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Details

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
Structure of PRADIGASTAT

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-

HIDE SMILES / InChI

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

Description

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

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
1065 ng/mL
300 mg single, oral
PRADIGASTAT plasma
Homo sapiens
184 ng/mL
40 mg single, oral
PRADIGASTAT plasma
Homo sapiens
10500 ng/mL
115 mg single, intravenous
PRADIGASTAT plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
18561 ng × h/mL
300 mg single, oral
PRADIGASTAT plasma
Homo sapiens
37200 ng × h/mL
40 mg single, oral
PRADIGASTAT plasma
Homo sapiens
428000 ng × h/mL
115 mg single, intravenous
PRADIGASTAT plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
80.2 h
300 mg single, oral
PRADIGASTAT plasma
Homo sapiens
145 h
40 mg single, oral
PRADIGASTAT plasma
Homo sapiens
109 h
115 mg single, intravenous
PRADIGASTAT plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
0.6%
40 mg single, oral
PRADIGASTAT plasma
Homo sapiens

Doses

PubMed

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
Unknown
Substance Class Chemical
Record UNII
2U23G6VNUZ
Record Status Validated (UNII)
Record Version