Alpelisib

Alpelisib is a prescription medication used to treat the symptoms of Breast Cancer. 

• Alpelisib is available under the following different brand names: Piqray, Vijoice

Common side effects of Alpelisib include:

• Nausea,
• Vomiting,
• Loss of appetite,
• Weight loss,
• Weakness,
• Tiredness,
• Mouth sores,
• Rash,
• Hair loss, and
• Abnormal blood tests

Serious side effects of Alpelisib include:

• Hives,
• Difficulty breathing,
• Swelling of the face, lips, tongue, or throat,
• Fast heartbeats,
• Fever,
• Sore throat,
• Burning eyes,
• Skin pain,
• Red or purple skin rash with blistering and peeling,
• Chest pain,
• Cough,
• Shortness of breath,
• Severe or ongoing diarrhea,
• Blisters or ulcers in the mouth,
• Red or swollen gums,
• Trouble swallowing,
• Pale skin,
• Unusual tiredness,
• Cold hands and feet,
• Little or no urination,
• Increased thirst,
• Increased urination,
• Dry mouth,
• Fruity breath odor,
• Confusion,
• Hunger, and
• Weight loss

Rare side effects of Alpelisib include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Tablet (Piqray)

• 50 mg
• 150 mg
• 200 mg

Tablet (Vijoice)

• 50 mg
• 125 mg
• 200 mg

Breast Cancer

Adult dosage

• Piqray only
  • Alpelisib 300 mg orally once a day AND
  • Fulvestrant 500 mg Intramuscular on Days 1, 15, and 29, and once monthly thereafter
  • Continue treatment until disease progression or unacceptable toxicity occurs
  • Refer to the full prescribing information for fulvestrant
  • PIK3CA-Related Overgrowth Spectrum

Adult dosage

• Vijoice only
  • 250 mg orally once a day
  • Continue until disease progression or unacceptable toxicity

Pediatric dosage

• Vijoice only
• Indicated for patients aged above 2 years with severe manifestations of PIK3CA-related overgrowth spectrum (PROS) who require systemic therapy
• Children below 2 years: Safety and efficacy not established
• 2 to below 6 years
  • 50 mg orally once a day
  • Continue until disease progression or unacceptable toxicity
• 6 to below 18 years
  • Initial: 50 mg orally once a day
  • After 24 weeks: Consider increasing to 125 mg once a day for response optimization (clinical/radiological)
  • Continue until disease progression or unacceptable toxicity
• Above 18 years
  • Consider gradually increasing up to 250 mg once a day

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Alpelisib has severe interactions with no other drugs.
• Alpelisib has serious interactions with at least 58 other drugs.
• Alpelisib has serious interactions with at least 49 other drugs.
• Alpelisib has minor interactions with the following drugs
  • amobarbital
  • dapsone
  • levoketoconazole
  • ribociclib

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Hypersensitivity to alpelisib or any of its components

Effects of drug abuse

• None

Short-Term Effects

See “What Are Side Effects Associated with Using Alpelisib?”

Long-Term Effects

See “What Are Side Effects Associated with Using Alpelisib?”

