Overview

Generic Name(s):
irbinitinib
Trade Name(s):
Tukysa
NCI Definition [1]:
An orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. ErbB-2 inhibitor ARRY-380 selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. ErbB-2 is overexpressed in a variety of cancers and plays an important role in cellular proliferation and differentiation.

Biomarker-Directed Therapies

Tucatinib has been investigated in 20 clinical trials, of which 17 are open and 3 are closed. Of the trials investigating tucatinib, 4 are phase 1 (1 open), 5 are phase 1/phase 2 (5 open), 8 are phase 2 (8 open), 1 is phase 2/phase 3 (1 open), and 2 are phase 3 (2 open).

ERBB2 Amplification, HER2 Overexpression, and HER2 Positive are the most frequent biomarker inclusion criteria for tucatinib clinical trials.

Breast carcinoma, malignant solid tumor, and adenocarcinoma of the gastroesophageal junction are the most common diseases being investigated in tucatinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Tucatinib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Tucatinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating tucatinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
Tukysa, n6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)-n4-(3-methyl-4-((1,2,4)triazolo(1,5-a)pyridin-7-yloxy)phenyl)quinazoline-4,6-diamine, arry-380, irbinitinib, ont-380
Drug Categories [2]:
Tyrosine kinase inhibitors
Drug Target(s) [2]:
ERBB2
NCIT ID [1]:
C77896

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.