Overview

Generic Name(s):
defactinib
NCI Definition [1]:
An orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. Defactinib inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including those involving RAS/MEK/ERK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation, survival, and tumor angiogenesis. The tyrosine kinase FAK, a signal transducer for integrins, is normally activated by binding to integrins in the extracellular matrix (ECM) but may be upregulated and constitutively activated in various tumor cell types.

Defactinib has been investigated in 10 clinical trials, of which 7 are open and 3 are closed. Of the trials investigating defactinib, 3 are phase 1 (1 open), 2 are phase 1/phase 2 (2 open), and 5 are phase 2 (4 open).

KRAS Mutation, HRAS Mutation, and NRAS Mutation are the most frequent biomarker inclusion criteria for defactinib clinical trials.

Low grade ovarian serous adenocarcinoma, malignant pleural mesothelioma, and malignant solid tumor are the most common diseases being investigated in defactinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Defactinib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Defactinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating defactinib 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]:
vs-6063, benzamide, n-methyl-4-((4-(((3-(methyl(methylsulfonyl)amino)-2-pyrazinyl)methyl)amino)-5-(trifluoromethyl)-2-pyrimidinyl)amino)-, pf-04554878, defactinib, defactinib
Drug Categories [2]:
PTK2 (FAK) inhibitors, Therapeutic antibodies
Drug Target(s) [2]:
PTK2
NCIT ID [1]:
C79809

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.