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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5345 1108743-60-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • entrectinib
  • RXDX-101
  • NMS-E628
  • RG 6268
  • rozlytrek
Entrectinib is an inhibitor of the tropomyosin receptor tyrosine kinases (TRK) TRKA, TRKB, and TRKC (encoded by the neurotrophic tyrosine receptor kinase [NTRK] genes NTRK1, NTRK2, and NTRK3, respectively), proto-oncogene tyrosine-protein kinase ROS1 (ROS1), and anaplastic lymphoma kinase (ALK).
  • Molecular weight: 560.65
  • Formula: C31H34F2N6O2
  • CLOGP: 5.16
  • LIPINSKI: 2
  • HAC: 8
  • HDO: 3
  • TPSA: 85.52
  • ALOGS: -4.80
  • ROTB: 7
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.60 g O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.00 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 4.359 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 16.144 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 1.545 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 17.338 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 0.560 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 2.300 % High 1
herg hERG pIC50 5.354 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 5.702 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 49.091 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 0.490 % High 1
kinase-safety-class AAK1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GSK3A,GSK3B,HASPIN,IGF1R,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK7,MAPK9,MARK1,MARK4,MELK,MET,MINK1,MST1R,NTRK1,NTRK2,NTRK3,NUAK1,PAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CD,PIK3CG,PIM2,PIM3,PLK4,PRKAA1,PRKAA2,PRKCD,PRKDC,RET,RIPK3,ROCK1,ROCK2,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK33,STK4,SYK,TEK,TGFBR1,TNIK,TNK1,TTK,TYRO3,ULK1,ULK2,YES1 137
kinase-selectivity-class ABL2,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,CAMK2A,CAMK2B,CAMK2D,CDK16,CDK4,CLK4,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,ERBB2,FGFR1,FLT3,FYN,GAK,INSR,IRAK1,IRAK3,IRAK4,JAK1,JAK2,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK7,MARK4,MET,MINK1,NTRK1,NTRK3,NUAK1,PAK4,PDK1,PDK4,PRKCD,RET,SIK2,SIK3,SRC,STK33,SYK,TEK,TNIK,TNK1,TTK,ULK1,ULK2,YES1 68
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 12.853 High 1
mh-clint Mouse hepatocyte intrinsic clearance 24.266 High 1
mppb Mouse plasma protein binding (% unbound) 0.340 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 28.379 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 1 % High 1
rat-kpuu-brain Rat brain Kpuu 0.026 % High 1
rh-clint Rat hepatocyte intrinsic clearance 16.218 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 1.270 % High 1
rppb Rat plasma protein binding (% unbound) 0.420 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 1.982 uM High 1

Approvals:

DateAgencyCompanyOrphan
Aug. 15, 2019 FDA GENENTECH INC
June 18, 2019 PMDA Chugai Pharmaceutical

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
Disease progression 78.90 46.64 37 958 156578 90470874
Ataxia 72.69 46.64 20 975 18022 90609430
Dizziness 63.91 46.64 52 943 589232 90038220
Renal impairment 59.54 46.64 27 968 105394 90522058
Taste disorder 52.05 46.64 21 974 61525 90565927
Cardiac failure 49.32 46.64 24 971 109472 90517980

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
Taste disorder 78.07 43.80 21 780 10186 42610348
Disease progression 71.41 43.80 40 761 143616 42476918
Metastases to central nervous system 54.90 43.80 16 785 10339 42610195
Blood creatinine increased 47.46 43.80 28 773 109975 42510559

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
Disease progression 135.13 44.24 67 1530 243967 110343735
Taste disorder 111.28 44.24 40 1557 65347 110522355
Metastases to central nervous system 92.52 44.24 27 1570 22790 110564912
Blood creatinine increased 91.58 44.24 47 1550 182842 110404860
Renal impairment 81.72 44.24 44 1553 188401 110399301
Ataxia 68.87 44.24 23 1574 30085 110557617
Dizziness 63.41 44.24 63 1534 698130 109889572
Cardiac failure 57.59 44.24 35 1562 187591 110400111
Dysgeusia 53.20 44.24 24 1573 69961 110517741
Cognitive disorder 51.06 44.24 25 1572 87486 110500216
No adverse event 45.80 44.24 22 1575 73817 110513885

