Relationship between genetic polymorphism of drug transporters and the efficacy of Rosuvastatin, atorvastatin and simvastatin in patients with hyperlipidemia

Lipids Health Dis. 2021 Nov 8;20(1):157. doi: 10.1186/s12944-021-01586-7.

Abstract

Background: To determine the effect of genetic polymorphism of drug transporters on the efficacy of treatment with Rosuvastatin, Atorvastatin and Simvastatin in patients with hyperlipidemia.

Methods: The study consists of 180 patients, aged 40-75 years, with hyperlipidemia. All patients were divided into two equal groups: patients with different SLCO1B1 (521CC, 521CT and 521TT) and MDR1 (3435CC, 3435TC and 3435TT) genotypes. Each group was divided into rosuvastatin-treated, atorvastatin-treated and simvastatin-treated subgroups. The lipid-lowering effect of statins was assessed by tracing changes in total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C) levels.

Results: The use of statins over a 4-month period led to substantial reductions in TC and LDL-C levels. The hypolipidemic effect of studied agents was seen in both groups. However, it was less pronounced in patients with 521CC genotype. No statistically significantly differences were found between carriers of 3435TT, 3435CT and 3435CC genotypes.

Conclusions: The lipid-lowering efficacy of rosuvastatin was higher compared to other two statins. Patients with SLCO1B1 521CC genotype are more likely to encounter a decrease in the hypolipidemic effect of statins. Such a risk should be considered when treating this category of patients. MDR1 polymorphism had no significant effect on statin efficacy.

Keywords: Cardiovascular diseases; Cholesterol; Hydroxymethylglutaryl-CoA reductase inhibitors; Hyperlipidemia; Low-density lipoprotein; Pharmacogenetics.

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B / genetics
  • Adult
  • Aged
  • Anticholesteremic Agents / therapeutic use
  • Atorvastatin / therapeutic use
  • Cholesterol, LDL / blood
  • Cholesterol, LDL / genetics
  • Female
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / therapeutic use*
  • Hyperlipidemias / drug therapy*
  • Hyperlipidemias / genetics
  • Liver-Specific Organic Anion Transporter 1 / genetics*
  • Male
  • Middle Aged
  • Polymorphism, Genetic*
  • Rosuvastatin Calcium / therapeutic use
  • Simvastatin / therapeutic use
  • Treatment Outcome

Substances

  • ABCB1 protein, human
  • ATP Binding Cassette Transporter, Subfamily B
  • Anticholesteremic Agents
  • Cholesterol, LDL
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Liver-Specific Organic Anion Transporter 1
  • SLCO1B1 protein, human
  • Rosuvastatin Calcium
  • Atorvastatin
  • Simvastatin