Dosage & Administration
The recommended dosage of WELIREG in adult patients is 120 mg administered orally once daily with or without food. (
The recommended dosage of WELIREG in adult patients is 120 mg administered orally once daily.
The recommended dosage of WELIREG in pediatric patients 12 years and older is based on bodyweight:
Continue WELIREG until disease progression or unacceptable toxicity.
WELIREG should be taken at the same time each day and may be taken with or without food.
Advise patients to swallow tablets whole. Do not chew, crush, or split WELIREG prior to swallowing.
If a dose of WELIREG is missed, it can be taken as soon as possible on the same day. Resume the regular daily dose schedule for WELIREG the next day. Do not take extra tablets to make up for the missed dose.
If vomiting occurs any time after taking WELIREG, do not retake the dose. Take the next dose on the next day.
The recommended dosage of WELIREG in pediatric patients 12 years and older is based on bodyweight:
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Welireg Prescribing Information
- Exposure to WELIREG during pregnancy can cause embryo-fetal harm.
- Verify pregnancy status prior to the initiation of WELIREG.
- Advise patients of these risks and the need for effective non-hormonal contraception. WELIREG can render some hormonal contraceptives ineffective[see,
5.3 Embryo-Fetal ToxicityBased on findings in animals, WELIREG can cause fetal harm when administered to a pregnant woman. In an animal reproduction study, oral administration of belzutifan to pregnant rats during the period of organogenesis caused embryo-fetal lethality, reduced fetal body weight, and fetal skeletal malformations at maternal exposures ≥0.2 times the human exposures (AUC) at the recommended dose of 120 mg daily.
Advise pregnant women and females of reproductive potential of the potential risk to the fetus. Advise females of reproductive potential to use effective non-hormonal contraception during treatment with WELIREG and for 1 week after the last dose, since WELIREG can render some hormonal contraceptives ineffective
[see Drug Interactions (7.1)].Advise male patients with female partners of reproductive potential to use effective contraception during treatment with WELIREG and for 1 week after the last dose[see Use in Specific Populations (8.1, 8.3)].,7.2 Effect of WELIREG on Other DrugsCYP3A4 SubstratesAvoid coadministration of WELIREG with sensitive CYP3A4 substrates, for which minimal decrease in concentration may lead to therapeutic failures of the substrate. If coadministration cannot be avoided, increase the sensitive CYP3A4 substrate dosage in accordance with its Prescribing Information.
Coadministration of WELIREG with CYP3A4 substrates decreases concentrations of CYP3A substrates
[seeClinical Pharmacology (12.3)], which may reduce the efficacy of these substrates. The magnitude of this decrease may be more pronounced in patients who are dual UGT2B17 and CYP2C19 poor metabolizers[see Clinical Pharmacology (12.3)].Hormonal ContraceptivesCoadministration of WELIREG with hormonal contraceptives may lead to contraceptive failure or an increase in breakthrough bleeding
[seeClinical Pharmacology (12.3), Use in Specific Populations (8.3)].,8.1 PregnancyRisk SummaryBased on findings in animal studies, WELIREG can cause fetal harm when administered to a pregnant woman. There are no available data on the use of WELIREG in pregnant women to inform the drug-associated risk. In an animal reproduction study, oral administration of belzutifan to pregnant rats during the period of organogenesis caused embryo-fetal lethality, reduced fetal body weight, and fetal skeletal malformations at maternal exposures ≥0.2 times the human exposure (AUC) at the recommended dose of 120 mg daily (
see Data). Advise pregnant women and females of reproductive potential of the potential risk to a fetus.The background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2–4% and 15–20%, respectively.
DataAnimal DataIn a pilot embryo-fetal development study, pregnant rats received oral doses of 6, 60, or 200 mg/kg/day of belzutifan during the period of organogenesis. Belzutifan caused embryo-fetal lethality at doses ≥60 mg/kg/day (approximately 1 time the human exposure at the recommended dose based on AUC). Reduced fetal body weights, fetal rib malformations, and reduced skeletal ossification occurred at doses of 6 and 60 mg/kg/day (approximately ≥0.2 times the human exposure at the recommended dose based on AUC).
].8.3 Females and Males of Reproductive PotentialWELIREG can cause fetal harm when administered to a pregnant woman
[seeUse in Specific Populations (8.1)].Pregnancy TestingVerify the pregnancy status of females of reproductive potential prior to initiating treatment with WELIREG.
ContraceptionFemalesAdvise females of reproductive potential to use effective non-hormonal contraception during treatment with WELIREG and for 1 week after the last dose. WELIREG can render some hormonal contraceptives ineffective
[see Drug Interactions (7.2)].MalesAdvise males with female partners of reproductive potential to use effective contraception during treatment with WELIREG and for 1 week after the last dose.
