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Details

Stereochemistry ACHIRAL
Molecular Formula C26H29Cl2N5O3
Molecular Weight 530.447
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BOSUTINIB

SMILES

CN1CCN(CCCOc2cc3c(cc2OC)c(=Nc4cc(c(cc4Cl)Cl)OC)c(C#N)c[nH]3)CC1

InChI

InChIKey=UBPYILGKFZZVDX-UHFFFAOYSA-N
InChI=1S/C26H29Cl2N5O3/c1-32-6-8-33(9-7-32)5-4-10-36-25-13-21-18(11-24(25)35-3)26(17(15-29)16-30-21)31-22-14-23(34-2)20(28)12-19(22)27/h11-14,16H,4-10H2,1-3H3,(H,30,31)

HIDE SMILES / InChI

Molecular Formula C26H29Cl2N5O3
Molecular Weight 530.447
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: http://www.drugdevelopment-technology.com/projects/bosutinib-leukaemia/; http://www.pharmacodia.com/yaodu/html/v1/chemicals/d6bcb486f72ae7b5dc68b5b7df7ec887.html

Bosutinib (trade name Bosulif) originally synthesized by Wyeth, it is being developed by Pfizer. Bosutinib received US FDA and EU European Medicines Agency approval on September 4, 2012 and 27 March 2013 respectively for the treatment of adult patients with Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) with resistance, or intolerance to prior therapy. Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl and Src kinases with potential antineoplastic activity. Unlike imatinib, bosutinib inhibits the autophosphorylation of both Abl and Src kinases, resulting in inhibition of cell growth and apoptosis. Because of the dual mechanism of action, this agent may have activity in resistant CML disease, other myeloid malignancies and solid tumors. Abl kinase is upregulated in the presence of the abnormal Bcr-abl fusion protein which is commonly associated with chronic myeloid leukemia (CML). Overexpression of specific Src kinases is also associated with the imatinib-resistant CML phenotype.

CNS Activity

Curator's Comment:: Bosutinib penetrates the brain, inhibits Abl activity and induces autophagic clearance of α-Synuclein and p-Tau in A53T mice and lentiviral gene transfer models. In another study it was shown that although bosutinib does show wide tissue distribution it but does not cross the blood brain barrier (http://www.hc-sc.gc.ca/dhp-mps/prodpharma/sbd-smd/drug-med/sbd_smd_2014_bosulif_152211-eng.php)

Originator

Curator's Comment:: The drug was originally developed by Wyeth Pharmaceuticals, which was taken over by Pfizer in October 2009.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P12931
Gene ID: 6714
Gene Symbol: SRC
Target Organism: Homo sapiens (Human)
1.19999999999999996 nM [IC50]
Target ID: P00519
Gene ID: 25
Gene Symbol: ABL1
Target Organism: Homo sapiens (Human)
1 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
BOSULIF

Approved Use

Indicated for the treatment of adult patients with chronic, accelerated, or blast phase Ph+ chronic myelogenous leukemia (CML) with resistance or intolerance to prior therapy.

Launch Date

1333929600000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
62.1 ng/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
88 ng/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
200 ng/mL
500 mg 1 times / day multiple, oral
dose: 500 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
125 ng/mL
500 mg single, oral
dose: 500 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
182.425 ng/mL
600 mg 1 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
200 ng/mL
500 mg 1 times / day steady-state, oral
dose: 500 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
216 ng/mL
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: HIGH-FAT
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1150 ng × h/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
1768 ng × h/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
3650 ng × h/mL
500 mg 1 times / day multiple, oral
dose: 500 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
2950 ng × h/mL
500 mg single, oral
dose: 500 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
3160 ng × h/mL
600 mg 1 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3650 ng × h/mL
500 mg 1 times / day steady-state, oral
dose: 500 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
4000 ng × h/mL
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: HIGH-FAT
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
39.1 h
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
32.4 h
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
21.9 h
500 mg single, oral
dose: 500 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
21.4 h
600 mg 1 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
22.5 h
500 mg 1 times / day steady-state, oral
dose: 500 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
33.8 h
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: HIGH-FAT
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
4%
500 mg 1 times / day multiple, oral
dose: 500 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
4%
500 mg 1 times / day steady-state, oral
dose: 500 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BOSUTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
Doses

Doses

DosePopulationAdverse events​
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy, 18-91 years
Health Status: unhealthy
Age Group: 18-91 years
Sex: M+F
Sources:
Disc. AE: Thrombocytopenia, Elevated liver enzymes...
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (29 patients)
Elevated liver enzymes (17 patients)
Neutropenia (11 patient)
Sources:
800 mg single, oral
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy, adult
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy
AEs

