Alunbrig

Brigatinib

Patients w/ anaplastic lymphoma kinase (ALK) +ve advanced NSCLC; ALK +ve advanced NSCLC previously treated w/ crizotinib.

Initially 90 mg once daily for 1st 7 days, then 180 mg once daily. Severe renal impairment (eGFR <30 mL/min/1.73 m²) Reduce dose by approx 50% (eg, from 180 mg to 90 mg or 90 mg to 60 mg). Severe hepatic impairment (Child-Pugh class C) Reduce dose by approx 40% (eg, from 180 mg to 120 mg, 120 mg to 90 mg or 90 mg to 60 mg).

May be taken with or without food: Swallow whole, do not crush/chew. Avoid grapefruit or grapefruit juice.

Discontinue use in case of life-threatening bradycardia if no contributing concomitant medication is identified or in case of recurrence. W/hold use if pneumonitis is suspected; in case of severe HTN & photosensitivity reactions (≥Grade 3); if symptomatic bradycardia occurs. Monitor for new or worsening resp symptoms (eg, dyspnea, cough) particularly in 1st wk of treatment. Regularly monitor heart rate & BP, creatine phosphokinase levels, lipase & amylase during treatment. Perform ophth evaluation for new or worsening severe visual symptoms. Regularly monitor liver function including AST, ALT & total bilirubin during treatment specially during 1st 3 mth. Assess fasting serum glucose prior to initiation & monitor periodically thereafter. Avoid prolonged sun exposure during treatment & for at least 5 days after discontinuation. Combination w/ other agents causing bradycardia. Do not drive or operate machines if patient experiences visual disturbance, dizziness & fatigue. Females of reproductive potential should use effective non-hormonal contraception during treatment & for at least 4 mth following final dose. Male partners should use effective contraception during treatment & for at least 3 mth after last dose. May cause reduced fertility in males. Not to be used during pregnancy. Discontinue lactation during treatment. Ped patients <18 yr. Elderly >85 yr.

Pneumonia, URTI; anemia, decreased lymphocyte, WBC & neutrophil count, increased aPTT; hyperglycemia, hyperinsulinemia, hypophosphatemia, hypomagnesemia, hypercalcemia, hyponatremia, hypokalemia, decreased appetite; headache, peripheral neuropathy, dizziness; visual disturbance; HTN; cough, dyspnea; increased lipase & amylase, diarrhea, nausea, vomiting, abdominal pain, constipation, stomatitis; increased AST, ALT & alkaline phosphatase; rash, pruritus; increased blood CPK, myalgia, arthralgia; increased blood creatinine; fatigue, edema, pyrexia. Decreased platelet count; insomnia; dysgeusia, memory impairment; bradycardia, prolonged ECG QT, tachycardia, palpitations; pneumonitis; dry mouth, dyspepsia, flatulence; increased blood LDH; dry skin, photosensitivity reaction; musculoskeletal chest pain & stiffness, pain in extremity; non-cardiac chest pain, chest discomfort, pain; increased blood cholesterol, decreased wt.

Plasma conc may be increased w/ strong CYP3A inhibitors eg, certain antivirals (eg, indinavir, nelfinavir, ritonavir, saquinavir), macrolides (eg, clarithromycin, telithromycin, troleandomycin), antifungals (eg, ketoconazole, voriconazole), nefazodone; moderate CYP3A inhibitors eg, diltiazem, verapamil; grapefruit or grapefruit juice. Plasma conc may be decreased w/ strong CYP3A inducers eg, rifampin, carbamazepine, phenytoin, rifabutin, phenobarb, St. John's wort; moderate CYP3A inducers eg, efavirenz, modafinil, bosentan, etravirine, nafcillin. Reduced plasma conc of medications predominantly metabolized by CYP3A. May induce other enzymes & transporters eg, CYP2C, P-gp. May increase plasma conc of substrates of P-gp (eg, digoxin, dabigatran, colchicine, pravastatin), BCRP (eg, MTX, rosuvastatin, sulfasalazine), OCT1, MATE1, MATE2K.

Targeted Cancer Therapy

L01ED04 - brigatinib ; Belongs to the class of anaplastic lymphoma kinase (ALK) inhibitors. Used in the treatment of cancer.

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