Alpelisib belongs the group of cancer-fighting medications known as antineoplastics and more specifically to a class of medications called protein kinase inhibitors. It is an antitumour medication that works directly on cancer cells to slow down their growth and to slow down the growth of the tumour.

Alpelisib is used by women (who are past menopause) and men, in combination with anti-estrogen medications, to treat breast cancer that has specific characteristics. It is used to treat breast cancer that is hormone receptor (HR) positive, human epidermal growth factor receptor 2 (HER-2) negative, PIK3CA-mutated, and that has advanced or has metastasized (spread to other parts of the body) after treatment with other anti-estrogen medications.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

The usual adult dose of alpelisib is 300 mg (2 x 150 mg tablets) taken by mouth, once daily. It should be taken immediately after eating and at approximately the same time each day. If you experience a lot of side effects, your doctor may switch you to a lower dose.

Swallow the tablets whole. Do not crush, break, or chew the tablets. Safely discard any tablets that are broken or cracked. Do not take tablets that are not intact.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important to take this medication exactly as prescribed by your doctor.

If you miss a dose, take it as soon as possible after some food if it is within 9 hours of the missed dose. Then continue with your regular schedule. If it is more than 9 hours since the missed dose, skip the missed dose and continue with your regular dosing schedule. If you vomit after taking a dose, do not take another dose, and take the next dose at the regular time. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice.

Store this medication in its original package at room temperature, protect it from light and moisture, and keep it out of the reach of children.

50 mg
Each light pink, unscored, round and curved, bevelled-edged tablet, imprinted with "L7" on one side and "NVR" on the other side, contains 50 mg of alpelisib. Nonmedicinal ingredients:  hypromellose, magnesium stearate, mannitol, microcrystalline cellulose, sodium starch glycolate; tablet coating: hypromellose, iron oxide black, iron oxide red, macrogol / polyethylene glycol (PEG), talc, and titanium dioxide.

150 mg
Each pale red, unscored, ovaloid and curved, bevelled-edged tablet, imprinted with "UL7" on one side and "NVR" on the other side, contains 150 mg of alpelisib. Nonmedicinal ingredients:  hypromellose, magnesium stearate, mannitol, microcrystalline cellulose, sodium starch glycolate; tablet coating: hypromellose, iron oxide black, iron oxide red, macrogol / polyethylene glycol (PEG), talc, and titanium dioxide.

200 mg
Each light red, unscored, ovaloid and curved, bevelled-edged tablet, imprinted with "YL7" on one side and "NVR" on the other side, contains 200 mg of alpelisib. Nonmedicinal ingredients:  hypromellose, magnesium stearate, mannitol, microcrystalline cellulose, sodium starch glycolate; tablet coating: hypromellose, iron oxide black, iron oxide red, macrogol / polyethylene glycol (PEG), talc, and titanium dioxide.

Do not take this medication if you are allergic to alpelisib or any ingredients of the medication.

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

• blurred vision
• changed sense of taste
• chapped lips
• decreased appetite
• diarrhea
• dry eyes
• dry, cracked skin
• fatigue
• feeling bloated
• hair loss
• headache
• heartburn
• mouth sores
• muscle pain or cramps
• nausea
• red, sore, or swollen mouth, lips, and gums
• stomach pain
• toothache
• trouble sleeping
• vomiting

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

• burning foot pain
• high blood pressure (e.g., headache, fatigue, dizziness, ringing of the ears, fast or pounding heartbeat)
• problems with the jaw bone (e.g., jaw pain, loosened tooth, jaw numbness)
• reddening or swelling and peeling on the palms and soles
• signs of anemia (low red blood cells; e.g., dizziness, pale skin, unusual tiredness or weakness, shortness of breath)
• signs of bowel inflammation (e.g., fever that appears after starting the medication, watery and severe diarrhea [may also be bloody])
• signs of clotting problems (e.g., unusual nosebleeds, bruising, blood in urine, coughing blood, bleeding gums, cuts that don’t stop bleeding)
• signs of dehydration (e.g., decreased urine, dry skin, dry and sticky mouth, sleepiness, dizziness, headache, thirst, confusion)
• signs of infection (fever, severe chills, sore throat, mouth ulcers)
• signs of low potassium levels in the blood (e.g., weakness, fatigue, muscle cramps, irregular heartbeat)
• signs of lung inflammation (e.g., difficult, painful, rapid breathing; blue colour to the lips, tongue, or skin)
• symptoms of high blood sugar (e.g., frequent urination, increased thirst, excessive eating, unexplained weight loss, poor wound healing, infections, fruity breath odour)
• symptoms of a urinary tract infection (e.g. pain when urinating, urinating more often than usual, low back or flank pain)

Stop taking the medication and seek immediate medical attention if any of the following occur:

