Brigatinib

Brigatinib is a tyrosine kinase inhibitor (TKI) with in vitro activity at clinically achievable concentrations against multiple kinases including ALK, ROS1, insulin-like growth factor-1 receptor (IGF-1R), and FLT-3 as well as EGFR deletion and point mutations. Brigatinib inhibited autophosphorylation of ALK and ALK-mediated phosphorylation of the downstream signaling proteins STAT3, AKT, ERK1/2, and S6 in in vitro and in vivo assays.

• ALUNBRIG is indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) as detected by an FDA-approved test [see Dosage and Administration (2.1) ] . ALUNBRIG is a kinase inhibitor indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) as detected by an FDA-approved test.ICD-10: C34.90, C85.90

• None. None.contraindicated

90 mg orally once daily for the first 7 days; then increase to 180 mg orally once daily. May be taken with or without food. ( 2.2 ) 2.1 Patient Selection Select patients for the treatment of metastatic NSCLC with ALUNBRIG based on the presence of ALK positivity in tumor specimens [see Clinical Studies (14) ] . Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at http://www.fda.gov/CompanionDiagnostics. 2.2 Recommended Dosage The recommended dosage for ALUNBRIG is: 90 mg orally once daily for the first 7 days; then increase the dose to 180 mg orally once daily. Administer ALUNBRIG until disease progression or unacceptable toxicity. If ALUNBRIG 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. ALUNBRIG may be taken with or without food. Instruct patients to swallow tablets whole. Do not crush or chew tablets. If a dose of ALUNBRIG is missed or vomiting occurs after taking a dose, do not administer an additional dose and take the next dose of ALUNBRIG at the scheduled time. 2.3 Dosage Modifications for Adverse Reactions ALUNBRIG dosage reductions for adverse reactions are summarized in Table 1.

Interstitial Lung Disease (ILD)/Pneumonitis : Monitor for new or worsening respiratory symptoms, particularly during the first week of treatment. Withhold ALUNBRIG for new or worsening respiratory symptoms and promptly evaluate for ILD/pneumonitis. Upon recovery, either dose reduce or permanently discontinue ALUNBRIG. ( 2.3 , 5.1 ) Hypertension : Monitor blood pressure after 2 weeks and then at least monthly during treatment. For severe hypertension, withhold ALUNBRIG, then dose reduce or permanently discontinue. ( 2.3 , 5.2 ) Bradycardia : Monitor heart rate and blood pressure regularly during treatment. If symptomatic, withhold ALUNBRIG, then dose reduce or permanently discontinue. ( 2.3 , 5.3 ) Visual Disturbance : Advise patients to report visual symptoms. Withhold ALUNBRIG and obtain ophthalmologic evaluation, then dose reduce or permanently discontinue ALUNBRIG. ( 2.3 , 5.4 ) Creatine Phosphokinase (CPK) Elevation : Monitor CPK levels regularly during treatment. Based on the severity and with muscle pain or weakness, withhold ALUNBRIG, then resume or reduce dose. ( 2.3 , 5.5 ) Pancreatic Enzymes Elevation : Monitor lipase and amylase levels regularly during treatment. Based on the severity, withhold ALUNBRIG, then resume or reduce dose. ( 2.3 , 5.6 ) Hepatotoxicity : Monitor alanine aminotransferase (ALT), aspartate aminotransferase (AST) and total bilirubin levels regularly during treatment. Based on severity, withhold dose, then resume at lower level.

The following adverse reactions are discussed in greater detail in other sections of the prescribing information: Interstitial Lung Disease (ILD)/Pneumonitis [see Warnings and Precautions (5.1) ] Hypertension [see Warnings and Precautions (5.2) ] Bradycardia [see Warnings and Precautions (5.3) ] Visual Disturbance [see Warnings and Precautions (5.4) ] Creatine Phosphokinase (CPK) Elevation [see Warnings and Precautions (5.5) ] Pancreatic Enzymes Elevation [see Warnings and Precautions (5.6) ] Hepatotoxicity [see Warnings and Precautions (5.7) ] Hyperglycemia [see Warnings and Precautions (5.8) ] Photosensitivity [see Warnings and Precautions (5.9) ] The most common adverse reactions (≥25%) with ALUNBRIG were diarrhea, fatigue, nausea, rash, cough, myalgia, headache, hypertension, vomiting, and dyspnea. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Takeda Pharmaceuticals at 1-844-217-6468 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Advanced ALK-positive NSCLC Without Prior ALK-targeted Therapy In ALTA 1L, the safety of ALUNBRIG was evaluated in 136 patients with advanced ALK-positive NSCLC who had not previously received an ALK-targeted therapy [see Clinical Studies (14) ] .

