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.
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).

Tables

Table 1. Effects of Lipid-Lowering Drugs and Lp(a)-Specific Drugs on Lp(a)
 
Drug and referenceLp(a) levelDose, mgDuration, weekStudied subjectsComments
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/day8 - 24HC, CVD, T2DMDose 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/day8 - 24HC, HT, T2DM
Niacin [23]↓ (-22.9%)500 - 3,000/day8 - 12HC, CVD, T2DMDose independent effect
NPC1L1 inhibitor [24]↓ (-7.1%)10/day12HC
PCSK9 inhibitors [25]↓ (-26.9%)75 - 150/2weeks, 420/4weeks24 - 104HC
PCSK9 ASO [26]↓ (-21.9%)284/12 or 24 weeks77Severe HC
MTTP inhibitor [27]↓ (-13.0%)100 - 300/week26Severe HC
ApoB ASO [27]↓ (-32.0%)50 - 400/week26Severe HC
Pelacarsen [20]↓ (-80.0%)20/week24Severe HC, secondary prevention of CVDPhase II study (continued)
Olpasiran [28]↓ (-40.0%)225/12 weeks48CVDPhase II study (continued)
Zerlasiran [29]↓ (-80.0%)300 - 450/24 weeks60CVDPhase II study (continued)
Lp(a)-formation inhibitor [30]↓ (-65.0%)30 - 800/day2Healthy adultsPhase I study (continued)

 

Table 2. Effects of Estrogen-Related Drugs and Supplements on Lp(a)
 
Drug and referenceLp(a) levelDose, mgDuration, weekStudied subjectsComments
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 - 144Postmenopausal women
Tibolone [42]↓ (-25.3%)0.3 - 2.5/day12 - 240Postmenopausal womenDose and duration independent effect
Tamoxifen [43]↓ (-0.41 mg/dL)10 - 40/day8 - 260Postmenopausal women, CVD men
Raloxifene [44]↓ (-0.42 mg/dL)60 - 150/day3 - 24Postmenopausal women with healthy, hysterectomies, HC, T2DMNegative association between Lp(a) reduction and duration
L-carnitine [45]↓ (-8.82 mg/dL)4 g/day1 - 24HC, T2DMDose and duration independent effect
Coenzyme Q10 [46]↓ (-3.54 mg/dL)0.1 - 0.3 g/week4 - 12HC, T2DM, CVDInverse association between reduction of Lp(a) and dosage