AEs

AESignificanceDosePopulation
Neutropenia 11 patient
Disc. AE
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy, 18-91 years
Health Status: unhealthy
Age Group: 18-91 years
Sex: M+F
Sources:
Elevated liver enzymes 17 patients
Disc. AE
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy, 18-91 years
Health Status: unhealthy
Age Group: 18-91 years
Sex: M+F
Sources:
Thrombocytopenia 29 patients
Disc. AE
500 mg 1 times / day steady, oral
Recommended
Dose: 500 mg, 1 times / day
Route: oral
Route: steady
Dose: 500 mg, 1 times / day
Sources:
unhealthy, 18-91 years
Health Status: unhealthy
Age Group: 18-91 years
Sex: M+F
Sources:
OverviewDrug as perpetrator​Drug as victimTox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.
2001 Nov 8
SKI-606, a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiproliferative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice.
2003 Jan 15
[Research on the antimetastatic agents].
2005 Sep
In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells.
2006 Dec 1
SKI-606 decreases growth and motility of colorectal cancer cells by preventing pp60(c-Src)-dependent tyrosine phosphorylation of beta-catenin and its nuclear signaling.
2006 Feb 15
Kinase inhibitors in chronic myelogenous leukemia.
2006 May
A Src/Abl kinase inhibitor, SKI-606, blocks breast cancer invasion, growth, and metastasis in vitro and in vivo.
2007 Feb 15
New targeted therapies for chronic myelogenous leukemia: opportunities to overcome imatinib resistance.
2007 Jan
SRC-family kinases are activated in non-small cell lung cancer and promote the survival of epidermal growth factor receptor-dependent cell lines.
2007 Jan
[Novel anti-CML agents beyond imatinib].
2007 Jun
NS-187 (INNO-406), a Bcr-Abl/Lyn dual tyrosine kinase inhibitor.
2007 Nov 14
Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors.
2007 Sep
Management of patients with resistant or refractory chronic myelogenous leukemia.
2008 Apr 15
Facile preparation of new 4-phenylamino-3-quinolinecarbonitrile Src kinase inhibitors via 7-fluoro intermediates: identification of potent 7-amino analogs.
2008 Jan 1
Beyond dose escalation: clinical options for relapse or resistance in chronic myelogenous leukemia.
2008 Mar
AXL is a potential target for therapeutic intervention in breast cancer progression.
2008 Mar 15
SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells.
2008 May
Characterization of compound 584, an Abl kinase inhibitor with lasting effects.
2008 May
Abl tyrosine kinase inhibitors for overriding Bcr-Abl/T315I: from the second to third generation.
2008 Sep
Dasatinib in the treatment of imatinib refractory chronic myeloid leukemia.
2009
Second-generation tyrosine kinase inhibitors in the post-transplant period in patients with chronic myeloid leukemia or Philadelphia-positive acute lymphoblastic leukemia.
2009
Neuroprotective profile of novel SRC kinase inhibitors in rodent models of cerebral ischemia.
2009 Dec
Targeted treatment of imatinib-resistant chronic myeloid leukemia: Focus on dasatinib.
2009 Feb 18
[Development of novel tyrosine kinase inhibitors for treatment of imatinib-resistant CML patients].
2009 Jul
Tyrosine kinase inhibitor-induced platelet dysfunction in patients with chronic myeloid leukemia.
2009 Jul 9
Src activation in melanoma and Src inhibitors as therapeutic agents in melanoma.
2009 Jun
Impact of tyrosine kinase inhibitors on patient outcomes in Philadelphia chromosome-positive acute lymphoblastic leukaemia.
2009 Jun
Acid elution and one-dimensional shotgun analysis on an Orbitrap mass spectrometer: an application to drug affinity chromatography.
2009 Oct
Imatinib and beyond--exploring the full potential of targeted therapy for CML.
2009 Sep
Efficacy of dasatinib for the treatment of intractable chronic myeloid leukemia.
2010
Locking Src/Abl Tyrosine Kinase Activities Regulate Cell Differentiation and Invasion of Human Cervical Cancer Cells Expressing E6/E7 Oncoproteins of High-Risk HPV.
2010
Tyrosine kinase inhibitors: the first decade.
2010 Apr
Lung adenocarcinoma cells floating in lymphatic vessels resist anoikis by expressing phosphorylated Src.
2010 Apr
Novel dual Src/Abl inhibitors for hematologic and solid malignancies.
2010 Aug
Optimizing combination therapies with existing and future CML drugs.
2010 Aug 23
A comprehensive target selectivity survey of the BCR-ABL kinase inhibitor INNO-406 by kinase profiling and chemical proteomics in chronic myeloid leukemia cells.
2010 Jan
MASPECTRAS 2: An integration and analysis platform for proteomic data.
2010 Jul
Bosutinib: a review of preclinical studies in chronic myelogenous leukaemia.
2010 Jul
Synergistic activity of the Src/Abl inhibitor bosutinib in combination with imatinib.
2010 Jun
New developments in tyrosine kinase inhibitor therapy for newly diagnosed chronic myeloid leukemia.
2010 Mar 15
SKI-606 (Bosutinib) blocks prostate cancer invasion, growth, and metastasis in vitro and in vivo through regulation of genes involved in cancer growth and skeletal metastasis.
2010 May
Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.
2010 May 1
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
2010 Nov 24
First-line treatment for chronic myeloid leukemia: dasatinib, nilotinib, or imatinib.
2010 Nov 26
Molecular characterization of c-Abl/c-Src kinase inhibitors targeted against murine tumour progenitor cells that express stem cell markers.
2010 Nov 30
Comprehensive analysis of kinase inhibitor selectivity.
2011 Oct 30
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.
2011 Oct 30
LRIG1 modulates cancer cell sensitivity to Smac mimetics by regulating TNFα expression and receptor tyrosine kinase signaling.
2012 Mar 1
Novel aspects of therapy with the dual Src and Abl kinase inhibitor bosutinib in chronic myeloid leukemia.
2012 Sep
Development and validation of a high-throughput intrinsic ATPase activity assay for the discovery of MEKK2 inhibitors.
2013 Apr
Patents

