Drug intelligence / Profile preview

afuresertib + carboplatin + paclitaxel

Development stage
Unknown
Lead developer
Laekna
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Afuresertib (GSK2110183) is a potent, orally bioavailable small molecule inhibitor of the serine/threonine protein kinase Akt (protein kinase B), with high selectivity for Akt1, Akt2, and Akt3. It acts as an ATP-competitive inhibitor and blocks the PI3K/Akt signaling pathway, leading to inhibition of tumor cell proliferation and induction of apoptosis. Afuresertib has demonstrated antineoplastic activity in preclinical models and clinical trials. In combination with carboplatin and paclitaxel—two standard chemotherapeutic agents—it has been investigated for the treatment of recurrent ovarian cancer as well as other solid tumors. Carboplatin is a platinum-based DNA crosslinking agent that induces apoptosis by causing DNA damage; paclitaxel stabilizes microtubules to inhibit cell division. The combination aims to enhance anti-tumor efficacy by targeting multiple pathways involved in cancer growth and resistance[1][2][4][5][8].

Other names
afuresertib
02

Targets

AKT2 (Rac-beta serine/threonine-protein kinase)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)DNATUBB (Tubulin (alpha and beta subunits))

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