Hepatic Impairment : Reduce the dose of ALUNBRIG for patients with severe hepatic impairment. ( 2.6 , 8.6 ) Renal Impairment : Reduce the dose of ALUNBRIG for patients with severe renal impairment. ( 2.7 , 8.7 ) Lactation : Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on its mechanism of action and findings in animals, ALUNBRIG can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ] . There are no clinical data on the use of ALUNBRIG in pregnant women. Administration of brigatinib to pregnant rats during the period of organogenesis resulted in dose-related skeletal anomalies at doses as low as 12.5 mg/kg/day (approximately 0.7 times the human exposure by AUC at 180 mg once daily) as well as increased post-implantation loss, malformations, and decreased fetal body weight at doses of 25 mg/kg/day (approximately 1.26 times the human exposure at 180 mg once daily) or greater (see Data ) . Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Metabolism

The geometric mean (CV%) steady-state maximum concentration (C max ) of brigatinib at ALUNBRIG doses of 90 mg and 180 mg once daily was 552 (49%) ng/mL and 1452 (60%) ng/mL, respectively, and the corresponding area under the concentration-time curve (AUC 0-Tau ) was 8165 (45%) ng∙h/mL and 20276 (62%) ng∙h/mL. After a single dose and multiple dosing of ALUNBRIG, systemic exposure of brigatinib was dose proportional over the dose range of 60 mg (0.3 times the recommended dose of 180 mg) to 240 mg (1.3 times the recommended dose of 180 mg) once daily.

• Apr 28, 2017NDANDA208772Takeda Pharms Usa

1. 1Death429—
2. 2Non-small Cell Lung Cancer392—
3. 3Off Label Use300—
4. 4Diarrhoea253—
5. 5Metastases To Central Nervous System240—
6. 6Nausea233—
7. 7Lung Neoplasm Malignant223—
8. 8Blood Creatine Phosphokinase Increased222—
9. 9Fatigue215—
10. 10Product Dose Omission Issue203—
11. 11Drug Ineffective184—
12. 12Neoplasm Progression180—
13. 13Dyspnoea131—
14. 14Vomiting130—
15. 15Rash125—

The 10 most recently updated of 46 ClinicalTrials.gov registrations naming Brigatinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of Neladalkib (NVL-655) in Patients With Advanced NSCLC and Other Solid Tumors Harboring ALK Rearrangement or Activating ALK Mutation (ALKOVE-1)
  Recruiting · Phase 1 · Phase 2 · Interventional · 840 enrolled · Nuvalent Inc.
  NCT05384626updated 2026-05-27
• Innovative Trial for Understanding the Impact of Targeted Therapies in NF2-Related Schwannomatosis (INTUITT-NF2)
  Recruiting · Phase 2 · Interventional · 109 enrolled · Scott R. Plotkin, MD, PhD
  NCT04374305updated 2026-05-06
• Trial for Local Ablative Treatment (LAT) Optimization in Patients With Advanced Non-Small Cells Lung Cancer (NSCLC) Presenting an Anaplastic Lymphoma Kinase (ALK) Rearrangement Treated by Brigatinib
  Recruiting · Phase 2 · Interventional · 45 enrolled · Groupe Francais De Pneumo-Cancerologie
  NCT06620835updated 2026-04-29
• Targeted Treatment for ALK Positive Patients Who Have Previously Been Treated for Non-squamous Non-small Cell Lung Cancer
  Terminated · Phase 2 · Interventional · 10 enrolled · National Cancer Institute (NCI)
  NCT03737994updated 2026-04-23
• A Study of Brigatinib as Preferred First Therapy for Adults With Non-Small Cell Lung Cancer (NSCLC) ENTIRETY
  Active not recruiting · Observational · 50 enrolled · Takeda
  NCT05735327updated 2026-04-13
• Survey of Brigatinib Used To Treat People With Non-Small Cell Lung Cancer
  Recruiting · Observational · 500 enrolled · Takeda
  NCT05100069updated 2026-03-17
• Advancing Brigatinib Properties in ALK+ NSCLC Patients by Deep Phenotyping
  Active not recruiting · Phase 2 · Interventional · 118 enrolled · Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest
  NCT04318938updated 2026-03-02
• A Study to Learn About Brigatinib Treatment Information Available in Chinese Participants With Non-Small-cell Lung Cancer (NSCLC)
  Active not recruiting · Observational · 154 enrolled · Takeda
  NCT05721950updated 2026-02-18
• Clinical Utility of Liquid Biopsy in Brigatinib ALK+ Patients
  Active not recruiting · Phase 2 · Interventional · 33 enrolled · Fundación GECP
  NCT04223596updated 2026-02-04
• A Study of Usage of Brigatinib in the Treatment of Adult Participants for Approved Indications In South Korea
  Recruiting · Observational · 257 enrolled · Takeda
  NCT04592523updated 2025-12-24

Frequently asked questions

How does Brigatinib work?

Brigatinib is a tyrosine kinase inhibitor (TKI) with in vitro activity at clinically achievable concentrations against multiple kinases including ALK, ROS1, insulin-like growth factor-1 receptor (IGF-1R), and FLT-3 as well as EGFR deletion and point mutations. Brigatinib inhibited autophosphorylation of ALK and ALK-mediated phosphorylation of the downstream signaling proteins STAT3, AKT, ERK1/2, and S6 in in vitro and in vivo assays.

What is Brigatinib used for?

According to FDA labeling, Brigatinib carries indications including: ALUNBRIG is indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) as detected by an FDA-approved test [see Dosage and Administration (2.1) ] . ALUNBRIG is a kinase inhibitor indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) as detected by an FDA-approved test.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Brigatinib?

Brigatinib is classified as Anaplastic lymphoma kinase (ALK) inhibitors, Kinase Inhibitor, Cytochrome P450 3A Inducers, Tyrosine Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Brigatinib?

Brigatinib is marketed under brand names including Alunbrig.

What are the contraindications for Brigatinib?

Brigatinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.