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brigatinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tyrosine kinase inhibitors | 5233 | 1197953-54-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.18 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| 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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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:
| Source | Code | Description |
|---|---|---|
| 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
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |