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    DRUG CLASS:

    Tyrosine kinase inhibitor

    Related drugs:
    11d
    NEO COMBAT XL: H&N NEO-COMBAT XL: Neoadjuvant XL-092 (Zanzalintinib) and Pembrolizumab (Keytruda) in Surgically Resectable, HPV Negative Oral Cavity Squamous Cell Carcinoma (OCSCC) (clinicaltrials.gov)
    P2, N=26, Not yet recruiting, UNC Lineberger Comprehensive Cancer Center
    New P2 trial
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    PD-L1 (Programmed death ligand 1)
    |
    Keytruda (pembrolizumab) • zanzalintinib (XL092)
    12d
    KC1036 in Combination With PD-1 Antibody and Platinum-based Chemotherapy for First-line Advanced Esophageal Cancer (clinicaltrials.gov)
    P2, N=60, Recruiting, Beijing Konruns Pharmaceutical Co., Ltd.
    New P2 trial
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    cisplatin • paclitaxel • Loqtorzi (toripalimab-tpzi) • KC1036
    14d
    COMO: A Phase 3 Randomized, Double-Masked Study Comparing the Efficacy of EYP-1901 Against Aflibercept in DME (clinicaltrials.gov)
    P3, N=240, Recruiting, EyePoint Pharmaceuticals, Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Eylea (aflibercept intravitreal)
    14d
    Befotertinib restored chemosensitivity to multidrug-resistant cancer cells by inhibiting the drug efflux activity of ABCB1. (PubMed, J Pharm Pharmacol)
    These results identify befotertinib as a functional inhibitor of ABCB1 with the capacity to reverse MDR. The findings support its potential as a repurposed agent for combination therapy in tumors with high ABCB1 expression, offering a practical strategy to enhance chemotherapy efficacy.
    Journal
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    EGFR (Epidermal growth factor receptor) • ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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    Semena (befotertinib)
    17d
    A Multi-Center Single-Arm Phase 2 Trial Of Zanzalintinib In Combination With Cemiplimab In BRAF Wild-Type Anaplastic Thyroid Cancer: The ZEPHYR Trial (clinicaltrials.gov)
    P2, N=12, Not yet recruiting, M.D. Anderson Cancer Center
    New P2 trial
    |
    PD-L1 (Programmed death ligand 1) • BRAF (B-raf proto-oncogene)
    |
    BRAF V600E • BRAF V600 • BRAF wild-type
    |
    Libtayo (cemiplimab-rwlc) • zanzalintinib (XL092)
    26d
    CAPRI: A Phase 3 Randomized, Double-Masked Study Comparing the Efficacy of EYP-1901 Against Aflibercept in DME (clinicaltrials.gov)
    P3, N=240, Recruiting, EyePoint Pharmaceuticals, Inc.
    New P3 trial
    |
    Eylea (aflibercept intravitreal)
    26d
    COMO: A Phase 3 Randomized, Double-Masked Study Comparing the Efficacy of EYP-1901 Against Aflibercept in DME (clinicaltrials.gov)
    P3, N=240, Not yet recruiting, EyePoint Pharmaceuticals, Inc.
    New P3 trial
    |
    Eylea (aflibercept intravitreal)
    1m
    A Phase 2 Trial of Zanzalintinib in Advanced/Metastatic Bone Sarcomas (ZAMBONE) (clinicaltrials.gov)
    P2, N=70, Recruiting, M.D. Anderson Cancer Center | Active, not recruiting --> Recruiting
    Enrollment open
    |
    zanzalintinib (XL092)
    1m
    A Study of Zanzalintinib in Participants With Recurrent or Progressive Meningioma (clinicaltrials.gov)
    P2, N=100, Not yet recruiting, Exelixis
    New P2 trial
    |
    zanzalintinib (XL092)
    1m
    XL092-311: A Phase 2/3 clinical trial with zanzalintinib versus everolimus (2025-521043-20-00)
    P2/3, N=172, Not yet recruiting, Exelixis Inc.
    New P2/3 trial
    |
    SSTR (Somatostatin Receptor)
    |
    SSTR positive
    |
    everolimus • zanzalintinib (XL092)
    1m
    Myeloid-derived suppressor cells and regulatory T cells in colorectal cancer: a synergistic immunosuppressive axis and emerging therapeutic opportunities. (PubMed, Front Immunol)
    Emerging clinical and translational data indicate that disrupting this axis can sensitize MSS-CRC to ICIs: for example, Zanzalintinib combined with Atezolizumab reported survival benefit in the STELLAR-303 trial, and dual blockade of novel checkpoints with PD-(L)1 has been associated with enhanced immune activation in solid tumors. Targeting the MDSC-Treg axis therefore represents a promising strategy to overcome immunotherapy resistance in MSS/pMMR CRC.
    Review • Journal
    |
    HIF1A (Hypoxia inducible factor 1, alpha subunit) • CD73 (5'-Nucleotidase Ecto) • TIGIT (T Cell Immunoreceptor With Ig And ITIM Domains 2) • TLR4 (Toll Like Receptor 4) • CXCL3 (C-X-C Motif Chemokine Ligand 3)
    |
    Tecentriq (atezolizumab) • zanzalintinib (XL092)
    1m
    ctDNA Monitoring Guides the Treatment of NSCLC With Befotertinib Combined With Radiotherapy (clinicaltrials.gov)
    P2, N=84, Not yet recruiting, Hebei Medical University Fourth Hospital
    New P2 trial • Circulating tumor DNA
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion
    |
    Semena (befotertinib)