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WELIREG is a brand name for Belzutifan, supplied as a tablet. The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: WELIREG® (belzutifan) is indicated for: Von Hippel-Lindau (VHL) disease WELIREG® is indicated for the treatment of adult patients with von Hippel-Lindau (VHL) disease who require therapy for associated non-metastatic renal cell carcinoma (RCC), central nervous system (CNS) hemangioblastomas, or non-metastatic…
Verbatim from this product's HC label. Tap a section to expand.
5 Dual UGT2B17 and CYP2C19 Poor Metabolizers 12/2024 TABLE OF CONTENTS Sections or subsections that are not applicable at the time of authorization are not listed. RECENT MAJOR LABEL CHANGES ...........................................................................................
2 TABLE OF CONTENTS ............................................................................................................. 2 PART I: HEALTH PROFESSIONAL INFORMATION .....................................................................
4 1 INDICATIONS .............................................................................................................. 1 Pediatrics .......................................................................................................................
2 Geriatrics ....................................................................................................................... 4 2 CONTRAINDICATIONS .................................................................................................
4 3 SERIOUS WARNINGS AND PRECAUTIONS BOX ............................................................ 5 4 DOSAGE AND ADMINISTRATION................................................................................. 1 Dosing Considerations ..................................................................................................
2 Recommended Dose and Dosage Adjustment ............................................................. 4 Administration .............................................................................................................. 5 Missed Dose ..................................................................................................................
7 5 OVERDOSAGE............................................................................................................. 7
) Grade 3 • Withhold dosing until symptoms improve to ≤ Grade 2. • Consider resuming at a reduced dose (reduce by 40 mg). • Permanently discontinue WELIREG® if Grade 3 adverse reaction recurs Grade 4 • Permanently discontinue. 0 Pediatrics: Health Canada has not authorized an indication for pediatric use.
Geriatrics (≥ 65 years of age):
No dose adjustment is needed in patients ≥ 65 years of age (see 10 CLINICAL PHARMACOLOGY). 73 m2) renal insufficiency. 73 m2) renal insufficiency (see 10 CLINICAL PHARMACOLOGY). 5 x ULN and any AST) hepatic insufficiency. 5 x ULN and any AST) hepatic insufficiency (see 10 CLINICAL PHARMACOLOGY).
UGT2B17 and CYP2C19 Genetic Polymorphism:
No dose adjustment is recommended for patients who are dual UGT2B17 and CYP2C19 poor metabolizers (see 7 WARNINGS AND PRECAUTIONS, 10 CLINICAL PHARMACOLOGY). 3 Pharmacokinetics). Tablets should be swallowed whole. Treatment should continue until disease progression or unacceptable toxicity occurs.
5 Missed Dose If a dose of WELIREG® is missed, it can be taken as soon as possible on the same day. The regular daily dose schedule for WELIREG® should be resumed the next day. Extra tablets should not be taken to make up for the missed dose.
If vomiting occurs any time after taking WELIREG®, the dose should not be retaken. The next dose should be taken the next day. 5 OVERDOSAGE There is no specific treatment for WELIREG® overdose. In cases of suspected overdose, if necessary, consider withholding WELIREG® and instituting supportive care.
The highest dose of WELIREG® studied clinically was 240 mg total daily dose (120 mg twice a day or 240 mg once a day). Adverse reactions observed in patients receiving more than 120 mg once a day were generally similar to those observed at other doses.
, geriatrics) 2 CONTRAINDICATIONS • WELIREG® is contraindicated in patients who are hypersensitive to this drug or to any ingredient in the formulation, including any non-medicinal ingredient, or component of the container. For a complete listing, see 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING.
WELIREG® (belzutifan) Page 5 of 36 3 SERIOUS WARNINGS AND PRECAUTIONS BOX Serious Warnings and Precautions Embryo-fetal toxicity (see 7 WARNING AND PRECAUTIONS, 16 NON-CLINICAL TOXICOLOGY) • 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. 1 Dosing Considerations • Verify the pregnancy status of females of reproductive potential prior to initiating treatment with WELIREG® (see 7 WARNING AND PRECAUTIONS, Special Populations).
