Belzutifan
Belzutifan is the first HIF-2α inhibitor, born from Nobel-winning biology, and is now approved after kidney cancer surgery with pembrolizumab.
VHL disease (2021), advanced RCC after PD-1 and VEGF-TKI (LITESPARK-005, 2023), pheochromocytoma/paraganglioma (2025), and Q2 2026 adjuvant clear-cell RCC with pembrolizumab (LITESPARK-022). Merck.
1.Belzutifan binds the PAS-B pocket of HIF-2α
- Route
- Oral
- Schedule
- 120 mg once daily
- Dose modifications
- Hold for haemoglobin <8 g/dL or hypoxia; permanently discontinue for life-threatening hypoxia
- Monitoring
- Haemoglobin and oxygen saturation before and during treatment; embryo-fetal toxicity
Source: www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications. Doses are for orientation; the current label governs.
- Medicare
- Part D (self-administered)
Oral, self-administered, so it is a Part D drug: covered through a stand-alone Part D plan or Medicare Advantage drug benefit, usually on the specialty tier with 25 to 33% coinsurance until the annual cap ($2,000 in 2025, $2,100 in 2026).
- Commercial insurance
- covered with prior authorisation
Covered for FDA-labelled and NCCN-listed uses, but almost always behind prior authorisation confirming diagnosis, biomarker and line of therapy; dispensed through a specialty pharmacy. VHL disease or prior immunotherapy and VEGF-TKI for RCC.
- Assistance programmes
- Merck Access Program
- Merck Patient Assistance Program — Free medicine for eligible uninsured or underinsured patients.
- PAN Foundation — Disease-specific co-pay and premium funds; open and closed funds change monthly.
- HealthWell Foundation
- CancerCare Co-Payment Assistance Foundation
- Patient Advocate Foundation Co-Pay Relief
Part D out-of-pocket capped at $2,000 (2025) / $2,100 (2026). Medicare patients cannot use manufacturer co-pay cards; charity funds (PAN, HealthWell, CancerCare) and the Extra Help subsidy are the routes.
Sources: Medicare.gov: Drug coverage (Part D) · Medicare.gov: Costs for Medicare drug coverage (annual out-of-pocket cap). Not medical or financial advice; verify with your plan.
- Notes
- EU-licensed 2025 for VHL-associated tumours and previously treated RCC; UK licence and NICE position not yet researched.
Sources: NICE search: belzutifan. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.
- 13 Aug 2021ApprovalUS
VHL disease-associated RCC, CNS haemangioblastoma, pNET: first HIF-2α inhibitor source
- 14 Dec 2023ApprovalUS
Advanced RCC after PD-1/PD-L1 and VEGF-TKI (LITESPARK-005) source
- May 2025ApprovalUS
Pheochromocytoma/paraganglioma source
- Q2 2026ApprovalUS
Adjuvant clear-cell RCC with pembrolizumab (LITESPARK-022) source
Approvals
| Region | Year | Indication |
|---|---|---|
| US | 2021 | VHL-associated RCC, CNS haemangioblastoma, pNET |
| US | 2023 | Advanced RCC after PD-1/PD-L1 and VEGF-TKI |
| US | 2026 | Adjuvant clear-cell RCC with pembrolizumab |
| Adverse event |
|---|
| Anaemia |
| Hypoxia |
| Fatigue |
| Nausea |
| Oedema |
| Dyspnoea |
LITESPARK-005: ~83% any grade, ~33% grade 3. Events listed without rates were not read from a primary source; see the label. Blank cells mean the figure was not sourced, not that it is zero.
| Country | Reimbursement | List price | Assistance |
|---|---|---|---|
| United States | Medicare Part D (oral); commercial plans per formulary, often with prior authorisation | not disclosed | merckaccessprogram-welireg.com |
| United Kingdom | NICE: appraisal for RCC after IO and VEGF-TKI (2025-26) | not disclosed | — |
List prices are manufacturer or Medicare figures where publicly disclosed; net prices after rebates are usually lower. Reimbursement changes; check the payer.
Trials
topRecruiting now (live from ClinicalTrials.gov)
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Latest papers
topQuery for this drug: (TITLE:"Belzutifan" OR ABSTRACT:"Belzutifan" OR TITLE:"Welireg" OR ABSTRACT:"Welireg") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Belzutifan, not a curated reading list.