Details
Stereochemistry | ACHIRAL |
Molecular Formula | C14H18N2O |
Molecular Weight | 230.3055 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)C(=O)C1=C2C=CC=CN2N=C1C(C)C
InChI
InChIKey=ZJVFLBOZORBYFE-UHFFFAOYSA-N
InChI=1S/C14H18N2O/c1-9(2)13-12(14(17)10(3)4)11-7-5-6-8-16(11)15-13/h5-10H,1-4H3
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/11607039Curator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB05266 | https://www.ncbi.nlm.nih.gov/pubmed/27501293
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11607039
Curator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB05266 | https://www.ncbi.nlm.nih.gov/pubmed/27501293
Ibudilast (KETAS®) is a non-selective cyclic nucleotide phosphodiesterase (PDE) inhibitor. It is an antithrombotic, antiasthmatic drug that is used for improving prognosis and relieving symptoms in patients suffering from ischemic stroke and for the treatment of bronchial asthma. A definitive mechanism of its action is yet to be established. However, inhibition of the release of inflammatory cytokines, inhibition of leukocyte activation, and inhibition of the expression of cell adhesion molecules have been proposed as likely mechanisms of action of ibudilast (KETAS®). It is currently in development in the US (for instance as a potential therapy for multiple sclerosis), but is approved for use in Japan.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL241 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11607039 |
9.5 µM [Ki] | ||
Target ID: CHEMBL254 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11607039 |
3.3 µM [Ki] | ||
Target ID: CHEMBL4409 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11607039 |
1.27 µM [Ki] | ||
Target ID: CHEMBL2717 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11607039 |
8.9 µM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | KETAS Approved Use1. Bronchial asthma
2. Improvement of dizziness secondary to chronic cerebral circulation impairment associated with sequelae of cerebral infarction |
|||
Palliative | KETAS Approved Use1. Bronchial asthma
2. Improvement of dizziness secondary to chronic cerebral circulation impairment associated with sequelae of cerebral infarction |
Sample Use Guides
In case of bronchhial asthma:
The usual adult dosage for oral use is 10 mg of ibudulast (KETAS®) twice daily.
In case of cerebro-vascular disorders:
The usual dosage for oral use is 10 mg of ibudulast (KETAS®) three times daily. The dosage may be adjusted according to the patient's symptoms.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16674936
The inhibitory effect of ibudilast against the human phosphodiesterase (PDE) enzyme family was measured. Ibudilast did not exhibit PDE4 subfamily selectivity with Ki values ranging from 3.3 uM to 6.3 uM. Inhibition of PDE10 by ibudilast was essentially the same with cAMP and cGMP as substrates yielding Ki values of 2.2 uM and 1.3 uM, respectively. PDE11 was tested for inhibition using both cAMP and cGMP substrates and cAMP hydrolysis was sensitive to inhibition with a Ki value of 8.9 uM. PDE3A was inhibited by ibudilast with a Ki of 9.5 uM.
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
WHO-VATC |
QR03DC04
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
||
|
WHO-ATC |
R03DC04
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
||
|
FDA ORPHAN DRUG |
889222
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
||
|
EU-Orphan Drug |
EU/3/16/1801
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
||
|
NCI_THESAURUS |
C29707
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
||
|
FDA ORPHAN DRUG |
480015
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
||
|
FDA ORPHAN DRUG |
445814
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
||
|
NCI_THESAURUS |
C1327
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
||
|
FDA ORPHAN DRUG |
587717
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
M0TTH61XC5
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
50847-11-5
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
DB05266
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
7399
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
6068
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
SUB08096MIG
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
C038366
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
CHEMBL19449
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
1406
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
Ibudilast
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
m6188
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | Merck Index | ||
|
100000083667
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
C65876
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
3671
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY | |||
|
DTXSID7049007
Created by
admin on Fri Dec 15 15:37:55 GMT 2023 , Edited by admin on Fri Dec 15 15:37:55 GMT 2023
|
PRIMARY |
ACTIVE MOIETY