InfertilityBased on findings in animals, WELIREG may impair fertility in males and females of reproductive potential
[seeNonclinical Toxicology (13.1)]. The reversibility of the effect on fertility is unknown.
| Indications and Usage, Advanced Renal Cell Carcinoma (RCC), | |
Pheochromocytoma or Paraganglioma (PPGL) (1.3 Pheochromocytoma or Paraganglioma (PPGL) WELIREG is indicated for the treatment of adult and pediatric patients 12 years and older with locally advanced, unresectable, or metastatic pheochromocytoma or paraganglioma (PPGL). | 05/2025 |
Recommended Dosage (The recommended dosage of WELIREG in adult patients is 120 mg administered orally once daily. The recommended dosage of WELIREG in pediatric patients 12 years and older is based on bodyweight:
Continue WELIREG until disease progression or unacceptable toxicity. WELIREG should be taken at the same time each day and may be taken with or without food. Advise patients to swallow tablets whole. Do not chew, crush, or split WELIREG prior to swallowing. If a dose of WELIREG is missed, it can be taken as soon as possible on the same day. Resume the regular daily dose schedule for WELIREG the next day. Do not take extra tablets to make up for the missed dose. If vomiting occurs any time after taking WELIREG, do not retake the dose. Take the next dose on the next day. | 05/2025 |
Warnings and Precautions (WELIREG can cause severe anemia that can require blood transfusion. Monitor for anemia before initiation of, and periodically throughout, treatment with WELIREG. Transfuse patients as clinically indicated. For patients with hemoglobin <8g/dL, withhold WELIREG until ≥8g/dL, then resume at the same or reduced dose or permanently discontinue WELIREG, depending on the severity of anemia. For life threatening anemia or when urgent intervention is indicated, withhold WELIREG until hemoglobin ≥8g/dL, then resume at a reduced dose or permanently discontinue WELIREG [see Dosage and Administration (2.2)] .von Hippel-Lindau (VHL) disease In LITESPARK-004, decreased hemoglobin occurred in 93% of patients and 7% had Grade 3 events [see Adverse Reactions (6.1)] . Median time to onset of anemia was 31 days (range: 1 day to 8.4 months).The safety of erythropoiesis stimulating agents (ESAs) for treatment of anemia in patients with VHL disease treated with WELIREG has not been established. Randomized controlled trials in patients with cancer receiving myelosuppressive chemotherapy with ESAs have shown that ESAs increased the risks of death and serious cardiovascular reactions, and decreased progression-free survival and/or overall survival. See the prescribing information for ESAs for more information. Advanced Renal Cell Carcinoma (RCC) In LITESPARK-005, decreased hemoglobin occurred in 88% of patients and 29% had Grade 3 events [see Adverse Reactions (6.1)] . Median time to onset of anemia was 29 days (range: 1 day to 16.6 months). Of the patients with anemia, 22% received transfusions only, 20% of patients received ESAs only and 12% received both transfusion and ESAs.Pheochromocytoma or Paraganglioma (PPGL) In LITESPARK-015, anemia occurred in 96% of patients and 22% had Grade 3 events [see Adverse Reactions (6.1)] . Median time to onset of anemia was 29 days (range: 1 day to 22.1 months). Of the patients with anemia, 20% received transfusions only, 26% received ESAs only, and 6% received both transfusion and ESAs.WELIREG can cause severe hypoxia that may require discontinuation, supplemental oxygen, or hospitalization [see Dosage and Administration (2.2)]. Monitor oxygen saturation before initiation of, and periodically throughout, treatment with WELIREG. For decreased oxygen saturation with exercise (e.g., pulse oximeter <88% or PaO2≤55 mm Hg), consider withholding WELIREG until pulse oximetry with exercise is greater than 88%, then resume at the same dose or at a reduced dose. For decreased oxygen saturation at rest (e.g., pulse oximeter <88% or PaO2 ≤55 mm Hg) or urgent intervention indicated, withhold WELIREG until resolved and resume at a reduced dose or discontinue. For life-threatening hypoxia or for recurrent symptomatic hypoxia, permanently discontinue WELIREG [see Dosage and Administration (2.2)] .Advise patients to report signs and symptoms of hypoxia immediately to a healthcare provider. von Hippel-Lindau (VHL) disease In LITESPARK- 004, hypoxia occurred in 1.6% of patients [see Adverse Reactions (6.1)] .Advanced Renal Cell Carcinoma (RCC) In LITESPARK- 005, hypoxia occurred in 15% of patients and 10% had Grade 3 events [see Adverse Reactions (6.1)] . Of the patients with hypoxia, 69% were treated with oxygen therapy. Median time to onset of hypoxia was 30.5 days (range: 1 day to 21.1 months).Pheochromocytoma or Paraganglioma (PPGL) In LITESPARK-015, hypoxia occurred in 13% of patients and 10% had Grade 3 hypoxia [see Adverse Reactions (6.1)] . Median time to onset of hypoxia was 35 days (range: 6 days to 23.9 months). Of the patients with hypoxia, 67% were treated with oxygen therapy. | 05/2025 |
WELIREG is a hypoxia-inducible factor inhibitor indicated:
- for treatment of adult patients with von Hippel-Lindau (VHL) disease who require therapy for associated renal cell carcinoma (RCC), central nervous system (CNS) hemangioblastomas, or pancreatic neuroendocrine tumors (pNET), not requiring immediate surgery. ()
1.1 von Hippel-Lindau (VHL) diseaseWELIREG is indicated for treatment of adult patients with von Hippel-Lindau (VHL) disease who require therapy for associated renal cell carcinoma (RCC), central nervous system (CNS) hemangioblastomas, or pancreatic neuroendocrine tumors (pNET), not requiring immediate surgery.
