Brigatinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Brigatinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2017. Its mechanism of action is classified as Cytochrome P450 3A Inducers and Tyrosine Kinase Inhibitors. DrugCentral lists 69 molecular targets, including ALK, FER and ROS1. Recorded indications include Advanced/recurrent anaplasticlymphoma kinase (ALK)-positive non-small cell lung cancer and Non-small cell lung cancer.

• Approval status: onp (first approved 2017 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Cytochrome P450 3A Inducers; Tyrosine Kinase Inhibitors.
• Molecular targets: ALK, FER, ROS1 and FLT3 (69 listed in DrugCentral).
• Indications: Advanced/recurrent anaplasticlymphoma kinase (ALK)-positive non-small cell lung cancer and Non-small cell lung cancer.
• ATC code: L01ED04 (Anaplastic lymphoma kinase (ALK) inhibitors).
• Molecular formula: C29H39ClN7O2P; molecular weight 584.10 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Advanced/recurrent anaplasticlymphoma kinase (ALK)-positive non-small cell lung cancer
• Non-small cell lung cancer

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 3A Inducers; Tyrosine Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (69)

Target	Gene	Action	Activity
ALK tyrosine kinase receptor	ALK	inhibitor	IC50 9.22
Tyrosine-protein kinase Fer	FER	unknown	IC50 8.89
Proto-oncogene tyrosine-protein kinase ROS	ROS1	inhibitor	IC50 8.72
Receptor-type tyrosine-protein kinase FLT3	FLT3	inhibitor	IC50 8.68
Tyrosine-protein kinase Fes/Fps	FES	unknown	IC50 8.46
Focal adhesion kinase 1	PTK2	unknown	IC50 8.41
Protein-tyrosine kinase 6	PTK6	unknown	IC50 8.39
Testis-specific serine/threonine-protein kinase 1	TSSK1B	unknown	IC50 8.36
Serine/threonine-protein kinase Chk2	CHEK2	unknown	IC50 8.25
Ribosomal protein S6 kinase alpha-2	RPS6KA2	unknown	IC50 7.89
Leukocyte tyrosine kinase receptor	LTK	unknown	IC50 7.85
Tyrosine-protein kinase Yes	YES1	unknown	IC50 7.72
Proto-oncogene tyrosine-protein kinase receptor Ret	RET	unknown	IC50 7.66
Dual specificity protein kinase CLK1	CLK1	unknown	IC50 7.64
Protein-tyrosine kinase 2-beta	PTK2B	unknown	IC50 7.62
Ribosomal protein S6 kinase alpha-3	RPS6KA3	unknown	IC50 7.58
Receptor tyrosine-protein kinase erbB-4	ERBB4	unknown	IC50 7.57
Calcium/calmodulin-dependent protein kinase type II subunit delta	CAMK2D	unknown	IC50 7.54
Ribosomal protein S6 kinase alpha-1	RPS6KA1	unknown	IC50 7.52
Serine/threonine-protein kinase Chk1	CHEK1	unknown	IC50 7.52

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2021-01-22	PMDA	—	TAKEDA PHARMACEUTICAL COMPANY LIMITED
2018-09-22	EMA	—	TAKEDA PHARMA A/S
2017-04-28	FDA	—	ARIAD

ATC classification

ATC code	Therapeutic hierarchy
L01ED04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Anaplastic lymphoma kinase (ALK) inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: ALK · Testing Required
• FDA label: ALK · Testing Required
• HCSC label: ALK · Testing Required

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Metastases to central nervous system	604.4
Blood creatine phosphokinase increased	587.3
Neoplasm progression	334.0
Amylase increased	191.6
Death	155.2
Pulmonary toxicity	139.3
Metastasis	119.2
Lipase increased	112.9
Disease progression	108.9
Metastases to liver	107.7
Pneumonitis	88.1
Product dose omission issue	69.7

Chemical structure

• Molecular formula: C₂₉H₃₉ClN₇O₂P
• Molecular weight: 584.10 g/mol
• CAS number: 1197953-54-0
• InChIKey: AILRADAXUVEEIR-UHFFFAOYSA-N
• PubChem CID: 68165256

COC1=C(NC2=NC=C(Cl)C(NC3=CC=CC=C3P(C)(C)=O)=N2)C=CC(=C1)N1CCC(CC1)N1CCN(C)CC1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Brigatinib used for?

DrugCentral lists the following indications for Brigatinib: Advanced/recurrent anaplasticlymphoma kinase (ALK)-positive non-small cell lung cancer and Non-small cell lung cancer.

How does Brigatinib work?

Brigatinib is classified as Cytochrome P450 3A Inducers and Tyrosine Kinase Inhibitors; its molecular targets in DrugCentral include ALK (inhibitor), FER, ROS1 (inhibitor) and FLT3 (inhibitor).

When was Brigatinib first approved?

Brigatinib was first approved by the FDA in 2017.

What drug class does Brigatinib belong to?

Brigatinib is in the Kinase Inhibitor class.

What is the chemical formula of Brigatinib?

Brigatinib has the molecular formula C29H39ClN7O2P and a molecular weight of 584.10 g/mol.

Sources

• DrugCentral drug card 5233 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3545311 — compound record and bioactivity
• PubChem CID 68165256 — chemical identifiers
• DrugBank DB12267 — drug record
• FDA UNII HYW8DB273J — substance identity
• DailyMed: FDA labels for Brigatinib — current prescribing information (label search)
• UniProt Q9UM73 (ALK) — target protein
• UniProt P16591 (FER) — target protein
• UniProt P08922 (ROS1) — target protein
• UniProt P36888 (FLT3) — target protein
• UniProt P07332 (FES) — target protein
• UniProt Q05397 (PTK2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.