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November 16, 2025
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Brand Name :
Alunbrig
Synonyms :
brigatinib
Class :
Antineoplastics and Anaplastic Lymphoma Kinase Inhibitor
Brand Name :
Alunbrig
Synonyms :
brigatinib
Class :
Antineoplastics and Anaplastic Lymphoma Kinase Inhibitor
90
mg
Tablet
Orally
once a day
Maintenance dose is 180 mg orally once a day
Dose Adjustments
Hepatic impairment: Mild/moderate (Child-Pugh A/B): No dose adjustment required Severe (Child-Pugh C): Reduce one daily dose by 40% (like, from 180mg 120 mg, 120 mg to 90 mg) Renal impairment: Mild/moderate (CrCl 30-89 ml/min): No dose adjustment required Severe (CrCl 15-29 mL/min): Reduce dose by 50% (like, from 180 mg to 90 mg)
Safety and efficacy not established
it may increase the bradycardic effect of ceritinib
brigatinib: they may diminish the serum concentration of hormonal contraceptives
brigatinib: they may diminish the serum concentration of hormonal contraceptives
brigatinib: they may diminish the serum concentration of hormonal contraceptives
brigatinib: they may diminish the serum concentration of hormonal contraceptives
brigatinib: they may diminish the serum concentration of CYP3A4 Inducers
brigatinib: they may diminish the serum concentration of CYP3A4 Inducers
brigatinib: they may diminish the serum concentration of CYP3A4 Inducers
brigatinib: they may diminish the serum concentration of CYP3A4 Inducers
brigatinib: they may diminish the serum concentration of CYP3A4 Inducers
may enhance the concentration of serum when combined with brigatinib
may enhance the concentration of serum when combined with brigatinib
may enhance the concentration of serum when combined with brigatinib
may enhance the concentration of serum when combined with brigatinib
may enhance the concentration of serum when combined with brigatinib
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 Inhibitors
drospirenone/ethinyl estradiol/levomefolate
may diminish the serum concentration of Hormonal Contraceptives
etonogestrel/ethinyl estradiol
may diminish the serum concentration of Hormonal Contraceptives
it may decrease the serum concentration of brigatinib
It may diminish the effect when combined with phenobarbital by affecting the intestinal/hepatic enzyme CYP3A4
It may enhance the effect when combined with grapefruit by CYP3A4 metabolism
the effect of brigatinib is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
when both drugs are combined, there may be an increased effect of brigatinib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of brigatinib
it may increase the hypertensive effect of androgens
it may reduce the therapeutic effect of antidiabetic drugs
it may reduce the effect of antihypertensive agents
it may increase the effect of other bradycardia-causing agents
it decreases the efficacy of antihypertensive agents
it decreases the efficacy of antihypertensive agents
it decreases the efficacy of antihypertensive agents
it decreases the efficacy of antihypertensive agents
it decreases the efficacy of antihypertensive agents
may decrease the antihypertensive effect when combined with antihypertensive agents
may decrease the antihypertensive effect when combined with antihypertensive agents
may decrease the antihypertensive effect when combined with antihypertensive agents
may decrease the antihypertensive effect when combined with antihypertensive agents
may decrease the antihypertensive effect when combined with antihypertensive agents
brigatinib: they may decrease the antihypertensive effect when combined with antihypertensive drugs
When brigatinib is used together with fluconazole, this leads to reduction in the brigatinib metabolism
When brigatinib is used together with capsaicin, this leads to enhanced risk or seriousness of methemoglobinemia
brigatinib: they may increase the toxic effect of mu-opioid receptor agonists
brigatinib: they may increase the toxic effect of mu-opioid receptor agonists
When brigatinib is used together with ridaforolimus, this leads to enhanced concentration serum of brigatinib
brigatinib: it may enhance the metabolism of cerivastatin
when both drugs combine brigatinib will increase effect of ifosfamide by affecting the enzyme CYP3A4 metabolism.
when both drugs are combined, there may be an increased metabolism of brigatinib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
the serum levels of Brigatinib may be increased
it decreases the concentration of hormonal contraceptives in serum
Brigatinib is a tyrosine kinase inhibitor that targets several kinases, including ALK, ROS1, and the insulin-like growth factor 1 receptor. It is also effective against certain EGFR mutations and deletions. Its primary action is blocking ALK phosphorylation, which prevents the activation of signaling pathways involved in cancer cell growth and survival.
