Drug intelligence / Profile preview

amcasertib + paclitaxel

Development stage
Preclinical
Lead developer
Sumitomo Pharma America
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**Amcasertib + paclitaxel** is an investigational combination therapy for cancer, consisting of amcasertib, a first-in-class oral small molecule inhibitor of cancer stemness pathways, and paclitaxel, a widely used microtubule inhibitor chemotherapeutic. - **Amcasertib** (also known as BBI-503) targets multiple serine-threonine kinases involved in the maintenance and survival of cancer stem cells, notably inhibiting transcription factors like Nanog and other key stemness-related pathways, resulting in apoptosis and reduced invasion/migration of cancer stem cells[2][5][6][8]. - **Paclitaxel** is an established chemotherapeutic agent that works by stabilizing microtubules, preventing cell division, and inducing cell death. - This combination is being studied for synergistic anticancer effects, particularly against solid tumors such as breast, ovarian, and gastrointestinal cancers, by addressing chemoresistance and relapse driven by cancer stem cells[2][5][4]. - Amcasertib has shown efficacy in preclinical studies against breast and ovarian cancer stem cells, and has reached up to phase II trials in solid tumors as a single agent and in combination with other agents. However, there is no published evidence of regulatory approval or phase III clinical data for the amcasertib + paclitaxel combination.

02

Targets

Stemness-associated serine-threonine kinasesTUBB (Tubulin (alpha and beta subunits))

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