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Alpelisib Dosage

Medically reviewed by Drugs.com. Last updated on Jul 29, 2019.

Applies to the following strengths: 200 mg; 150 mg; 200 mg-50 mg

Usual Adult Dose for Breast Cancer

300 mg orally once a day with food until disease progression or unacceptable toxicity; when given with this drug, the recommended dose of fulvestrant is 500 mg orally on Days 1, 15, and 29, and once monthly thereafter

Use: In combination with fulvestrant for the treatment of postmenopausal women, and men, with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CAmutated, advanced or metastatic breast cancer as detected by an FDA-approved test following progression on or after an endocrine-based regimen.

Renal Dose Adjustments

Mild to moderate renal impairment (CrCl 30 to less than 90 mL/min): No adjustment recommended.
Severe renal impairment (CrCl less than 30 mL/min): Data not available

Liver Dose Adjustments

No adjustment recommended.

Dose Adjustments

DOSE MODIFICATIONS FOR ADVERSE REACTIONS:
-Starting dose: 300 mg orally once a day
-First dose reduction: 250 mg orally once a day
-Second dose reduction: 200 mg orally once a day
-If further dose reduction below 200 mg once daily is required, discontinue therapy.
NOTE: Only one dose reduction is permitted for pancreatitis.

DOSE MODIFICATIONS FOR HYPERGLYCEMIA:
-GRADE 1 (FPG greater than ULN minus 160 mg/dL or greater than ULN minus 8.9 mmol/L): No adjustment required; initiate or intensify antidiabetic treatment (*2).
-GRADE 2 (FPG greater than 160 to 250 mg/dL or greater than 8.9 to 13.9 mmol/L): No adjustment required; initiate or intensify antidiabetic treatment (*2); if FPG does not decrease to 160 mg/dL or less or 8.9 mmol/L or less within 21 days with antidiabetic treatment, reduce the dose of this drug by 1 dose level and follow FPG value specific recommendations.
-GRADE 3 (greater than 250 to 500 mg/dL or greater than 13.9 to 27.8 mmol/L): Interrupt this drug; initiate or intensify antidiabetic treatment (*2) and consider additional antidiabetic medications (*3) for 1 to 2 days until hyperglycemia improves. Administer IV hydration and consider treatment (e.g., intervention for electrolyte/ketoacidosis/hyperosmolar disturbances). If FPG decreases to 160 mg/dL or less or 8.9 mmol/L or less within 3 to 5 days under antidiabetic treatment, resume this drug at 1 lower dose level. If FPG does not decrease to 160 mg/dL or less or 8.9 mmol/L or less within 3 to 5 days under antidiabetic treatment, consultation with a physician with expertise in the treatment of hyperglycemia is recommended. If FPG does not decrease to 160 mg/dL or less or 8.9 mmol/L or less within 21 days following antidiabetic treatment (*2), permanently discontinue this drug.
-GRADE 4 (greater than 500 mg/dL or greater than 27.8 mmol/L): Interrupt this drug; initiate or intensify antidiabetic treatment (*2) and consider additional antidiabetic treatment (administer IV hydration and consider treatment (e.g., intervention for electrolyte/ketoacidosis/hyperosmolar disturbances)), re-check FPG within 24 hours and as clinically indicated. If FPG decreases to 500 mg/dL or less or 27.8 mmol/L or less, follow FPG value specific recommendations for Grade 3. If FPG is confirmed at greater than 500 mg/dL or greater than 27.8 mmol/L, permanently discontinue this drug.
NOTE:
(*1) FPG/Blood Glucose/Grade levels reflect hyperglycemia grading according to Common Terminology Criteria for Adverse Events (CTAE).
(*2) Initiate applicable antidiabetic medications, including metformin and insulin sensitizers (such as thiazolidinediones or dipeptidyl peptidase-4 inhibitors), and review respective prescribing information for dosing and dose titration recommendations, including local diabetic treatment guidelines. Metformin was recommended in the SOLAR-1 trial with the following guidance: Initiate metformin 500 mg once daily. Based on tolerability, metformin dose may be increased to 500 mg twice daily, followed by 500 mg with breakfast, and 1000 mg with dinner, followed by further increase to 1000 mg twice daily if needed.
(*3) As recommended in the SOLAR-1 trial, insulin may be used for 1 to 2 days until hyperglycemia resolves; however, this may not be necessary in the majority of alpelisib-induced hyperglycemia, given the short half-life of alpelisib and the expectation of glucose levels normalizing after interruption of alpelisib.

