Lovastatin and Gemfibrozil: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Gemfibrozil
Lovastatin
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
What happens
Increased exposure of lovastatin acid (active metabolite) and an increased risk of myopathy or rhabdomyolysis
Interaction Deep Dive
Concomitant use of lovastatin and gemfibrozil (an OATP1B1 transporter inhibitor) has resulted in an increase in the AUC of lovastatin acid (active metabolite)3 and concomitant use should be avoided 1. In several case reports, the concurrent use of lovastatin and gemfibrozil has resulted in severe myopathy and rhabdomyolysis 112124.
Why it happens (mechanism)
Inhibition of OATP1B1-mediated lovastatin transport by gemfibrozil
Literature reports
8 reports — tap to read
a) Concomitant use of lovastatin and gemfibrozil (an OATP1B1 transporter inhibitor) resulted in a 2.8-fold increase in the AUC of lovastatin acid (active metabolite) 3.
b) Concomitant administration of gemfibrozil 600 mg twice daily for 3 days with lovastatin 40 mg daily in 11 subjects resulted in an AUC ratio (with concomitant lovastatin/without concomitant lovastatin) for lovastatin of 0.96 and lovastatin acid of 2.8 1.
c) The Food and Drug Administration received 12 case reports of severe myopathy or rhabdomyolysis associated with concomitant use of lovastatin and gemfibrozil 4. All patients' serum creatine kinase levels rose to more than 10,000 International Units/L. Symptoms resolved when both drugs were discontinued. Because of the potential for severe myopathy or rhabdomyolysis, and because of the availability of alternative drug combinations for treating hyperlipidemia, the use of lovastatin in combination with gemfibrozil is discouraged.
d) The results of a prospective clinical trial in which 12 patients with heterozygous familial hypercholesterolemia were treated with the combination of lovastatin 80 mg daily and gemfibrozil 1200 mg daily indicated an increased risk of myopathy with this regimen. One patient developed an asymptomatic increase in creatine kinase (CK) with lovastatin monotherapy; however, the patient developed symptomatic myopathy (CK of 7840 Units/L) on the combination regimen, but recovered when the medications were withdrawn 5.
e) In a retrospective review, the authors concluded that the combination of lovastatin and gemfibrozil is safe in patients with normal renal function when the dose of lovastatin is carefully titrated and limited, and the CK and liver function tests are closely monitored. The researchers reviewed records for 70 patients (none had significant renal dysfunction) treated with a combination of lovastatin and gemfibrozil and determined that five patients had experienced mild CK elevations, one had a mild alanine aminotransferase (ALT) elevation, and one had both. However, there were no reports of muscle pain and/or weakness 6.
f) Researchers at the Cholesterol Center, Jewish Hospital of Cincinnati conducted two separate retrospective studies of their patients. In the first, the records of 25 patients with primary hyperlipoproteinemias who had undergone an average of 12.5 months of combination therapy with gemfibrozil and lovastatin indicated no myalgias, myositis, muscle weakness or tenderness in any patient 7. In the second retrospective study, the researchers reviewed records of 80 patients with primary mixed hyperlipidemia. The patients underwent at least six months of combination lovastatin/gemfibrozil treatment. They found no significant difference in the percentage of high CK levels per patient taking combination therapy verses lovastatin monotherapy. Three patients discontinued the regimen because of muscle symptoms or elevated CPK attributed to drug therapy; however, no patients experienced rhabdomyolysis, myoglobinuria, or renal failure 8.
g) A muscle biopsy performed as part of another case study confirmed the absence of inflammatory cells in a 57-year-old woman experiencing weakness after adding gemfibrozil to her drug regimen which included lovastatin. The author speculated that an immune-mediated mechanism is not the cause of the myopathy/rhabdomyolysis 9.
