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What is Piqray® (alpelisib)?

Piqray® (alpelisib) is a medication that was recently approved by the Food and Drug Administration (FDA) to treat women after menopause as well as men with certain types of advanced or metastatic breast cancer. Alpelisib is used to treat breast cancer that is hormone-receptor-positive, HER2 negative, and contains a particular genetic mutation. Alpelisib is given to people whose cancer progresses during or after hormone therapy. It is supposed to be used in combination with fulvestrant, a specific hormonal therapy.1

Breast cancer tumors have different characteristics. These help doctors understand how the cancers grow and how best to treat the disease. Some tumors grow in the presence of the natural hormones estrogen or progesterone. These tumors contain special receptors, like molecular docking stations, that allow the hormones to attach. Cancers with these receptors are called hormone-receptor-positive (HR+) and those without receptors are called hormone-receptor-negative (HR-).2

Breast cancer tumors can also be characterized as HER2+ or HER2- cancers. HER2 refers to a particular protein that appears on the surface of cancer cells and makes the cells multiply faster. When cancer cells produce too many HER2 molecules, they are referred to as HER2+ tumors. HER2- cancers produce few or no HER2 molecules.2 Advanced breast cancer has spread beyond the breast tissue into other parts of the body.

What are the ingredients in Piqray?

The active ingredient in Piqray is alpelisib.

How does alpelisib work?

Alpelisib belongs to a class of medications called kinase inhibitors. A kinase is an enzyme, or protein, that is responsible for activating important cellular growth processes. About 40% of HR+/HER2- breast cancers contain a genetic mistake in a specific protein called PIK3CA.3 Mutations in PIK3CA lead to fast cell growth and tumor formation. Alpelisib blocks the molecular signaling proteins that are produced by the PIK3 gene.

Since alpelisib works only with tumors with the PIK3CA mutation, your doctor will test your tumor for it before prescribing this medication.3

What are the possible side effects of alpelisib?

Common side effects with alpelisib include4:

  • Rash
  • Nausea
  • Tiredness and weakness
  • Decreased appetite
  • Mouth sores
  • Vomiting
  • Weight loss
  • Hair loss
  • Changes in certain blood tests

In some patients, alpelisib may cause more harmful, sometimes life-threatening side effects. These include1:

  • Severe skin reactions, including severe rash as well as peeling and blistering on the skin, lips, eyes, or mouth
  • Dangerously high blood sugar levels in the blood
  • Lung problems, called pneumonitis, which may result in cough, trouble breathing, and chest pain
  • Severe diarrhea, which can lead to dangerous levels of water loss
  • Serious allergic reactions

Alpelisib has been shown to harm fetuses, so it is important not to become pregnant while you or your male partner are taking it. Alpelisib can also make it harder to get pregnant. This is not a complete list of all potential side effects of alpelisib. For more information, consult your doctor or healthcare provider. If you notice any new or worsening side effects, contact your doctor or healthcare provider immediately.

Things to note about alpelisib

Before taking alpelisib, tell your doctor if you:

  • Have a history of diabetes
  • Have a history of skin rash, peeling, redness, or blistering around the eyes, mouth, or lips
  • Are pregnant or plan to become pregnant or are breastfeeding

Tell your doctor about any medications or supplements you are taking while on alpelisib, since it does not mix well with certain medicines. Because alpelisib may cause dangerously high levels of blood sugar, your doctor will take blood tests before you start the medicine and will monitor your levels during treatment.

Dosing information

Alpelisib is a pill that is swallowed whole by mouth. Typically, alpelisib is taken once daily, and your healthcare provider will determine the appropriate dosing regimen for you. Try to take the medicine at about the same time each day. It is important to take the pills whole and not to crush, chew, or split them.5 For more information about alpelisib, read the complete prescribing information.

Written by: Editorial Team | Last reviewed: October 2019.
  1. Piqray. May 30, 2019. Available at: Accessed July 25, 2019.
  2. Tumor Characteristics: Hormone Receptor Status. Susan G. Komen Breast Cancer Foundation. January 31, 2019. Available at: Accessed July, 12, 2019.
  3. FDA Approves First PI3K Inhibitor for Breast Cancer. U.S. Food and Drug Administration. Published May 24, 2019. Accessed July 25, 2019.
  4. Prescribing Information. Piqray. Novartis Pharmaceuticals Corporation. May 2019. Available at: Accessed July 25, 2019.
  5. Piqray. DailyMed. US National Library of Medicine. May 24, 2019. Available at: Accessed July 25, 2019.