DOSE MODIFICATIONS FOR RASH:
-GRADE 1 (less than 10% body surface area [BSA] with active skin toxicity): No adjustment required; initiate topical corticosteroid treatment; consider adding oral antihistamine to manage symptoms
-GRADE 2 (10% to 30% BSA with active skin toxicity): No adjustment required; initiate or intensify topical corticosteroid and oral antihistamine treatment; consider low dose systemic corticosteroid treatment
-GRADE 3 (e.g., severe rash not responsive to medical management) (greater than 30% BSA with active skin toxicity): Interrupt this drug; initiate or intensify topical/systemic corticosteroid and oral antihistamine treatment when improved to Grade 1 or less, resume this drug at the same dose level for first occurrence of rash, or at next lower dose level in case of second occurrence
-Grade 4 (e.g., severe bullous, blistering or exfoliating skin conditions) (any % BSA associated with extensive superinfection, with IV antibiotics indicated; life-threatening consequences): Permanently discontinue this drug.
NOTE:
-Grading according to CTCAE.
-For all grades of rash, consider consultation with a dermatologist.
-Antihistamines administered prior to rash onset may decrease incidence and severity of rash.

DOSE MODIFICATIONS FOR DIARRHEA:
-Grade 1: No adjustment required; initiate medical therapy and monitor as clinically indicated.
-Grade 2: Initiate or intensify medical therapy and monitor as clinically indicated; interrupt this drug until recovery to Grade 1 or less, then resume this drug at same dose level.
-Grade 3 and 4: Initiate or intensify medical therapy and monitor as clinically indicated. Interrupt this drug until recovery to Grade 1 or less, then resume this drug at the next lower dose level.
NOTE:
-Grading according to CTCAE.

DOSE MODIFICATIONS OTHER TOXICITIES (excluding hyperglycemia, rash, and diarrhea):
-Grade 1 or 2: No dose adjustment required; initiate medical therapy and monitor as clinically indicated (*2) (*3).
-Grade 3: Interrupt this drug until recovery to Grade 1 or less, then resume this drug at the next lower dose level.
-Grade 4: Permanently discontinue this drug.
NOTE:
(*1) Grading according to CTCAE.
(*2) For Grade 2 and 3 pancreatitis, interrupt this drug until recovery to less than Grade 2 and resume at next lower dose level; only one dose reduction is permitted; if toxicity reoccurs, permanently discontinue this drug.
(*3) For Grade 2 total bilirubin elevation, interrupt this drug dose until recovery to Grade 1 or less and resume at the same dose if resolved in 14 days or less or resume at the next lower dose level if resolved in greater than 14 days.

Refer to the prescribing information of fulvestrant for dose modification guidelines in the event of toxicity.

Precautions

CONTRAINDICATIONS:
-Hypersensitivity to the active component or any of the ingredients

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Other Comments

Administration advice:
-Select patients for the treatment of HR-positive, HER2-negative advanced or metastatic breast cancer with this drug based on the presence of one or more PIK3CA mutations in tumor tissue or plasma specimens. If no mutation is detected in a plasma specimen, test tumor tissue.
-This drug should be taken at approximately the same time each day with food.
-Swallow tablets whole; do not chew, crush, or split.
-No tablet should be ingested if it is broken, cracked, or otherwise not intact.
-If a dose is missed, it can be taken with food within 9 hours after the time it is usually taken. After more than 9 hours, skip the dose for that day. The next day, take at the usual time.
-If the patient vomits after taking the dose they should not to take an additional dose on that day and should resume the dosing schedule the next day at the usual time.

Storage requirements:
Store at 20C to 25C (68F to 77F); excursions permitted between 15C and 30C (59F and 86F).

Patient advice:
-Read the approved patient labeling.
-Contact your healthcare provider immediately for signs hypersensitivity or severe cutaneous reactions.
-Monitor blood glucose periodically during therapy and contact your healthcare provider immediately for signs hyperglycemia.
-Contact your healthcare provider if you experience respiratory problems.
-This drug may cause diarrhea, which may be severe in some cases. Start antidiarrheal treatment, increase oral fluids, and notify your healthcare provider if diarrhea occurs.
-This drug can harm a developing fetus.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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