belzutifan at a glance
Medicine class
HIF-2 alpha inhibitor and targeted antineoplastic treatment
How it is taken
Film-coated tablets swallowed whole, with or without food
Important monitoring
Blood haemoglobin and oxygen saturation require monitoring, particularly early in treatment
What is belzutifan used for?
Licensed uses include:
Adults with von Hippel-Lindau disease requiring treatment for associated renal cell carcinoma, central nervous system haemangioblastomas or pancreatic neuroendocrine tumours, when localised procedures are unsuitable or undesirable.
Adults with advanced renal cell carcinoma that has progressed on or after both PD-1 or PD-L1 inhibitor treatment and a VEGF tyrosine-kinase inhibitor.
Adults and eligible adolescents with locally advanced, unresectable or metastatic pheochromocytoma or paraganglioma.
How does belzutifan work?
HIF-2 alpha activates genes involved in blood-vessel formation, cell growth and adaptation to low oxygen. Belzutifan blocks it from forming an active transcription complex, reducing signals that can support tumour growth.
belzutifan preparations and strengths
Tablet
Route: Oral
Strengths: 40 mg
How to take belzutifan
Follow the specialist team's prescription and do not change treatment yourself.
Swallow the tablets whole.
They may be taken with or without food.
Do not drive or use machinery until you know whether dizziness or fatigue affects you.
belzutifan side effects
Common or expected effects
- Anaemia or reduced haemoglobin
- Tiredness
- Dizziness
- Nausea
- Breathlessness or reduced blood oxygen
- Weight gain
- Peripheral swelling, particularly in pheochromocytoma or paraganglioma studies
Get urgent medical advice
- Severe or rapidly worsening breathlessness, which may indicate significant hypoxia
- Marked weakness, breathlessness, paleness, dizziness or palpitations, which may indicate severe anaemia
- A severe allergic reaction, including swelling or difficulty breathing
belzutifan in pregnancy
Belzutifan may harm an unborn baby and is not recommended during pregnancy. Pregnancy status should be checked before treatment where relevant. Highly effective contraception is needed during treatment and for the SmPC-specified period afterwards. Hormonal contraception may be less effective, so discuss contraception with the specialist team.
belzutifan while breastfeeding
It is unknown whether belzutifan enters breast milk, and harm to a breastfed child cannot be excluded. Breastfeeding should stop during treatment and for the SmPC-specified period after the final tablet; seek specialist advice before restarting.
belzutifan interactions
The cancer team and pharmacist should review all prescribed, over-the-counter and herbal products.
Hormonal contraceptives
Belzutifan can reduce their effectiveness and may increase breakthrough bleeding. Suitable non-hormonal or additional barrier contraception is required.
Sensitive CYP3A4 substrates
Belzutifan can lower their concentrations and potentially cause treatment failure; avoid combinations where a small reduction would be clinically important.
UGT2B17 inhibitors
These may increase belzutifan exposure and the likelihood or severity of anaemia and hypoxia.
Common questions about belzutifan
Answers are fully visible for fast scanning and source review.
Is belzutifan chemotherapy?
It is a targeted anticancer treatment rather than conventional cytotoxic chemotherapy. It specifically inhibits HIF-2 alpha.
Can belzutifan be taken with food?
Yes. The tablets may be taken with or without food.
Why are blood tests needed?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.