Uses of Alpelisib

Alpelisib is used in combination with fulvestrant (Faslodex) to treat a certain type of breast cancer that has spread to nearby tissues or other parts of the body in women who have already gone through menopause (”change of life,” end of menstrual periods) or in men, whose cancer got worse during or after certain other treatments. Alpelisib is in a class of medications called kinase inhibitors. It works by blocking the signals that cause cancer cells to multiply. This helps to stop the spread of cancer cells.

Side Effects of Alpelisib

Alpelisib may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • nausea
  • vomiting
  • extreme tiredness
  • decreased appetite
  • change in the way things taste
  • weight loss
  • abdominal pain
  • heartburn
  • hair loss
  • headache
  • itching
  • dry skin
  • dry mouth
  • vaginal dryness
  • fever
  • swelling of the arms or legs

Some side effects can be serious. If you experience any of these symptoms call your doctor immediately or get emergency medical treatment:

  • trouble swallowing or breathing, rash, flushing, fever, or fast heartbeat
  • blistering, peeling skin, rash, reddened skin, sores on the lips or in the mouth, fever, flu-like symptoms
  • increased thirst, dry mouth, increased appetite with weight loss, urinating more often or larger amounts than usual, breath that smells like fruit
  • shortness of breath, cough, chest pain, difficulty breathing
  • severe diarrhea, dry mouth, cramps, weakness, decreased urination, swelling of legs or ankles
  • frequent, painful, or urgent urination

Alpelisib may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.

Warnings & Precautions

Before taking alpelisib:

  • tell your doctor and pharmacist if you are allergic to alpelisib, any other medications, or any of the ingredients in alpelisib tablets. Ask your pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, or nutritional supplements you are taking or plan to take. Be sure to mention any of the following: carbamazepine (Carbatrol, Equetro, Tegretol, others), cyclosporine (Gengraf, Neoral, Sandimmune), efavirenz (Sustiva, in Atripla, Symfi), eltrombopag (Promacta), nevirapine (Viramune), phenobarbital, phenytoin (Dilantin, Phenytek), pioglitazone (Actos, in Oseni, Duetact), rifabutin (Mycobutin), rifampin (Rifadin, Rimactane, in Rifamate, Rifater), and warfarin (Coumadin, Jantoven). Your doctor may need to change the doses of your medications or monitor you carefully for side effects. Many other medications may also interact with alpelisib, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
  • tell your doctor what herbal products you are taking, especially curcumin and St. John’s wort.
  • tell your doctor if you have ever had a rash with red sores on the lips, mouth or skin, or shedding, blistering skin; or have or have ever had diabetes or kidney disease.
  • tell your doctor if you or your partner are pregnant, or plan to become pregnant. You or your partner should not become pregnant during your treatment with alpelisib. If you are a female that can become pregnant, you will need to have a pregnancy test before you begin treatment, and you should use effective birth control during your treatment and for 1 week after your final dose. If you are a male with a female partner that can become pregnant, use a condom during your treatment and for 1 week after your final dose. If you or your partner become pregnant while taking alpelisib, call your doctor.
  • tell your doctor if you are breast-feeding. Your doctor may tell you not to breast-feed during your treatment and for 1 week after your final dose.
  • you should know that this medication may decrease fertility in men and women. Talk to your doctor about the risks of taking alpelisib.


Alpelisib comes as a tablet to take by mouth. It is usually taken with food once a day for as long as your doctor recommends treatment. Take alpelisib at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take alpelisib exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Swallow the tablets whole; do not split, chew, or crush them. Do not take a tablet that is broken, cracked, or is damaged.

If you vomit after taking alpelisib, do not take another dose. Continue your regular dosing schedule.

Your doctor may decrease your dose of alpelisib, treat you with other medications, or interrupt or stop your treatment if you experience certain side effects. Be sure to tell your doctor how you are feeling during your treatment with alpelisib.

Ask your pharmacist or doctor for a copy of the manufacturer’s information for the patient


Keep all appointments with your doctor and the laboratory. Your doctor will order a lab test before you begin your treatment to see whether your cancer can be treated with alpelisib. Your doctor will also order certain lab tests before and during your treatment to check your body’s response to alpelisib.

It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.


All information has been provided courtesy of MedLinePlus from the National Library of Medicine and from the FDA.