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX14 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
CHEBI has role CHEBI:33282 antibacterial agent
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:62434 EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
CHEBI has role CHEBI:68495 apoptosis inducer

Related Drugs by ATC class:

L01EX Other protein kinase inhibitors 21 drugs
avapritinibcabozantinibcapivasertibgilteritiniblarotrectiniblenvatinibmidostaurinnintedanibpazopanibpexidartinibpralsetinibquizartinib show all 21 →

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

DiseaseRelationSNOMED_IDDOID
Reactive oxygen species 1 positive non-small cell lung cancer indication 72242500
Solid neoplasm with neurotrophic receptor tyrosine kinase gene fusion indication 786710002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.61 acidic
pKa2 12.21 acidic
pKa3 8.43 Basic
pKa4 1.79 Basic
pKa5 1.11 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 8673893 July 8, 2028 TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 8673893 July 8, 2028 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 9255087 July 8, 2028 TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 9255087 July 8, 2028 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 9616059 July 8, 2028 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 8673893 July 8, 2028 TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 8673893 July 8, 2028 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 9255087 July 8, 2028 TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 9255087 July 8, 2028 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 9616059 July 8, 2028 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 9649306 May 22, 2033 TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 9649306 May 22, 2033 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 9649306 May 22, 2033 TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 9649306 May 22, 2033 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 10231965 Feb. 17, 2035 TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 10231965 Feb. 17, 2035 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 10231965 Feb. 17, 2035 TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 10231965 Feb. 17, 2035 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 10561651 Feb. 19, 2035 TREATMENT OF NEUROBLASTOMAS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 10561651 Feb. 19, 2035 TREATMENT OF NEUROBLASTOMAS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 10738037 May 18, 2037 TREATMENT OF COLORECTAL CANCER THAT HAS A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 11091469 May 18, 2037 TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 11091469 May 18, 2037 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 10738037 May 18, 2037 TREATMENT OF COLORECTAL CANCER THAT HAS A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 11091469 May 18, 2037 TREATMENT OF ROS1-POSITIVE NON-SMALL CELL LUNG CANCER
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL 11091469 May 18, 2037 TREATMENT OF SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL Aug. 15, 2026 INDICATED FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION WITHOUT A KNOWN ACQUIRED RESISTANCE MUTATION, ARE METASTATIC OR WHERE SURGICAL RESECTION IS LIKELY TO RESULT IN SEVERE MORBIDITY, AND HAVE EITHER PROGRESSED FOLLOWING TREATMENT OR HAVE NO SATISFACTORY ALTERNATIVE THERAPY
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL Aug. 15, 2026 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS ARE ROS1-POSITIVE
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL Aug. 15, 2026 INDICATED FOR THE TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION WITHOUT A KNOWN ACQUIRED RESISTANCE MUTATION, ARE METASTATIC OR WHERE SURGICAL RESECTION IS LIKELY TO RESULT IN SEVERE MORBIDITY, AND HAVE EITHER PROGRESSED FOLLOWING TREATMENT OR HAVE NO SATISFACTORY ALTERNATIVE THERAPY
