BRIGATINIB

Details

Stereochemistry	ACHIRAL
Molecular Formula	C29H39ClN7O2P
Molecular Weight	584.092
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=C(NC2=NC=C(Cl)C(NC3=C(C=CC=C3)P(C)(C)=O)=N2)C=CC(=C1)N4CCC(CC4)N5CCN(C)CC5

InChI

InChIKey=AILRADAXUVEEIR-UHFFFAOYSA-N

InChI=1S/C29H39ClN7O2P/c1-35-15-17-37(18-16-35)21-11-13-36(14-12-21)22-9-10-24(26(19-22)39-2)33-29-31-20-23(30)28(34-29)32-25-7-5-6-8-27(25)40(3,4)38/h5-10,19-21H,11-18H2,1-4H3,(H2,31,32,33,34)

HIDE SMILES / InChI

Molecular Formula	C29H39ClN7O2P
Molecular Weight	584.092
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.ariad.com/research-development/brigatinib/
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/27780853

Brigatinib (AP26113) is an investigational, targeted cancer medicine discovered internally at ARIAD Pharmaceuticals, Inc. Brigatinib has exhibited activity as a potent dual inhibitor of anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR). It is in development for the treatment of patients with anaplastic lymphoma kinase positive (ALK+) non-small cell cancer (NSCLC) whose disease is resistant to crizotinib. Brigatinib is currently being evaluated in the global Phase 2 ALTA (ALK in Lung Cancer Trial of AP26113) trial that is anticipated to form the basis for its initial regulatory review. ARIAD has also initiated the Phase 3 ALTA 1L trial to assess the efficacy of brigatinib in comparison to crizotinib. Brigatinib was granted orphan drug designation by the U.S. Food and Drug Administration (FDA) in May 2016 for the treatment of certain subtypes of non-small cell lung cancer (NSCLC). The designation is for anaplastic lymphoma kinase-positive (ALK+), c-ros 1 oncogene positive (ROS1+), or epidermal growth factor receptor positive (EGFR+) non-small cell lung cancer (NSCLC). Brigatinib received breakthrough therapy designation from the FDA in October 2014 for the treatment of patients with ALK+ NSCLC whose disease is resistant to crizotinib. Both designations were based on results from an ongoing Phase 1/2 trial that showed anti-tumor activity of brigatinib in patients with ALK+ NSCLC, including patients with active brain metastases.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
ALK tyrosine kinase receptor 25 Target ID: CHEMBL4247 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27049722 \| https://www.ncbi.nlm.nih.gov/pubmed/27780853	Inhibitor 8297		10.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
ALK-positive metastatic non-small cell lung cancer 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208772lbl.pdf	Primary		Approved 8429	ALUNBRIG Approved Use ALUNBRIG is indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. Launch Date 2017
ALK-positive advanced non-small cell lung cancer 1 Sources: https://clinicaltrials.gov/ct2/show/NCT02737501	Primary		Phase III 656	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
552 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208772lbl.pdf	180 mg 1 times / day steady-state, oral dose: 180 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BRIGATINIB plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN
701.3 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30570839	180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered:		BRIGATINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
8165 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208772lbl.pdf	180 mg 1 times / day steady-state, oral dose: 180 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BRIGATINIB plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN
13261 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30570839	180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered:		BRIGATINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
25 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208772lbl.pdf	180 mg 1 times / day steady-state, oral dose: 180 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BRIGATINIB plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN
31 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/30570839	180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered:		BRIGATINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
34% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208772lbl.pdf	180 mg 1 times / day steady-state, oral dose: 180 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		BRIGATINIB plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