• signs of ketoacidosis (e.g., confusion, extreme thirst, loss of appetite, stomach pain, trouble breathing, nausea, vomiting, or unusual tiredness)
• signs of kidney problems (e.g., change in urinating – more or less than usual, swollen ankles and feet or around the eyes, tiredness, confusion, nausea, seizures, chest pain)
• signs of pancreatitis (e.g., abdominal pain on the upper left side, back pain, nausea, fever, chills, rapid heartbeat, swollen abdomen)
• signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
• signs of hyperglycemic hyperosmolar non-ketotic syndrome (severe complications of high blood sugar; e.g., confusion, dry mouth, dry or flushed skin, nausea, vomiting, tiredness, increased need to urinate, thirst)
• signs of a severe skin reaction such as blistering, peeling, a rash covering a large area of the body, a rash that spreads quickly, or a rash combined with fever or discomfort

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.

Anemia: Alpelisib may cause low levels of red blood cells. If you experience symptoms of reduced red blood cell count (anemia) such as shortness of breath, feeling unusually tired, or pale skin, contact your doctor as soon as possible.

Your doctor will do blood tests regularly to monitor the number of specific types of blood cells, including red blood cells, in your blood.

Birth control: People who may become pregnant should use effective birth control while taking this medication and for at least 1 week after stopping alpelisib. People taking this medication who have partners who may become pregnant should also use effective birth control while taking this medication and for at least 1 week after stopping alpelisib.

Bleeding: Alpelisib may cause a reduced number of platelets in the blood, which can make it difficult to stop cuts from bleeding. If you notice any signs of bleeding, such as frequent nosebleeds, unexplained bruising, or black and tarry stools, notify your doctor as soon as possible. Your doctor will order routine blood tests to make sure potential problems are caught early.

Bowel inflammation: Irritation in the digestive system has been reported by people using alpelisib. This can contribute to dehydration if it is not controlled. If you experience abdominal pain and bloating, diarrhea with blood or mucous, or the feeling of constantly having to pass a bowel movement, contact your doctor.

Dehydration: Severe dehydration can occur with the use of alpelisib. This may be due to severe or persistent diarrhea, vomiting, or decreased fluid intake. Dehydration can lead to kidney failure, if it is severe enough. During treatment with this medication, you may be encouraged to drink extra water. Your doctor will do blood tests to check the function of your kidneys.

Diabetes: Alpelisib may cause an increase in blood sugar levels (may cause a loss of blood glucose control) and glucose tolerance may change. Cases of severely increased blood sugar levels causing diabetic ketoacidosis or hyperglycemic hyperosmolar non-ketotic syndrome have occurred.

If you develop symptoms of high blood sugar levels such as difficulty breathing, feeling very thirsty, vomiting, abdominal pain, nausea, loss of appetite, confusion, and unusual tiredness, seek urgent medical attention.

People with diabetes may find it necessary to monitor their blood sugar more frequently while using this medication.

Deterioration of the jaw bone: People with cancer who are being treated with alpelisib and fulvestrant have reported developing osteonecrosis of the jaw (deterioration of the jaw bone). Report any pain, swelling, or infection of the jaw to your doctor, and avoid invasive dental procedures such as tooth extractions. Your doctor may recommend that you see a dentist before starting this medication. It is important to practice good oral hygiene while taking this medication.

Hypersensitivity syndrome: A severe allergic reaction called hypersensitivity syndrome has occurred for some people with the use of alpelisib. This reaction involves a number of organs in the body and may be fatal if not treated quickly. Stop taking the medication and get immediate medical attention if you have symptoms of a severe allergic reaction, including fever, swollen glands, yellowing of the skin or eyes, or flu-like symptoms with skin rash or blistering.

Infection: As well as killing cancer cells, alpelisib can reduce the number of cells that fight infection in the body (white blood cells). If possible, avoid contact with people with contagious infections.

Tell your doctor immediately if you notice signs of an infection, such as fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, headache, stiff neck, weight loss, or listlessness. Your doctor will do blood tests regularly to monitor the number of specific types of blood cells in your blood.

Lung inflammation: Lung inflammation (interstitial lung disease), causing difficulty breathing has occurred rarely in some people taking this medication. This complication can be serious and sometimes fatal. If you experience new or worsening shortness of breath or cough (with or without fever) at any time while you are taking alpelisib, contact your doctor immediately.

Race: People of Asian heritage who take alpelisib are more likely to experience severe reactions to this medication, such allergic reactions, severe skin reactions, and pancreatitis.

Pregnancy: This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: It is not known if alpelisib passes into breast milk. If you are breast-feeding and taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

Children: The safety and effectiveness of using this medication have not been established for children.

Seniors: People over the age of 65 are more likely to experience side effects from this medication.

For a full list of interactions, use the Drug Interaction Checker available on the Drugs.com website.

If you are taking other medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

• stop taking one of the medications,
• change one of the medications to another,
• change how you are taking one or both of the medications, or
• leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.