Drug intelligence / Profile preview

AT13148

Development stage
Phase 1
Lead developer
Cancer Research UK
Modality
Small Molecules
Administration
Oral
01

Overview

AT13148 is an orally active, ATP-competitive small molecule inhibitor that targets multiple AGC kinases, most notably Rho-associated protein kinase (ROCK) and protein kinase B (AKT). It was developed as a dual ROCK-AKT inhibitor with the aim of blocking cancer cell proliferation and metastasis by inhibiting key signaling pathways involved in tumor growth and survival. Preclinical studies demonstrated anti-metastatic and anti-proliferative activity across several cancer models. In clinical trials, AT13148 was evaluated for advanced solid tumors but did not demonstrate significant tumor shrinkage; its development was discontinued due to a narrow therapeutic index and unfavorable pharmacokinetic profile[1][5][6].

02

Targets

SGK1RPS6KB1 (Ribosomal protein S6 kinase beta-1)ROCK2 (Rho-associated coiled-coil containing protein kinase 2)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)ROCK1 (Rho-associated coiled-coil containing protein kinase 1)PKA (Cyclic amp-dependent protein kinase)

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