Alpelisib

Alpelisib
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Uma Maveli[2]

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Black Box Warning

WARNING: SEVERE HYPERSENSITIVITY TO ALPELISIB See full prescribing information for complete Boxed Warning. Severe hypersensitivity: Anaphylaxis and Anaphylactic shock The symptoms of these hypersensitivity reactions include dyspnea, flushing, rash, fever, and/or tachycardia About 0.7% of the patients showed signs of these symptoms. In cases of anaphylaxis or anaphylactic shock, patients showed Grade 3 or 4 hypersensitivity reactions Patients should be advised of the severe hypersensitivity reaction In the case that patients show signs/ symptoms of hypersensitivity, Alpelisib should be discontinued immediately

Overview

Alpelisib is a kinase inhibitors that is FDA approved for the treatment of . There is a Black Box Warning for this drug as shown here. Common adverse reactions include The most common adverse reactions for patients indicated for Alpelisib come in the form of laboratory abnormalities. They include increase in glucose, creatinine, GGT, ALT, or lipase, decrease in lymphocyte count, hemoglobin, appetite, calcium, weight, calcium, or glucose, the presence of diarrhea, rash, nausea, fatigue or alopecia.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

ALPELISIB is indicated for:

• PIQRAY is indicated for advanced metastatic breast cancer- hormone receptor positive, human epidermal growth factor receptor 2 negative, and PIK3CA mutated
• The breast cancer is measured by an approved FDA test
• It is a kinase inhibitor that is given concurrently with fulvestrant, a medication used to treat post menopause women with the conditions listed above

Limitations of Use

Recommended Vaccination and Prophylaxis

Recommended Weight-Based Dosage Regimen

Recommended Weight-Based Dosage Regimen

Dosing Considerations

• Alpelisib appears as tablets, and comes in the dose strengths 50 mg, 150 mg, and 200 mg

Preparation of ALPELISIB

Administration of ALPELISIB

• The recommended dose for patients is 300 mg taken orally daily once along with food
• The tablets appear in various strengths because adverse reactions (see adverse reactions) may cause patients to temporarily or permanently discontinue this medication

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding ALPELISIB Off-Label Guideline-Supported Use and Dosage (Adult) in the drug label.

Non–Guideline-Supported Use

There is limited information regarding ALPELISIB Off-Label Non-Guideline-Supported Use and Dosage (Adult) in the drug label.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding ALPELISIB FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding ALPELISIB Off-Label Guideline-Supported Use and Dosage (Pediatric) in the drug label.

Non–Guideline-Supported Use

There is limited information regarding ALPELISIB Off-Label Non-Guideline-Supported Use and Dosage (Pediatric) in the drug label.

Contraindications

• Patients may be advised to withhold this medication for a certain time period because of severe hypersensitivity to Alpelisib or any of its components (check components on the label or talk to a medical professional for more information)

Warnings

WARNING: SEVERE HYPERSENSITIVITY TO ALPELISIB See full prescribing information for complete Boxed Warning. Severe hypersensitivity: Anaphylaxis and Anaphylactic shock The symptoms of these hypersensitivity reactions include dyspnea, flushing, rash, fever, and/or tachycardia About 0.7% of the patients showed signs of these symptoms. In cases of anaphylaxis or anaphylactic shock, patients showed Grade 3 or 4 hypersensitivity reactions Patients should be advised of the severe hypersensitivity reaction In the case that patients show signs/ symptoms of hypersensitivity, Alpelisib should be discontinued immediately

Severe Cutaneous Reaction

• Less than 2 percent of the patients have shown these possibly lethal reactions connected to the skin and mucous membranes that could be linked to eyes, ears, nose, mouth, lips etc
• Diseases including Stevens-Johns Syndrome (0.4% of the patients) and Erythema Multiforme (1.1% of the patients) were linked to patients consuming or using this medication
• Treatment with Piqray will not be initiated in patients with histories of this disease. Additionally patients who have had severe cutaneous reactions while undergoing treatment with this disease will not be reintroduced to Piqray
• If symptoms appear in patients, temporarily discontinue the medications immediately
  • If the signs/ symptoms are confirmed to be associated with Severe Cutaneous Reactions, patients will have to permanently discontinue the medication
• If the reactions are not associated with Severe Cutaneous Reactions, there may be a need of dose modifications

Hyperglycemia

• Hyperglycemia has been reported in 65% of patients utilizing this medication. Some signs and symptoms of this disease could include excessive thirst, urinating more often than usual or higher amount of urine than usual, or increased appetite with weight loss.
  • Ketoacidosis was reported in 0.7% of patients
• Studies have shown patients usually show signs of hyperglycemia a median time of 15 days into treatment
• It is advised for patients to be tested to track FPG, HbA1c levels, and to optimize the blood glucose before initiating Piqray treatment
• The FPG and blood glucose levels should be monitored for at least the first 8 weeks, once a week. Later, there should be a checkup every 2 weeks, and the time indicated by the doctor.
• Patients should consider meeting with a professional with expertise in treating hyperglycemia. They may be able to help counsel the patients on lifestyle changes.
• Clinical studies have not tested the effect of Piqray on patients with Type 1 diabetes and uncontrolled Type 2 diabetes. Therefore, the safety of combining these diseases with Piqray has not yet been established. Patients should check with a medical practitioner and weight the pros and cons.
  • Patients with controlled Type 2 diabetes and Diabetes Mellitus were included, and it is advised to closely monitor these patients using Piqray.
• Patients may have to temporarily or permanently discontinue or reduce dose and treatment of Piqray based on the severity of the hyperglycemia present.

