Drug intelligence / Profile preview

tas0612

Development stage
Preclinical
Lead developer
Taiho Oncology
Modality
Small Molecules
Administration
Oral
01

Overview

TAS0612 is a potent, orally available small molecule inhibitor that targets three key kinases involved in cancer cell growth and survival: p90 ribosomal S6 kinase (RSK), AKT (RAC-alpha serine/threonine-protein kinase), and p70 S6 kinase (S6K). By simultaneously inhibiting these kinases, TAS0612 disrupts both the MAPK and PI3K signaling pathways, which are frequently dysregulated in various cancers. Preclinical studies have shown that TAS0612 exhibits strong antitumor activity across multiple tumor models, particularly those with PTEN loss or mutations. The drug has demonstrated greater efficacy than inhibitors targeting only AKT, PI3K, MEK, BRAF, or EGFR/HER2. Its unique profile as a triple kinase inhibitor may help overcome resistance mechanisms associated with single-pathway inhibition. TAS0612 is currently being investigated in phase 1 clinical trials for advanced or metastatic solid tumors[1][2][5][7].

02

Targets

RPS6KB2 (Ribosomal protein S6 kinase 2)RPS6KB1 (Ribosomal protein S6 kinase beta-1)RPS6KA3 (RSK2)RPS6KA1 (Ribosomal S6 kinase Alpha-1)RPS6KA2 (Ribosomal protein S6 kinase alpha-2)AKT2 (Rac-beta serine/threonine-protein kinase)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)

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