Lorviqua

Monotherapy for adults w/ anaplastic lymphoma kinase (ALK) +ve advanced NSCLC previously untreated w/ ALK inhibitor or whose disease has progressed after alectinib or ceritinib as 1st ALK tyrosine kinase inhibitors (TKI) therapy; or crizotinib & at least 1 other ALK TKI.

100 mg once daily. 1st dose reduction: 75 mg once daily. 2nd dose reduction: 50 mg once daily. Concomitant use w/ strong CYP3A inhibitor, severe renal impairment (absolute eGFR <30 mL/min) Initially 75 mg once daily.

May be taken with or without food: Take at the same time each day. Swallow whole, do not chew/crush/split.

Hypersensitivity. Concomitant use of strong CYP3A inducers.

Permanently discontinue &/or withhold use if severe pneumonitis, HTN & hyperglycemia occur. Hyperlipidemia; CNS effects; AV block; decreased left ventricular ejection fraction (LVEF); increased lipase & amylase. Monitor serum cholesterol & triglycerides prior to & 2, 4 & 8 wk after initiating & periodically thereafter; ECG prior to & mthly thereafter; cardiac monitoring including LVEF assessment at baseline & during treatment; lipase & amylase elevations prior to & regularly thereafter; fasting serum glucose prior to & periodically thereafter. Control BP prior to initiation then monitor after 2 wk & mthly thereafter. Not to be used concomitantly w/ any strong CYP3A inducers. May affect ability to drive & use machines. Not recommended in moderate to severe hepatic impairment. Severe renal impairment. May compromise male fertility. Women of childbearing potential should use effective contraception during & for at least 21 days after last dose. Male partners should use effective contraception during & for at least 97 days after last dose. Not recommended during pregnancy or for women of childbearing potential not using contraception. Not be used during lactation. Ped. Elderly ≥65 yr.

Anaemia; hypercholesterolaemia, hypertriglyceridaemia; mood & cognitive effects, peripheral neuropathy, headache; vision disorder; HTN; diarrhoea, nausea, constipation; rash; arthralgia, myalgia; oedema, fatigue; increased wt, lipase & amylase. Hyperglycaemia; psychotic & speech effects, mental status changes; pneumonitis; proteinuria.

Increased plasma conc w/ strong CYP3A inhibitors eg, boceprevir, cobicistat, conivaptan, itraconazole, ketoconazole, posaconazole, telaprevir, troleandomycin, voriconazole, ritonavir, paritaprevir w/ ritonavir & ombitasvir &/or dasabuvir, ritonavir w/ danoprevir, elvitegravir, indinavir, lopinavir, saquinavir, tipranavir; grapefruit. Decreased plasma conc w/ strong CYP3A inducers eg, rifampin, carbamazepine, enzalutamide, mitotane, phenytoin, St. John's wort. Reduced plasma conc of CYP3A substrates w/ narrow therapeutic indices eg, hormonal contraceptives, alfentanil, cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, tacrolimus; P-gp substrates w/ narrow therapeutic index eg, digoxin.

Targeted Cancer Therapy

L01ED05 - lorlatinib ; Belongs to the class of anaplastic lymphoma kinase (ALK) inhibitors. Used in the treatment of cancer.

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