Overview

NCI Definition [1]:
An orally bioavailable, receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Upon administration, sitravatinib binds to and inhibits the activity of several RTKs including hepatocyte growth factor receptor (HGFR; c-Met; MET), tyrosine-protein kinase receptor UFO (AXL receptor tyrosine kinase; AXL), mast/stem cell growth factor receptor (SCFR; c-kit; KIT), the receptor tyrosine kinase MER, discoidin domain receptor 2 (DDR2), vascular endothelial growth factor receptor (VEGFR) types 1 (VEGFR-1; FLT1), 2 (VEGFR-2; KDR; Flk-1) and 3 (VEGFR-3), members of the platelet-derived growth factor receptor (PDGFR) family, RET (rearranged during transfection), tropomyosin-related kinases (TRK) and members of the ephrin (Eph) family of receptor tyrosine kinases. This may result in both the inhibition of signal transduction pathways mediated by these RTKs and the reduction of tumor cell proliferation in cancer cell types that overexpress these RTKs.

Sitravatinib has been investigated in 14 clinical trials, of which 14 are open and 0 are closed. Of the trials investigating sitravatinib, 4 are phase 1 (4 open), 1 is phase 1/phase 2 (1 open), 8 are phase 2 (8 open), and 1 is phase 3 (1 open).

EGFR A763_Y764insFQEA, EGFR Codon 719 Missense, and EGFR Exon 19 Deletion are the most frequent biomarker inclusion criteria for sitravatinib clinical trials.

Clear cell renal cell carcinoma, non-small cell lung carcinoma, and malignant solid tumor are the most common diseases being investigated in sitravatinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Sitravatinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating sitravatinib 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]:
multitargeted kinase inhibitor mgcd516, sitravatinib, mgcd516, 1,1-cyclopropanedicarboxamide, n-(3-fluoro-4-((2-(5-(((2-methoxyethyl)amino)methyl)-2-pyridinyl)thieno(3,2-b)pyridin-7-yl)oxy)phenyl)-n'-(4-fluorophenyl)-
Drug Categories [2]:
NTRK1/2/3 inhibitors, RET inhibitors, Tyrosine kinase inhibitors
Drug Target(s) [2]:
AXL, DDR1, DDR2, EPHA1, EPHA10, EPHA2, EPHA3, EPHA4, EPHA5, EPHA7, EPHA8, EPHB1, EPHB2, EPHB4, EPHB6, FLT1, FLT3, KDR, KIT, MET, NTRK1, NTRK2, NTRK3, PDGFRA, RET, TYRO3
NCIT ID [1]:
C117734

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.