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL Aug. 15, 2026 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS ARE ROS1-POSITIVE
50MG/PACKET ROZLYTREK GENENTECH INC N218550 Oct. 20, 2023 RX PELLETS ORAL Aug. 15, 2026 FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL Oct. 20, 2026 NEW PATIENT POPULATION
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL Oct. 20, 2026 NEW PATIENT POPULATION
50MG/PACKET ROZLYTREK GENENTECH INC N218550 Oct. 20, 2023 RX PELLETS ORAL Oct. 20, 2026 NEW PRODUCT
100MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL Oct. 20, 2030 TREATMENT OF PEDIATRIC PATIENTS OLDER THAN 1 MONTH UP TO 12 YEARS OF AGE WITH SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST WITHOUT A KNOWN ACQUIRED RESISTANCE MUTATION, ARE METASTATIC OR WHERE SURGICAL RESECTION IS LIKELY TO RESULT IN SEVERE MORBIDITY, AND HAVE PROGRESSED FOLLOWING TREATMENT OR HAVE NO SATISFACTORY ALTERNATIVE THERAPY
200MG ROZLYTREK GENENTECH INC N212725 Aug. 15, 2019 RX CAPSULE ORAL Oct. 20, 2030 TREATMENT OF PEDIATRIC PATIENTS OLDER THAN 1 MONTH UP TO 12 YEARS OF AGE WITH SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST WITHOUT A KNOWN ACQUIRED RESISTANCE MUTATION, ARE METASTATIC OR WHERE SURGICAL RESECTION IS LIKELY TO RESULT IN SEVERE MORBIDITY, AND HAVE PROGRESSED FOLLOWING TREATMENT OR HAVE NO SATISFACTORY ALTERNATIVE THERAPY
50MG/PACKET ROZLYTREK GENENTECH INC N218550 Oct. 20, 2023 RX PELLETS ORAL Oct. 20, 2030 TREATMENT OF PEDIATRIC PATIENTS OLDER THAN 1 MONTH UP TO 12 YEARS OF AGE WITH SOLID TUMORS THAT HAVE A NEUROTROPHIC TYROSINE RECEPTOR KINASE (NTRK) GENE FUSION, AS DETECTED BY AN FDA-APPROVED TEST WITHOUT A KNOWN ACQUIRED RESISTANCE MUTATION, ARE METASTATIC OR WHERE SURGICAL RESECTION IS LIKELY TO RESULT IN SEVERE MORBIDITY, AND HAVE PROGRESSED FOLLOWING TREATMENT OR HAVE NO SATISFACTORY ALTERNATIVE THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
High affinity nerve growth factor receptor Kinase INHIBITOR IC50 9 SCIENTIFIC LITERATURE DRUG LABEL
ALK tyrosine kinase receptor Kinase INHIBITOR IC50 7.92 SCIENTIFIC LITERATURE DRUG LABEL
BDNF/NT-3 growth factors receptor Kinase INHIBITOR IC50 8.52 SCIENTIFIC LITERATURE DRUG LABEL
NT-3 growth factor receptor Kinase INHIBITOR IC50 8.30 SCIENTIFIC LITERATURE DRUG LABEL
Proto-oncogene tyrosine-protein kinase ROS Kinase INHIBITOR IC50 8.15 SCIENTIFIC LITERATURE DRUG LABEL
Insulin-like growth factor 1 receptor Kinase IC50 6.91 CHEMBL
Insulin receptor Kinase IC50 6.68 CHEMBL
Focal adhesion kinase 1 Kinase IC50 6.85 CHEMBL
Tyrosine-protein kinase JAK1 Kinase IC50 6.95 CHEMBL
Aurora kinase A Kinase IC50 6.67 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase IC50 6.78 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 5.83 CHEMBL
Aurora kinase B Kinase IC50 6.47 CHEMBL
Serine/threonine-protein kinase LMTK3 Kinase IC50 5.33 CHEMBL
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 7.40 SCIENTIFIC LITERATURE
Activated CDC42 kinase 1 Kinase INHIBITOR IC50 7.15 SCIENTIFIC LITERATURE
Protein-tyrosine kinase 6 Kinase IC50 6.71 CHEMBL
Serine/threonine-protein kinase receptor R3 Kinase IC50 7.92 CHEMBL
Tyrosine-protein kinase JAK3 Kinase IC50 6.46 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase IC50 6.79 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase IC50 6.41 CHEMBL

External reference:

IDSource
L5ORF0AN1I UNII
4038664 VANDF
C4086264 UMLSCUI
CHEBI:195558 CHEBI
YMX PDB_CHEM_ID
CHEMBL1983268 ChEMBL_ID
25141092 PUBCHEM_CID
DB11986 DRUGBANK_ID
D10926 KEGG_DRUG
10132 INN_ID
C000607349 MESH_SUPPLEMENTAL_RECORD_UI
8290 IUPHAR_LIGAND_ID
789356007 SNOMEDCT_US
789364001 SNOMEDCT_US
322129 MMSL
37312 MMSL
d09348 MMSL
018089 NDDF
2197862 RXNORM
L5ORF0AN1I INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rozlytrek HUMAN PRESCRIPTION DRUG LABEL 1 50242-091 CAPSULE 100 mg ORAL NDA 32 sections
Rozlytrek HUMAN PRESCRIPTION DRUG LABEL 1 50242-094 CAPSULE 200 mg ORAL NDA 32 sections
Rozlytrek HUMAN PRESCRIPTION DRUG LABEL 1 50242-623 PELLET 50 mg ORAL NDA 32 sections