- for treatment of adult patients with advanced renal cell carcinoma (RCC) with a clear cell component following a programmed death receptor-1 (PD-1) or programmed death-ligand 1 (PD-L1) inhibitor and a vascular endothelial growth factor tyrosine kinase inhibitor (VEGF-TKI). ()1.2 Advanced Renal Cell Carcinoma (RCC)WELIREG is indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC) with a clear cell component following a programmed death receptor-1 (PD-1) or programmed death-ligand 1 (PD-L1) inhibitor and a vascular endothelial growth factor tyrosine kinase inhibitor (VEGF-TKI).
- for treatment of adult and pediatric patients 12 years and older with locally advanced, unresectable, or metastatic pheochromocytoma or paraganglioma (PPGL). ()1.3 Pheochromocytoma or Paraganglioma (PPGL)WELIREG is indicated for the treatment of adult and pediatric patients 12 years and older with locally advanced, unresectable, or metastatic pheochromocytoma or paraganglioma (PPGL).
The recommended dosage of WELIREG in adult patients is 120 mg administered orally once daily with or without food. (
The recommended dosage of WELIREG in adult patients is 120 mg administered orally once daily.
The recommended dosage of WELIREG in pediatric patients 12 years and older is based on bodyweight:
- Patients weighing ≥ 40 kg: 120 mg orally once daily
- Patients weighing < 40 kg: 80 mg orally once daily
Continue WELIREG until disease progression or unacceptable toxicity.
WELIREG should be taken at the same time each day and may be taken with or without food.
Advise patients to swallow tablets whole. Do not chew, crush, or split WELIREG prior to swallowing.
If a dose of WELIREG is missed, it can be taken as soon as possible on the same day. Resume the regular daily dose schedule for WELIREG the next day. Do not take extra tablets to make up for the missed dose.
If vomiting occurs any time after taking WELIREG, do not retake the dose. Take the next dose on the next day.
The recommended dosage of WELIREG in pediatric patients 12 years and older is based on bodyweight:
- Patients weighing ≥ 40 kg: 120 mg orally once daily
- Patients weighing < 40 kg: 80 mg orally once daily
Tablets: 40 mg, blue, oval shaped, film-coated, debossed with “177” on one side and plain on the other side.
- Lactation: Advise not to breastfeed. ()
8.2 LactationRisk SummaryThere are no data on the presence of belzutifan or its metabolites in human milk or their effects on the breastfed child or on milk production. Because of the potential for serious adverse reactions in a breastfed child, advise women not to breastfeed during treatment with WELIREG and for 1 week after the last dose.
- Infertility: May impair fertility in males and females. ()
8.3 Females and Males of Reproductive PotentialWELIREG can cause fetal harm when administered to a pregnant woman
[seeUse in Specific Populations (8.1)].Pregnancy TestingVerify the pregnancy status of females of reproductive potential prior to initiating treatment with WELIREG.
ContraceptionFemalesAdvise females of reproductive potential to use effective non-hormonal contraception during treatment with WELIREG and for 1 week after the last dose. WELIREG can render some hormonal contraceptives ineffective
[see Drug Interactions (7.2)].MalesAdvise males with female partners of reproductive potential to use effective contraception during treatment with WELIREG and for 1 week after the last dose.
InfertilityBased on findings in animals, WELIREG may impair fertility in males and females of reproductive potential
[seeNonclinical Toxicology (13.1)]. The reversibility of the effect on fertility is unknown.