Alpelisib
Indications
Alpelisib is a targeted cancer medicine taken by mouth. It is used together with Fulvestrant to treat adults with advanced or metastatic breast cancer that is hormone receptor positive and HER2 negative, and whose tumour has a change (mutation) in the PIK3CA gene, usually after the cancer has grown during or after hormone therapy.
How It Works
Alpelisib blocks an enzyme called PI3K-alpha. In cancers with a PIK3CA mutation this enzyme is overactive and drives cancer cells to grow and survive. Blocking it slows the growth of these cancer cells and helps hormone therapy work better.
Dosage and Administration
Alpelisib is a specialist cancer medicine: take it exactly as prescribed by your oncologist, usually once a day immediately after food at about the same time each day. Swallow tablets whole. The doctor may lower the dose or pause treatment if side effects occur. A test confirming the PIK3CA mutation is needed before starting.
Interactions
- Strong inducers of the CYP3A4 enzyme, such as Rifampicin, Carbamazepine, Phenytoin and St John's Wort, can lower its levels; avoid them.
- BCRP inhibitors such as Eltrombopag or Lapatinib may raise its levels.
- It can lower the effect of some medicines broken down by CYP2C9 such as Warfarin.
- Tell your doctor about all medicines, including those for diabetes, as blood sugar control may change.
Contraindications
- Allergy to Alpelisib or any ingredient of the tablet.
- It is not suitable for people with type 1 diabetes or uncontrolled type 2 diabetes unless the specialist decides otherwise after careful assessment.
Side Effects
Very common side effects include high blood sugar, diarrhoea, nausea, loss of appetite, weight loss, rash, mouth sores, tiredness and hair loss. Blood tests may show low blood counts and changes in kidney or liver function.
Get urgent medical help if you have extreme thirst, passing large amounts of urine, confusion or fruity-smelling breath (very high blood sugar or ketoacidosis), a widespread rash with blisters or peeling skin, swelling of the face or throat, new or worsening cough or breathlessness, or severe diarrhoea causing dehydration.
Pregnancy and Lactation
Alpelisib can harm an unborn baby. Women who can become pregnant must use effective non-hormonal contraception during treatment and for at least one week after the last dose; male patients with female partners should use condoms over the same period. Do not breastfeed during treatment and for at least one week after the last dose.
Precautions and Warnings
- Blood sugar must be checked before starting and frequently during treatment, especially in the first weeks.
- Tell your doctor at once about rash, diarrhoea or breathing problems; early treatment helps.
- Inform your doctor if you have a history of severe skin reactions or pancreatitis.
- Regular blood tests and follow-up visits are needed.
Overdose
Overdose may cause very high blood sugar, nausea, tiredness and rash. Seek medical help immediately if you take more than prescribed.
Therapeutic Class
Antineoplastic, PI3K-alpha inhibitor (targeted therapy)
Storage
Store below 30°C in a dry place in the original pack, away from light and out of the reach of children.
Prepared by the Oshud Alo team from standard drug references. For information only; always follow your doctor's advice.
All brands of Alpelisib