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Belzutifan(Welireg)

Acetylcysteine Injection, FLUIMUCIL, Acetylcysteine InjectionAcetylcysteine Injection, FLUIMUCIL, Acetylcysteine InjectionAcetylcysteine Injection, FLUIMUCIL, Acetylcysteine Injection

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Formulation:

TABLET

Validity period:

The "Revised: 04/2025" date on the document appears to be the revision date of the prescribing information, not the drug's shelf life or period of validity.

Reminder: The outer packaging is for reference only, please purchase and use under the guidance of a pharmacist. For read by medical and pharmaceutical professionals only.

WELIREG, with the active pharmaceutical ingredient belzutifan, is an orally administered medication available as 40 mg film-coated tablets. Chemically, belzutifan is 3-[[(1S,2S,3R)-2,3-Difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluorobenzonitrile. It is designed for therapeutic use in adult patients with specific oncological conditions, including tumors associated with von Hippel-Lindau disease and certain types of advanced kidney cancer.

The therapeutic effect of belzutifan is derived from its activity as an inhibitor of hypoxia-inducible factor 2 alpha (HIF-2αα). HIF-2αα is a key transcription factor that plays a significant role in the body's oxygen-sensing mechanisms by modulating genes involved in adaptation to hypoxic (low oxygen) conditions. By targeting and inhibiting HIF-2αα, WELIREG interferes with cellular pathways that contribute to the growth and progression of certain cancers.

Generic name

Belzutifan(Welireg)

English name

Belzutifan

Alternative Names

Welireg

Drug prices

Indications

WELIREG is a hypoxia-inducible factor inhibitor indicated for:

Von Hippel-Lindau (VHL) disease: For the 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. Advanced Renal Cell Carcinoma (RCC): 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).

Therapeutic Target

Hypoxia-inducible factor 2 alpha (HIF-2 α α).

Active Ingredients

Belzutifan. Each tablet contains 40 mg of belzutifan.

Dosage form

TABLET

specifications

Not specified in the specification beyond the tablet description (40 mg tablets).

Description

Belzutifan is an inhibitor of hypoxia-inducible factor-2αα (HIF-2αα). The chemical name is 3-[[(1S,2S,3R)-2,3-Difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluorobenzonitrile. The molecular formula is C1717H1212F33NO44S, and the molecular weight is 383.34 Daltons. Belzutifan is a white to light brown powder. It is soluble in acetonitrile, dimethoxyethane, and acetone; sparingly soluble in ethyl acetate; very slightly soluble in isopropanol and toluene; and insoluble in water. WELIREG tablets are supplied as blue, film-coated tablets for oral use containing 40 mg of belzutifan and the following 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.

Dosage and Administration

Recommended Dosage: The recommended dosage of WELIREG is 120 mg administered orally once daily until disease progression or unacceptable toxicity. It should be taken at the same time each day and may be taken with or without food.

Administration: Advise patients to swallow tablets whole. Do not chew, crush, or split WELIREG prior to swallowing.

Missed Dose: If a dose is missed, it can be taken as soon as possible on the same day. Resume the regular daily dose schedule the next day. Do not take extra tablets to make up for the missed dose.

Vomiting: If vomiting occurs any time after taking WELIREG, do not retake the dose. Take the next dose on the next day.

Dosage Modifications for Adverse Reactions:

Recommended dose reductions:

First dose reduction: WELIREG 80 mg orally once daily.

Second dose reduction: WELIREG 40 mg orally once daily.

Third dose reduction: Permanently discontinue.

Anemia:

Hemoglobin < 8 g/dL or transfusion indicated: Withhold until hemoglobin ≥≥ 8 g/dL. Resume at the same or reduced dose; or discontinue depending on severity.

Life-threatening or urgent intervention indicated: Withhold until hemoglobin ≥≥ 8 g/dL. Resume at a reduced dose or permanently discontinue.

Hypoxia:

Decreased oxygen saturation with exercise (e.g., pulse oximeter <88%): Consider withholding until resolved. Resume at the same dose or at a reduced dose depending on severity.

Decreased oxygen saturation at rest (e.g., pulse oximeter <88% or PaO22 $\le$55 mm Hg) or urgent intervention indicated: Withhold until resolved. Resume at reduced dose or discontinue depending on severity.

Life-threatening or recurrent symptomatic hypoxia: Permanently discontinue.

Other Adverse Reactions:

Grade 3: Withhold dosing until resolved to ≤≤ Grade 2. Consider resuming at a reduced dose. Permanently discontinue upon recurrence of Grade 3.

Grade 4: Permanently discontinue.

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