180 mg 1 times / day steady, oral Recommended Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208772lbl.pdf	unhealthy, 54 years (range: 18 - 82 years) n = 109 Health Status: unhealthy Condition: locally advanced or metastatic ALK-positive non-small cell lung cancer Age Group: 54 years (range: 18 - 82 years) Sex: M+F Population Size: 109 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208772lbl.pdf	Disc. AE: Pneumonitis, Pneumonitis... Other AEs: Nausea, Nausea... AEs leading to discontinuation/dose reduction: Pneumonitis (all grades, 37%) Pneumonitis (grade 3-4, 1.8%) Hypertension (grade 3-4, 5.5%) Pneumonia (all grades, 4.6%) Pneumonia (grade 3-4, 1.83%) Hyperglycemia (grade 3-4, 3.7%) Creatine phosphokinase increased (all grades, 27%) Creatine phosphokinase increased (grade 3-4, 2.8%) Other AEs: Nausea (all grades, 33%) Nausea (grade 3-4, 0.9%) Diarrhea (all grades, 19%) Vomiting (all grades, 24%) Vomiting (grade 3-4, 1.8%) Constipation (all grades, 19%) Constipation (grade 3-4, 0.9%) Abdominal distension (all grades, 17%) Abdominal pain (all grades, 17%) Epigastric discomfort (all grades, 17%) Asthenia (all grades, 29%) Asthenia (grade 3-4, 1.8%) Fatigue (all grades, 29%) Fatigue (grade 3-4, 1.8%) Pyrexia (all grades, 14%) Cough (all grades, 18%) Dyspnea (all grades, 27%) Dyspnea (grade 5, 1 patient) Exertional dyspnea (all grades, 27%) Dyspnea (grade 3-4, 2.8%) Exertional dyspnea (grade 3-4, 2.8%) Hypoxia (all grades, 0.9%) Headache (all grades, 28%) Sinus headache (all grades, 28%) Peripheral sensory neuropathy (all grades, 13%) Paresthesia (all grades, 13%) Peripheral sensory neuropathy (grade 3-4, 0.9%) Paresthesia (grade 3-4, 0.9%) Acneiform dermatitis (all grades, 15%) Exfoliative rash (all grades, 15%) Rash (all grades, 15%) Pruritic rash (all grades, 15%) Pustular rash (all grades, 15%) Acneiform dermatitis (grade 3-4, 1.8%) Exfoliative rash (grade 3-4, 1.8%) Rash (grade 3-4, 1.8%) Pruritic rash (grade 3-4, 1.8%) Pustular rash (grade 3-4, 1.8%) Hypertension (all grades, 11%) Muscle spasms (all grades, 12%) Back pain (all grades, 10%) Back pain (grade 3-4, 1.8%) Musculoskeletal pain (all grades, 9.2%) Myalgia (all grades, 9.2%) Arthralgia (all grades, 14%) Arthralgia (grade 3-4, 0.9%) Pain in extremity (all grades, 11%) Decreased appetite (all grades, 22%) Decreased appetite (grade 3-4, 0.9%) Diplopia (all grades, 7.3%) Photophobia (all grades, 7.3%) Blurred vision (all grades, 7.3%) Visual acuity reduced (all grades, 7.3%) Visual impairment (all grades, 7.3%) Vitreous floaters (all grades, 7.3%) Visual field defect (all grades, 7.3%) Macular edema (all grades, 7.3%) Vitreous detachment (all grades, 7.3%) Pneumonia (grade 5, 1 patient) Insomnia (all grades, 11%) Aspartate aminotransferase increased (all grades, 38%) Aspartate aminotransferase increased (grade 3-4, 0.9%) Hyperglycemia (all grades, 38%) Lipase increased (all grades, 21%) Lipase increased (grade 3-4, 4.6%) Alanine aminotransferase increased (all grades, 34%) Amylase increased (all grades, 27%) Amylase increased (grade 3-4, 3.7%) Alkaline phosphatase increased (all grades, 15%) Alkaline phosphatase increased (grade 3-4, 0.9%) Phosphate decreased (all grades, 15%) Phosphate decreased (grade 3-4, 1.8%) Anemia (all grades, 23%) Anemia (grade 3-4, 0.9%) Lymphopenia (all grades, 19%) Lymphopenia (grade 3-4, 2.8%) Respiratory failure (grade 5, 1 patient) Pulmonary embolism (grade 5, 1 patient) Bacterial meningitis (grade 5, 1 patient) Urosepsis (grade 5, 1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208772lbl.pdf
300 mg 1 times / day multiple, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: https://www.firstwordpharma.com/node/1096205?tsid=17	unhealthy Health Status: unhealthy Condition: advanced non-small cell lung cancer Sources: https://www.firstwordpharma.com/node/1096205?tsid=17	DLT: Dyspnea, Hypoxia... Dose limiting toxicities: Dyspnea (1 patient) Hypoxia (1 patient) Sources: https://www.firstwordpharma.com/node/1096205?tsid=17
240 mg 1 times / day multiple, oral Dose: 240 mg, 1 times / day Route: oral Route: multiple Dose: 240 mg, 1 times / day Sources: https://www.firstwordpharma.com/node/1096205?tsid=17	unhealthy Health Status: unhealthy Condition: advanced non-small cell lung cancer Sources: https://www.firstwordpharma.com/node/1096205?tsid=17	DLT: Alanine aminotransferase increased... Dose limiting toxicities: Alanine aminotransferase increased (1 patient) Sources: https://www.firstwordpharma.com/node/1096205?tsid=17