Adverse drug reactions:
Frequency defined
>10%
Increased AST
Hyperglycemia
Increased ALT
Nausea
Fatigue
Headache
Increased CPK
Increased amylase
Dyspnea
Vomiting
Anemia
Decreased appetite
Prolonged aPTT
Increased lipase
Diarrhea
Lymphopenia
Cough
Abdominal pain
Pain in extremity
Insomnia
1-10%
Back pain
Myalgia
Visual disturbances
Pneumonia
Interstitial lung disease/pneumonitis
<1%
Hypoxia
Pulmonary Toxicity (Early-Onset): Severe, life-threatening, or fatal interstitial lung disease (ILD)/pneumonitis has been reported, often occurring within the first week of treatment. Patients should be closely monitored for new or worsening respiratory symptoms such as shortness of breath, cough, or fever. If symptoms develop, withhold brigatinib and evaluate promptly. Discontinue permanently if ILD/pneumonitis is confirmed and severe.
Contraindication
Hypersensitivity
Cautions
Pulmonary toxicity: Risk of early-onset interstitial lung disease (ILD)/pneumonitis; monitor closely, especially during the first week of therapy.
Hypertension: May cause new or worsening high blood pressure; monitor blood pressure regularly.
Bradycardia: Use with caution in patients on other drugs that lower heart rate; monitor heart rate during treatment.
Hyperglycemia: May increase blood glucose levels; use cautiously in diabetic patients and monitor glucose levels.
Elevated creatine phosphokinase (CPK): Monitor for muscle pain or weakness; check CPK levels regularly.
Visual disturbances: May cause blurred vision or other visual symptoms; assess promptly if visual changes occur.
Pregnancy warnings:
Breastfeeding warnings:
Pregnancy Categories:
Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first trimester or the later trimester.
Category B: No evidence shown of risk to the fetus found in animal reproduction studies, and there are not enough studies on pregnant women
Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a result in humans must take care of potential risks in pregnant women
Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits
Category X: Drugs listed in this category outweigh risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Brigatinib is an orally administered anaplastic lymphoma kinase inhibitor (ALKi) that effectively targets tumor cells harboring ALK mutations, including those linked to resistance to crizotinib. It demonstrates potent anti-tumor activity, particularly in ALK-positive non-small cell lung cancer (NSCLC).
In early-phase clinical studies (NCT02094573), brigatinib showed a 74% objective response rate among 78 evaluable ALK-positive NSCLC patients, most of whom had previously been treated with crizotinib. Notably, it also exhibited intracranial activity, with measurable brain lesion responses observed in over half of patients evaluated with brain metastases.
Pharmacokinetics
Absorption
Brigatinib is well absorbed orally, with dose-proportional exposure. At 90 mg, the C<sub>max</sub> is 552 ng/mL and AUC is 8165 ng·h/mL; at 180 mg, C<sub>max</sub> increases to 1452 ng/mL and AUC to 20276 ng·h/mL. Peak plasma concentrations (T<sub>max</sub>) occur within 1 to 4 hours post-dose. A high-fat meal reduces C<sub>max</sub> by about 13% but has no effect on overall drug exposure (AUC).
Distribution
The apparent volume of distribution at steady state is approximately 153 L. Brigatinib binds to plasma proteins at a rate of about 66%, with a blood-to-plasma concentration ratio of 0.69.
Metabolism
Brigatinib is primarily metabolized by CYP2C8 (72.4%) and to a lesser extent by CYP3A4 (27.6%). Major metabolites include a N-demethylated product and a cysteine conjugate. After oral administration, about 91.5% remains in the unchanged form, with only 3.5% converted to the metabolite AP26123, which has significantly lower activity.
Elimination/Excretion
Elimination occurs mainly via feces (65%) and urine (25%). Unchanged brigatinib accounts for 41% of the fecal and 86% of the urinary excretion.
The elimination half-life at steady state is approximately 25 hours.
At 180 mg oral dose, the apparent oral clearance is around 12.7 L/h.
Pharmacodynamics
Brigatinib inhibits the growth and survival of cancer cells expressing the EML4-ALK fusion protein and 17 ALK mutations resistant to crizotinib. It also acts against cells with EGFR deletions and mutations in ROS1 and FLT3 (L2026M, F691L, D835Y). In animal models with EML4-ALK tumors, brigatinib shows dose-dependent tumor suppression and improved survival. However, its time course and exposure-response relationship remain unclear.
Start with 90 mg orally once daily for the first 7 days, then increase to 180 mg orally once daily if tolerated.
Continue treatment until disease progression or unacceptable toxicity occurs.
Tablets should be swallowed whole, not crushed or chewed.
Brigatinib may be taken with or without food.
Avoid grapefruit and grapefruit juice during treatment, as they may affect drug levels.
If the treatment is interrupted for 14 days or more (not due to side effects), restart at 90 mg once daily for 7 days before returning to the previously tolerated dose.
Generic Name: brigatinib
Pronounced: BRIH-ga-ti-nib
Why do we use brigatinib?
Brigatinib is used to treat advanced non-small cell lung cancer (NSCLC). It belongs to the class of kinase inhibitors and works by blocking abnormal proteins that promote the growth of cancer cells.
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