Details
Stereochemistry | ACHIRAL |
Molecular Formula | C26H29Cl2N5O3 |
Molecular Weight | 530.446 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC(NC2=C(C=NC3=CC(OCCCN4CCN(C)CC4)=C(OC)C=C23)C#N)=C(Cl)C=C1Cl
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)
DescriptionCurator's Comment: description was created based on several sources, including
http://www.drugdevelopment-technology.com/projects/bosutinib-leukaemia/; http://www.pharmacodia.com/yaodu/html/v1/chemicals/d6bcb486f72ae7b5dc68b5b7df7ec887.html
Curator's Comment: description was created based on several sources, including
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
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=25635231
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)
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P12931 Gene ID: 6714.0 Gene Symbol: SRC Target Organism: Homo sapiens (Human) |
1.2 nM [IC50] | ||
Target ID: P00519 Gene ID: 25.0 Gene Symbol: ABL1 Target Organism: Homo sapiens (Human) |
1.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | BOSULIF Approved UseIndicated 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 Date2012 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
273 ng/mL |
500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
190 ng/mL |
400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
76.6 ng/mL |
300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
95.4 ng/mL |
200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
19.6 ng/mL |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
6.9 ng/mL |
50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
4.89 ng/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
17 ng/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
43.1 ng/mL |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
63.7 ng/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
117 ng/mL |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
125 ng/mL |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
206 ng/mL |
600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
200 ng/mL |
500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
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 plasma | 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 plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT |
|
125 ng/mL |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
278.12 ng/mL |
600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
62.1 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27113346 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27113346 |
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 |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3580 ng × h/mL |
500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2900 ng × h/mL |
400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1170 ng × h/mL |
300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1670 ng × h/mL |
200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
329 ng × h/mL |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
114 ng × h/mL |
50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
129 ng × h/mL |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
284 ng × h/mL |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
920 ng × h/mL |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1200 ng × h/mL |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2340 ng × h/mL |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2950 ng × h/mL |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
4300 ng × h/mL |
600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
3650 ng × h/mL |
500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED |
|
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 plasma | 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 plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT |
|
2950 ng × h/mL |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
4084.7 ng × h/mL |
600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1150 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27113346 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27113346 |
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 |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
23.3 h |
500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
19.89 h |
400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
19.4 h |
300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
30 h |
200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
64.7 h |
100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
25.8 h |
50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
12.9 h |
50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
18.6 h |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
20.79 h |
200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
17.1 h |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
18.6 h |
400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
21.9 h |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
19.9 h |
600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | 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 plasma | 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 plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT |
|
21.9 h |
500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
|
15.4 h |
600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
39.1 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27113346 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27113346 |
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 |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4% |
500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
BOSUTINIB plasma | 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 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED |
Doses
Dose | Population | Adverse 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) Sources: Elevated liver enzymes (17 patients) Neutropenia (11 patient) |
800 mg single, oral Dose: 800 mg Route: oral Route: single Dose: 800 mg Sources: |
healthy, adult Health Status: healthy Age Group: adult Sources: |
|
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 Health Status: unhealthy Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes [IC50 2 uM] | ||||
yes [Ki 10 uM] | ||||
yes [Ki 27 uM] | ||||
yes [Ki 27 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major | yes (co-administration study) Comment: ketoconazole increased cmax of bosutinib by 5x, auc by 9x |
|||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
New targeted therapies for chronic myelogenous leukemia: opportunities to overcome imatinib resistance. | 2007 Jan |
|
Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors. | 2007 Sep |
|
Targeted drugs in chronic myeloid leukemia. | 2008 |
|
Gateways to clinical trials. | 2008 Apr |
|
Therapeutic options for chronic myeloid leukemia: focus on imatinib (Glivec, Gleevectrade mark). | 2008 Feb |
|
The chemistry of multi-protic drugs Part 1: a potentiometric, multi-wavelength UV and NMR pH titrimetric study of the micro-speciation of SKI-606. | 2008 Jun 9 |
|
AXL is a potential target for therapeutic intervention in breast cancer progression. | 2008 Mar 15 |
|
Targeted treatment of imatinib-resistant chronic myeloid leukemia: Focus on dasatinib. | 2009 Feb 18 |
|
Severe toxicity of skin rash, fever and diarrhea associated with imatinib: case report and review of skin toxicities associated with tyrosine kinase inhibitors. | 2009 Feb 6 |
|
New mechanisms of resistance in Philadelphia chromosome acute lymphoblastic leukemia. | 2009 Jun |
|
Src activation in melanoma and Src inhibitors as therapeutic agents in melanoma. | 2009 Jun |
|
Bosutinib: a dual SRC/ABL kinase inhibitor for the treatment of chronic myeloid leukemia. | 2009 Oct |
|
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 |
|
[Development of ABL tyrosine kinase inhibitors]. | 2010 Aug |
|
SRC: a century of science brought to the clinic. | 2010 Aug |
|
Optimizing combination therapies with existing and future CML drugs. | 2010 Aug 23 |
|
Src inhibitors in lung cancer: current status and future directions. | 2010 Jul 1 |
|
Gene expression analysis after receptor tyrosine kinase activation reveals new potential melanoma proteins. | 2010 Jul 21 |
|
The dual kinase complex FAK-Src as a promising therapeutic target in cancer. | 2010 Jun 24 |
|
Molecular measurement of BCR-ABL transcript variations in chronic myeloid leukemia patients in cytogenetic remission. | 2010 Nov 18 |
|
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 |
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
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=11689083
Bosutinib potently inhibits Src-dependent cell proliferation with an IC50 of 100 nM.
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Classification Tree | Code System | Code | ||
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WHO-ATC |
L01XE14
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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FDA ORPHAN DRUG |
274808
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admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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EU-Orphan Drug |
EU/3/10/762
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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NDF-RT |
N0000175605
Created by
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LIVERTOX |
NBK547951
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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WHO-VATC |
QL01XE14
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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NCI_THESAURUS |
C155700
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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Code System | Code | Type | Description | ||
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N0000185503
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | P-Glycoprotein Inhibitors [MoA] | ||
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C471992
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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39112
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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5710
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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CHEMBL288441
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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m2627
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | Merck Index | ||
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DB06616
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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100000090716
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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RR-46
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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Bosutinib
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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SUB29176
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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5018V4AEZ0
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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DTXSID10861568
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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1307619
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | RxNorm | ||
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8715
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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5328940
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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5018V4AEZ0
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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68533
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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BOSUTINIB
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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C60809
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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4359
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY | |||
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380843-75-4
Created by
admin on Mon Mar 31 18:45:12 GMT 2025 , Edited by admin on Mon Mar 31 18:45:12 GMT 2025
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PRIMARY |
ACTIVE MOIETY
METABOLITE INACTIVE (PARENT)
PARENT (METABOLITE INACTIVE)
PARENT (METABOLITE INACTIVE)
SALT/SOLVATE (PARENT)
SALT/SOLVATE (PARENT)
SALT/SOLVATE (PARENT)