Overview

NCI Definition [1]:
An orally bioavailable, multi-targeted kinase inhibitor with potential antineoplastic activity. Upon oral administration, multi-kinase inhibitor TPX-0022 binds to and inhibits three tyrosine kinases that are often overexpressed in a variety of cancer cell types, including MET (c-Met; hepatocyte growth factor receptor; HGFR) , Src, and colony stimulating factor 1 receptor (CSF1R; CSF-1R; C-FMS; CD115; macrophage colony-stimulating factor receptor; M-CSFR) thereby disrupting their respective signaling pathways. MET, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays an important role in tumor cell proliferation, survival, invasion, and metastasis, and in tumor angiogenesis. Src, a non-receptor tyrosine kinase upregulated in many tumor cell types, plays an important role in tumor cell proliferation, motility, invasiveness and survival. CSF1R is a cell-surface receptor for colony stimulating factor 1 (CSF1); this receptor tyrosine kinase is overexpressed by tumor-associated macrophages (TAMs) in the tumor microenvironment (TME), and plays a major role in both immune suppression and the induction of tumor cell proliferation.

Tpx-0022 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating tpx-0022, 1 is phase 1 (1 open).

EGFR A763_Y764insFQEA, EGFR Codon 719 Missense, and EGFR Exon 19 Deletion are the most frequent biomarker inclusion criteria for tpx-0022 clinical trials.

Adenocarcinoma of the gastroesophageal junction, gastric carcinoma, and hepatocellular carcinoma are the most common diseases being investigated in tpx-0022 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Tpx-0022
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating tpx-0022 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]:
met/src/csf1r tyrosine kinase inhibitor tpx-0022, tpx0022, tpx 0022, multikinase inhibitor tpx-0022, multi-kinase inhibitor tpx-0022
Drug Target(s) [2]:
CSF1R, MET, SRC
NCIT ID [1]:
C162676

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.