Drug intelligence / Profile preview

ceritinib

Development stage
Approved
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Ceritinib is a second-generation, orally active small molecule tyrosine kinase inhibitor developed for the treatment of anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC). It selectively and potently inhibits ALK by blocking its autophosphorylation and downstream signaling pathways, thereby preventing proliferation of ALK-dependent cancer cells. Ceritinib also inhibits other kinases to a lesser extent, including insulin-like growth factor 1 receptor (IGF-1R), insulin receptor, and ROS1. It is particularly effective in patients who have developed resistance to crizotinib or as a first-line therapy for ALK-positive NSCLC. Ceritinib was developed by Novartis and received FDA approval in April 2014.

Brand names
Zykadia
Other names
ceritinibLDK378LDK-378LDK 378Zykadia
02

Targets

ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)IGF-1R (Insulin-like growth factor 1 receptor)INSR (Insulin receptor)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)

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