, including GBM, pancreatic, colorectal, and head and neck cancers.

Other names
BLZ945 + PDR001sotuletinib + spartalizumab
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)CSF1R (Macrophage colony-stimulating factor receptor)

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