h) Gemfibrozil markedly increases the plasma concentrations of lovastatin acid resulting in an increased risk of developing myopathy. In addition, the resulting myopathy may be of pharmacokinetic origin. Eleven volunteers were included in a randomized, placebo-controlled, crossover, 3-phase study design. A two-week washout period separated the phases. Bezafibrate 400 mg slow release given once daily, gemfibrozil 600 mg twice daily, or placebo for 3 days. Lovastatin 40 mg was administered on day 4. During the gemfibrozil phase, the mean AUC (0-24) of lovastatin acid was 280% (p less than 0.001) and the maximum plasma concentration (Cmax) was 280% (p less than 0.05) of the values in the placebo phase. Gemfibrozil had no significant effects on the AUC (0-24) or Cmax of lovastatin. The AUC (0-24) ratio of lovastatin acid to lovastatin during the gemfibrozil phase was 3.2 times as high as the values in the placebo phase. Bezafibrate 400 mg had no marked effects on any of the pharmacokinetic variables of lovastatin or lovastatin acid. The results of this study demonstrate that gemfibrozil increases the plasma levels of active lovastatin acid without affecting the levels of parent lovastatin. Gemfibrozil increased the AUC and Cmax of lovastatin acid approximately 3-fold. The author concludes that the risk of developing myopathy may be smaller with bezafibrate as compared to gemfibrozil 10.
Common questions
Can I take Lovastatin and Gemfibrozil together?
Increased exposure of lovastatin acid (active metabolite) and an increased risk of myopathy or rhabdomyolysis Always confirm with your pharmacist or prescriber before making any change.
How serious is the Lovastatin and Gemfibrozil interaction?
It is rated major. Potentially serious — often needs a change or close monitoring.
How quickly could this interaction happen?
The documented onset is "delayed". Effects tend to build up gradually over days to weeks.
How strong is the evidence for this interaction?
The evidence is graded "established". Well documented — supported by controlled studies or strong clinical data.
Questions for your pharmacist
- Does my dose of Lovastatin or Gemfibrozil need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (12)
- Product Information: MEVACOR(R) oral tablets, lovastatin oral tablets. Merck & Co, Inc. (Per FDA), Whitehouse Station, NJ, 2012. DailyMed
- Marais GE & Larsen KK: Rhabdomyolysis and acute renal failure induced by combination lovastatin and gemfibrozil therapy. Ann Intern Med 1990; 112:228-230. PubMed
- Tornio A, Neuvonen PJ, Niemi M, et al: Role of gemfibrozil as an inhibitor of CYP2C8 and membrane transporters. Expert Opin Drug Metab Toxicol 2017; 13(1):83-95. PubMed
- Pierce LR, Wysowski DK, & Gross TP: Myopathy and rhabdomyolysis associated with lovastatin-gemfibrozil combination therapy. JAMA 1990; 264:71-75. DOI
- Illingworth DR & Bacon S: Influence of lovastatin plus gemfibrozil on plasma lipids and lipoproteins in patients with heterozygous familial hypercholesterolemia. Circulation 1989; 79:590-596. PubMed
- Wirebaugh SR, Shapiro ML, McIntyre TH, et al: A retrospective review of the use of lipid-lowering agents in combination, specifically, gemfibrozil and lovastatin. Pharmacotherapy 1992; 12:445-450. DOI
- Glueck CJ, Speirs J, & Tracy T: Safety and efficacy of combined gemfibrozil-lovastatin therapy for primary dyslipoproteinemias. J Lab Clin Med 1990; 115:603-609.
- Glueck CJ, Oakes N, Speirs J, et al: Gemfibrozil-lovastatin therapy for primary hyperlipoproteinemias. Am J Cardiol 1992; 70:1-9. PubMed
- Chucrallah I, DeGirolami U, Freeman K, et al: Lovastatin/gemfibrozil myopathy: a clinical, histochemical, and ultrastructural study. Eur Neurol 1992; 32:293-296. PubMed
- Kyrklund C: Plasma concentrations of active lovastatin acid are markedly increased by gemfibrozil but not by bezafibrate. Clin Pharmacol Ther 2001; 69(5):340-345. PubMed
- East C, Bilheimer DW, & Grundy SM: Combination drug therapy for familial combined hyperlipidemia. Ann Intern Med 1988; 109:25-32. PubMed
- East C, Alivizatos PA, Grundy SM, et al: Rhabdomyolysis in patients receiving lovastatin after cardiac transplantation (letter). N Engl J Med 1988a; 318:47-48.
Keep reading about Gemfibrozil
Keep reading about Lovastatin
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