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navarixin

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Overview

NCI Definition [1]:
An orally available small molecule antagonist of the C-X-C motif chemokine receptor 1 (CXCR1; interleukin-8 receptor alpha; IL8RA) and 2 (CXCR2; interleukin-8 receptor beta; IL8RB), with potential immunomodulating and antineoplastic activities. Upon administration, navarixin binds to and inhibits the activation of CXCR 1 and 2. This inhibits CXCR1/2-mediated signaling, reduces both recruitment and migration of immunosuppressive myeloid-derived suppressor cells (MDSCs) and neutrophils in the tumor microenvironment (TME), inhibits inflammatory processes and abrogates the immunosuppressive nature of the TME. This allows effector cells, such as natural killer (NK) cells and cytotoxic T-lymphocytes (CTLs), to kill and eliminate cancer cells. This inhibits tumor cell migration, metastasis, angiogenesis and tumor cell proliferation. CXCR 1 and 2, G protein-coupled receptor proteins located on myeloid cells and certain tumor cells, play key roles in the immunosuppressive nature of the TME, tumor metastasis, therapy-resistance, myeloid cell suppression, and inflammation.

Clinical Trials

View Clinical Trials for navarixin

Navarixin has been investigated in 1 clinical trial, of which 0 are open and 1 is closed. Of the trial investigating navarixin, 1 is phase 2 (0 open).

Deficient DNA Mismatch Repair (dMMR), MLH1 Deficient Expression, and MSH2 Deficient Expression are the most frequent biomarker inclusion criteria for navarixin clinical trials.

Colorectal carcinoma, non-small cell lung carcinoma, and prostate adenocarcinoma are the most common diseases being investigated in navarixin clinical trials [2].

Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Navarixin
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating navarixin 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]:
2-hydroxy-n,n-dimethyl-3-((2-((1r)-1-(5-methylfuran-2-yl)propyl)amine)-3,4- dioxocyclobut-1-enyl)amino)benzamide monohydrate, ccr2 antagonist pf-04136309, sch 527123, ps291822, mk-7123
Drug Target(s) [2]:
CXCR1, CXCR2
NCIT ID [1]:
C156730

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.