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    DRUG CLASS:

    CXCR2 antagonist

    Related drugs:
    3d
    SX-682 and Atezolizumab for the Treatment of Advanced or Metastatic, Recurrent Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=32, Not yet recruiting, University of Washington | Initiation date: Jun 2026 --> Sep 2026
    Trial initiation date • Checkpoint inhibition
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    ALK (Anaplastic lymphoma kinase) • RET (Ret Proto-Oncogene) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • CXCL8 (Chemokine (C-X-C motif) ligand 8)
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    RET fusion • ALK fusion • ROS1 fusion
    |
    SX-682 • Tecentriq Hybreza (atezolizumab and hyaluronidase-tqjs)
    8d
    SYNERGY-201: Study of SX-682 Plus Enzalutamide in Men With ARPI-Resistant Metastatic Castration Resistant Prostate Cancer (clinicaltrials.gov)
    P2, N=53, Recruiting, Syntrix Biosystems, Inc. | Trial primary completion date: Jun 2026 --> Jun 2027
    Trial primary completion date
    |
    enzalutamide • SX-682
    1m
    Reparixin in Patients With Myelofibrosis Myeloproliferative Neoplasms Research Consortium (MPN-RC 120) (clinicaltrials.gov)
    P2, N=10, Recruiting, Icahn School of Medicine at Mount Sinai | N=26 --> 10 | Trial primary completion date: Dec 2026 --> Dec 2027
    Enrollment change • Trial primary completion date
    |
    reparixin (DF 1681Y)
    2ms
    A Study of Eltrekibart (LY3041658) in Healthy Participants (clinicaltrials.gov)
    P1, N=60, Not yet recruiting, Eli Lilly and Company
    New P1 trial
    3ms
    SX-682 and Atezolizumab for the Treatment of Advanced or Metastatic, Recurrent Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=32, Not yet recruiting, University of Washington | Initiation date: Mar 2026 --> Jun 2026
    Trial initiation date • Checkpoint inhibition
    |
    ALK (Anaplastic lymphoma kinase) • RET (Ret Proto-Oncogene) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • CXCL8 (Chemokine (C-X-C motif) ligand 8)
    |
    RET fusion • ALK fusion • ROS1 fusion
    |
    SX-682 • Tecentriq Hybreza (atezolizumab and hyaluronidase-tqjs)
    3ms
    DysUFMylation reprograms immunosuppressive neutrophils to potentiate anti-PD-1 therapy in hepatocellular carcinoma. (PubMed, Cancer Lett)
    Low UFL1 expression synergized with anti-PD-1 therapy to prolong survival in orthotopic and spontaneous HCC models, whereas pharmacologic inhibition of CXCL8-CXCR1/2 signaling using SX-682 recapitulated these effects. Clinically, patients who responded to immunotherapy exhibited reduced UFL1, PRMT5 and CXCL8 expression; decreased neutrophil infiltration; elevated CD8+ T-cell activity; and lower serum CXCL8 levels. These findings reveal a UFL1-PRMT5-NF-κB p65-CXCL8 axis that governs neutrophil-driven immunosuppression and identify CXCL8 as both a predictive biomarker and therapeutic target to optimize immunotherapy in patients with HCC.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    CD8 (cluster of differentiation 8) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • PRMT5 (Protein Arginine Methyltransferase 5) • CXCR1 (Chemokine (C-X-C motif) receptor 1)
    |
    SX-682
    4ms
    FRY Mediates THP1-Driven Ovarian Cancer Invasion Through the PI3K/AKT Pathway. (PubMed, Cells)
    Pharmacological inhibition of the CXCR1/2 axis with reparixin effectively blocked OCM-mediated induction of both NFIX and FRY, suggesting that chemokine signaling initiates this pro-invasive loop. Collectively, these findings suggest that FRY is a macrophage-driven mediator of invasion and underscore its potential relevance in ovarian cancer.