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inducer 781	inhibitor 1767	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT1 512 MATE1 306 MATE2 263 CYP1A2 1524 CYP2C8 911 CYP2C19 1478 CYP2B6 810 CYP3A4/5 278 P-gp 1461 BCRP 699 OATP1B1 788 OATP1B3 706 OAT1 599 OAT3 642 OCT2 647 BSEP 402	CYP2C8 693 P-gp 1537 BCRP 561 OATP1B1 406 OATP1B3 350 OAT1 326 OAT3 339 OCT1 327 OCT2 355 MATE1 135 MATE2 96 BSEP 52

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
BSEP 403	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=66 Page: -	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=66 Page: -	no
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=66 Page: -	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=66 Page: -	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=66 Page: -	no
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=66 Page: -	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=43 Page: -	weak	unlikely Comment: Induction of CYP3A4 mRNA (mean 6-fold change at 1 μM), but no induction of CYP3A4 activity. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=43 Page: -
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=66 Page: -	yes
MATE1 308	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=66 Page: -	yes
MATE2 263	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=66 Page: -	yes
OCT1 543	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=66 Page: -	yes
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=66 Page: -	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	major	yes (co-administration study) Comment: Coadministration of gemfibrozil (a strong CYP2C8 inhibitor) 600 mg BID with a single dose of 90 mg brigatinib decreased brigatinib AUC by 12% (90% CI: 6%, 17%) and Cmax by 41% (90% CI: 35%, 46%) as compared with brigatinib alone. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	minor	yes (co-administration study) Comment: Coadministration of itraconazole (a strong CYP3A4 inhibitor) increased brigatinib AUC by 2-fold. Coadministration of rifampin (a strong CYP3A4 inducer) decreased brigatinib AUC by 80% (90% CI: 79%, 82%) and Cmax by 60% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -
BSEP 52	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
MATE1 135	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
MATE2 96	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
OAT1 326	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
OAT3 339	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
OCT1 327	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
OCT2 355	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	no
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	yes
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=44 Page: -	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208772Orig1s000MultidisciplineR.pdf#page=42 Page: -

