Drug intelligence / Profile preview

brigatinib + neratinib

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

**Brigatinib + neratinib** is a putative oral combination of two small molecule tyrosine kinase inhibitors: **brigatinib**, approved for anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC), and **neratinib**, approved for HER2-positive breast cancer. Brigatinib inhibits ALK, ROS1, insulin-like growth factor 1 receptor (IGF-1R), and several other kinases by blocking phosphorylation and subsequent oncogenic signaling. Neratinib is an irreversible pan-HER tyrosine kinase inhibitor, targeting EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4), with clinical utility in various HER2-positive cancers. No clinical or preclinical studies currently report the combination of brigatinib + neratinib as either a therapeutic regimen or investigational product; therefore, all mechanistic and disease context is inferred from their respective monotherapies.

02

Targets

ALK (Anaplastic lymphoma kinase receptor tyrosine kinase)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)ROS1 (Proto-oncogene tyrosine-protein kinase ROS)IGF-1R (Insulin-like growth factor 1 receptor)ERBB4 (Erb-b2 receptor tyrosine kinase 4)

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