Drug intelligence / Profile preview

alisertib + esomeprazole

Development stage
Phase 1
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

**alisertib + esomeprazole** is a *combination* of alisertib, a selective small molecule inhibitor of Aurora A kinase developed primarily for advanced malignancies, and esomeprazole, a proton pump inhibitor used to reduce gastric acid secretion. Alisertib inhibits Aurora A kinase, leading to disruption of mitosis and antitumor effects. It is administered orally as an enteric-coated tablet due to its pH-dependent solubility. Esomeprazole increases gastric pH and, when co-administered, has been shown to increase alisertib systemic exposure (AUC) by 28% and peak concentration (Cmax) by 14%, likely due to improved solubility of alisertib at higher gastric pH. The combination has been studied in patients with advanced solid tumors or lymphomas to evaluate potential drug-drug interactions, with common adverse events including diarrhea, alopecia, neutropenia, and fatigue.

02

Targets

AURKA (Aurora kinase A)AURKB (Aurora kinase B)ATP4A (Potassium–transporting ATPase alpha chain 1)

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