Pneumonitis

• Pneumonitis was discovered in 1.8% of the patients who were treated with Piqray
• Common forms of pneumonitis present within these patients are acute interstitial pneumonitis and interstitial lung disease
• If patients begin showing signs and symptoms of pneumonitis, immediately discontinue the drug until the presence of the disease is either confirmed or denied.
  • Symptoms of non-infectious pneumonitis include hypoxia, cough, dyspnea, or interstitial infiltrates on radiologic exams. There are no studies performed on patients with infectious or neoplastic pneumonitis because there are no means for an appropriate investigation.
• If patients are diagnosed with pneumonitis, discontinue the drug immediately. If they continue to have worsening symptoms, contact a medical professional immediately.

Diarrhea

• Severe diarrhea, that resulted in dehydration and acute kidney injury, have been present in 58% of patients undergoing treatment with Piqray.
• In a study, 6% of patients required dose reduction, and 2.8% of the people were required to permanently discontinue the drug. There were a total of 164 patients that experienced a case of diarrhea, and 63% of the patients needed to take anti-diarrheal medications.
• Patients may have to temporarily or permanently discontinue the drug, or reduce the dose if a problem with diarrhea persists or becomes severe

Embryo-Fetal Toxicity

• Female rats and rabbits pregnant were administered doses of Piqray. These studies have shown the effect Piqray can have on the mothers, and fetuses. It caused adverse developmental outcomes including embryo-fetal mortality, loss of fetal weight, and increased cases in fetal malformation.
• Pregnant females, and females with reproductive potential should be advised to use effective contraception during treatment, and 1 week after the last dose. Male patients should also use effective contraception and condoms during treatment and for 1 week after the last dose.

Monitoring Disease Manifestations after ALPELISIB Discontinuation

Infusion Reactions

Adverse Reactions

Clinical Trials Experience

Paroxysmal Nocturnal Hemoglobinuria (PNH)

Atypical Hemolytic Uremic Syndrome (aHUS)

Immunogenicity

Postmarketing Experience

There is limited information regarding Alpelisib Postmarketing Experience in the drug label.

Drug Interactions

CYP3A4 Inducer

Administering Alpelisib along with a CYP3A4 Inducer may result in a decrease in Alpelisib concentration, and a decrease in effectiveness and activity. Patients should avoid co-administering Alpelisib with strong CYP3A4 inducers.

BCRP Inhibitors

Administering Alpelisib with BCRP inhibitors increases Alpelisib concentrations that can result in the risk of toxicity in patients. Coadministering Alpelisib with BCRP inhibitors should be avoided. If it is not possible to completely avoid, patients should be closely monitored for adverse reactions.

CYP2C9 Substrates

Administering Alpelisib with CYP2C9 substrates may result in reduced plasma concentrations of the drug. It is advised to monitor patients closely for a decrease in plasma concentrations because that can cause reduced activity and effectiveness of the drug.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There are no available data on ALPELISIB use in pregnant women to inform a drugassociated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Alpelisib in women who are pregnant.

Labor and Delivery

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

Nursing Mothers

There is no FDA guidance on the use of Alpelisib in women who are nursing.

Pediatric Use

The safety and efficacy of ALPELISIB for the treatment of PNH in pediatric patients have not been established.

Geriatic Use

Clinical studies of ALPELISIB did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.

Gender

There is no FDA guidance on the use of ALPELISIB with respect to specific gender populations.

Race

There is no FDA guidance on the use of ALPELISIB with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of ALPELISIB in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of ALPELISIB in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of ALPELISIB in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of ALPELISIB in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Alpelisib Administration in the drug label.

Monitoring

There is limited information regarding Alpelisib Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Alpelisib and IV administrations.

Overdosage

If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

Alpelisib
Systematic (IUPAC) name
?
Identifiers
CAS number	1803171-55-2
ATC code	?
PubChem	?
Chemical data
Formula	?
Mol. mass	188303.705 Da
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Mechanism of Action

• Ravulizumab-cwvz is a terminal complement inhibitor that specifically binds to the complement protein C5 with high affinity, thereby inhibiting its cleavage to C5a (the proinflammatory anaphylatoxin) and C5b (the initiating subunit of the terminal complement complex [C5b-9]) and preventing the generation of the terminal complement complex C5b9.

Structure

There is limited information regarding ALPELISIB Structure in the drug label.

Pharmacodynamics

There is limited information regarding Alpelisib Pharmacodynamics in the drug label.

Pharmacokinetics

Distribution

Elimination

Specific Populations

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

Clinical Studies

There is limited information regarding Alpelisib Clinical Studies in the drug label.

How Supplied

There is limited information regarding Alpelisib How Supplied in the drug label.

Storage

There is limited information regarding Alpelisib Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

Severe Hypersensitivity

Severe Cutaneous Reaction

Hyperglycemia

Pneumonitis

Diarrhea

Embryo-Fetal Toxicity

Discontinuation

Infusion reactions

• Advise patients that administration of ALPELISIB may result in infusion reactions.

Precautions with Alcohol

Alcohol-Alpelisib interaction has not been established. Talk to your doctor regarding the effects of taking alcohol with this medication.

Brand Names

Piqray

Look-Alike Drug Names

There is limited information regarding ALPELISIB Look-Alike Drug Names in the drug label.

Drug Shortage Status

Drug Shortage

Price

References

The contents of this FDA label are provided by the National Library of Medicine.