Stereochemistry | ACHIRAL |
Molecular Formula | C25H24F3N3O2 |
Molecular Weight | 455.4722 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=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=GXALXAKNHIROPE-QAQDUYKDSA-N
InChI=1S/C25H24F3N3O2/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)/t16-,17-
Molecular Formula | C25H24F3N3O2 |
Molecular Weight | 455.4722 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
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
Doses
Sourcing
PubMed
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