brigatinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5233 1197953-54-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • brigatinib
  • alunbrig
  • AP26113
Brigatinib is a tyrosine kinase inhibitor 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. Brigatinib also inhibited the in vitro proliferation of cell lines expressing EML4-ALK and NPM-ALK fusion proteins and demonstrated dose-dependent inhibition of EML4-ALK-positive NSCLC xenograft growth in mice. At clinically achievable concentrations (<= 500 nM), brigatinib inhibited the in vitro viability of cells expressing EML4-ALK and 17 mutant forms associated with resistance to ALK inhibitors including crizotinib, as well as EGFR-Del (E746-A750), ROS1-L2026M, FLT3-F691L, and FLT3-D835Y. Brigatinib exhibited in vivo anti-tumor activity against 4 mutant forms of EML4-ALK, including G1202R and L1196M mutants identified in NSCLC tumors in patients who have progressed on crizotinib. Brigatinib also reduced tumor burden and prolonged survival in mice implanted intracranially with an ALK-driven tumor cell line.
  • Molecular weight: 584.10
  • Formula: C29H39ClN7O2P
  • CLOGP: 2.08
  • LIPINSKI: 1
  • HAC: 9
  • HDO: 2
  • TPSA: 85.86
  • ALOGS: -4.42
  • ROTB: 8
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.18 g O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.15 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.804 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 31.261 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 5.272 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 2.786 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 39.070 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 52.010 % High 1
herg hERG pIC50 4.576 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.021 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 5.260 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 31.220 % High 1
kinase-safety-class AAK1,ABL1,ABL2,ACVR2A,ACVR2B,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK1,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK2,CDK3,CDK4,CDK5,CDK7,CDK9,CHEK1,CHEK2,CLK1,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1A,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,HASPIN,IGF1R,INSR,INSRR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK3,MAPK7,MAPK9,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,MST1R,MYLK,NTRK1,NTRK2,NUAK1,PAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIM1,PIM3,PLK1,PLK2,PLK3,PLK4,PRKAA1,PRKAA2,PRKACA,PRKCD,PRKCI,PRKCQ,PRKCZ,PRKDC,PTK2,PTK6,RET,RIPK3,ROCK1,ROCK2,RPS6KA1,SIK2,SIK3,SRC,SRPK1,STK10,STK16,STK17A,STK3,STK33,STK4,SYK,TBK1,TEK,TNIK,TNK1,TTK,ULK1,ULK2,YES1,ZAP70 155
kinase-selectivity-class AAK1,ABL2,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BTK,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK4,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1A,DYRK1B,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK2,IGF1R,INSR,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K3,MAP4K5,MAPK7,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,MST1R,MYLK,NTRK1,NUAK1,PAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK4,PIM3,PLK1,PLK2,PLK3,PLK4,PRKAA1,PRKAA2,PRKCD,PRKCI,PRKCZ,PTK2,RET,RIPK3,SIK2,SIK3,SRC,STK10,STK33,STK4,SYK,TNIK,TNK1,TTK,ULK1,ULK2,YES1 112
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 60.954 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 27.990 High 1
mh-clint Mouse hepatocyte intrinsic clearance 7.047 High 1
mppb Mouse plasma protein binding (% unbound) 27.680 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 36.813 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 50 % High 1
rat-kpuu-brain Rat brain Kpuu 0.016 % High 1
rh-clint Rat hepatocyte intrinsic clearance 2.692 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 51.610 % High 1
rppb Rat plasma protein binding (% unbound) 27.270 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 928.966 uM High 1

Approvals:

DateAgencyCompanyOrphan
Jan. 22, 2021 PMDA TAKEDA PHARMACEUTICAL COMPANY LIMITED
Sept. 22, 2018 EMA TAKEDA PHARMA A/S
April 28, 2017 FDA ARIAD

