Drug intelligence / Profile preview

ZX-4081

Development stage
Phase 1
Lead developer
Zenshine Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

ZX-4081 is an orally bioavailable, highly selective small molecule inhibitor of the gamma isoform of phosphoinositide 3-kinase (PI3Kγ). It is being developed primarily for the treatment of solid tumors, including but not limited to breast cancer, urothelial cancer, ovarian cancer, melanoma, non-small cell lung cancer, renal cell carcinoma, head and neck squamous cell carcinoma, colorectal cancer, and hepatocellular carcinoma. The drug acts by inhibiting PI3Kγ—a molecular switch that controls immune suppression in the tumor microenvironment and promotes immune suppressive myeloid polarization during tumor progression. Inhibition of PI3Kγ has been shown to overcome resistance to checkpoint blockade therapy. ZX-4081 has demonstrated favorable pharmacokinetic properties and efficacy in preclinical solid tumor models. It is currently in Phase I clinical trials as both a single agent and in combination with other anticancer agents[1][3][4][5][6].

Other names
pi3k-gamma inhibitor zx-4081pi-3k-gamma inhibitor zx-4081pi 3k-gamma inhibitor zx-4081
02

Targets

PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)

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