Table 5.
Selected drug molecules with potential action on atherosclerosis.
| Active molecule | Experimental Design/ Model | Target Molecule | Results | Future Implications |
|---|---|---|---|---|
| BRP-7 | Human PMNs – ex vivo | FLAP | Novel inhibitors of leukotriene biosynthesis by targeting 5-lipoxygenase-activating protein | Improved MK886-like drugs |
| BRP-7 with nitrile at C(5)-BI position | HEK293s – in vitro | FLAP | Addition of nitrile group to BRP-7 significantly enhances FLAP binding | Improved FLAP inhibitors – in vitro |
| PGF2α | Micromini pigs | Estrogen Progesterone |
Corpus luteum regression results from treatment lowered estrogen and progesterone | PGF2α-like eicosanoid derived contraceptive trials |
| Varespladib: Inhibitors of PLA2 | Patients with Cardiovascular Disease | PLA2 | Reduces inflammation, atherogenic lipids | FDA considered varespladib an orphan drug for its potential to treat patients with sickle cell disease |
| VIA‐2291 (atreleuton) | Patients with recent acute coronary syndrome (ACS) | 5‐lipoxygenase inhibitor | Slowed plaque progression | Atreleuton has been used in trials studying the treatment of Atherosclerosis and Coronary Artery Disease. |
| Darapladib: Inhibitors of PLA2 | Double-blind trial, assigned patients with stable coronary heart disease to receive once-daily darapladib | Lp-PLA2 | Reduces inflammation, atherogenic lipids | The study failed to reduce the risk of coronary heart disease death |