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    DRUG CLASS:

    ROR1-targeted antibody-drug conjugate

    Related drugs:
    9d
    ROR1-PI3K/AKT signaling drives adaptive resistance to cell cycle blockade in TP53 mutated ovarian cancer. (PubMed, Cell Death Dis)
    In this study, we developed long-term resistant (lt-res, several months) pre-clinical models of two drugs inducing mitotic arrest in TP53-mutated cells: adavosertib (ADA), an investigational WEE1 inhibitor targeting the DNA damage response and currently evaluated in clinical trials, and paclitaxel (PTX), a widely used chemotherapeutic agent in cancer care targeting microtubules. Notably, upregulation of receptor tyrosine kinases, such as ROR1, was observed in both ADA and PTX lt-res models with activated PI3K/AKT signaling. Targeting ROR1 with zilovertamab-vedotin, a monoclonal antibody-drug conjugate, resulted in enhanced cytotoxicity, demonstrating a new approach against recurrent drug-resistant ovarian cancer.
    Journal
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    TP53 (Tumor protein P53) • ROR1 (Receptor Tyrosine Kinase Like Orphan Receptor 1)
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    TP53 mutation
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    paclitaxel • adavosertib (AZD1775) • zilovertamab vedotin (MK-2140)
    17d
    IM-1021-101: A Phase 1 Study of IM-1021 in Participants with Advanced Cancer (2025-523160-20-00)
    P1, N=23, Not yet recruiting, Immunome Inc.
    New P1 trial
    22d
    waveLINE-004: A Study to Evaluate Zilovertamab Vedotin (MK-2140) for Relapsed or Refractory Diffuse Large B-Cell Lymphoma (DLBCL) (MK-2140-004) (clinicaltrials.gov)
    P2, N=140, Active, not recruiting, Merck Sharp & Dohme LLC | Trial completion date: Jan 2026 --> Apr 2026 | Trial primary completion date: Jan 2026 --> Apr 2026
    Trial completion date • Trial primary completion date
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    zilovertamab vedotin (MK-2140)
    1m
    Targeting WTAP/ROR1/WNT5A-Mediated Crosstalk Between Glioma Stem Cells and Macrophages to Normalize Tumor Vasculature and Enhance Chemotherapy. (PubMed, Adv Sci (Weinh))
    Therapeutically, targeting ROR1 via endothelial-specific Adno-Associated Virus (AAV) knockdown or the antibody-drug conjugate Zilovertamab vedotin (VLS-101) normalizes vasculature, improves temozolomide delivery, and sensitizes tumors in glioblastoma organoids and xenografts. These findings highlight the ROR1-WNT5A axis as a promising target in glioblastomas treatment.
    Journal
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    ROR1 (Receptor Tyrosine Kinase Like Orphan Receptor 1) • WNT5A (Wnt Family Member 5A) • WTAP (WT1 Associated Protein)
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    temozolomide • zilovertamab vedotin (MK-2140)
    4ms
    A Study of BR111 in Patients With Advanced Malignancies (clinicaltrials.gov)
    P1, N=166, Recruiting, BioRay Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting | Trial completion date: Dec 2028 --> Dec 2027 | Trial primary completion date: Aug 2028 --> Oct 2027
    Enrollment open • Trial completion date • Trial primary completion date
    7ms
    waveLINE-006: A Study of Zilovertamab Vedotin (MK-2140) as Monotherapy and in Combination in Participants With Aggressive and Indolent B-cell Malignancies (MK-2140-006) (clinicaltrials.gov)
    P2, N=223, Recruiting, Merck Sharp & Dohme LLC | Trial primary completion date: Mar 2027 --> Mar 2029
    Trial primary completion date • Pan tumor
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    zilovertamab vedotin (MK-2140) • nemtabrutinib (MK-1026)
    7ms
    CS5001-101: A Study of CS5001 in Patients With Advanced Solid Tumors and Lymphomas (clinicaltrials.gov)
    P1, N=480, Recruiting, CStone Pharmaceuticals | N=156 --> 480 | Trial completion date: Jun 2026 --> Dec 2027 | Trial primary completion date: Mar 2026 --> Jun 2027
    Enrollment change • Trial completion date • Trial primary completion date
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    gemcitabine • Rituxan (rituximab) • lenalidomide • doxorubicin hydrochloride • cyclophosphamide • oxaliplatin • vincristine • prednisone • CS5001
    7ms
    A Study of HDM2005 in Combination With Standard of Care in Patients With Diffuse Large B-Cell Lymphoma (clinicaltrials.gov)
    P1/2, N=97, Recruiting, Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd.
    New P1/2 trial
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    gemcitabine • doxorubicin hydrochloride • cyclophosphamide • oxaliplatin • prednisone • prednisolone
    7ms
    A Clinical Trial Evaluating TQB2101 in Subjects With Advanced Hematologic Malignancies (clinicaltrials.gov)
    P1, N=114, Recruiting, Chia Tai Tianqing Pharmaceutical Group Nanjing Shunxin Pharmaceutical Co., Ltd.
    New P1 trial
    7ms
    Phase 2 Study of Zilovertamab Vedotin in Participants With Metastatic Solid Tumors. (PubMed, Cancer Res Commun)
    Zilovertamab vedotin had minimal antitumor activity, with only a single responder, and manageable safety in participants with previously-treated metastatic solid tumors.
    P2 data • Journal
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    HER-2 (Human epidermal growth factor receptor 2) • ROR1 (Receptor Tyrosine Kinase Like Orphan Receptor 1)
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    HR positive • HER-2 negative
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    zilovertamab vedotin (MK-2140)
    8ms
    waveLINE-004: A Study to Evaluate Zilovertamab Vedotin (MK-2140) for Relapsed or Refractory Diffuse Large B-Cell Lymphoma (DLBCL) (MK-2140-004) (clinicaltrials.gov)
    P2, N=140, Active, not recruiting, Merck Sharp & Dohme LLC | Trial completion date: Jun 2025 --> Jan 2026 | Trial primary completion date: Jun 2025 --> Jan 2026
    Trial completion date • Trial primary completion date
    |
    zilovertamab vedotin (MK-2140)
    9ms
    A Study of HDM2005 in Patients With Advanced Solid Tumor (clinicaltrials.gov)
    P1, N=72, Recruiting, Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd.
    New P1 trial