Sample Use Guides

Recommended Dose: 500 mg orally once daily with food. Consider dose escalation to 600 mg daily in patients who do not reach complete hematologic response by week 8 or complete cytogenetic response by week 12 and do not have Grade 3 or greater adverse reactions.
Route of Administration: Oral
Bosutinib potently inhibits Src-dependent cell proliferation with an IC50 of 100 nM.
Substance Class Chemical
Created
by admin
on Sat Jun 26 02:39:32 UTC 2021
Edited
by admin
on Sat Jun 26 02:39:32 UTC 2021
Record UNII
5018V4AEZ0
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BOSUTINIB
DASH   INN   MART.   MI   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
BOSUTINIB [USAN]
Common Name English
BOSULIF
Common Name English
BOSUTINIB [MI]
Common Name English
SK-606
Code English
BOSUTINIB [MART.]
Common Name English
BOSUTINIB [WHO-DD]
Common Name English
3-QUINOLINECARBONITRILE, 4-((2,4-DICHLORO-5-METHOXYPHENYL)AMINO)-6-METHYL-1-PIPERAZINYL)PROPOXY)-
Common Name English
4-((2,4-DICHLORO-5-METHOXYPHENYL)AMINO)-6-METHOXY-7-(3-(4-METHYLPIPERAZIN-1-YL)PROPOXY)QUINOLINE-3-CARBONITRILE
Systematic Name English
BOSUTINIB [VANDF]
Common Name English
SKI-606
Code English
BOSUTINIB [INN]
Common Name English
Classification Tree Code System Code
WHO-ATC L01XE14
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
FDA ORPHAN DRUG 274808
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
EU-Orphan Drug EU/3/10/762
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
NDF-RT N0000175605
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
LIVERTOX 120
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
WHO-VATC QL01XE14
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
NCI_THESAURUS C155700
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
Code System Code Type Description
NDF-RT
N0000185503
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY P-Glycoprotein Inhibitors [MoA]
MESH
C471992
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
IUPHAR
5710
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
ChEMBL
CHEMBL288441
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
MERCK INDEX
M2627
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY Merck Index
DRUG BANK
DB06616
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
LACTMED
Bosutinib
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
EVMPD
SUB29176
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
FDA UNII
5018V4AEZ0
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
RXCUI
1307619
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY RxNorm
INN
8715
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
PUBCHEM
5328940
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
WIKIPEDIA
BOSUTINIB
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
NCI_THESAURUS
C60809
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
DRUG CENTRAL
4359
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
CAS
380843-75-4
Created by admin on Sat Jun 26 02:39:32 UTC 2021 , Edited by admin on Sat Jun 26 02:39:32 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
EXCRETED UNCHANGED->SUBSTANCE
IN-VIVO
FECAL
OFF-TARGET->INHIBITOR
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TARGET -> INHIBITOR
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TRANSPORTER -> SUBSTRATE
a high-fat meal increased bosutinib AUC 1.7-fold and Cmax 1.8-fold compared with bosutinib administration under fasting conditions
MAJOR
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
IC50
TARGET -> INHIBITOR
TARGET -> INHIBITOR
INHIBITOR
TARGET -> INHIBITOR
TARGET -> INHIBITOR
EXCRETED UNCHANGED->SUBSTANCE
IN-VIVO
URINE
Related Record Type Details
PARENT -> METABOLITE INACTIVE
MAJOR
FECAL; PLASMA; URINE
PARENT -> METABOLITE INACTIVE
MAJOR
FECAL; PLASMA
METABOLITE INACTIVE -> PARENT
MINOR
PLASMA
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Cmax PHARMACOKINETIC TMAX
PHARMACOKINETIC
DOSE
PHARMACOKINETIC
ROUTE OF ADMINISTRATION
PHARMACOKINETIC