Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C25H23F3N3O2.Na |
| Molecular Weight | 477.454 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].[O-]C(=O)C[C@H]1CC[C@@H](CC1)C2=CC=C(C=C2)C3=CC=C(NC4=CC=C(N=C4)C(F)(F)F)C=N3
InChI
InChIKey=MUZRGKSNUTWRAF-BHQIMSFRSA-M
InChI=1S/C25H24F3N3O2.Na/c26-25(27,28)23-12-10-21(15-30-23)31-20-9-11-22(29-14-20)19-7-5-18(6-8-19)17-3-1-16(2-4-17)13-24(32)33;/h5-12,14-17,31H,1-4,13H2,(H,32,33);/q;+1/p-1/t16-,17-;
DescriptionCurator's Comment: Description was created based on several sources, including
http://adisinsight.springer.com/drugs/800030516
Curator's Comment: Description was created based on several sources, including
http://adisinsight.springer.com/drugs/800030516
LCQ908 (Pradigastat) is a diacylglycerol acyltransferase-1 (DGAT-1) inhibitor. DGAT-1 is one of the two DGAT enzymes that catalyse the formation of triglycerides from diacylglycerol and acyl- coenzyme A. DGAT-1 catalyses the final committed step in processing dietary fatty acids into triglycerides carried on chylomicrons for transport around the body. Pradigastat may decrease the level of triglycerides in the blood and is intended for the first line treatment of FCS. It is administered orally at 10-40mg daily in addition to a low fat diet. Pradigastat is also in phase II clinical trials for type 2 diabetes and severe hypertriglyceridaemia (familial hyperchylomicronaemia phenotypes I and V). Pradigastat is a designated orphan drug in the EU. In a phase III clinical trial.
Originator
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1065 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25854859 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
PRADIGASTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
184 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25627776 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
PRADIGASTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
10500 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27274009 |
115 mg single, intravenous dose: 115 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PRADIGASTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
18561 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25854859 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
PRADIGASTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
37200 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25627776 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
PRADIGASTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
428000 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27274009 |
115 mg single, intravenous dose: 115 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PRADIGASTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
80.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25854859 |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
PRADIGASTAT plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED |
|
145 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25627776 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
PRADIGASTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
109 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27274009 |
115 mg single, intravenous dose: 115 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
PRADIGASTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.6% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25627776 |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
PRADIGASTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
| Dose | Population | Adverse events |
|---|---|---|
300 mg single, oral Highest studied dose Dose: 300 mg Route: oral Route: single Dose: 300 mg Sources: Page: p.1037 |
unhealthy, ADULT n = 8 Health Status: unhealthy Condition: obesity Age Group: ADULT Sex: M Food Status: FASTED Population Size: 8 Sources: Page: p.1037 |
|
115 mg single, intravenous Studied dose Dose: 115 mg Route: intravenous Route: single Dose: 115 mg Sources: Page: p.9 |
healthy, ADULT n = 9 Health Status: healthy Age Group: ADULT Sex: M+F Food Status: FASTED Population Size: 9 Sources: Page: p.9 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Effect of pradigastat, a diacylglycerol acyltransferase 1 inhibitor, on the pharmacokinetics of a combination oral contraceptive in healthy female subjects. | 2015 Apr |
|
| Pharmacokinetics, pharmacodynamics, safety, and tolerability of pradigastat, a novel diacylglycerol acyltransferase 1 inhibitor in overweight or obese, but otherwise healthy human subjects. | 2015 Sep |
Patents
Sample Use Guides
Experimental: LCQ908 (Pradigastat) 20 mg
In period II (0-12 weeks) double-blind treatment: one LCQ908 (Pradigastat) 20 mg active tablet, once daily
In period III (12-52 weeks) double blind treatment: Without down titration, the period II dosing regimen will follow. Following decision to down titrate: one LCQ908 (Pradigastat) 10 mg active tablet, once daily.
Route of Administration:
Oral
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956136-98-4
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53387034
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100000183197
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X0EWE8TT2H
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EU/3/12/1036 (POSITIVE)
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PRIMARY | Treatment of familial chylomicronaemia syndrome (type-I hyperlipoproteinaemia). | ||
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AB-09
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C170340
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CHEMBL2364624
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SUB197601
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ACTIVE MOIETY
SUBSTANCE RECORD
