Table 1.
Atherogenic Target | Class | Compound | Molecular Target | Stage of Development | Refs |
---|---|---|---|---|---|
Hypertension | β-blockers | Metoprolol, Carvedilol, Bisoprolol | adrenergic β-receptors | Marketed | [56,57,60,61] |
ACE inhibitors | Captopril, Benazepril, Perindopril, Ramipril | Angiotensin-converting enzyme | |||
Ca2+-channel blockers | Amlodipine, Nifedipine | Voltage-dependent L−, N−, and T-type Ca2+ channels | |||
Diuretics | Thiazide | Solute carrier family 12 members | |||
Angiotensin-Receptor blockers | Losartan, Valsartan | Angiotensin receptor | Marketed | [60,61,62,63] | |
Dyslipidemia | HGM-CoA inhibitors | Statins | HMG-CoA | Marketed | [17,62] |
PCSK9 inhibitors | Evolucumab, Alirocumab | PCSK9 | |||
Cholesterol absorption inhibitors | Ezetimibe | NPC1L1, SOAT1 | |||
Inflammation | Antibodies | Canakinumab; Adalimumab, Infliximab, Inclacumab | Cytokines (IL1β, TNFα), adhesion molecules (P-selectin) | I-III | [64,65,66] |
Lipoxygenase inhibitors | Atreleutron, Veliflapon | 5-LO, FLAP | II | [67,68] | |
Phospholipase inhibitors | Darapladib, Varespladib | Lp-PLA2, sPLA2 | III | [69,70] | |
CCL2-CCR2 inhibitors | CCR2 | I | [71] | ||
Thrombosis | Thromboxane A2 inhibitors | Aspirin | Cyclooxygenases | Marketed | [72,73] |
P2Y12 inhibitors | Clopidegril, Ticagrelor, Prasugrel, Cangrelor | P2Y purinoceptor 12 | |||
GPIIb/IIIa inhibitors | Tirofiban, Eptifibatide, Abciximb | platelet glycoprotein (GP) IIb/IIIa receptor | |||
PAR-1 inhibitors | Vorapaxar | Proteinase-activated receptor 1 |
5-LO = 5-lipoxygenase; CCL2 = C-C motif chemokine ligand 2 (monocyte chemoattractant protein (MCP)-1); CCR2 = C-C chemokine receptor type 2; FLAP = 5-LO activating protein; HMG-CoA = β-hydroxy-β-methylglutaryl-CoA; Lp-PLA2 = lipoprotein-associated phospholipase A2; NPC1L1 = Niemann–Pick C1-like protein 1; PSCK9 = proprotein convertase subtilisin/kexin type 9; SOAT1 = sterol O-acyltransferase 1; sPLA2 = secretory phospholipase A2.