Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C30H35F2N3O |
| Molecular Weight | 491.6152 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC=CC(C)=C1NC(=O)CN2CCN(CCCC(C3=CC=C(F)C=C3)C4=CC=C(F)C=C4)CC2
InChI
InChIKey=ZBIAKUMOEKILTF-UHFFFAOYSA-N
InChI=1S/C30H35F2N3O/c1-22-5-3-6-23(2)30(22)33-29(36)21-35-19-17-34(18-20-35)16-4-7-28(24-8-12-26(31)13-9-24)25-10-14-27(32)15-11-25/h3,5-6,8-15,28H,4,7,16-21H2,1-2H3,(H,33,36)
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL240 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15135665 |
16.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | CLINIUM Approved UseAngina pectoris resulting from ischaemic heart disease. Prophylaxis and after-treatment (after the acute phase) of myocardial infarcation. |
Doses
| Dose | Population | Adverse events |
|---|---|---|
120 mg 3 times / day multiple, oral Highest studied dose Dose: 120 mg, 3 times / day Route: oral Route: multiple Dose: 120 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: |
Disc. AE: arrhythmia... AEs leading to discontinuation/dose reduction: arrhythmia (lethal, 3 patients) Sources: |
360 mg/day multiple, oral Highest studied dose Dose: 360 mg/day Route: oral Route: multiple Dose: 360 mg/day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| arrhythmia | lethal, 3 patients Disc. AE |
120 mg 3 times / day multiple, oral Highest studied dose Dose: 120 mg, 3 times / day Route: oral Route: multiple Dose: 120 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FASTED Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| inconclusive [IC50 10 uM] | ||||
| inconclusive [IC50 15.8489 uM] | ||||
| inconclusive [IC50 15.8489 uM] | ||||
| no [IC50 >10 uM] | ||||
Page: 191.0 |
no | |||
Page: 205.0 |
no | |||
| yes [IC50 5.0119 uM] | ||||
Page: 46.0 |
yes |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Page: 9 | 205 |
no |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Identification of human Ether-à-go-go related gene modulators by three screening platforms in an academic drug-discovery setting. | 2010-12 |
|
| Comparative evaluation of HERG currents and QT intervals following challenge with suspected torsadogenic and nontorsadogenic drugs. | 2006-03 |
|
| Molecular cloning and characterization of a nitrobenzylthioinosine-insensitive (ei) equilibrative nucleoside transporter from human placenta. | 1997-12-15 |
|
| Ventricular tachyarrhythmias induced by disopyramide and other similar anti-arrhythmic drugs. | 1981-06-06 |
Sample Use Guides
In Vivo Use Guide
Sources: http://home.intekom.com/pharm/janssen/clinium.html
The dosage ranges between 2 and 4 tablets daily. Dosage should be adapted individually and started gradually as follows:
first week –1 tablet daily.
second week –1 tablet every morning and evening.
third week –1 tablet three times per day.
An appreciable beneficial effect may sometimes be manifest after a few days or weeks of treatment but the full therapeutic result can usually only be assessed after 6 months of treatment.
If no marked improvement is noticeable after 3 months then the dosage may gradually be increased to 6 tablets per day using as guidelines the therapeutic response, possible non-transient side-effects and ECG controls.
Tablets are preferably taken during meals. Gastrointestinal disturbances can be avoided by taking an antacid con-currently. Clinical findings indicate that uninterrupted therapy, at the optimum dosage level, must be maintained indefinitely to consolidate the favourable results.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2175795
The neuronal cell degeneration was Ca+(+)-dependent because, in the absence of extracellular Ca++, 16 hr of exposure to 30 microM veratridine failed to produce release of LDH. Ca++ antagonists, nonselective for slow Ca++ channels (flunarizine, cinnarizine, lidoflazine, prenylamine and bepridil) inhibited veratridine-induced release of LDH with IC50 values between 0.11 and 0.47 microM.
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QC08EX01
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C333
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ACTIVE MOIETY