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    DRUG:

    Welireg (belzutifan)

    i
    Other names: PT2977, MK6482, MK 6482, MK-6482, PT 2977, PT-2977
    Company:
    Merck (MSD)
    Drug class:
    HIF-2α inhibitor
    Related drugs:
    3d
    Substudy 03C: A Study of Combination Therapies in Participants With Renal Cell Carcinoma With Recurrent Disease During or After Anti-PD-(L)1 Therapy (MK-3475-03C/KEYMAKER-U03) (clinicaltrials.gov)
    P1/2, N=140, Recruiting, Merck Sharp & Dohme LLC
    Trial initiation date
    |
    Keytruda (pembrolizumab) • Welireg (belzutifan) • zanzalintinib (XL092)
    8d
    A clinical study of belzutifan and zanzalintinib in people with advanced kidney cancer (MK-6482-034) (2024-516993-31-00)
    P2/3, N=154, Not yet recruiting, Merck Sharp & Dohme LLC
    New P2/3 trial
    |
    Welireg (belzutifan) • zanzalintinib (XL092)
    8d
    Molecular Glue cc-885 Inhibits VHL-Deficient Clear Cell Renal Cell Carcinoma via ETS1 Degradation. (PubMed, Adv Sci (Weinh))
    Moreover, combining cc-885 with an EPAS1 inhibitor, belzutifan, significantly enhanced the anti-tumor efficacy. Our findings provide a novel and precise therapeutic strategy for VHL-deficient ccRCC by targeting ETS1 degradation and disrupting the ETS1-EPAS1 complex.
    Journal
    |
    VHL (von Hippel-Lindau tumor suppressor) • EPAS1 (Endothelial PAS domain protein 1) • ETS1 (ETS Proto-Oncogene 1)
    |
    VHL mutation
    |
    Welireg (belzutifan)
    14d
    Phase 1 LITESPARK-001 study of belzutifan in participants with advanced solid tumors: Results of the glioblastoma expansion cohort. (PubMed, Neurooncol Adv)
    The glioblastoma cohort of the phase 1 LITESPARK-001 trial enrolled participants who had received radiotherapy and temozolomide. Although targeting HIF-2α may have a role in advancing treatment options for patients with glioblastoma, single-agent belzutifan did not have antitumor activity in this cohort.
    P1 data • Journal
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    EPAS1 (Endothelial PAS domain protein 1)
    |
    IDH wild-type
    |
    temozolomide • Welireg (belzutifan)
    15d
    A clinical trial of belzutifan and other treatments in people with solid tumors or von Hippel-Lindau (VHL)-related tumors (MK-6482-043) (2025-524160-38-00)
    P2/3, N=25, Not yet recruiting, Merck Sharp & Dohme LLC
    New P2/3 trial
    |
    Lenvima (lenvatinib) • Welireg (belzutifan)
    16d
    Belzutifan VHL RCC HK Prospective Registry (clinicaltrials.gov)
    P=N/A, N=100, Not yet recruiting, Chinese University of Hong Kong
    New trial
    |
    Welireg (belzutifan)
    18d
    VHIO24002: Moonlanding: A phase 2 study of pembrolizumab plus belzutifan, with or without lenvatinib, given before the main treatment for localized kidney cancer (renal cell carcinoma) (2024-519673-18-00)
    P1/2, N=90, Not yet recruiting, Vall D Hebron Institute Of Oncology
    New P1/2 trial
    |
    CD4 (CD4 Molecule)
    |
    Keytruda (pembrolizumab) • Lenvima (lenvatinib) • Welireg (belzutifan)
    20d
    Hypoxia-inducible factors: Regulatory functions and status as a therapeutic target in gastric cancer (Review). (PubMed, Oncol Lett)
    In the field of cancer therapeutics, targeting the HIF pathway has emerged as a promising strategy, and the Food and Drug Administration approval in 2021 of Welireg, a novel agent designed to target HIF-2α for the primary treatment of von Hippel-Lindau syndrome, has further validated its favorable prospects in tumor therapy...Currently, a range of therapeutic approaches are available for patients diagnosed with GC, yet the 5-year survival rate remains suboptimal for those with advanced-stage disease. The present review summarizes the regulatory and target roles of HIFs in GC, thus providing references for GC treatment and emphasizing the potential of HIF-targeted therapies to disrupt cancer-associated signaling pathways.
    Review • Journal
    |
    EPAS1 (Endothelial PAS domain protein 1)
    |
    Welireg (belzutifan)
    21d
    A Clinical Study of Belzutifan (MK-6482) and Zanzalintinib in People With Renal Cell Carcinoma (RCC) (LITESPARK-034/LS-034/MK-6482-034) (clinicaltrials.gov)
    P3, N=758, Recruiting, Merck Sharp & Dohme LLC | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Welireg (belzutifan) • zanzalintinib (XL092)
    21d
    Safety and Efficacy of Belzutifan in Preoperative Preparation for Patients with Pheochromocytoma/Paraganglioma (PPGL): A Pilot Study (ChiCTR2600120686)
    P4, N=20, Xiangya Hospital of Central South University; Xiangya Hospital of Central South University
    New P4 trial
    |
    Welireg (belzutifan)
    30d
    LITESPARK-015: Belzutifan/MK-6482 for the Treatment of Advanced Pheochromocytoma/Paraganglioma (PPGL), Pancreatic Neuroendocrine Tumor (pNET), Von Hippel-Lindau (VHL) Disease-Associated Tumors, Advanced Gastrointestinal Stromal Tumor (wt GIST), or Solid Tumors With HIF-2α Related Genetic Alterations (MK-6482-015) (clinicaltrials.gov)
    P2, N=322, Recruiting, Merck Sharp & Dohme LLC | N=170 --> 322
    Enrollment change
    |
    EPAS1 (Endothelial PAS domain protein 1)
    |
    Welireg (belzutifan)
    1m
    LITESPARK-004: A Phase 2 Study of Belzutifan (PT2977, MK-6482) for the Treatment of Von Hippel Lindau (VHL) Disease-Associated Renal Cell Carcinoma (RCC) (MK-6482-004) (clinicaltrials.gov)
    P2, N=50, Active, not recruiting, Peloton Therapeutics, Inc., a subsidiary of Merck & Co., Inc. (Rahway, New Jersey USA) | Trial completion date: Mar 2026 --> Apr 2027 | Trial primary completion date: Mar 2026 --> Apr 2027
    Trial completion date • Trial primary completion date
    |
    VHL mutation
    |
    Welireg (belzutifan)