Piqray (chemical name: alpelisib) is a PI3K inhibitor. Piqray is used to treat advanced-stage hormone-receptor-positive, HER2-negative breast cancer with a PIK3CA mutation that has grown after treatment with hormonal therapy in postmenopausal women and men.

Piqray (chemical name: alpelisib) is approved to be used in combination with the hormonal therapy Faslodex (chemical name: fulvestrant) to treat advanced-stage or metastatic hormone-receptor-positive, HER2-negative breast cancer with a PIK3CA mutation that has grown after treatment with hormonal therapy in postmenopausal women and men.

Piqray is a pill taken by mouth.


How Piqray works

Piqray is a targeted therapy medicine called a PI3K inhibitor that blocks the PI3K pathway. The PI3K pathway helps all cells — both healthy and cancer cells — get the energy they need. When this pathway is overactivated because of a mutation in the PIK3CA gene, it can allow cancer cells to survive and grow. PI3K inhibitors block this pathway, with the goal of killing cancer cells.

Different mutations in the PIK3CA gene make different forms of the PI3 protein, called isoforms by researchers. There are several isoforms of PI3; one of them is the alpha isoform. Piqray specifically targets the alpha isoform.


Is Piqray right for you?

Piqray is prescribed with the hormonal therapy Faslodex to treat postmenopausal women and men diagnosed with advanced-stage or metastatic hormone-receptor-positive, HER2-negative breast cancer with a PIK3CA mutation that has grown after treatment with hormonal therapy.

Piqray only works on breast cancers with a PIK3CA mutation. The cancer must be tested to make sure the mutation is present.

Advanced-stage breast cancer is cancer that has come back (recurred) or spread beyond the breast to the chest wall below the breast. Metastatic breast cancer is advanced-stage cancer that has spread to parts of the body away from the breast, such as the bones or liver.

Faslodex is an estrogen receptor downregulator (ERD), a type of hormonal therapy. Faslodex blocks the effect of estrogen on breast tissue by sitting in the estrogen receptor in breast cells. Faslodex is a liquid given as an injection into a muscle.

To find out if a cancer is estrogen-receptor-positive, most testing labs use a special staining process that makes the hormone receptors show up in a tissue sample. The test is called an immunohistochemical staining assay, or ImmunoHistoChemistry (IHC). Not all labs use the same method for analyzing the results of the test, and they do not have to report the results in exactly the same way. So you may see any of the following on your pathology report:

  • A percentage that tells you how many cells out of 100 stain positive for hormone receptors. You will see a number between 0% (none have receptors) and 100% (all have receptors).

  • An Allred score between 0 and 8. This scoring system is named for the doctor who developed it. The system looks at what percentage of cells test positive for hormone receptors, along with how well the receptors show up after staining (this is called “intensity”). This information is then combined to score the sample on a scale from 0 to 8. The higher the score, the more receptors were found and the easier they were to see in the sample.

  • The word “positive” or “negative.”

Learn more about hormone receptor test results.


What to expect when taking Piqray

The recommended dose of Piqray is 300 mg taken as two 150 mg tablets once per day with food.

When given with Piqray, the recommended dose of Faslodex is 500 mg given as an injection on days 1, 15, and 29 of Piqray. After day 29, Faslodex is given once per month.

You stay on the Piqray-Faslodex combination as long as you are getting benefits from the medicine and aren’t having troubling side effects.

There are certain medicines, supplements, and foods you should not take if you are taking Piqray:

  • You should not take a type of medicine called a strong CYP3A4 inducer because it decreases the effects of Piqray. This class of medicines includes Rifamate (chemical name: rifampin), an antibiotic used to treat tuberculosis, and Carbatrol (chemical name: carbamazepine), which is used to control certain types of seizures in people with epilepsy.

  • You should not take a type of medicine called a BCRP inhibitor because it increases the effects of Piqray. This class of medicines includes Zegerid and Prilosec (chemical name: omeprazole) and the antibiotic novobiocin.

  • You should not take St. John’s wort, an herb that is sometimes used to control depression and anxiety, because it can decrease the effects of Piqray.

  • You should not eat grapefruit or drink grapefruit juice because they can increase the effects of Piqray.

  • Piqray may reduce the effects of medicines called CYP2C9 substrates. The blood thinner warfarin (brand names: Coumadin and Jantoven) is a CYP2C9 substrate. If you are on warfarin and are prescribed Piqray, your doctor will closely monitor levels of warfarin in your blood.

It’s important to know that Piqray can harm a developing fetus. Women who are taking Piqray should use effective birth control during treatment and for 1 week after the last dose. Men with female partners should use condoms and effective birth control while taking Piqray and for 1 week after the last dose.

Women who are breastfeeding or plan to breastfeed should not take Piqray. Together, you and your doctor will decide if you should take Piqray or breastfeed.


Paying for Piqray

If your doctor prescribes Piqray and you have problems getting it covered by insurance, or you don’t have insurance, the Novartis Patient Assistance NOW Oncology program may be able to help. You also can call the Piqray patient support line at 1-800-282-7630.


Piqray side effects

The most common side effects of Piqray are:

Piqray also may cause serious side effects, including:

  • Severe skin reactions: In some people, Piqray may cause Stevens-Johnson syndrome or erythema multiforme, skin disorders that may begin with flu-like symptoms followed by a painful rash that blisters. If you have a history of either of these two conditions or other skin disorders, discuss them with your doctor before you start treatment with Piqray.

  • High blood sugar: The safety of Piqray has not been established in people diagnosed with Type 1 or uncontrolled Type 2 diabetes. If you have diabetes, your doctor will measure your fasting blood sugar levels and will monitor these levels while you’re being treated with Piqray. If you have symptoms of untreated high blood sugar, including frequent urination, blurred vision, or an increase in thirst, tell your doctor immediately.

  • Pneumonia: Piqray may make some people more likely to develop pneumonia or other upper respiratory infections. Tell your doctor right away if you have chest pain when you breathe or cough, a fever, or chills.

  • Diarrhea: While moderate diarrhea is common side effect of Piqray, the medicine also can cause severe diarrhea, which can lead to dehydration and may cause kidney problems. Your doctor will recommend an antidiarrheal medicine while you’re being treated with Piqray. If you have diarrhea, tell your doctor immediately.

Because Piqray is given with Faslodex, you also may have side effects from that medicine. Common side effects of Faslodex are hot flashes and nausea.


Piqray (alpelisib) prescribing information. Novartis Pharmaceuticals Corporation, East Hanover, New Jersey. 2019. Available at: (PDF)

— Last updated on April 1, 2022, 1:30 PM

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