Drug intelligence / Profile preview

GSK-2636771

Development stage
Phase 2
Lead developer
GSK
Modality
Prodrugs/Conditional Activator Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

GSK-2636771 is an orally bioavailable, selective small molecule inhibitor of the phosphatidylinositol 3 kinase beta (PI3Kβ) isoform, developed primarily for the treatment of solid tumors. It acts by selectively inhibiting PI3Kβ kinase activity within the PI3K/Akt/mTOR pathway, which can result in tumor cell apoptosis and growth inhibition in PI3Kβ-expressing and/or PTEN-deficient tumor cells. Dysregulation of this pathway is common in various cancers and contributes to tumor growth, survival, and resistance to therapy. The drug was developed by GSK (GlaxoSmithKline), with Yonsei University Health System also involved as a developer. Clinical development reached Phase I/II for gastric cancer but was discontinued for malignant melanoma, prostate cancer, and other solid tumors[1][2][3][5].

Other names
1372540-25-42-methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acidUNII-DW94IAT0LSUNII-DW-94IAT0LSUNII-DW 94IAT0LS
02

Targets

GPR39 (G protein-coupled receptor 39)

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