Drug intelligence / Profile preview

ipatasertib + docetaxel

Development stage
Phase 2
Lead developer
Genentech
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Ipatasertib + docetaxel is a combination therapy consisting of **ipatasertib**, an oral, selective, ATP-competitive inhibitor of **AKT (protein kinase B)**, and **docetaxel**, an intravenous chemotherapeutic agent classified as a taxane that acts as a microtubule inhibitor. Ipatasertib targets the PI3K/AKT signaling pathway, which is frequently dysregulated in human cancers, especially those with PTEN loss, leading to unregulated cell proliferation and survival. Docetaxel stabilizes microtubules and inhibits their depolymerization, disrupting cell division. The combination aims to leverage potential synergy, as AKT inhibition can sensitize tumor cells to chemotherapy. Clinical trials are evaluating this combination primarily in advanced solid tumors, metastatic non-small cell lung cancer (NSCLC), and metastatic castration-resistant prostate cancer (mCRPC)[1][2][5].

02

Targets

AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)AKT2 (Rac-beta serine/threonine-protein kinase)AKT3 (RAC-gamma serine/threonine-protein kinase)TUBB (Tubulin (alpha and beta subunits))

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