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Blood creatine phosphokinase increased 303.59 30.36 88 2726 33935 90591698
Metastases to central nervous system 271.33 30.36 70 2744 17472 90608161
Neoplasm progression 183.58 30.36 64 2750 44422 90581211
Amylase increased 88.98 30.36 24 2790 7048 90618585
Pulmonary toxicity 77.38 30.36 24 2790 11507 90614126
Lipase increased 74.03 30.36 23 2791 11088 90614545
Death 66.48 30.36 76 2738 456475 90169158
Pneumonitis 64.08 30.36 30 2784 44140 90581493
Product dose omission issue 48.27 30.36 52 2762 291635 90333998
Drug resistance 48.26 30.36 22 2792 30427 90595206
Disease progression 35.20 30.36 33 2781 156582 90469051
Aspartate aminotransferase increased 33.91 30.36 27 2787 102910 90522723
Anaplastic lymphoma kinase gene mutation 31.98 30.36 4 2810 12 90625621
Photosensitivity reaction 31.83 30.36 14 2800 17793 90607840

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Blood creatine phosphokinase increased 239.60 31.75 87 1796 48251 42571201
Metastases to central nervous system 200.07 31.75 53 1830 10302 42609150
Neoplasm progression 99.33 31.75 40 1843 28960 42590492
Metastases to liver 79.06 31.75 29 1854 16297 42603155
Amylase increased 64.58 31.75 20 1863 6709 42612743
Pulmonary toxicity 55.69 31.75 19 1864 8636 42610816
Disease progression 53.89 31.75 47 1836 143609 42475843
Death 46.74 31.75 78 1805 471107 42148345
Pericardial effusion 33.43 31.75 19 1864 29256 42590196

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Blood creatine phosphokinase increased 493.32 29.57 159 3964 72918 110512258
Metastases to central nervous system 397.99 29.57 104 4019 22713 110562463
Neoplasm progression 168.84 29.57 70 4053 64525 110520651
Amylase increased 161.30 29.57 45 4078 12474 110572702
Pulmonary toxicity 137.37 29.57 43 4080 17703 110567473
Metastases to liver 108.35 29.57 43 4080 35343 110549833
Lipase increased 87.49 29.57 31 4092 18641 110566535
Disease progression 80.33 29.57 69 4054 243965 110341211
Death 76.82 29.57 111 4012 698758 109886418
Pneumonitis 55.72 29.57 35 4088 76496 110508680
Pleural effusion 49.95 29.57 46 4077 177663 110407513
Hepatic function abnormal 46.13 29.57 33 4090 89262 110495914
Product dose omission issue 44.07 29.57 57 4066 321725 110263451
Aspartate aminotransferase increased 40.34 29.57 39 4084 159897 110425279
Diarrhoea 39.65 29.57 112 4011 1139393 109445783
Drug resistance 39.07 29.57 25 4098 56349 110528827
Photosensitivity reaction 38.83 29.57 19 4104 25570 110559606
Pericardial effusion 38.73 29.57 25 4098 57192 110527984
Metastases to adrenals 36.20 29.57 9 4114 1594 110583582
Interstitial lung disease 35.17 29.57 34 4089 139300 110445876
Non-small cell lung cancer 32.75 29.57 12 4111 7923 110577253
Decreased appetite 32.31 29.57 61 4062 475785 110109391

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01ED04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Anaplastic lymphoma kinase (ALK) inhibitors
FDA MoA N0000020001 Tyrosine Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000190118 Cytochrome P450 3A Inducers
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:38637 tyrosine kinase inhibitor

Related Drugs by ATC class:

L01ED Anaplastic lymphoma kinase (ALK) inhibitors 4 drugs
alectinibceritinibcrizotiniblorlatinib

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Non-small cell lung cancer indication 254637007 DOID:3908
Advanced/recurrent anaplasticlymphoma kinase (ALK)-positive non-small cell lung cancer indication 830151004




