What is alpelisib?
Alpelisib (Piqray brand) is used to treat types of breast cancer in men and postmenopausal women, and Vijoice brand of alpelisib is used to treat a condition called PROS (PIK3CA-Related Overgrowth Spectrum) in certain patients. Alpelisib is a targeted therapy from a class of medicines called PI3K inhibitors (phosphoinositide 3-kinase inhibitors) and is sometimes called a kinase inhibitor. Alpelisib is only used for PIK3CA-mutated tumors as detected by an FDA-approved test.
Piqray became an FDA-approved medicine on May 24, 2019, as the first PI3K Inhibitor for specific breast cancers. Vijoice became an FDA-approved medicine on April 5, 2022, to treat specific patients with PIK3CA-Related Overgrowth Spectrum (PROS).
What is PI3K and PIK3CA?
PI3K is an enzyme involved in cellular functions such as cell growth, proliferation, differentiation, motility, and survival. PI3K is the short name for Phosphatidylinositol-3-kinase.
PIK3CA is a small part of PI3K. PIK3CA is the short name for Phosphatidylinositol-3-kinase catalytic subunit alpha. When there is a mutation in the PIK3CA gene it can allow cancer cells to grow and survive, which results in tumors.
How does alpelisib work?
Alpelisib works by blocking PIK3CA and is used to treat conditions that have a specific genetic mutation in the PIK3CA gene. In breast cancer, the mutation in the PIK3CA gene results in the generation of tumors, Piqray works to block PI3K which reduces breast cancer growth. The combination of Piqray and fulvestrant has an increased anti-tumor activity compared to either treatment alone.
In PIK3CA-Related Overgrowth Spectrum (PROS) the mutation in the PIK3CA gene causes cells to grow and divide abnormally. This causes overgrowths and malformations which may affect different parts of the body with symptoms varying widely with a range of clinically recognizable disorders. Vijoice works for PROS by blocking PI3K which reduces cell growth and may improve PROS symptoms or prevent them from worsening.
What is alpelisib used to treat?
Piqray brand of alpelisib is used to treat breast cancer in men and postmenopausal women if their cancer is:
- PIK3CA-mutated as detected by an FDA-approved test,
- advanced or metastatic breast cancer,
- cancer has progressed on or after an endocrine-based regimen,
- hormone receptor (HR)-positive,
- human epidermal growth factor receptor 2 (HER2)-negative, and
- treatment is used in combination with a hormone therapy fulvestrant (Faslodex), used for certain types of breast cancer treatment.
Vijoice brand of alpelisib is used to treat PIK3CA-Related Overgrowth Spectrum (PROS) with severe manifestations in patients who:
- require systemic therapy,
- are 2 years and older.
Vijoice is approved under accelerated approval based on response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).
Alpelisib side effects
Common alpelisib side effects may include:
- nausea, vomiting;
- loss of appetite, weight loss;
- feeling weak or tired;
- mouth sores;
- hair loss; or
- abnormal blood tests.
Serious alpelisib side effects
Get emergency medical help if you have signs of an allergic reaction (hives, warmth or tingling, difficulty breathing, fast heartbeats, swelling in your face or throat) or a severe skin reaction (fever, sore throat, burning eyes, skin pain, red or purple skin rash with blistering and peeling).
Seek medical treatment if you have a serious drug reaction that can affect many parts of your body. Symptoms may include skin rash, fever, swollen glands, muscle aches, severe weakness, unusual bruising, or yellowing of your skin or eyes.
Alpelisib may cause other serious side effects. Call your doctor at once if you have:
- chest pain, cough, feeling short of breath;
- severe or ongoing diarrhea;
- blisters or ulcers in your mouth, red or swollen gums, trouble swallowing;
- pale skin, unusual tiredness, cold hands and feet;
- little or no urination; or
- high blood sugar with symptoms of increased thirst, increased urination, dry mouth, fruity breath odor, confusion, hunger, weight loss;
Your cancer treatments may be delayed or permanently discontinued if you have certain side effects.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Call your doctor right away if you have severe diarrhea.
Before taking this medicine
You should not use alpelisib if you are allergic to it or any of the inactive ingredients.
Tell your doctor if you have ever had:
- diabetes; or
- a severe skin rash (skin pain, redness, peeling, burning eyes, blistering of your lips or mouth).
Alpelisib can cause fetal harm when administered to a pregnant woman, you may need to have a negative pregnancy test before starting this treatment. Tell your doctor if you think you may be pregnant.