Cautions

• Angioedema reported in the n post-marketing setting
• Severe hypersensitivity reactions (. g, anaphylaxis, anaphylactic shock, angioedema) reported; reactions manifested by symptoms including, but not limited to, dyspnea, flushing, rash, fever, or tachycardia; permanently discontinue if hypersensitivity occurs
• Severe pneumonitis, including acute interstitial pneumonitis and interstitial lung disease, reported; consider noninfectious pneumonitis in patients presenting with nonspecific respiratory signs and symptoms (. g, hypoxia, cough, dyspnea, or interstitial infiltrates on radiologic examinations) and in whom infectious, neoplastic, and other causes have been excluded; permanently discontinue in all patients if confirmed; advise patients to immediately report new or worsening respiratory symptoms
• Based on findings in animals and their mechanism of action, fetal harm may occur when administered to pregnant women
• Diarrhea or Colitis
  • Severe diarrhea, including dehydration and acute kidney injury, occurred; based on the severity of diarrhea, therapy may require dose interruption, reduction, or discontinuation; advise patients to start antidiarrheal treatment, increase oral fluids, and notify their healthcare provider if diarrhea occurs
  • Colitis reported in the post-marketing setting
  • Monitor for diarrhea and additional symptoms of colitis, such as abdominal pain and mucus or blood in stool; based on severe diarrhea or colitis, dose interruption, reduction, or discontinuation may be necessary
  • For patients with colitis, additional treatment, such as enteric-acting and/or systemic steroids, may be required
• Severe cutaneous adverse reactions
  • Severe cutaneous reactions, including Stevens-Johnson syndrome (SJS) and erythema multiforme (EM), reported
  • Do not initiate with a history of SJS, EM, or toxic epidermal necrolysis (TEN), and drug reaction with eosinophilia and systemic symptoms (DRESS)
  • If signs or symptoms of cutaneous reactions occur, interrupt therapy until the etiology of the reaction determined
  • If SJS, TEN, or EM is confirmed, permanently discontinue; do not reintroduce in patients who have experienced previous severe cutaneous reactions during treatment
  • If cutaneous reactions are not confirmed, therapy may require dose modifications, topical corticosteroids, or oral antihistamine treatment
• Severe hyperglycemia
  • Closely monitor patients with diabetes
  • Based on the severity of hyperglycemia, therapy may require dose interruption, reduction, or discontinuation
  • In some cases, associated with the hyperglycemic hyperosmolar non-ketotic syndrome (HHNKS) or ketoacidosis; some fatal cases of ketoacidosis have occurred in the post-marketing setting
  • Before initiating treatment, test FPG, and HbA1c, and optimize blood glucose
  • After initiation, monitor fasting glucose more frequently for the first few weeks during treatment in patients with risk factors for hyperglycemia such as obesity (BMI greater than or equal to 30), elevated FPG, HbA1c at the upper limit of normal or above, use of concomitant systemic corticosteroids, or age greater than or equal to 75
  • Monitor blood glucose and/or FPG at least every Week for the first 2 weeks, then at least q4Weeks, and as clinically indicated; monitor HbA1c every 3 months and as clinically indicated
  • During treatment with antidiabetic medication, continue monitoring blood glucose or FPG at least once a week for 8 weeks, followed by once every 2 weeks and as clinically indicated
  • Advise patients of signs and symptoms of hyperglycemia (.g, excessive thirst, urinating more often than usual or higher amount of urine than usual, or increased appetite with weight loss)
• Drug interactions overview
  • Alpelisib: CYP3A4 and BCRP substrate; CYP2C9 inducer
  • CYP3A4 inducers
    • Avoid coadministration
  • Strong CYP3A4 inducers may decrease alpelisib concentration and/or activity
  • BCRP inhibitors
    • Avoid coadministration; if unable to avoid or use alternant drugs, closely monitor for increased adverse effects of alpelisib
    • BCRP inhibitors may increase alpelisib concentration and/or risk of toxicities
  • CYP2C9 substrates
    • Closely monitor for the potential reduced activity of the CYP2C9 substrate
    • Coadministration of alpelisib with CYP2C9 substrates (.g, warfarin) may reduce the plasma concentration of CYP2C9 substrates

Pregnancy and Lactation

• Based on animal data and mechanism of action, fetal harm may occur when administered to pregnant women
• No data available on pregnant women to inform the drug-associated risk
• Advise pregnant women and females of the reproductive potential of fetal risk
• Verify pregnancy status in females of reproductive potential before initiating
• Contraception
  • Females of reproductive potential: Use effective contraception during treatment and for 1 week after the last dose
  • Male patients with female partners of reproductive potential: Use condoms and effective contraception during treatment and for 1 week after the last dose
• Infertility
  • Based on findings from animal studies, fertility in males and females’ reproductive potential may be impaired
• Lactation
  • There are no data on the presence of alpelisib in human milk, its effects on milk production, or the breastfed child
  • Because of the potential for serious adverse reactions in the breastfed child, advise lactating women to not breastfeed during treatment and for 1 week after the last dose