Belzutifan

What is Belzutifan?

• Belzutifan (Welireg) is a hypoxia-inducible factor inhibitor used to treat von Hippel-Lindau disease under certain conditions.

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Belzutifan

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Belzutifan

What are the uses of this medicine?

• Belzutifan (Welireg) is a prescription medicine used to treat adults with von Hippel-Lindau (VHL) disease who need treatment for a type of kidney cancer called renal cell carcinoma (RCC), tumors in the brain and spinal cord called central nervous system hemangioblastomas, or a type of pancreatic cancer called pancreatic neuroendocrine tumors, that do not require surgery right away.

How does this medicine work?

• Belzutifan is an inhibitor of hypoxia-inducible factor 2 alpha (HIF-2α).
• HIF-2α is a transcription factor that plays a role in oxygen sensing by regulating genes that promote adaptation to hypoxia.
• Upon oral administration, belzutifan binds to and blocks the function of HIF-2alpha, thereby preventing HIF-2alpha heterodimerization and its subsequent binding to DNA.
• This results in decreased transcription and expression of HIF-2alpha downstream target genes, many of which regulate hypoxic signaling.
• This inhibits cell growth and survival of HIF-2alpha-expressing tumor cells.
• HIF-2alpha, the alpha subunit for the heterodimeric transcription factor HIF-2, is overexpressed in many cancers and promotes tumorigenesis.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Welireg and certain other medicines can affect each other and cause serious side effects.
• Coadministration of Welireg with inhibitors of UGT2B17 or CYP2C19 increases plasma exposure of belzutifan. Monitor for signs and symptoms of anemia and hypoxia and reduce the dosage of Welireg as recommended.
• Coadministration of Welireg with CYP3A4 substrates decreases concentrations of CYP3A substrates, which may reduce the efficacy of these substrates. If coadministration cannot be avoided, increase the sensitive CYP3A4 substrate dosage.
• Coadministration of Welireg with hormonal contraceptives may lead to contraceptive failure or an increase in breakthrough bleeding.

Is this medicine FDA approved?

• Belzutifan was approved for medical use in the United States in August 2021.

How should this medicine be used?

Recommended dosage:

• The recommended dosage of Welireg is 120 mg administered orally once daily with or without food.

Administration:

• Take your prescribed dose of Welireg 1 time a day, at the same time each day.
• Your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with Welireg if you have certain side effects.
• Take Welireg with or without food.
• Swallow Welireg tablets whole. Do not chew, crush, or split Welireg tablets.
• If you miss a dose of Welireg, take it as soon as possible on the same day. Then take your next dose of Welireg at your regular time the next day. Do not take extra tablets to make up for the missed dose.
• If you vomit after taking a dose of Welireg, do not take an extra dose. Take your next dose at your regular time the next day.
• If you take too much Welireg, call your healthcare provider or go to the nearest emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 40 mg

This medicine is available in fallowing brand namesː

• Welireg

What side effects can this medication cause?

The most common side effects of this medicine include:

• feeling tired
• increased creatinine (kidney function test)
• headache
• feeling dizzy
• increased blood sugar (glucose) levels
• nausea

Welireg may cause serious side effects, including:

• Low red blood cell counts (anemia)
• Low oxygen levels in your body
• Harm to your unborn baby
• fertility problems in males and females

What special precautions should I follow?

• Welireg can cause severe anemia that can require blood transfusion. Monitor for anemia before initiation of and periodically throughout treatment with Welireg. Withhold Welireg until hemoglobin ≥9g/dL, then resume at reduced dose or discontinue. For life threatening anemia, or for anemia requiring urgent intervention, withhold Welireg until hemoglobin ≥9g/dL and resume at a reduced dose or permanently discontinue Welireg.
• Welireg can cause severe hypoxia that may require discontinuation, supplemental oxygen, or hospitalization. Monitor oxygen saturation before initiation of, and periodically throughout, treatment with Welireg. For hypoxia at rest, withhold until resolved, resume at reduced dose, or discontinue depending on severity. For life-threatening hypoxia, permanently discontinue Welireg.
• Based on findings in animals, Welireg can cause fetal harm when administered to a pregnant woman. 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.
• 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.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• hypoxia
• thrombocytopenia

Treatment of overdosage:

• There is no specific treatment for Welireg overdose.
• In cases of suspected overdose, withhold Welireg and institute supportive care.

Can this medicine be used in pregnancy?

• Treatment with Welireg during pregnancy can cause harm to your unborn baby.
• You should use an effective form of non-hormonal birth control (contraception) during treatment with Welireg and for 1 week after your last dose.
• Birth control methods that contain hormones (such as birth control pills, injections, or transdermal system patches) may not work as well during treatment with Welireg.

Can this medicine be used in children?

• It is not known if Welireg is safe and effective in children.

What are the active and inactive ingredients in this medicine?

• Active ingredient: belzutifan
• Inactive ingredients: croscarmellose sodium, hypromellose acetate succinate, magnesium stearate, mannitol, microcrystalline cellulose, and silicon dioxide. The film-coating contains FD&C Blue #2 aluminum lake, polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide.

Who manufactures and distributes this medicine?

Manufactured for:

• Merck Sharp & Dohme Corp., a subsidiary of
• MERCK & CO., INC., Whitehouse Station, NJ, USA

What should I know about storage and disposal of this medication?

• Store Welireg at room temperature between 68°F to 77°F (20°C to 25°C).
• The Welireg bottle contains 2 desiccant canisters that help keep your medicine dry.
• Do not eat the desiccant canisters.

• Dailymed label info on Belzutifan
• FDA Belzutifan

Belzutifan Resources
Latest articles Most recent articles Ongoing trials	Wikipedia

Belzutifan Resources
Latest articles Most recent articles Ongoing trials	Wikipedia