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As a new dual inhibitor of ALK and EGFR, brigatinib significantly enhances its binding force with ALK protein through its unique dimethylphosphorus oxide (DMPO) structure, thereby improving drug activity.
1. Generic name: Brigatinib
2. Trade name: ALUNBRIG
3. English name: Brigatinib
Brigatinib is a kinase inhibitor used to treat patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have disease progression or are intolerant after treatment with crizotinib.
Specifications: 180 mg/tablet.
1. Active ingredient: brigatinib.
2. Inactive ingredients: The tablet core contains lactose monohydrate, microcrystalline cellulose, sodium type A starch glycolate, magnesium stearate and hydrophobic colloidal silica. The coating contains talc, polyethylene glycol, polyvinyl alcohol and titanium dioxide.
1. Recommended dosage regimen: Take 90 mg orally once a day for the first 7 days; if tolerated in the first 7 days, increase to 180 mg orally once a day starting from the 8th day.
2. How to take: It can be taken with food or on an empty stomach. Tablets should be swallowed whole and not crushed or chewed.
3. Missed dose or vomiting: If you miss a dose or vomit after taking the medicine, you should not take additional doses and resume taking the medicine at the next scheduled time.
1. Dose reduction steps: For patients with a starting dose of 180 mg, the first dose is reduced to 120 mg; the second dose is reduced to 90 mg; and the third dose is reduced to 60 mg. For patients starting at 90 mg, reduce initial dose to 60 mg; if not tolerated, permanently discontinue. Once the dose is reduced due to adverse reactions, the dose must not be increased subsequently.
2. Adjustment for adverse reactions: The dose needs to be suspended, reduced or permanently discontinued according to the severity of adverse reactions.
3. Adjustments due to drug interactions: simultaneous use with strong CYP3A inhibitors should be avoided. If unavoidable, the once-daily dose of brigatinib should be reduced by approximately 50% (ie, from 180 mg to 90 mg or from 90 mg to 60 mg). After discontinuing a strong CYP3A inhibitor, resume brigatinib at the dose that was tolerated before using the inhibitor.
1. Medication time: once a day, preferably at a fixed time, before or after meals.
2. Missed dose handling: Skip the missed dose and take the next dose at the next regular time. Do not take a double dose to make up for a missed dose.
3. Vomiting treatment: If vomiting occurs after taking the medicine, there is no need to take a supplementary dose, just take the next dose as planned.
4. Monitoring requirements: During treatment, pulmonary symptoms (especially in the first week of treatment), blood pressure (after 2 weeks of treatment and at least once a month thereafter), heart rate and rhythm, visual changes, serum creatine phosphokinase (CPK), lipase and amylase, fasting blood sugar, etc. need to be monitored regularly.
1. Pregnant women: Based on the mechanism of action and animal studies, it may cause fetal harm. Pregnant women should be informed of the potential risk to the fetus.
2. Breastfeeding women: It is recommended not to breastfeed during treatment and within 1 week after the last dose.
Women and men of childbearing potential: Women should use effective non-hormonal contraception during treatment and for at least 4 months after the last dose because brigatinib may render certain hormonal contraceptives ineffective. Men with a female partner of childbearing potential should use effective contraception during treatment and for at least 3 months after the last dose.
3. Pediatric patients: Safety and effectiveness have not been established.
4. Elderly patients: Clinical studies have found no clinically relevant differences with younger patients.
5. Patients with liver damage: Patients with mild liver damage do not need to adjust the dosage. Pharmacokinetics and safety have not been studied in patients with moderate or severe hepatic impairment.
6. Patients with renal impairment: Patients with mild to moderate renal impairment do not need to adjust the dosage. Pharmacokinetics and safety have not been studied in patients with severe renal impairment.
1. The most common adverse reactions (≥25%) include: nausea, diarrhea, fatigue, cough, headache.
2. Common laboratory abnormalities include: elevated aspartate aminotransferase, hyperglycemia, elevated creatine phosphokinase, elevated lipase, elevated alanine aminotransferase, elevated amylase, anemia, lymphopenia, etc.
3. Serious adverse reactions include: interstitial lung disease/pneumonitis, hypertension, bradycardia, visual impairment, elevated creatine phosphokinase, elevated pancreatic enzymes, hyperglycemia, etc.
There are no clear contraindications, but it is prohibited for those who are allergic to this product or excipients.
1. Combination with strong CYP3A inhibitors (such as itraconazole, clarithromycin, etc.) should be avoided because it will increase the plasma concentration of brigatinib. If unavoidable, the dose of brigatinib needs to be reduced.
2. Combination with strong CYP3A inducers (such as rifampicin, carbamazepine, St. John's wort, etc.) should be avoided, as it will reduce the plasma concentration of brigatinib and affect its efficacy.
3. Brigatinib is a CYP3A inducer and may reduce the plasma concentration of CYP3A substrates (including hormonal contraceptives), resulting in loss of efficacy. Effective non-hormonal contraceptive methods should be used.
4. Avoid eating grapefruit or drinking grapefruit juice, as it may increase the concentration of brigatinib in the blood.
Store at controlled room temperature 20°C to 25°C (68°F to 77°F); short-distance transportation allowed between 15°C and 30°C (59°F to 86°F).