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY459486	https://www.001chemical.com/chem/1197953-54-0
AA Blocks	AA000PKR	https://www.aablocks.com/goods/Goods/detail?id=AA000PKR
Aaron Chemicals	AR000QCJ	http://www.aaronchem.com/1197953-54-0
AbMole Bioscience	M5317	http://www.abmole.com/products/brigatinib.html
Achemtek	0102-028644	http://www.achemtek.com/1197953-54-0
Adooq BioScience	A13450	https://www.adooq.com/brigatinib.html
Angel Pharmatech	AG-10397	http://www.angelpharmatech.com/1197953-54-0.html
Ark Pharm	AK547077	http://www.arkpharminc.com/products/1197953-54-0.html
Ark Pharma Scientific Limited	A-1739	http://www.arkpharmtech.com/product/33690.html
AvaChem Scientific	6168	https://www.avachem.com/productSearch.asp?6168
Axon MedChem	2978	https://www.axonmedchem.com/product/2978
BOC Sciences	1197953-54-0	https://www.bocsci.com/brigatinib-cas-1197953-54-0-item-470820.html
BioChemPartner	BCP17214	http://www.biochempartner.com/1197953-54-0-BCP17214
CSNpharm	CSN17547	https://www.csnpharm.com/products/brigatinib.html
Chem Scene	CS-4278	http://www.chemscene.com/1197953-54-0.html
Chemodex	B0374	http://www.chemodex.com/products/B0374
Chemspace	CSSB00020668000	https://chem-space.com/CSSB00020668000
Clearsynth	CS-EK-01749	https://www.clearsynth.com/en/CSEK01749.html
DC Chemicals	DC23147	http://www.dcchemicals.com/product_show-DC23147.html
Debye Scientific	DB-118419	http://www.debyesci.com/cas_1197953-54-0.html
Excenen	EX-A775	http://www.excenen.com/searchresultlist.php?id=1197953-54-0
Finetech	FT-0700112	http://www.finetechnology-ind.com/prod/detail/pub/1197953-54-0.html
MedChem Express	HY-12857	https://www.medchemexpress.com/Brigatinib.html
MolPort	MolPort-044-561-640	https://www.molport.com/shop/molecule-link/MolPort-044-561-640
Molcore	MC459486	https://www.molcore.com/product/1197953-54-0
Smolecule	S522029	http://www.smolecule.com/products/s522029
Synblock Inc	SB40412	http://www.synblock.com/product/1197953-54-0.html
THE BioTek	bt-261484	https://www.thebiotek.com/product/inhibitors/bt-261484
abcr GmbH	AB479723	http://www.abcr.com/shop/en/AB479723
eNovation Chemicals	D570938	https://www.enovationchem.com/ProductDetails.asp?ProductID=D570938
eNovation Chemicals	Y0975935	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0975935
eNovation Chemicals	Y1040649	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y1040649

PubMed

Title	Date	PubMed
Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice.	2016 May 17	27049722

Patents

Sample Use Guides

In Vivo Use Guide

90 mg tablet, taken orally once daily,continuously in a 28-day cycle

Route of Administration: Oral

In Vitro Use Guide

Brigatinib inhibited ALK phosphorylation in a dose-dependent manner, and at 50 nM brigatinib, phosphorylation of ALK was abolished in ALK addicted neuroblastoma lines

Substance Class	Chemical Created by `admin` on `Sat Dec 16 09:25:20 GMT 2023` Edited by `admin` on `Sat Dec 16 09:25:20 GMT 2023`
Record UNII	HYW8DB273J
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BRIGATINIB

Official Name

English

BRIGATINIB [ORANGE BOOK]

Common Name

English

AP26113

Code

English

5-CHLORO-N4-(2-(DIMETHYLPHOSPHORYL)PHENYL)-N2-(2-METHOXY-4-(4-(4-METHYLPIPERAZIN-1- YL)PIPERIDIN-1-YL)PHENYL)PYRIMIDINE-2,4-DIAMINE

Systematic Name

English

BRIGATINIB [USAN]

Common Name

English

Brigatinib [WHO-DD]

Common Name

English

(2-((5-CHLORO-2-((2-METHOXY-4-(4-(4-METHYLPIPERAZIN-1-YL)PIPERIDIN-1-YL)PHENYL)AMINO)PYRIMIDIN-4-YL)AMINO)PHENYL)DIMETHYL-,.DELTA.5-PHOSPHANONE

Systematic Name

English

2,4-PYRIMIDINEDIAMINE, 5-CHLORO-N4-(2-(DIMETHYLPHOSPHINYL)PHENYL)-N2-(2-METHOXY-4-(4-(4-METHYL-1-PIPERAZINYL)-1-PIPERIDINYL)PHENYL)-

Systematic Name

English

ALUNBRIG

Brand Name

English

AP-26113

Code

English

BRIGATINIB [MI]

Common Name

English

brigatinib [INN]

Common Name

English

BRIGATINIB [JAN]

Common Name

English

Classification Tree Code System Code

WHO-ATC

L01XE43