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sx-682

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Overview

NCI Definition [1]:
An orally bioavailable, selective and reversible antagonist of C-X-C motif chemokine receptors 1 (CXCR1) and 2 (CXCR2), with potential anti-inflammatory and antineoplastic activities. Upon administration CXCR1/2 inhibitor SX-682 selectively and allosterically binds to CXCR 1 and 2 and inhibits their activation by tumor-secreted chemokines. 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-induced 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. CXCR1 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 and myeloid cell suppression. They play a key role in inflammation and their expression is elevated in several inflammatory-driven diseases.

Clinical Trials

View Clinical Trials for sx-682

Sx-682 has been investigated in 5 clinical trials, of which 5 are open and 0 are closed. Of the trials investigating sx-682, 3 are phase 1 (3 open) and 2 are phase 1/phase 2 (2 open).

ER Negative, ER No Expression, and HER2 Deficient Expression are the most frequent biomarker inclusion criteria for sx-682 clinical trials.

Breast carcinoma, colorectal adenocarcinoma, and malignant solid tumor are the most common diseases being investigated in sx-682 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Sx-682
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating sx-682 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-(((5-((4-fluorophenyl)carbamoyl)pyrimidin-2-yl)thio)methyl)-4-(trifluoromethoxy)phenyl)boronic acid, cxcr1/2 inhibitor sx-682, sx 682, sx682
Drug Target(s) [2]:
CXCR1, CXCR2
NCIT ID [1]:
C150389

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.