Drug intelligence / Profile preview

alectinib + esomeprazole

Development stage
Unknown
Lead developer
Chugai Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

**Alectinib + esomeprazole** is a combination of two drugs: **alectinib**, a small-molecule, oral, highly selective inhibitor of anaplastic lymphoma kinase (ALK) and RET tyrosine kinases, and **esomeprazole**, a proton pump inhibitor that suppresses gastric acid secretion. This combination is relevant primarily from a pharmacokinetic and drug-interaction perspective, as esomeprazole is used to evaluate or manage potential pH-dependent changes in alectinib absorption. Co-administration of esomeprazole does not have a clinically relevant effect on the systemic exposure (AUC or Cmax) of alectinib or its main active metabolite (M4); therefore, alectinib may be administered without concern for absorption changes due to concomitant PPI use. The primary indication for alectinib is the treatment of ALK-positive locally advanced or metastatic non-small cell lung cancer (NSCLC); esomeprazole is not indicated for cancer, but for acid-related GI disorders.

02

Targets

ATP4A (Potassium–transporting ATPase alpha chain 1)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)RET (Rearranged during transfection receptor tyrosine kinase)

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