All drug targets were taken from Citeline Pharmaproject53
| Drug name/drug class | Drug target | Targeting biomarker(s) | MR study of drug target | Summary of MR study results | RCTs | Summary of RCT results |
|---|---|---|---|---|---|---|
| Statins (ex. atorvastatin) | HMGCR | LDL-C | N/A | N/A | WOSCOPS18 AFCAPS/TexCAPS19 | Lowers LDL-C Improves CHD outcomes |
| PCSK9 inhibitors (ex. evolocumab) | PCSK9 | LDL-C HDL-C TG Lp(a) | Cohen et al 23 | Supports causal role in CHD | MENDEL-224 | Presently In Phase III clinical trials |
| CETP inhibitors (ex. torcetrapib) | CETP | HDL-C Lp(a) | Thompson et al33 | Supports a weak association with CHD | ILLUMINATE28 dal-OUTCOMES29 | 2 trials terminated due to lack of efficacy or adverse events 2 phase III trials are ongoing |
| sPLA2 inhibitor (ex. varespladib) | sPLA2 | sPLA2 LDL-C | Holmes et al12 | Reported no association | VISTA-1636 | Terminated due to adverse events |
| IL-6R monoclonal antibody (ex. tocilizumab) | IL6R | IL6R | Sarwar et al14 Hingorani et al38 | Supports a causal role in CHD | No RCTs for treatment of CHD | N/A |
| Niacin | HCAR2 | TG HDL-C LDL-C Lp(a) | N/A | N/A | AIM-HIGH47 HPS2-Thrive48 | Improves TG, HDL-C profiles Does not improve CHD outcomes |
| Fibrates (ex. fenofibrate) | PPARα | TG HDL-C LDL-C | MIGC et al. 201457 | N/A | FIELD67 DAIS65 | Improves lipid profiles Uncertainty regarding CHD outcomes |
| Anti-APO3C inhibitors | APO3C | TG | Jørgensen et al13 Do et al49 | Supports a causal role of in CHD | NCT0152942452 | Presently in phase II clinical trials Awaiting full results of IMPROVE-IT |
| ACAT inhibitors (ex. pactimibe) | SOAT-1 | LDL-C | N/A | N/A | ACTIVATE54 | Terminated due to adverse events |
| Ezetimibe | NPC1L1 | LDL-C | Polisecki et al11 | Supports a causal role in CHD | ENHANCE56 IMPROVE-IT59 | Lowers LDL-C Does not improve CHD outcomes |
ACAT, acyl-CoA cholesterol acyltransferase; CETP, cholesterylester transfer protein; CHD, coronary heart disease; HMGCR, HMG-CoA reductase; HDL-C, high-density lipoprotein cholesterol; LDL-C, low-density lipoprotein cholesterol; MR, Mendelian randomisation; TG, triglyceride.