    Journal
    |
    AKT1 (V-akt murine thymoma viral oncogene homolog 1) • CXCR1 (Chemokine (C-X-C motif) receptor 1) • GLI2 (GLI Family Zinc Finger 2)
    |
    reparixin (DF 1681Y)
    5ms
    Exploratory research on therapeutic agents combined with early diagnostic biomarkers for colorectal cancer. (PubMed, Front Pharmacol)
    This study systematically delineates a novel panel of early-detection biomarkers for CRC and identifies SB-225002 as a repurposed candidate therapeutic agent. The integrative strategy combining multi-cohort transcriptomic analysis, drug-repositioning platforms, molecular docking, and experimental validation offers a feasible framework for discovering clinically actionable biomarkers and small-molecule therapies for CRC.
    Journal
    |
    ALDH1A1 (Aldehyde Dehydrogenase 1 Family Member A1) • MELK (Maternal Embryonic Leucine Zipper Kinase) • CXCL3 (C-X-C Motif Chemokine Ligand 3) • FABP4 (Fatty Acid Binding Protein 4) • MAD2L1 (Mitotic Arrest Deficient 2 Like 1) • MCM2 (Minichromosome maintenance complex component 2)
    |
    SB225002
    5ms
    NR4A2 induces perineural invasion in head and neck squamous cell carcinoma and pancreatic ductal adenocarcinoma via CXCL5/CXCR2 signaling axis. (PubMed, Cancer Lett)
    Further treatment with CXCL5 ligand significantly induced neuritogenesis, while the neurite outgrowth was abrogated when cotreated with CXCR2 (receptor for CXCL5) inhibitor SCH527123...NR4A2 knockdown in UMSCC1 cells impaired tumor formation in vivo, and the xenograft tissues exhibited significant downregulation of CXCL5, providing direct in vivo evidence for the NR4A2-CXCL5 axis in tumor progression. NR4A2 is a key driver of CXCL5-mediated PNI and the NR4A2/CXCL5/CXCR2 signaling axis is a potential therapeutic target in HNSCC and PDAC.
    Journal
    |
    RAC1 (Rac Family Small GTPase 1) • CCL2 (Chemokine (C-C motif) ligand 2) • TIMP2 (TIMP Metallopeptidase Inhibitor 2) • CXCL5 (Chemokine (C-X-C motif) ligand 5) • CXCR2 (Chemokine (C-X-C motif) receptor 2) • NR4A2 (Nuclear Receptor Subfamily 4 Group A Member 2)
    |
    navarixin (MK-7123)
    5ms
    SX-682 and Nivolumab for the Treatment of RAS-Mutated, MSS Unresectable or Metastatic Colorectal Cancer, the STOPTRAFFIC-1 Trial (clinicaltrials.gov)
    P1/2, N=51, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Jan 2026 --> Jul 2026 | Trial primary completion date: Jan 2026 --> Jul 2026
    Trial completion date • Trial primary completion date
    |
    BRAF (B-raf proto-oncogene)
    |
    Opdivo (nivolumab) • SX-682
    5ms
    Unlocking the Power of CXCR2 Inhibition to Overcome Gemcitabine Resistance in Pancreatic Cancer. (PubMed, FASEB Bioadv)
    We treated parental and GemR cell lines with gemcitabine in combination with a CXCR2 antagonist, Navarixin. In conclusion, these findings highlight the critical role of the CXCR2 axis in PDAC therapy resistance. Targeting CXCR2 enhances gemcitabine efficacy, offering a potential therapeutic strategy to overcome resistance in PDAC.
    Journal
    |
    CXCL8 (Chemokine (C-X-C motif) ligand 8) • CXCL5 (Chemokine (C-X-C motif) ligand 5) • CXCR2 (Chemokine (C-X-C motif) receptor 2) • ITGB2 (Integrin Subunit Beta 2) • CXCL1 (Chemokine (C-X-C motif) ligand 1)
    |
    gemcitabine • navarixin (MK-7123)
    5ms
    SX-682 and Atezolizumab for the Treatment of Advanced or Metastatic, Recurrent Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=32, Not yet recruiting, University of Washington
    New P2 trial • Checkpoint inhibition
    |
    ALK (Anaplastic lymphoma kinase) • RET (Ret Proto-Oncogene) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • CXCL8 (Chemokine (C-X-C motif) ligand 8)
    |
    RET fusion • ALK fusion • ROS1 fusion
    |
    SX-682 • Tecentriq Hybreza (atezolizumab and hyaluronidase-tqjs)