Piqray

In combination w/ fulvestrant for the treatment of postmenopausal women & men w/ hormone receptor (HR) +ve, human epidermal growth factor receptor 2 (HER2) -ve, advanced or metastatic breast cancer w/ a PIK3CA mutation following progression on or after an endocrine-based regimen.

300 mg (2 x 150 mg) once daily. Max daily dose: 300 mg.

Should be taken with food: Take immediately after meals. Swallow whole, do not chew/crush/split.

Hypersensitivity.

Permanently discontinue & do not reintroduce in patients w/ serious hypersensitivity reactions. Do not initiate treatment in patients w/ history of severe cutaneous reactions; permanently discontinue if severe cutaneous reaction is confirmed. Risk of severe hyperglycaemia that may be associated w/ hyperglycaemic hyperosmolar nonketotic syndrome or ketoacidosis; severe diarrhoea, including dehydration & acute kidney injury. May require dose interruption, reduction or discontinuation based on severity of hyperglycaemia/diarrhoea. Reports of pneumonitis including serious cases of pneumonitis/acute ILD. Permanently discontinue in all patients w/ confirmed pneumonitis. Minor influence on the ability to drive & use machines. Caution in patients w/ severe renal impairment. May impair fertility in males & females of reproductive potential. Should not be used during pregnancy unless benefits to the mother outweigh risk to the fetus. If used during pregnancy, advise patient of the potential risk to the fetus. Use effective contraception during treatment & for at least 4 days after stopping treatment. Women should not breast-feed during treatment & for at least 4 days after the last dose. Safety & efficacy have not been established in ped patients.

Hyperglycaemia, diarrhoea, rash, nausea, fatigue, asthenia, decreased appetite, stomatitis, vomiting, decreased wt.

Increased systemic exposure w/ BCRP inhibitors (eg, eltrombopag, lapatinib, pantoprazole). Altered exposure of CYP3A4 substrates that also possess an additional time-dependent inhibition & induction potential on CYP3A4 that affects their own metabolism (eg, rifampicin, ribociclib, encorafenib). Caution w/ concomitant CYP2C9 substrates w/ narrow therapeutic index eg, warfarin. Reduced clinical activity of sensitive CYP2B6 substrates (eg, bupropion) or CYP2B6 substrates w/ narrow therapeutic window. Increased AUC w/ food. Clinically relevant inhibition of oral absorption of P-gp substrates & hepatic uptake of OCT1, OATP1B1 & OAT1B3 substrates may occur. Potential to increase plasma conc of OAT3 substrates.

Targeted Cancer Therapy

L01EM03 - alpelisib ; Belongs to the class of phosphatidylinositol-3-kinase (Pi3K) inhibitors. Used in the treatment of cancer.

P₁S₁S₃