Belzutifan
Belzutifan is an oral anticancer medication that inhibits hypoxia-inducible factor 2 alpha (HIF-2α), a protein that promotes tumor growth in certain conditions. It is primarily used to treat Von Hippel-Lindau disease, a genetic disorder that causes tumors to form in various organs, and is also approved for advanced renal cell carcinoma.
Belzutifan is a HIF-2α inhibitor used to treat Von Hippel-Lindau disease and advanced kidney cancer by blocking tumor growth pathways.
This medication carries a boxed (black box) warning — the strongest type of FDA warning. Review the full prescribing information before use.
Key facts at a glance
- ATC
- L01XX74
- RxNorm
- 2567226
- Generic
- Belzutifan
- Class
- atc-l01
- Brands
- Welireg
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 500mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 250mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 400mg daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
11 groupspregnancy
first trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks to the fetus
regular fetal monitoring including ultrasound assessments
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
second trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks to the fetus
regular fetal monitoring including ultrasound assessments
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
third trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks to the fetus
regular fetal monitoring including ultrasound assessments
Use of this medication in this population requires careful consideration of risks and benefits.
lactation
breastfeedingnot applicable
do not breastfeed during treatment and for at least 1 week after last dose
monitor infant for adverse reactions
Use of this medication in this population requires careful consideration of risks and benefits.
pediatric_age
not establishednot established
safety and efficacy not established in pediatric patients; use only if benefits outweigh risks
monitor growth and development closely if treatment is necessary
geriatric
elderlyno adjustment needed
no specific dose adjustment required; monitor for increased sensitivity
routine monitoring of renal and hepatic function
Use with caution and monitor for adverse effects.
renal_impairment
mildno adjustment needed
no dose adjustment for mild renal impairment
routine renal function monitoring
renal_impairment
moderateno adjustment needed
no dose adjustment for moderate renal impairment; monitor closely
more frequent renal function monitoring recommended
Use with caution and monitor for adverse effects.
renal_impairment
severeuse with caution
not studied in severe renal impairment; use only if benefits outweigh risks
close monitoring of renal function and adverse effects
Use with caution and monitor for adverse effects.
hepatic_impairment
mildno adjustment needed
no dose adjustment for mild hepatic impairment
routine hepatic function monitoring
hepatic_impairment
moderateno adjustment needed
no dose adjustment for moderate hepatic impairment; monitor closely
more frequent hepatic function monitoring recommended
Use with caution and monitor for adverse effects.
Statistics and clinical data
FDA approval year
FDA approval information for Welireg (Belzutifan)
Drug class
Pharmacological class - hypoxia-inducible factor-2 alpha inhibitor
Primary indication
Therapeutic indication for VHL-associated renal cell carcinoma, pancreatic neuroendocrine tumors, and hemangioblastomas
Belzutifan is indicated for patients with Von Hippel-Lindau disease who require treatment for associated renal cell carcinoma, central nervous system hemangioblastomas, or pancreatic neuroendocrine tumors. It is also approved for relapsed or refractory advanced renal cell carcinoma following prior treatment.
Belzutifan works by inhibiting hypoxia-inducible factor 2 alpha (HIF-2α), a transcription factor that regulates genes involved in oxygen adaptation and tumor growth. By blocking this pathway, it reduces tumor progression in conditions where HIF-2α is overactive, such as VHL disease and certain kidney cancers.
Belzutifan can cause serious side effects including anemia, hypoxia, and fetal harm. Regular blood monitoring is required during treatment. Women who are pregnant or breastfeeding should not take this medication. Patients should be monitored for new or worsening symptoms and report any shortness of breath, fatigue, or signs of infection to their healthcare provider.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy