What Is Piqray® (alpelisib)?

Reviewed by: HU Medical Review Board | Last reviewed: June 2023

Piqray® (alpelisib) is used to treat women after menopause and men with certain types of advanced or metastatic breast cancer. It is used in combination with fulvestrant, a specific hormonal therapy. Piqray is used along with fulvestrant in people:1

  • With advanced or metastatic breast cancer that is hormone-receptor-positive, HER2 negative, and contains a particular genetic mutation called PIK3CA
  • Whose cancer progressed during or after hormone therapy

Breast cancer tumors have different features. 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 that allow the hormones to attach. Cancers with these receptors are called hormone-receptor-positive (HR+). Those without receptors are called hormone-receptor-negative (HR-).2,3

Breast cancer tumors can also be defined as HER2+ or HER2- cancers. HER2 refers to a 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 called HER2+ tumors. HER2- cancers produce few or no HER2 molecules.2,3

What are the ingredients in Piqray?

The active ingredient in Piqray is alpelisib.4,5

How does alpelisib work?

Alpelisib belongs to a class of drugs called kinase inhibitors. A kinase is a protein that activates important cellular growth processes. About 40 percent of breast cancers contain a genetic mistake in a specific protein called PIK3CA. Mutations in PIK3CA lead to fast cell growth and tumor formation. Alpelisib blocks the molecular signaling proteins that are produced by the PIK3 gene.3

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

What are the possible side effects?

The most common side effects of alpelisib include:4,5

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

Alpelisib may also cause serious side effects, including:4,5

  • Skin reactions with symptoms like rash, skin peeling and/or blistering on the lips, eyes, or mouth
  • High blood sugar levels with symptoms like excessive thirst, dry mouth, and frequent urination
  • Lung problems (pneumonitis) with symptoms like shortness of breath, cough, and chest pain
  • Severe diarrhea, which can lead to dehydration and kidney problems
  • Serious allergic reactions with symptoms like trouble breathing, rash, and fever

If you have any signs of a serious side effect, contact your doctor right away.

These are not all the possible side effects of alpelisib. Talk to your doctor about what to expect or if you experience any changes that concern you during treatment with alpelisib.

Other things to know

Your doctor will take blood tests to check your blood sugar levels before and during treatment with alpelisib.4,5

Before taking alpelisib, tell your doctor if you have a history of:4,5

  • Diabetes
  • Skin rash, peeling, redness, or blistering around the eyes, mouth, or lips

Alpelisib can harm an unborn baby. If you can become pregnant, you should use birth control during treatment and for some time after the last dose of alpelisib. You should also not breastfeed during treatment with alpelisib and for some time after the last dose. Talk to your doctor about your options for birth control and breastfeeding while taking alpelisib.4,5

Before beginning treatment for breast cancer, tell your doctor about all your health conditions and any other drugs, vitamins, or supplements you are taking. This includes over-the-counter drugs.

For more information, read the full prescribing information of alpelisib.

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