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.76 Basic
pKa2 5.51 Basic
pKa3 4.76 Basic
pKa4 2.49 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
180MG ALUNBRIG TAKEDA PHARMS USA N208772 Oct. 2, 2017 RX TABLET ORAL 9273077 May 21, 2029 TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)
30MG ALUNBRIG TAKEDA PHARMS USA N208772 April 28, 2017 RX TABLET ORAL 9273077 May 21, 2029 TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)
90MG ALUNBRIG TAKEDA PHARMS USA N208772 April 28, 2017 RX TABLET ORAL 9273077 May 21, 2029 TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)
180MG ALUNBRIG TAKEDA PHARMS USA N208772 Oct. 2, 2017 RX TABLET ORAL 9611283 April 10, 2034 TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)
30MG ALUNBRIG TAKEDA PHARMS USA N208772 April 28, 2017 RX TABLET ORAL 9611283 April 10, 2034 TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)
90MG ALUNBRIG TAKEDA PHARMS USA N208772 April 28, 2017 RX TABLET ORAL 9611283 April 10, 2034 TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)
180MG ALUNBRIG TAKEDA PHARMS USA N208772 Oct. 2, 2017 RX TABLET ORAL 10385078 Nov. 10, 2035 TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)
30MG ALUNBRIG TAKEDA PHARMS USA N208772 April 28, 2017 RX TABLET ORAL 10385078 Nov. 10, 2035 TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)
90MG ALUNBRIG TAKEDA PHARMS USA N208772 April 28, 2017 RX TABLET ORAL 10385078 Nov. 10, 2035 TREATMENT OF ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
180MG ALUNBRIG TAKEDA PHARMS USA N208772 Oct. 2, 2017 RX TABLET ORAL May 22, 2027 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, NOT INCLUDING PATIENTS WHO HAVE PROGRESSED ON OR ARE INTOLERANT TO CRIZOTINIB
30MG ALUNBRIG TAKEDA PHARMS USA N208772 April 28, 2017 RX TABLET ORAL May 22, 2027 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, NOT INCLUDING PATIENTS WHO HAVE PROGRESSED ON OR ARE INTOLERANT TO CRIZOTINIB
90MG ALUNBRIG TAKEDA PHARMS USA N208772 April 28, 2017 RX TABLET ORAL May 22, 2027 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, NOT INCLUDING PATIENTS WHO HAVE PROGRESSED ON OR ARE INTOLERANT TO CRIZOTINIB

