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.

Call your doctor right away if you have severe diarrhea.

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.

If you have diarrhea while taking alpelisib: start taking anti-diarrhea medicine such as loperamide (Imodium) to treat diarrhea quickly. Drink extra fluids and call your doctor.

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.

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.
Maintenance dose:
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.

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).

Pregnancy

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.

Breastfeeding

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.

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.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Follow your doctor's instructions about any restrictions on food, beverages, or activity.