3 Pharmacokinetics). Tablets should be swallowed whole. Treatment should continue until disease progression or unacceptable toxicity occurs. Dose Modification Guidelines Dosage modifications for WELIREG® for adverse reactions are summarized in Table 1.
The recommended dose reductions are: • First dose reduction:
WELIREG® 80 mg orally once daily • Second dose reduction: WELIREG® 40 mg orally once daily • Third dose reduction: Permanently discontinue Table 1 - Recommended Dose Modifications for Adverse Reactions Adverse Reactions Severity* Dose Modification Anemia (see 7 WARNINGS AND PRECAUTIONS) Grade 3 or transfusion indicated • Withhold until resolved to ≤ Grade 2.
• Resume at the same or reduced dose (reduce by 40 mg) or discontinue; consider discontinuing depending on the severity and persistence of anemia. Grade 4 • Withhold until resolved to ≤ Grade 2. • Resume at a reduced dose (reduce by 40 mg) or permanently discontinue upon recurrence of Grade 4.
• WELIREG® is contraindicated in patients who are hypersensitive to this drug or to any ingredient in the formulation, including any non-medicinal ingredient, or component of the container. For a complete listing, see 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING.
WELIREG® (belzutifan) Page 5 of 36
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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Dose-limiting toxicities included Grade 3 hypoxia (120 mg twice a day) and Grade 4 thrombocytopenia (240 mg once daily). For management of a suspected drug overdose, contact your regional poison control centre. 6 DOSAGE FORMS, STRENGTHS, COMPOSITION AND PACKAGING Table 2 – Dosage Forms, Strengths, Composition and Packaging Description 40 mg tablets of WELIREG®: blue, oval, film-coated tablet with “177” on one side.
Available in bottle of 90 tablets with desiccant and blisters of 90 tablets (3 cartons of 30 tablets inside of a larger, master carton). 7 WARNINGS AND PRECAUTIONS Please see 3 SERIOUS WARNINGS AND PRECAUTIONS BOX Driving and Operating Machinery No studies on the effects on the ability to drive and use machines have been performed.
Dizziness and fatigue may occur following administration of WELIREG® which could influence the ability to drive or use machines (see 8 ADVERSE REACTIONS).
Hematologic Anemia:
WELIREG® can cause severe anemia that can require blood transfusion and erythropoiesis stimulating agents. Route of Administration Dosage Form / Strength/Composition Non-medicinal Ingredients oral Tablet / 40 mg / belzutifan croscarmellose sodium, FD&C Blue #2 aluminum lake, hypromellose acetate succinate, magnesium stearate, mannitol, microcrystalline cellulose, polyethylene glycol, polyvinyl alcohol, colloidal silicon dioxide, talc and titanium dioxide.
WELIREG® (belzutifan) Page 8 of 36 Monitor for anemia before initiation of and routinely throughout treatment with WELIREG®. For patients who develop Grade 3 anemia, withhold WELIREG® and treat according to standard medical practice until resolved to ≤ Grade 2; then resume at the same or reduced dose.
For recurrent Grade 3 anemia, consider discontinuing WELIREG®. 2 Pharmacodynamics). A significant baseline (≤ 120 g/L) effect was found for risk of developing ≥ Grade 3 anemia in a Phase 1 study. 2%). 5%) (see 8 ADVERSE REACTIONS). 38 months).
Of the 14 patients that were treated with an erythropoiesis-stimulating agent (ESA), 5 received treatment with both an ESA and blood transfusions, while 9 received treatment with an ESA alone. 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. 5%) had Grade 4 anemia (see 8 ADVERSE REACTIONS). Median time to onset of anemia was 29 days (range: 1 day to 28 months). Of the patients with anemia, […]
Hypoxia Grade 2 • Consider whether to continue or withhold until WELIREG® (belzutifan) Page 6 of 36 Adverse Reactions Severity* Dose Modification (see 7 WARNINGS AND PRECAUTIONS) resolved. • If withheld, consider resuming at a reduced dose depending on severity and persistence of hypoxia.
Grade 3 • Withhold until resolved. • Resume at reduced dose (reduce by 40 mg) or discontinue depending on the severity and persistence of hypoxia. Grade 4 or recurrent symptomatic hypoxia • Permanently discontinue. Other Adverse Reactions (see