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
ALK tyrosine kinase receptor Kinase INHIBITOR IC50 9.22 SCIENTIFIC LITERATURE DRUG LABEL
Mast/stem cell growth factor receptor Kit Kinase IC50 7.08 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase IC50 6.80 CHEMBL
Tyrosine-protein kinase Lck Kinase IC50 6.29 CHEMBL
Tyrosine-protein kinase Yes Kinase IC50 7.72 CHEMBL
Tyrosine-protein kinase Fyn Kinase IC50 6.70 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase IC50 7.66 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase IC50 6.09 CHEMBL
Vascular endothelial growth factor receptor 3 Kinase IC50 7.24 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase IC50 6.45 CHEMBL
Receptor tyrosine-protein kinase erbB-2 Kinase IC50 7.38 CHEMBL
Ribosomal protein S6 kinase alpha-3 Kinase IC50 7.58 CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform Kinase IC50 6.97 CHEMBL
Fibroblast growth factor receptor 3 Kinase IC50 6.45 CHEMBL
Focal adhesion kinase 1 Kinase IC50 8.41 CHEMBL
Tyrosine-protein kinase HCK Kinase IC50 6.70 CHEMBL
Serine/threonine-protein kinase PLK1 Kinase IC50 6.21 CHEMBL
Receptor tyrosine-protein kinase erbB-4 Kinase IC50 7.57 CHEMBL
Tyrosine-protein kinase JAK2 Kinase IC50 6.81 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase IC50 7.54 CHEMBL
Tyrosine-protein kinase CSK Kinase IC50 6.48 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma Kinase IC50 7.32 CHEMBL
Serine/threonine-protein kinase MARK2 Kinase IC50 7.03 CHEMBL
Hepatocyte growth factor receptor Kinase IC50 7.16 CHEMBL
Tyrosine-protein kinase Lyn Kinase IC50 6.62 CHEMBL
Ribosomal protein S6 kinase alpha-2 Kinase IC50 7.89 CHEMBL
Fibroblast growth factor receptor 1 Kinase IC50 7.39 CHEMBL
Serine/threonine-protein kinase 10 Kinase IC50 6.91 CHEMBL
Tyrosine-protein kinase Fer Kinase IC50 8.89 CHEMBL
Fibroblast growth factor receptor 2 Kinase IC50 6.69 CHEMBL
Tyrosine-protein kinase Fgr Kinase IC50 6.31 CHEMBL
Aurora kinase A Kinase IC50 6.84 CHEMBL
Tyrosine-protein kinase FRK Kinase IC50 7.28 CHEMBL
Dual specificity protein kinase CLK1 Kinase IC50 7.64 CHEMBL
Dual specificity protein kinase CLK2 Kinase IC50 6.62 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase IC50 7.09 CHEMBL
Insulin receptor Kinase INHIBITOR IC50 6.80 SCIENTIFIC LITERATURE
MAP/microtubule affinity-regulating kinase 3 Kinase IC50 6.90 CHEMBL
Testis-specific serine/threonine-protein kinase 1 Kinase IC50 8.36 CHEMBL
Protein-tyrosine kinase 6 Kinase IC50 8.39 CHEMBL
Tyrosine-protein kinase BTK Kinase IC50 6.17 CHEMBL
Serine/threonine-protein kinase D1 Kinase IC50 6.71 CHEMBL
Ribosomal protein S6 kinase alpha-6 Kinase IC50 7.38 CHEMBL
Serine/threonine-protein kinase Chk1 Kinase IC50 7.52 CHEMBL
Protein-tyrosine kinase 2-beta Kinase IC50 7.62 CHEMBL
Maternal embryonic leucine zipper kinase Kinase IC50 6.05 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 1 Kinase IC50 7.06 CHEMBL
Insulin receptor-related protein Kinase IC50 7.35 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase IC50 6.33 CHEMBL
Leukocyte tyrosine kinase receptor Kinase IC50 7.85 CHEMBL
NUAK family SNF1-like kinase 1 Kinase IC50 7.33 CHEMBL
Tyrosine-protein kinase Blk Kinase IC50 6.87 CHEMBL
Serine/threonine-protein kinase BRSK1 Kinase IC50 6.47 CHEMBL
Serine/threonine-protein kinase MARK1 Kinase IC50 6.90 CHEMBL
Mitogen-activated protein kinase kinase kinase 9 Kinase IC50 6.66 CHEMBL
Serine/threonine-protein kinase BRSK2 Kinase IC50 6.90 CHEMBL
Serine/threonine-protein kinase D2 Kinase IC50 6.54 CHEMBL
Serine/threonine-protein kinase D3 Kinase IC50 7.02 CHEMBL
Tyrosine-protein kinase Fes/Fps Kinase IC50 8.46 CHEMBL
Fibroblast growth factor receptor 4 Kinase IC50 6.74 CHEMBL
Tyrosine-protein kinase ABL1 Kinase IC50 6.77 CHEMBL
Serine/threonine-protein kinase Chk2 Kinase IC50 8.25 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase IC50 6.31 CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2 Kinase IC50 7.29 CHEMBL
Epidermal growth factor receptor Kinase INHIBITOR IC50 7.17 SCIENTIFIC LITERATURE
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR IC50 8.68 SCIENTIFIC LITERATURE
Insulin-like growth factor 1 receptor Kinase INHIBITOR IC50 7.14 SCIENTIFIC LITERATURE
Proto-oncogene tyrosine-protein kinase ROS Kinase INHIBITOR IC50 8.72 SCIENTIFIC LITERATURE
Ribosomal protein S6 kinase alpha-1 Kinase IC50 7.52 CHEMBL

External reference:

IDSource
HYW8DB273J UNII
4036651 VANDF
C4287815 UMLSCUI
6GY PDB_CHEM_ID
CHEMBL3545311 ChEMBL_ID
68165256 PUBCHEM_CID
DB12267 DRUGBANK_ID
D10866 KEGG_DRUG
10085 INN_ID
C000598580 MESH_SUPPLEMENTAL_RECORD_UI
7741 IUPHAR_LIGAND_ID
736634002 SNOMEDCT_US
763704002 SNOMEDCT_US
CHEBI:232810 CHEBI
256904 MMSL
32700 MMSL
d08581 MMSL
017195 NDDF
1921217 RXNORM
HYW8DB273J INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Alunbrig HUMAN PRESCRIPTION DRUG LABEL 1 63020-090 TABLET, FILM COATED 90 mg ORAL NDA 30 sections
Alunbrig HUMAN PRESCRIPTION DRUG LABEL 1 63020-113 TABLET, FILM COATED 30 mg ORAL NDA 30 sections
Alunbrig HUMAN PRESCRIPTION DRUG LABEL 1 63020-180 TABLET, FILM COATED 180 mg ORAL NDA 30 sections