Drug intelligence / Profile preview

GSK-690693

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Intravenous
01

Overview

GSK-690693 is a small molecule, ATP-competitive pan-Akt kinase inhibitor developed by GSK (GlaxoSmithKline) for oncology indications. It potently inhibits all three Akt isoforms (Akt1 IC50 = 2 nM, Akt2 IC50 = 13 nM, Akt3 IC50 = 9 nM), with some activity against other AGC kinase family members such as AMPK and PKA at higher concentrations. The drug was investigated in clinical trials for the treatment of various cancers including solid tumors, lymphoma, and hematologic malignancies. Preclinical studies showed antiproliferative and pro-apoptotic effects in tumor cell lines and xenograft models; however, its clinical development was terminated due to dose-limiting toxicity—specifically transient hyperglycemia[1][2][4][6].

02

Targets

AKT2 (Rac-beta serine/threonine-protein kinase)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)

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