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Details

Stereochemistry ACHIRAL
Molecular Formula C25H23F3N3O2.Na
Molecular Weight 477.4549
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PRADIGASTAT SODIUM

SMILES

C1C[C@@]([H])(CC[C@@]1([H])CC(=O)[O-])c2ccc(cc2)-c3ccc(cn3)Nc4ccc(C(F)(F)F)nc4.[Na+]

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-;

HIDE SMILES / InChI

Molecular Formula C25H23F3N3O2
Molecular Weight 454.4652
Charge -1
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula Na
Molecular Weight 22.9898
Charge 1
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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

Curator's Comment:: # Novartis

Approval Year

PubMed

PubMed

TitleDatePubMed
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
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Sat Jun 26 07:49:58 UTC 2021
Edited
by admin
on Sat Jun 26 07:49:58 UTC 2021
Record UNII
X0EWE8TT2H
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PRADIGASTAT SODIUM
USAN  
USAN  
Official Name English
LCQ908A
Code English
LCQ-908 SODIUM SALT
Common Name English
PRADIGASTAT SODIUM [USAN]
Common Name English
LCQ-908A
Common Name English
LCQ-908-ABA
Code English
LCQ908-ABA
Code English
CYCLOHEXANEACETIC ACID, 4-(4-(5-((6-(TRIFLUOROMETHYL)-3-PYRIDINYL)AMINO)-2-PYRIDINYL)PHENYL)-, SODIUM SALT (1:1), TRANS-
Common Name English
LCQ-908ABA
Code English
Code System Code Type Description
CAS
956136-98-4
Created by admin on Sat Jun 26 07:49:59 UTC 2021 , Edited by admin on Sat Jun 26 07:49:59 UTC 2021
PRIMARY
PUBCHEM
53387034
Created by admin on Sat Jun 26 07:49:59 UTC 2021 , Edited by admin on Sat Jun 26 07:49:59 UTC 2021
PRIMARY
FDA UNII
X0EWE8TT2H
Created by admin on Sat Jun 26 07:49:59 UTC 2021 , Edited by admin on Sat Jun 26 07:49:59 UTC 2021
PRIMARY
EU-Orphan Drug
EU/3/12/1036 (POSITIVE)
Created by admin on Sat Jun 26 07:49:59 UTC 2021 , Edited by admin on Sat Jun 26 07:49:59 UTC 2021
PRIMARY Treatment of familial chylomicronaemia syndrome (type-I hyperlipoproteinaemia).
NCI_THESAURUS
C170340
Created by admin on Sat Jun 26 07:49:59 UTC 2021 , Edited by admin on Sat Jun 26 07:49:59 UTC 2021
PRIMARY
ChEMBL
CHEMBL2364624
Created by admin on Sat Jun 26 07:49:59 UTC 2021 , Edited by admin on Sat Jun 26 07:49:59 UTC 2021
PRIMARY
EVMPD
SUB197601
Created by admin on Sat Jun 26 07:49:59 UTC 2021 , Edited by admin on Sat Jun 26 07:49:59 UTC 2021
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY