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DRUG CLASS:

HIF-2α inhibitor

8d
Targeting of HIF2-driven cachexia in kidney cancer. (PubMed, Nat Med)
Consistent with these observations, two different allosteric HIF2 inhibitors, belzutifan and NKT2152, rapidly ameliorated hypercalcemia and cachexia in patients with ccRCC, including in some who did not exhibit objective tumor shrinkage. Our findings support prospective clinical studies to determine whether HIF2 inhibitors can be leveraged not only for tumor control, but also for the treatment of cancer-associated cachexia in renal cell carcinoma.
Journal
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PTHLH (Parathyroid Hormone Like Hormone)
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Welireg (belzutifan) • NKT2152
9d
Emerging Diagnostics and Therapies in Neuroendocrine Neoplasms: A Critical Review. (PubMed, Cancers (Basel))
In treatment, radioligand therapy (PRRT) is used earlier in appropriate receptor-positive disease; cabozantinib improves progression-free survival after prior therapy; and belzutifan offers a biomarker-guided option for malignant pheochromocytoma/paraganglioma...We appraise strengths and limitations of key trials, note issues of access and toxicity, and highlight active areas in development (SSTR antagonists, alpha emitters, and dose-guided PRRT). Our goal is to provide a concise, evidence-based map of the field to support informed clinical judgment and future research priorities.
Review • Journal • IO biomarker
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ATRX (ATRX Chromatin Remodeler) • SSTR (Somatostatin Receptor) • DAXX (Death-domain associated protein)
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Cabometyx (cabozantinib tablet) • Welireg (belzutifan)
10d
Identification of Degradation Products and a Stability-Indicating RP-HPLC Method for the Determination of Belzutifan in Pharmaceutical Dosage Forms. (PubMed, J Pharm Bioallied Sci)
Relative standard deviations (RSD) were below 2%, indicating precision and reproducibility. Owing to its simplicity and efficiency, the method is suitable for routine quality control in pharmaceutical laboratories.
Journal
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EPAS1 (Endothelial PAS domain protein 1)
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Welireg (belzutifan)
21d
Different forms of selenium improve laying performance and ovarian antioxidant capacity: regulating gut microbiota and ovarian metabolism. (PubMed, Poult Sci)
Compared with the sodium selenite (SeS), nano-selenium (SeN), selenomethionine (SeM), and selenium-enriched yeasts (SeY), as novel selenium sources, are increasingly popular in laying hen production...Meanwhile, the gut microbiota and differential metabolites of ovary were closely related to laying performance and antioxidant capacity of ovary. Therefore, 0.4 mg/kg SeN, SeM, and SeY showed an advantage on improving laying rate, ovary function, and gut microbiota in laying hens, and they could be potential additives using in laying hen production.
Journal
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GPX2 (Glutathione peroxidase 2 (gastrointestinal)) • SOD2 (Superoxide Dismutase 2)
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selenomethionine (SLM)
23d
Drug-Drug Interaction Study of Casdatifan in Healthy Adult Participants (ARC-29) (clinicaltrials.gov)
P1, N=14, Completed, Arcus Biosciences, Inc. | Active, not recruiting --> Completed
Trial completion
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itraconazole • casdatifan (AB521)
23d
Multigenerational VHL family characterized by pathogenic germline ELOC variant: Response to belzutifan. (PubMed, Urol Oncol)
These findings indicate that the p.E92G ELOC variant is responsible for the VHL manifestations in this family, and that these tumors are being driven by loss of the VCB-Cul2 E3-ubiquitin ligase complex activity.
Journal
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VHL (von Hippel-Lindau tumor suppressor) • CUL2 (Cullin 2)
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Welireg (belzutifan)
24d
NKT2152-101: A Study of NKT2152, a HIF2α Inhibitor, in Patients With Advanced Clear Cell Renal Cell Carcinoma (clinicaltrials.gov)
P1/2, N=120, Terminated, NiKang Therapeutics, Inc. | Trial completion date: Sep 2026 --> Sep 2025 | Active, not recruiting --> Terminated | Trial primary completion date: May 2025 --> Aug 2025; This study was terminated as a result of Sponsor portfolio reprioritization.
Trial completion date • Trial termination • Trial primary completion date
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PD-L1 (Programmed death ligand 1)
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NKT2152
24d
NKT2152-202: Ph2 Study NKT2152 With Palbociclib & Sasanlimab in Subjects With Advanced Clear Cell Renal Cell Carcinoma (ccRcc) (clinicaltrials.gov)
P2, N=18, Terminated, NiKang Therapeutics, Inc. | N=172 --> 18 | Trial completion date: Jun 2026 --> Sep 2025 | Active, not recruiting --> Terminated; This study was terminated as a result of Sponsor portfolio reprioritization.
Enrollment change • Trial completion date • Trial termination
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Ibrance (palbociclib) • sasanlimab (PF-06801591) • NKT2152
24d
New P3 trial
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Cabometyx (cabozantinib tablet) • Welireg (belzutifan) • zanzalintinib (XL092)
1m
Belzutifan for patients with Von Hippel-Lindau (VHL) disease-associated heterogeneous tumors - a retrospective single center analysis. (PubMed, BMC Cancer)
Belzutifan represents a promising treatment option for VHL disease, particularly in patients for whom surgery carries significant risks. The therapy demonstrated effective tumor control and delayed disease progression in most cases. However, anemia remains a key side effect requiring close monitoring and management. Larger, long-term studies are needed to further assess the efficacy and safety of belzutifan in VHL patients and to refine treatment strategies.
Retrospective data • Journal
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EPAS1 (Endothelial PAS domain protein 1)
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Welireg (belzutifan)
1m
Belzutifan for Advanced Pheochromocytoma or Paraganglioma. (PubMed, N Engl J Med)
Belzutifan showed antitumor activity with durable responses in participants with advanced pheochromocytoma or paraganglioma. (Funded by Merck Sharp and Dohme, a subsidiary of Merck [Rahway, NJ]; LITESPARK-015 ClinicalTrials.gov number, NCT04924075.).
Journal
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EPAS1 (Endothelial PAS domain protein 1)
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Welireg (belzutifan)
2ms
Updated 2025 French Guidelines for Renal Cell Carcinoma. (PubMed, Fr J Urol)
In hereditary syndromes, progress includes improved characterization of BAP1-TPDS-associated RCC and the expanding role of belzutifan in von Hippel-Lindau disease. Beyond twelve months after pembrolizumab, standard first-line PD-1-based combinations remain the recommended approach. Finally, for localized or oligometastatic recurrences, local treatments should be considered within a multidisciplinary tumour board.
Review • Journal • PD(L)-1 Biomarker • IO biomarker
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PD-1 (Programmed cell death 1) • BAP1 (BRCA1 Associated Protein 1) • KIM1 (Kidney injury molecule 1)
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Keytruda (pembrolizumab) • Welireg (belzutifan)