Alpelisib

What is Alpelisib?

• Alpelisib (Piqray) is a kinase inhibitor used in combination with the medicine fulvestrant to treat women who have gone through menopause and men with advanced or metastatic breast cancer.

What are the uses of this medicine?

This medicine is used in combination with the medicine fulvestrant to treat women who have gone through menopause and men:

• who have hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer or breast cancer that has spread to other parts of the body (metastatic), with an abnormal phosphatidylinositol-3-kinase catalytic subunit alpha (PIK3CA) gene, and
• whose disease has progressed on or after endocrine therapy.

How does this medicine work?

• An orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.
• Alpelisib specifically inhibits PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway.
• This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations.
• Activation of the PI3K signaling pathway is frequently associated with tumorigenesis.
• Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• severe hypersensitivity to it or any of its components

What drug interactions can this medicine cause?

• Avoid coadministration of Piqray with strong CYP3A4 inducers. Coadministration of Piqray with a strong CYP3A4 inducer may decrease alpelisib concentration , which may decrease alpelisib activity.
• Avoid the use of BCRP inhibitors in patients treated with Piqray.
• Coadministration of Piqray with a breast cancer resistance protein (BCRP) inhibitor may increase alpelisib concentration , which may increase the risk of toxicities.

Is this medicine FDA approved?

• It was approved for use in the United States in 2019.

How should this medicine be used?

• Select patients for the treatment of HR-positive, HER2-negative advanced or metastatic breast cancer with Piqray, based on the presence of one or more PIK3CA mutations in tumor tissue or plasma specimens.

Recommended Dosage

• Recommended Dose: 300 mg (two 150 mg tablets) taken orally once daily with food.
• For adverse reactions, consider dose interruption, dose reduction, or discontinuation.

Administration

• Take Piqray exactly as your healthcare provider tells you.
• Do not change your dose or stop taking Piqray unless your healthcare provider tells you.
• Take Piqray 1 time each day, at about the same time each day.
• Take Piqray with food.
• Swallow Piqray tablets whole. Do not chew, crush or split the tablets.
• Do not take any Piqray tablets that are broken, cracked, or that look damaged.
• If you miss a dose of Piqray, you may still take it with food up to 9 hours after the time you usually take it. If it has been more than 9 hours after you usually take your dose, skip the dose for that day. The next day, take the dose at your usual time. Do not take 2 doses to make up for a missed dose.
• If you vomit after taking a dose of Piqray, do not take another dose on that day. Take your next dose at your usual time.
• If you take too much Piqray, call your healthcare provider or go to the nearest hospital 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: 50 mg, 150 mg, and 200 mg

This medicine is available in fallowing brand namesː

• Piqray

What side effects can this medication cause?

The most common side effects of this medicine include:

• rash
• nausea
• tiredness and weakness
• decreased appetite
• mouth sores
• vomiting
• weight loss
• hair loss
• changes in certain blood tests

Piqray may cause serious side effects, including:

• Severe allergic reactions
• Severe skin reactions
• High blood sugar levels (hyperglycemia)
• Lung problems (pneumonitis)
• Diarrhea

What special precautions should I follow?

• Severe hypersensitivity reactions, including anaphylaxis and anaphylactic shock, can occur in patients treated with Piqray. Advise patients of the signs and symptoms of severe hypersensitivity reactions. Permanently discontinue Piqray in the event of severe hypersensitivity.
• Severe cutaneous adverse reactions (SCARs), including Stevens-Johnson Syndrome (SJS), erythema multiforme (EM), toxic epidermal necrolysis (TEN), and drug reaction with eosinophilia and systemic symptoms (DRESS) can occur in patients treated with Piqray. Advise patients of the signs and symptoms of SCARs (e.g., a prodrome of fever, flu-like symptoms, mucosal lesions, progressive skin rash, or lymphadenopathy).
• Severe hyperglycemia, including ketoacidosis, can occur in patients treated with Piqray. Based on the severity of the hyperglycemia, Piqray may require dose interruption, reduction, or discontinuation.
• Severe pneumonitis, including acute interstitial pneumonitis and interstitial lung disease, can occur in patients treated with Piqray. Permanently discontinue Piqray in all patients with confirmed pneumonitis.
• Severe diarrhea, including dehydration and acute kidney injury, can occur in patients treated with Piqray. Based on the severity of the diarrhea, Piqray may require dose interruption, reduction, or discontinuation.
• Piqray can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception.

What to do in case of emergency/overdose?

In cases where accidental overdosage of Piqray was reported in the clinical studies, the adverse reactions associated with the overdose were hyperglycemia, nausea, asthenia, and rash.

Management for overdosage: Initiate general symptomatic and supportive measures in all cases of overdosage where necessary. There is no known antidote for Piqray.

Can this medicine be used in pregnancy?

• Piqray can cause fetal harm when administered to a pregnant woman . There are no available data in pregnant women to inform the drug-associated risk.

Can this medicine be used in children?

• The safety and efficacy of Piqray in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: alpelisib
• Inactive ingredients: hypromellose, magnesium stearate, mannitol, microcrystalline cellulose, and sodium starch glycolate. The film-coating contains hypromellose, iron oxide black, iron oxide red, macrogol/polyethylene glycol (PEG) 4000, talc, and titanium dioxide.

Who manufactures and distributes this medicine?

• Distributed by: Novartis Pharmaceuticals Corporation, East Hanover, New Jersey

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

• Store Piqray at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep Piqray and all medicines out of the reach of children.

• Dailymed label info on Alpelisib
• FDA Alpelisib

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