Drug intelligence / Profile preview

pradigastat + metformin

Development stage
Discontinued
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Pradigastat (LCQ908A) is a small molecule inhibitor of diacylglycerol O-acyltransferase 1 (DGAT1), an enzyme responsible for the final step of triglyceride synthesis in the intestine and liver. By inhibiting DGAT1, pradigastat reduces the formation of chylomicrons and the absorption of dietary fats, which has been explored for treating hypertriglyceridemia and type 2 diabetes. Metformin is a biguanide that primarily works by decreasing hepatic glucose production and improving insulin sensitivity through the activation of AMP-activated protein kinase (AMPK). The combination of LCQ908A and metformin was evaluated by Novartis in Phase 2 clinical trials for patients with type 2 diabetes who were inadequately controlled on metformin monotherapy. However, development for this indication was ultimately discontinued.

Other names
LCQ908A + metforminpradigastat + metformin
02

Targets

SLC22A8 (Organic anion transporter 3)DGAT1 (Diacylglycerol O-acyltransferase 1)OATP1B1 (Organic anion transporting polypeptide 1B1)SLCO1B3 (Organic anion transporting polypeptide 1B3)ABCG2 (Breast cancer resistance protein)CYP2B6 (Cytochrome P450 2B6)CYP2C8 (Cytochrome P450 2C8)

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