Table 3 DGAT inhibitors in clinical trials

PF-04620110

DGAT1

Phase I

NCT01064492

12 healthy volunteers

Phase IB

NCT01298518

48 type 2 diabetes mellitus subjects

Reduced postprandial TG excursions [159]

AZD7687

DGAT1

Phase I

NCT01046357

80 healthy male subjects

Decreased postprandial TG excursions approximately 75% compared to placebo following a fat containing meal (p < 0.0001) [160]

Pradigastat

(LCQ-908)

DGAT1

Phase I [172]

Overweight or obese healthy subjects (single-dose cohorts, n = 72) (multiple-dose cohorts, n = 106)

Pradigastat treatment (single and multiple doses) led to dose-dependent suppression of postprandial triglyceride excursions over 9 h following a high-fat meal test. Pradigastat was safe and tolerated at single and multiple doses in healthy subjects

Phase III

NCT01514461

45 adults with familial chylomicronemia syndrome (FCS) (Hyperlipoproteinemia type I)

Reduced both postprandial and fasting triglycerides from baseline to 12 weeks after treatment (fasting TG: LCQ908 vs placebo: − 13.9 vs 45.6, p = 0.0182)

Ervogastat

(PF-06865571)

DGAT2

Phase I

NCT04044053

12 healthy adult participants

Phase I

NCT03092232

17 healthy adult participants

Phase I

NCT03230383

60 healthy adults including overweight and obese

Phase I

NCT03513588

48 people with nonalcoholic fatty liver disease

Relative change from baseline in whole liver fat at Day 15 after treatment (PF-06865571 300 mg vs placebo: − 41.14 vs − 10.94, p < 0.001)

Phase II

NCT04399538

75 adult participants with presumed nonalcoholic steatohepatitis

DGAT2i combined with ACC inhibitors significantly reduced percentage of liver fat after 6 weeks treatment compared to placebo (− 58.80% vs − 3.58, p < 0.001)

Phase II

NCT04321031

450 non-alcoholic steatohepatitis with fibrosis