Ayvakit

Avapritinib

Monotherapy for the treatment of adults w/ unresectable or metastatic GI stromal tumours harbouring the platelet-derived growth factor receptor α D842V mutation.

300 mg once daily.

Should be taken on an empty stomach: Avoid grapefruit or grapefruit juice.

Hypersensitivity.

Associated w/ an increased incidence of haemorrhagic events eg, GI haemorrhage, hepatic, tumour & intracranial haemorrhages. Permanently discontinue if intracranial haemorrhage is observed during treatment. Cognitive effects eg, memory impairment, cognitive disorder, confusional state, encephalopathy; fluid retention; QT interval prolongation; diarrhoea, nausea, vomiting; anaemia, neutropenia, thrombocytopenia; elevations in bilirubin & liver transaminases. Caution in patients w/ known QT interval prolongation or at risk of QT interval prolongation. Perform CBC on a regular basis during treatment. Regularly monitor liver function (transaminases, bilirubin). Avoid or minimise exposure to direct sunlight due to risk of phototoxicity. Avoid co-administration w/ strong or moderate CYP3A inhibitors or inducers. May influence the ability to drive & use machines. Not recommended in patients w/ severe hepatic impairment or severe renal impairment or end-stage renal disease. May cause foetal harm. Women of childbearing potential should use effective contraception during treatment & for 1 mth after the last dose. Not recommended during pregnancy & in women of childbearing potential not using contraception. Discontinue breastfeeding during treatment & for 2 wk following the final dose.

Anaemia, decreased WBC, decreased neutrophil count; decreased appetite; memory impairment, cognitive disorder, dizziness, taste effect; increased lacrimation; abdominal pain, vomiting, diarrhoea, nausea, dryness, GERD; hyperbilirubinaemia; hair colour changes, rash; oedema, fatigue; increased transaminases.

Increased plasma conc w/ strong or moderate CYP3A inhibitors (eg, antifungals including ketoconazole, itraconazole, posaconazole, voriconazole; certain macrolides eg, erythromycin, clarithromycin & telithromycin; active substances to treat HIV/AIDS eg, cobicistat, indinavir, lopinavir, nelfinavir, ritonavir & saquinavir; as well as conivaptan & boceprevir) including grapefruit or grapefruit juice. Decreased plasma conc w/ strong or moderate CYP3A4 inducers [eg, dexamethasone, phenytoin, carbamazepine, rifampicin, phenobarb, fosphenytoin, primidone, bosentan, efavirenz, etravirine, modafinil, dabrafenib, nafcillin or Hypericum perforatum (St. John's wort)]. May have potential to increase or decrease plasma conc of CYP3A substrates. Has potential to alter conc of co-administered substrates of P-gp, BCRP, MATE1, MATE2-K, & BSEP.

Targeted Cancer Therapy

L01EX18 - avapritinib ; Belongs to the class of other protein kinase inhibitors. Used in the treatment of cancer.

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