- Bladder, kidney, and other urologic cancers
- CNS cancers
- Pancreatic, thyroid, and other endocrine cancers
Bladder, kidney, and other urologic cancers:
Indications for: WELIREG
In adults 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.
Adult Dosage:
Swallow whole. Take at the same time each day. 120mg once daily until disease progression or unacceptable toxicity. Dose modifications for adverse reactions: see full labeling.
Children Dosage:
Not established.
Boxed Warning:
Embryo-fetal toxicity.
WELIREG Warnings/Precautions:
Monitor for anemia, oxygen saturation prior to initiation and periodically during therapy. Withhold for hemoglobin <9g/dL or transfusion indicated until resolved; resume at reduced dose or permanently discontinue based on severity of anemia. For life-threatening anemia or when urgent intervention is indicated; withhold until resolved; resume at reduced dose or permanently discontinue. Consider withholding therapy for decreased oxygen saturation with exercise (eg, pulse oximeter <88% or PaO2 ≤55mmHg) until resolved, then resume at same or reduced dose. Withhold for decreased oxygen saturation at rest (eg, pulse oximeter <88% or PaO2 ≤55mmHg) or urgent intervention indicated until resolved; resume at reduced dose or discontinue based on severity of hypoxia. Permanently discontinue if life-threatening or recurrent symptomatic hypoxia occurs. Poor metabolizers (dual UGT2B17/CYP2C19): monitor closely. Severe renal impairment (eGFR 15–29mL/min/1.73m2). Moderate or severe hepatic impairment (total bilirubin >1.5×ULN and any AST). Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective non-hormonal contraception during and for 1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 week after the last dose).
WELIREG Classification:
Hypoxia-inducible factor inhibitor.
WELIREG Interactions:
Potentiated by UGT2B17 or CYP2C19 inhibitors; monitor and reduce belzutifan dose. Antagonizes CYP3A4 substrates (esp. in dual UGT2B17/CYP2C19 poor metabolizers). Avoid concomitant sensitive CYP3A4 substrates; if unavoidable, increase the dose of these substrates. May antagonize hormonal contraceptives.
Adverse Reactions:
Decreased hemoglobin, anemia, fatigue, increased creatinine, headache, dizziness, increased glucose, nausea; hypoxia, anaphylaxis reaction, retinal disorders.
Generic Drug Availability:
NO
How Supplied:
Tabs—90
CNS cancers:
Indications for: WELIREG
In adults 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.
Adult Dosage:
Swallow whole. Take at the same time each day. 120mg once daily until disease progression or unacceptable toxicity. Dose modifications for adverse reactions: see full labeling.
Children Dosage:
Not established.
Boxed Warning:
Embryo-fetal toxicity.
WELIREG Warnings/Precautions:
Monitor for anemia, oxygen saturation prior to initiation and periodically during therapy. Withhold for hemoglobin <9g/dL or transfusion indicated until resolved; resume at reduced dose or permanently discontinue based on severity of anemia. For life-threatening anemia or when urgent intervention is indicated; withhold until resolved; resume at reduced dose or permanently discontinue. Consider withholding therapy for decreased oxygen saturation with exercise (eg, pulse oximeter <88% or PaO2 ≤55mmHg) until resolved, then resume at same or reduced dose. Withhold for decreased oxygen saturation at rest (eg, pulse oximeter <88% or PaO2 ≤55mmHg) or urgent intervention indicated until resolved; resume at reduced dose or discontinue based on severity of hypoxia. Permanently discontinue if life-threatening or recurrent symptomatic hypoxia occurs. Poor metabolizers (dual UGT2B17/CYP2C19): monitor closely. Severe renal impairment (eGFR 15–29mL/min/1.73m2). Moderate or severe hepatic impairment (total bilirubin >1.5×ULN and any AST). Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective non-hormonal contraception during and for 1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 week after the last dose).
WELIREG Classification:
Hypoxia-inducible factor inhibitor.
WELIREG Interactions:
Potentiated by UGT2B17 or CYP2C19 inhibitors; monitor and reduce belzutifan dose. Antagonizes CYP3A4 substrates (esp. in dual UGT2B17/CYP2C19 poor metabolizers). Avoid concomitant sensitive CYP3A4 substrates; if unavoidable, increase the dose of these substrates. May antagonize hormonal contraceptives.
Adverse Reactions:
Decreased hemoglobin, anemia, fatigue, increased creatinine, headache, dizziness, increased glucose, nausea; hypoxia, anaphylaxis reaction, retinal disorders.
Generic Drug Availability:
NO
How Supplied:
Tabs—90
Pancreatic, thyroid, and other endocrine cancers:
Indications for: WELIREG
In adults 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.
Adult Dosage:
Swallow whole. Take at the same time each day. 120mg once daily until disease progression or unacceptable toxicity. Dose modifications for adverse reactions: see full labeling.
Children Dosage:
Not established.
Boxed Warning:
Embryo-fetal toxicity.
WELIREG Warnings/Precautions:
Monitor for anemia, oxygen saturation prior to initiation and periodically during therapy. Withhold for hemoglobin <9g/dL or transfusion indicated until resolved; resume at reduced dose or permanently discontinue based on severity of anemia. For life-threatening anemia or when urgent intervention is indicated; withhold until resolved; resume at reduced dose or permanently discontinue. Consider withholding therapy for decreased oxygen saturation with exercise (eg, pulse oximeter <88% or PaO2 ≤55mmHg) until resolved, then resume at same or reduced dose. Withhold for decreased oxygen saturation at rest (eg, pulse oximeter <88% or PaO2 ≤55mmHg) or urgent intervention indicated until resolved; resume at reduced dose or discontinue based on severity of hypoxia. Permanently discontinue if life-threatening or recurrent symptomatic hypoxia occurs. Poor metabolizers (dual UGT2B17/CYP2C19): monitor closely. Severe renal impairment (eGFR 15–29mL/min/1.73m2). Moderate or severe hepatic impairment (total bilirubin >1.5×ULN and any AST). Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective non-hormonal contraception during and for 1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 week after the last dose).
WELIREG Classification:
Hypoxia-inducible factor inhibitor.
WELIREG Interactions:
Potentiated by UGT2B17 or CYP2C19 inhibitors; monitor and reduce belzutifan dose. Antagonizes CYP3A4 substrates (esp. in dual UGT2B17/CYP2C19 poor metabolizers). Avoid concomitant sensitive CYP3A4 substrates; if unavoidable, increase the dose of these substrates. May antagonize hormonal contraceptives.
Adverse Reactions:
Decreased hemoglobin, anemia, fatigue, increased creatinine, headache, dizziness, increased glucose, nausea; hypoxia, anaphylaxis reaction, retinal disorders.
Generic Drug Availability:
NO
How Supplied:
Tabs—90
