• Metastatic non-small cell lung cancer (NSCLC) that is positive for anaplastic lymphoma kinase (ALK).

Contraindicated in:

• Concurrent use of moderate or strong inhibitors/inducers of the CYP3A enzyme system
• OB: Pregnancy (may cause fetal harm)
• Lactation: Lactation.

Use Cautiously in:

• Diabetes
• Severe renal or hepatic impairment
• Rep: Women of reproductive potential and men with female sexual partners of reproductive potential
• Pedi: Safety and effectiveness not established in children.

CV: hypertension, bradycardia.

Derm: rash, photosensitivity.

EENT: ↓ visual acuity, blurred vision, diplopia, cataracts, macular edema, photophobia.

Endo: hyperglycemia.

F and E: hypophosphatemia.

GI: ↓ appetite, ↑ amylase, ↑ lipase, ↑ liver enzymes, abdominal pain, constipation, diarrhea, nausea, vomiting.

Hemat: ↑ activated partial thromboplastin time, anemia, lymphopenia.

MS: ↑ creatine kinase, arthralgia, back pain, muscle spasms, myalgia.

Neuro: headache, insomnia, peripheral neuropathy.

Resp: cough, dyspnea, hypoxia, INTERSTITIAL LUNG DISEASE/PNEUMONITIS, pneumonia.

Misc: fatigue, fever.

Drug-Drug:

• Strong or moderate CYP3A inhibitors, including, clarithromycin, cobicistat, conivaptan, itraconazole, ketoconazole, lopinavir, nefazodone, nelfinavir, posaconazole, ritonavir, and voriconazole may ↑ levels; concurrent use should be avoided; if concurrent therapy must be used, ↓ brigatinib dose.
• Strong CYP3A inducers, including carbamazepine, phenytoin, and rifampin may ↓ levels and effectiveness; concurrent use should be avoided; if concurrent therapy with moderate CYP3A inducer must be used, ↓ brigatinib dose.
• Beta-blockers, verapamil, diltiazem, digoxin, and clonidine may ↑ risk of bradycardia; avoid concurrent use, if possible.

Drug-Natural Products:

• Concurrent use of St. John's wort may ↓ levels and effectiveness and should be avoided.

Drug-Food:

• Grapefruit or grapefruit juice may ↑ levels and should be avoided.

• Film-coated tablets: 30 mg; 90 mg; 180 mg;

• PO (Adults): 90 mg once daily for 7 days, then 180 mg once daily. Continue until disease progression or unacceptable toxicity. Concurrent use of strong CYP3A inhibitor: If previously taking 180 mg once daily, ↓ dose to 90 mg once daily; if previously taking 90 mg once daily, ↓ dose to 60 mg once daily; Concurrent use of moderate CYP3A inhibitor: If previously taking 180 mg once daily, ↓ dose to 120 mg once daily; if previously taking 120 mg once daily, ↓ dose to 90 mg once daily; if previously taking 90 mg once daily, ↓ dose to 60 mg once daily; Concurrent use of moderate CYP3A inducer: ↑ daily dose in 30–mg increments after 7 days of treatment with the dose used prior to initiation of moderate CYP3A inducer; dose may be ↑ up to a maximum of twice the dose that was tolerated prior to initiating the moderate CYP3A inducer.

Alunbrig

• Inhibits receptor tyrosine kinases including anaplastic lymphoma kinase (ALK), insulin-like growth factor—1 receptor (IGF-1R), ROS1, and FMS-like tyrosine kinase-3 (FLT-3).

• Improved progression free survival in NSCLC.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Absorption: Well absorbed following oral administration. Bioavailability reduced by high fat meals.

Distribution: Extensively distributed to tissues.

Metabolism/Excretion: Mostly metabolized by the liver (CYP2C8 and CYP3A4 isoenzymes); also induces CYP3A. 27% excreted in feces unchanged, 22% eliminated unchanged in urine.

Half-life: 25 hr.

(blood levels)

• Instruct patient to take brigatinib as directed. If patient vomits or misses a dose, omit dose and take next dose as scheduled. Do not double doses. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
• Advise patient to avoid eating grapefruit or drinking grapefruit juice during therapy.
• Advise patient to notify health care professional if signs and symptoms of lung problems (cough, chest pain, fever), hypertension (headaches, dizziness, blurred vision, chest pain, shortness of breath), bradycardia (dizziness, lightheadedness, feeling faint), visual changes (double vision, seeing flashes of light, blurry vision, light hurting eyes, new or increased floaters), symptoms of pancreatitis (upper abdominal pain, weight loss, nausea), new or worsening symptoms of myalgia (unexplained muscle pain, tenderness, or weakness), or hyperglycemia (feeling very thirsty, needing to urinate more than usual, feeling very hungry, nausea, feeling weak or tired, feeling confused) occur, may require dose reduction or discontinuation.
• Advise patients to limit sun exposure while taking brigatinib, and for at least 5 days after stopping therapy. Wear a hat and protective clothing, and use a broad-spectrum Ultraviolet A (UVA)/ Ultraviolet B (UVB) sunscreen and lip balm (SPF ≥30) to help protect against sunburn. Sunburn may require interrupting or discontinuing therapy based on severity.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. John's wort.
• Rep: May cause fetal harm. Advise females of reproductive potential to use effective non-hormonal contraception during and for at least 4 mo after final dose. Advise males with female partners of reproductive potential to use effective contraception during and for at least 3 mo after last dose of brigatinib. Advise patient to avoid breast feeding during and for 1 wk after last dose. Inform male patient that brigatinib may impair fertility.

bri-GA-ti-nib

NDC Code^*

• 63020- Millennium Pharmaceuticals, Inc.
  • 63020-090- Alunbrig
    • 63020-090-07- 7 TABLET, FILM COATED in 1 BOTTLE (63020-090-07)

• 63020- Millennium Pharmaceuticals, Inc.
  • 63020-090- Alunbrig
    • 63020-090-30- 30 TABLET, FILM COATED in 1 BOTTLE (63020-090-30)

• 63020- Millennium Pharmaceuticals, Inc.
  • 63020-113- Alunbrig
    • 63020-113-18- 180 TABLET, FILM COATED in 1 BOTTLE (63020-113-18)

• 63020- Millennium Pharmaceuticals, Inc.
  • 63020-113- Alunbrig
    • 63020-113-21- 21 TABLET, FILM COATED in 1 BOTTLE (63020-113-21)

• 63020- Millennium Pharmaceuticals, Inc.
  • 63020-113- Alunbrig
    • 63020-113-30- 30 TABLET, FILM COATED in 1 BOTTLE (63020-113-30)

• 63020- Millennium Pharmaceuticals, Inc.
  • 63020-180- Alunbrig
    • 63020-180-30- 30 TABLET, FILM COATED in 1 BOTTLE (63020-180-30)

• 63020- Millennium Pharmaceuticals, Inc.
  • 63020-198- Alunbrig
    • 63020-198-30- 1 KIT in 1 CARTON (63020-198-30) * 7 TABLET, FILM COATED in 1 BOTTLE (63020-090-07) * 23 TABLET, FILM COATED in 1 BOTTLE (63020-180-23)

• 76189- ARIAD Pharmaceuticals Inc.
  • 76189-113- Alunbrig
    • 76189-113-18- 180 TABLET, COATED in 1 BOTTLE (76189-113-18)

• 76189- ARIAD Pharmaceuticals Inc.
  • 76189-113- Alunbrig
    • 76189-113-21- 21 TABLET, COATED in 1 BOTTLE (76189-113-21)