What is Piqray® (alpelisib)?

Piqray® (alpelisib) is a medication 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 called PIK3CA. 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

Tumor characteristics

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

HER2+ or HER2- cancers

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.2Advanced breast cancer has often 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 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

More severe side effects

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

Piqray and fertility implications

Alpelisib may cause harm fetuses, so it is important not to become pregnant while you or your male partner are taking it. While taking alpelisib, males with female partners who can become pregnant, and females who can become pregnant, should both use contraceptives during treatment and for one week after completing treatment (patients should discuss appropriate birth control methods with their doctor). Females should not breastfeed during alpelisib treatment and for 1 week after the final dose. 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, patients should talk to their doctor about all their health conditions, especially if they:

  • 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

Before beginning treatment with alpelisib, patients should talk to their doctor about all their medications (prescription and over-the-counter), vitamins, and herbal supplements they are taking. Some medications or supplements may interfere with each other and may cause serious side effects. 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.

Receiving alpelisib

Alpelisib is a pill that is swallowed whole by mouth. Your healthcare provider will determine the appropriate alpelisib dosing regimen and administration schedule for you. It is important to follow this schedule exactly as instructed, and not to stop taking alpelisib or any accompanying medications on your own, unless you are instructed to do so by your healthcare provider.5 For more information about alpelisib, read the complete prescribing information.

More on this topic

Patients should take their medication as prescribed by their doctor. Patients should talk to their doctor if they have any questions, or if they have questions regarding their alpelisib regimen.

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Written by: Editorial Team | Last reviewed: October 2020.