Piqray (alpelisib): What to Expect, Side Effects, and More
If you’ve been diagnosed with advanced-stage or metastatic, hormone receptor-positive, HER2-negative breast cancer that has grown after treatment with hormonal therapy, your doctor may recommend Piqray.
Piqray only works on breast cancers with a PIK3CA mutation. Your doctor will need to confirm the breast cancer has the PIK3CA mutation before prescribing Piqray. This can be accomplished through a blood test or an examination of biopsy tissue.
See Piqray prescribing information.
How Piqray works
Breast cancers that have a PIK3CA gene mutation are able to grow rapidly. Piqray is a targeted therapy medicine called a PI3K inhibitor that blocks the signal these cells use to survive and grow. .
Different mutations in the PIK3CA gene make different forms of the protein PIK3 , called isoforms by researchers. There are several isoforms of PIK3; one of them is the alpha isoform. Piqray specifically targets the alpha isoform.
Piqray is given with Faslodex (chemical name: fulvestrant).
What to expect during Piqray treatment
Piqray is available as a pill and should be taken with food, at the same time each day. The starting dose is 300 mg once daily. Depending on how well you tolerate Piqray, your dosage may be reduced to 250 mg or 200 mg daily.
Each Faslodex treatment is made up of two injections — one into each butt cheek. You’ll receive an injection on days one, 15, and 29 of your Piqray prescription. After day 29, you’ll receive Faslodex once a month.
There are certain medicines, supplements, and foods you should avoid if you are taking Piqray:
CYP3A4 inducers decrease 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.
BCRP inhibitors, such as Verenzio (chemical name: abemaciclib), can increase the effects of Piqray.
St. John’s wort, an herb that is sometimes used to control depression and anxiety, can decrease the effects of Piqray.
Grapefruit and grapefruit juice 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 must closely monitor levels of warfarin in your blood.
Piqray side effects
Like most breast cancer medicines, Piqray can cause side effects, some of them severe.
The most common side effects of Piqray are:
high blood sugar levels
high creatinine levels, which can mean kidney problems
You will need close monitoring of your blood sugar levels while taking Piqray. Some doctors may prescribe medications that reduce blood sugar levels in order to prevent increases in blood sugar, or to reduce blood sugar levels if they become elevated while taking Piqray.
Since Piqray is taken with Faslodex, you also may also experience side effects associated with that medicine.
Piqray can also cause other 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. Before starting Piqray, your doctor should test your fasting blood sugar level. 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, or if you have a fever or chills.
Diarrhea: Although moderate diarrhea is a common side effect of Piqray, it may cause severe diarrhea, which can lead to dehydration and may cause kidney problems. If you have diarrhea, tell your doctor immediately. They can recommend an antidiarrheal medicine while you’re taking Piqray.
Colitis: In some people, Piqray may cause colitis, which is swelling of the large intestine. Symptoms include bloody stools, bloating, and diarrhea that isn’t helped by medicine. Colitis can be serious and cause life-threatening complications, such as a tear in the intestine. Contact your doctor immediately if you have any symptoms.
If you’re pregnant or planning to get pregnant, you should not be given Piqray. Piqray can cause embryo death and birth defects. You must use effective birth control while being treated and for one week after the last dose. You also shouldn’t take Piqray while breastfeeding.
Real patient reviews
Members of our community discuss their experiences with Piqray in the community forum. Here are some of their comments. Remember, it's essential to talk to your doctor about any side effects you're having and ask about ways to manage them.
“Piqray … seems to affect everyone differently. I have been on it since June and tolerate the 300 mg dose well with the blood sugars being my biggest challenge. They do have lower dose options so that might work better for you too.” —emac877
“I was on Piqray 300 mg for 6 months. Yes, the side effects are not good, but my PET scan after the first four and a half months showed it was actually working. It did affect my mouth and gag reflex, and I could not eat. I also lost 30 pounds in 6 weeks. The yeast infection in my mouth has been bad. They finally prescribed magic mouthwash, and it is helping. I also chose to continue taking Piqray at 200 mg because I have a pic3 mutation, and it had shown good results in a short time.” —al36526
“It’s been almost 2 weeks. So far, my only side effects are nausea and a mild headache. It also seems like my taste buds have gone off. Some things taste metallic, like during chemo. And my appetite has kind of decreased.” —katyblu
Read more in our Piqray discussion forum.
Paying for Piqray
The cost of Piqray may vary. The price you’ll pay depends on the drug manufacturer, your health insurance provider and plan, where you live, and the pharmacy you use.
Note: Your insurance company may require you to get prior authorization before covering Piqray.
Learn more about financial assistance and medicine cost-lowering tips.
— Last updated on May 31, 2025 at 6:45 PM
