Drug intelligence / Profile preview

pifusertib

Development stage
Phase 2
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

TAS-117 (also known as pifusertib) is a highly potent, selective, orally active allosteric inhibitor of Akt (protein kinase B), targeting all three isoforms (Akt1, Akt2, and Akt3). It is being developed primarily for the treatment of advanced or metastatic solid tumors with aberrations in the PI3K/Akt pathway, including those harboring mutations in PIK3CA or loss-of-function mutations in PTEN. TAS-117 inhibits cell proliferation by blocking downstream signaling from activated Akt, which plays a central role in tumor cell survival and growth. Preclinical studies have demonstrated its ability to induce cell cycle arrest and apoptosis in cancer cells. Clinical trials have evaluated its safety and efficacy particularly in patients with advanced solid tumors refractory to standard therapies[1][2][4][5][6].

Other names
pifusertib
02

Targets

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

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