Journal of Clinical Medicine Research, ISSN 1918-3003 print, 1918-3011 online, Open Access
Article copyright, the authors; Journal compilation copyright, J Clin Med Res and Elmer Press Inc
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Review

Volume 17, Number 4, April 2025, pages 181-186

Lipoprotein(a)-Lowering Drugs: A Mini Review

Figure

↓  Figure 1. Lp(a) regulation by drugs; a simple schematic illustration. Bold arrow indicates acceleration; bold T-bar indicates inhibition. Since statins modulate both apoB synthesis and LDLR activation, resulting in a varied effect on Lp(a), they are not described in the figure. Apo(a): apolipoprotein(a); apoB: apolipoprotein B; ASO: antisense oligonucleotide; LDL: low-density lipoprotein; LDLR: low-density lipoprotein receptor; MTTP: microsomal triglyceride transfer protein; PCSK9: proprotein convertase subtilisin/kexin type 9; Lp(a): lipoprotein(a).
Figure 1.

Tables

↓  Table 1. Effects of Lipid-Lowering Drugs and Lp(a)-Specific Drugs on Lp(a)
 
Drug and reference Lp(a) level Dose, mg Duration, week Studied subjects Comments
Apo(a): apoprotein(a); ASO: antisense oligonucleotide; CVD: cardiovascular disease; HC: hypercholesterolemia; HT: heart transplant; LDL-C: low-density lipoprotein cholesterol; Lp(a): lipoprotein(a); MTTP: microsomal triglyceride transfer protein; NPC1L1: Niemann-Pick C1-Like1; PCSK9: proprotein convertase subtilisin kexin 9; T2DM: type 2 diabetes mellitus.
Statins [21] ↑ (+10.6%) 2 - 80/day 8 - 24 HC, CVD, T2DM Dose dependent effect
Increase of Lp(a) returned to the baseline levels in long-term treatment.
Note: a study describing Lp(a) reduction by atorvastatin (-0.20 mg/dL) with duration independent [14]
Fibrates [22] → (-1.76 mg/dL) 145 - 1,200/day 8 - 24 HC, HT, T2DM
Niacin [23] ↓ (-22.9%) 500 - 3,000/day 8 - 12 HC, CVD, T2DM Dose independent effect
NPC1L1 inhibitor [24] ↓ (-7.1%) 10/day 12 HC
PCSK9 inhibitors [25] ↓ (-26.9%) 75 - 150/2weeks, 420/4weeks 24 - 104 HC
PCSK9 ASO [26] ↓ (-21.9%) 284/12 or 24 weeks 77 Severe HC
MTTP inhibitor [27] ↓ (-13.0%) 100 - 300/week 26 Severe HC
ApoB ASO [27] ↓ (-32.0%) 50 - 400/week 26 Severe HC
Pelacarsen [20] ↓ (-80.0%) 20/week 24 Severe HC, secondary prevention of CVD Phase II study (continued)
Olpasiran [28] ↓ (-40.0%) 225/12 weeks 48 CVD Phase II study (continued)
Zerlasiran [29] ↓ (-80.0%) 300 - 450/24 weeks 60 CVD Phase II study (continued)
Lp(a)-formation inhibitor [30] ↓ (-65.0%) 30 - 800/day 2 Healthy adults Phase I study (continued)

 

↓  Table 2. Effects of Estrogen-Related Drugs and Supplements on Lp(a)
 
Drug and reference Lp(a) level Dose, mg Duration, week Studied subjects Comments
Lp(a): lipoprotein(a); CVD: cardiovascular disease; HC: hypercholesterolemia; T2DM: type 2 diabetes mellitus.
Hormone replacement therapy [41] ↓ (-20.4%) 0.025 - 0.175/day (dermal) 12 - 144 Postmenopausal women
Tibolone [42] ↓ (-25.3%) 0.3 - 2.5/day 12 - 240 Postmenopausal women Dose and duration independent effect
Tamoxifen [43] ↓ (-0.41 mg/dL) 10 - 40/day 8 - 260 Postmenopausal women, CVD men
Raloxifene [44] ↓ (-0.42 mg/dL) 60 - 150/day 3 - 24 Postmenopausal women with healthy, hysterectomies, HC, T2DM Negative association between Lp(a) reduction and duration
L-carnitine [45] ↓ (-8.82 mg/dL) 4 g/day 1 - 24 HC, T2DM Dose and duration independent effect
Coenzyme Q10 [46] ↓ (-3.54 mg/dL) 0.1 - 0.3 g/week 4 - 12 HC, T2DM, CVD Inverse association between reduction of Lp(a) and dosage