alpelisib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
alpelisib: clinical details
Prescribing considerations
- Confirm a PIK3CA mutation using a validated tumour or plasma test; test tumour tissue if plasma is negative and tissue is available.
- Treatment should be initiated by a clinician experienced in anticancer therapy.
- Optimise glycaemic control before initiation. Seek diabetes expertise for existing diabetes and consider specialist input for pre-diabetes, obesity, advanced age or substantially raised fasting glucose.
- Efficacy after previous fulvestrant is not established because clinical data are limited.
- Safety and efficacy are not established in children or in symptomatic visceral disease.
- Use caution in severe renal impairment because clinical experience is absent.
Contraindications and cautions
- Hypersensitivity to alpelisib or an excipient.
- Do not initiate in patients with a history of severe cutaneous reactions.
- Do not initiate where osteonecrosis of the jaw remains active following bisphosphonate or denosumab treatment.
Monitoring
- Check fasting plasma glucose and HbA1c before treatment and optimise glycaemic control.
- Monitor fasting glucose closely after initiation, particularly during the first weeks, and increase monitoring for diabetes, pre-diabetes, obesity or older age.
- Repeat HbA1c during treatment and monitor more frequently if hyperglycaemia develops.
- Monitor for rash, severe cutaneous reactions, diarrhoea or colitis, pneumonitis, hypersensitivity and oral or dental symptoms.
- Follow blood counts, renal and hepatic markers, electrolytes and other relevant laboratory abnormalities.
Clinical pharmacology
Alpelisib is an alpha-selective class I PI3K inhibitor. It is absorbed more reliably with food, undergoes mainly hydrolytic metabolism with a smaller CYP3A4 contribution, and has an approximate steady-state half-life of 8–9 hours.
Formulation and product differences
- Film-coated tablets are available in 50 mg, 150 mg and 200 mg strengths.
- The strengths differ in colour, shape, size and tablet imprint.
- All strengths must be swallowed intact and are essentially sodium-free.
alpelisib preparations and strengths
Tablet
Route: Oral
Strengths: 50 mg, 150 mg, 200 mg
alpelisib interactions
The oncology team should review prescription, non-prescription and herbal products before treatment.
Strong CYP3A4 inducers, including rifampicin, carbamazepine, phenytoin, apalutamide, enzalutamide, mitotane and St John’s wort
These can substantially reduce alpelisib exposure and should generally be avoided in favour of an alternative.
BCRP inhibitors, including eltrombopag, lapatinib and pantoprazole
These may increase alpelisib exposure, so monitor for toxicity.
Proton-pump inhibitors, H2-receptor antagonists and antacids
Acid-reducing treatments may be co-administered provided alpelisib is taken immediately after food.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.