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Brigatinib is indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC).
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✅ Description:
- Brigatinib, also known as Alunbrig, is a targeted cancer drug treatment specifically designed for non-small cell lung cancer (NSCLC).
- It is indicated for the treatment of advanced or metastatic NSCLC, but specifically for those with a mutation in the anaplastic lymphoma kinase (ALK) gene. Genetic testing is performed on tissue samples to confirm this gene change.
- Brigatinib is classified as a tyrosine kinase inhibitor (TKI), falling under the category of cancer growth blockers. It works by inhibiting tyrosine kinase proteins, blocking the chemical signals (enzymes) responsible for sending growth signals in cells.
- By blocking these signals, Brigatinib prevents the growth and division of cancer cells.
- Brigatinib is available in tablet form, which should be swallowed whole with a glass of water.
- It can be taken with or without food, and the dosage should strictly follow the instructions provided by the doctor or pharmacist.
- It is crucial not to alter the prescribed dosage unless advised by the healthcare team.
- Brigatinib is typically taken once a day.
- The treatment continues as long as it remains effective, and the side effects are manageable.
- Regular blood tests are conducted before and during the treatment to assess blood cell levels and other substances.
- Monitoring of liver and kidney function is also part of the testing process.
- Blood pressure, heart rate, and ECG (heart trace test) may be monitored at different intervals during the treatment.
- Brigatinib can interact with other medicines and herbal products. It is crucial to inform the healthcare team about all medications, including vitamins and herbal supplements.
- Grapefruit and grapefruit juice consumption should be avoided during treatment, as it may increase side effects.
- Brigatinib contains lactose (milk sugar). Individuals with lactose intolerance should consult their doctor before taking this medicine.
- Brigatinib may pose a risk to a developing fetus. Adequate non-hormonal contraception (such as condoms) is recommended during treatment to prevent pregnancy.
- Women are advised not to become pregnant for 4 months after finishing treatment, and men should avoid fathering a child for 3 months post-treatment.
- The impact of Brigatinib on fertility is not well-defined. Patients concerned about future fertility should discuss this with their doctor before starting treatment.
- Breastfeeding is not recommended during Brigatinib treatment.
- Inform other healthcare providers about ongoing Brigatinib treatment.
- Avoid live vaccines during treatment and for a specified period afterward, depending on the treatment received. The duration should be discussed with the doctor or pharmacist.
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✔️ Mechanism of Action:
- Brigatinib is a tyrosine kinase inhibitor with in vitro activity against multiple kinases, including ALK, ROS1, IGF-1R, FLT-3, EGFR deletion, and point mutations.
✔️ Inhibition:
It inhibits autophosphorylation of ALK and ALK-mediated phosphorylation of downstream signaling proteins such as STAT3, AKT, ERK1/2, and S6 in vitro and in vivo assays.
✔️ Proliferation Inhibition:
Demonstrated dose-dependent inhibition of EML4-ALK-positive NSCLC xenograft growth in mice.
✔️ Metabolism:
Primarily metabolized by CYP2C8 and CYP3A4 in vitro. The major metabolite, AP26123, has lower potency against ALK compared to Brigatinib.
✔️ Excretion:
Excreted mainly through feces (65%) and urine (25%).
✔️ Dosage and Administration:
The recommended dosing regimen for Brigatinib is as follows:
- 90mg orally once daily for the first 7 days.
- If 90mg is tolerated during the initial 7 days, increase the dose to 180mg orally once daily.
- Continue administering Brigatinib until disease progression or unacceptable toxicity.
- If Brigatinib is interrupted for 14 days or longer for reasons other than adverse reactions, resume treatment at 90 mg once daily for 7 days before increasing to the previously tolerated dose.
- Brigatinib may be taken with or without food.
- Instruct patients to swallow tablets whole; tablets should not be crushed or chewed.
- If a dose of Brigatinib is missed or vomiting occurs after taking a dose, an additional dose should not be administered, and the next dose of Brigatinib should be taken at the scheduled time.
Note: Patients should follow the dosage instructions as directed by the registered physician.
✔️ Interaction:
Avoid strong CYP3A inhibitors; if unavoidable, reduce the Biganib dose by approximately 50%. Strong CYP3A inducers should be avoided as they may decrease Brigatinib efficacy.
✔️ Contraindications:
- Hypersensitivity: Contraindicated in patients with known hypersensitivity to Brigatinib or any other components.
✔️ Side Effects:
- Interstitial Lung Disease (ILD)/Pneumonitis
- Hypertension
- Bradycardia
- Visual Disturbance
- Creatine Phosphokinase (CPK) Elevation
- Pancreatic Enzyme Elevation
- Hyperglycemia
✔️ Use in Pregnancy and Lactation:
- Pregnancy: Brigatinib can cause fetal harm when administered to a pregnant woman. There are no clinical data on the use of Brigatinib in pregnant women. Pregnant women should be advised of the potential risk to a fetus.
- Lactation: There is no data regarding the secretion of Brigatinib in human milk or its effects on the breastfed infant or milk production. Due to the potential for adverse reactions in breastfed infants, lactating women should not be advised to breastfeed during treatment with Brigatinib and for 1 week following the final dose.
✔️ Precautions & Warnings:
- ILD/Pneumonitis: Severe reactions observed; evaluate promptly for ILD/pneumonitis.
- Hypertension: Monitor blood pressure; withhold for Grade 3 hypertension.
- Bradycardia: Monitor heart rate; use caution with concomitant bradycardia-inducing agents.
- Visual Disturbance: Withhold for Grade 2 or greater severity; permanently discontinue for Grade 4.
- CPK Elevation: Monitor for muscle pain; withhold for Grade 3 or 4 CPK elevation.
- Pancreatic Enzyme Elevation: Monitor amylase and lipase; withhold for Grade 3 or 4 elevation.
- Hyperglycemia: Monitor glucose levels; adjust antihyperglycemic medications as needed.
✔️ Storage Conditions
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
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