Male patients with female partners of reproductive potential should be advised to use condoms and effective contraception during treatment with Alpelisib and for 1 week after the last dose.
Alpelisib and fulvestrant both can harm an unborn baby or cause birth defects if the mother or the father is using these medicines.
- If you are a woman, do not use alpelisib if you are pregnant. Use effective birth control to prevent pregnancy while you are using alpelisib and for at least 1 week after your last dose.
- If you are a man, use condoms and effective birth control if your sex partner is pregnant or is able to get pregnant. Keep using condoms and birth control for at least 1 week after your last dose.
- Tell your doctor right away if a pregnancy occurs while either the mother or the father is using alpelisib.
- Women who also take fulvestrant may need to prevent pregnancy for at least 1 year after treatment ends. Ask your doctor about how long to keep using birth control.
Alpelisib and fulvestrant may affect fertility (ability to have children) in both men and women. However, it is important to use birth control to prevent pregnancy because these medicines can harm an unborn baby.
Do not breastfeed while using alpelisib, and for at least 1 week after your last dose. If you are also using fulvestrant then you may not be able to breastfeed for 1 year after your last dose of fulvestrant. Ask your doctor.
How should I take alpelisib?
Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed.
Take alpelisib tablets with food, at the same time each day.
Swallow the tablet whole and do not crush, chew, or break it. Do not use a cracked or broken tablets
If you vomit shortly after taking alpelisib, do not take another dose. Wait until your next scheduled dose time to take the medicine again.
Alpelisib can cause severe diarrhea, which can be life-threatening if it leads to dehydration or kidney damage.
Your blood sugar will need to be checked often, and you may need other blood tests at your doctor's office.
Alpelisib and fulvestrant are usually given until your body no longer responds to the treatment, or until you have a serious side effect. Your doctor will determine how long to treat you.
Alpelisib dosing information
Usual Piqray Adult Dose for Breast Cancer:
Recommended dose: 300 mg (two 150 mg film-coated tablets) orally once a day with food, at approximately the same time each day.
Comments: Treatment is usually until disease progression or unacceptable toxicity. When fulvestrant is prescribed with alpelisib the recommended dose of fulvestrant is 500 mg orally on Days 1, 15, and 29, and once monthly thereafter. The alpelisib dose may be changed due to adverse reactions.
Usual Vijoice Adult Dose for PIK3CA-Related Overgrowth Spectrum:
Recommended dose: 250 mg orally once a day.
Comments: Treatment is usually until disease progression or unacceptable toxicity.
Usual Vijoice Pediatric Dose for PIK3CA-Related Overgrowth Spectrum:
Initial dose: 50 mg orally once a day.
Patients younger than 6 years old: 50 mg orally once a day.
Patients 6 years and older: Increase to 125 mg orally once a day after 24 weeks of 50 mg/day.
Maximum dose: 125 mg/day oral
Duration of therapy: Until disease progression or unacceptable toxicity.
Comment: When the pediatric patient turns 18 years old, consider a gradual dose increase up to 250 mg/day.
What happens if I miss a dose?
Take the medicine (with food) as soon as you can, but skip the missed dose if you are more than 9 hours late for the dose. Do not use two doses at one time.
Call your doctor for instructions if you miss an appointment for your fulvestrant injection.
What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.
What should I avoid while taking alpelisib?
Follow your doctor's instructions about any restrictions on food, beverages, or activity.
What other drugs will affect alpelisib?
Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective.
Other drugs may affect alpelisib, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all your current medicines and any medicine you start or stop using.
- Store Vijoice at 68°F to 77°F (20°C to 25°C) excursions permitted between 15°C and 30°C (59°F and 86°F).
- Store Piqray at room temperature between 68°F to 77°F (20°C to 25°C).
Active ingredient: alpelisib
Piqray 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.
Vijoice inactive ingredients: hypromellose, magnesium stearate, mannitol, microcrystalline cellulose, and sodium starch glycolate. The film-coating contains hypromellose, iron oxide red (applicable only to 50 mg and 200 mg strengths), iron oxide yellow, macrogol/polyethylene glycol (PEG) 4000, talc, and titanium dioxide.
Piqray Distributed by: Novartis Pharmaceuticals Corporation, East Hanover, New Jersey 07936.
Vijoice Distributed by: Novartis Pharmaceuticals Corporation, East Hanover, New Jersey 07936.
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