Inxight Drugs

U.S. Department of Health & Human Services Divider Arrow

National Institutes of Health Divider Arrow

NCATS

This repository is under review for potential modification in compliance with Administration directives.

Return Home Inxight Drugs

Home
Browse Drugs
Search
- Structure Search
- Sequence Search
Downloads
About

Show Filters

Hide Filters

Development Status

US Approved Rx

4

All Match

Any Match

Exclude Selected

Exclude Selected

Primary Target

Proto-oncogene tyrosine-protein kinase Src

4

Tyrosine-protein kinase ABL1

4

All Match

Any Match

Exclude Selected

Exclude Selected

Highest Phase

Approved

4

All Match

Any Match

Exclude Selected

Exclude Selected

Approval Year

2012

4

All Match

Any Match

Exclude Selected

Exclude Selected

Condition

Leukemia, myelogenous, chronic, BCR-ABL positive

4

All Match

Any Match

Exclude Selected

Exclude Selected

Treatment Modality

Primary

4

All Match

Any Match

Exclude Selected

Exclude Selected

CNS Activity

CNS Penetrant

4

All Match

Any Match

Exclude Selected

Exclude Selected

Originator

Wyeth

4

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Class

Chemical

4

All Match

Any Match

Exclude Selected

Exclude Selected

Code System

FDA UNII

4

PUBCHEM

4

CAS

3

EPA CompTox

3

SMS_ID

3

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 1

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 2

ANTINEOPLASTIC AGENTS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 3

OTHER ANTINEOPLASTIC AGENTS

1

All Match

Any Match

Exclude Selected

Exclude Selected

ATC Level 4

Protein kinase inhibitors

1

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Form

Salts, Hydrates, Esters, etc.

3

Principal Form

1

All Match

Any Match

Exclude Selected

Exclude Selected

Showing 1 - 4 of 4 results

First page disabled
Previous page disabled
1
Next page disabled
Next page disabled

BOSUTINIB

5018V4AEZ0

Export Data
Search for Structure

Status:

US Approved Rx (2023)

First approved in 2012

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Proto-oncogene tyrosine-protein kinase Src

Tyrosine-protein kinase ABL1

Conditions:

Leukemia, myelogenous, chronic, BCR-ABL positive

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 patien...

ts 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.

BOSUTINIB DIHYDRATE

8897ZFQ8MU

Export Data
Search for Structure

Status:

US Approved Rx (2023)

First approved in 2012

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Proto-oncogene tyrosine-protein kinase Src

Tyrosine-protein kinase ABL1

Conditions:

Leukemia, myelogenous, chronic, BCR-ABL positive

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 patien...

ts 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.

Bosutinib methanoate

EZM4KL4P89

Export Data
Search for Structure

Status:

US Approved Rx (2023)

First approved in 2012

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Proto-oncogene tyrosine-protein kinase Src

Tyrosine-protein kinase ABL1

Conditions:

Leukemia, myelogenous, chronic, BCR-ABL positive

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 patien...

ts 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.

BOSUTINIB MONOHYDRATE

844ZJE6I55

Export Data
Search for Structure

Status:

US Approved Rx (2023)

First approved in 2012

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Proto-oncogene tyrosine-protein kinase Src

Tyrosine-protein kinase ABL1

Conditions:

Leukemia, myelogenous, chronic, BCR-ABL positive

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 patien...

ts 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.

HHS VULNERABILITY DISCLOSURE

For language access assistance, contact the NCATS Public Information Officer

National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966


			version 1.1