Drug intelligence / Profile preview

ASP-3026

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

Overview

**ASP‑3026** is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK). It binds to and inhibits ALK tyrosine kinase, including ALK fusion proteins and point mutation variants. This inhibition disrupts ALK-mediated signaling pathways and suppresses cell growth in tumor cells expressing ALK. ASP‑3026 has also demonstrated inhibitory activity against ROS1 and Ack kinases. The drug was developed by Astellas Pharma for the treatment of various cancers, including solid tumors, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and other advanced malignancies. Clinical development reached phase 1 trials but was discontinued for strategic reasons[1][3][4][5][7].

Other names
N2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)-N4-(2-(propane-2-sulfonyl)phenyl)-1,3,5-triazine-2,4-diamine
02

Targets

TNK2 (Activated Cdc42-associated kinase 1)ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)

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