Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H21ClN4O5 |
| Molecular Weight | 420.847 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C2=C(N(CCOC(=O)C(C)(C)OC3=CC=C(Cl)C=C3)C=N2)C(=O)N(C)C1=O
InChI
InChIKey=KYAKGJDISSNVPZ-UHFFFAOYSA-N
InChI=1S/C19H21ClN4O5/c1-19(2,29-13-7-5-12(20)6-8-13)17(26)28-10-9-24-11-21-15-14(24)16(25)23(4)18(27)22(15)3/h5-8,11H,9-10H2,1-4H3
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/7728839Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/theofibrate.html | https://www.ncbi.nlm.nih.gov/pubmed/7045566 | https://www.drugs.com/international/etofylline-clofibrate.html | https://www.ncbi.nlm.nih.gov/pubmed/7045566
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7728839
Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/theofibrate.html | https://www.ncbi.nlm.nih.gov/pubmed/7045566 | https://www.drugs.com/international/etofylline-clofibrate.html | https://www.ncbi.nlm.nih.gov/pubmed/7045566
Theofibrate (Etofylline clofibrate, trade name Duolip) is the clofibric acid ester of theophylline, used for the treatment of hyperlipoproteinaemia with elevated triglycerides and cholesterol. The low dose of Etophylline clofibrate (750mg) has a similar lipid-lowering effect as pure clofibrate (1500mg), probably due to a synergistic hypolipidemic effect with theophylline, which has no lipid-lowering effect per se. Secondly, etophylline clofibrate substantially decreases platelet aggregability and plasma viscosity, properties which may be desirable in the prevention of coronary heart disease (CHD). Finally, etophylline clofibrate is clearly a less potent inducer of peroxisomal proliferation in the rat liver than clofibrate, bezafibrate or fenofibrate. Theofibrate increases lipoprotein lipase activity to promote the conversion of Very low-density lipoprotein (VLDL) to Low-density lipoprotein (LDL), and hence reduce the level of VLDL.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: GO:0034372 Sources: https://www.ncbi.nlm.nih.gov/pubmed/4004984 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Duolip forte Approved UseUnknown |
Doses
| Dose | Population | Adverse events |
|---|---|---|
750 mg 3 times / day multiple, oral Highest studied dose Dose: 750 mg, 3 times / day Route: oral Route: multiple Dose: 750 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: |
|
750 mg 3 times / day multiple, oral Highest studied dose Dose: 750 mg, 3 times / day Route: oral Route: multiple Dose: 750 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: unknown Food Status: UNKNOWN Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Page: 102.0 |
no |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Page: 1 | 72 | 103 |
no [IC50 18.3564 uM] | |||
Page: 99.0 |
yes [Activation 18.3564 uM] |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Page: 50.0 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7728839
500 - 750 mg once daily for 12-16 weeks
Route of Administration:
Oral
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C98150
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C152583
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m10705
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ACTIVE MOIETY