Annotation of FDA Label for simvastatin and SLCO1B1
PharmGKB ID
Summary
The FDA-approved label for simvastatin (ZOCOR) states that simvastatin acid is a substrate of the transport protein OATP1B1 (SLCO1B1) and concomitant administration of medicinal products that are inhibitors of the transport protein OATP1B1 may lead to increased plasma concentrations of simvastatin acid and an increased risk of myopathy.
Annotation
Excerpts from the simvastatin (ZOCOR) drug label:
Simvastatin acid is a substrate of the transport protein OATP1B1. Concomitant administration of medicinal products that are inhibitors of the transport protein OATP1B1 may lead to increased plasma concentrations of simvastatin acid and an increased risk of myopathy. For example, cyclosporine has been shown to increase the AUC of statins; although the mechanism is not fully understood, the increase in AUC for simvastatin acid is presumably due, in part, to inhibition of CYP3A4 and/or OATP1B1.
For the complete drug label text with sections containing pharmacogenetic information highlighted, see the simvastatin drug label.
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FDA PGx Associations
| Category | Drug | Gene | Affected Subgroup | Interaction Description |
|---|---|---|---|---|
| Safety or Response | Simvastatin | SLCO1B1 | 521 TC or 521 CC (intermediate or poor function transporters) | Results in higher systemic concentrations and higher adverse reaction risk (myopathy). The risk of adverse reaction (myopathy) is higher for patients on 80 mg than for those on lower doses. |
Evidence for Clinical Annotations
This annotation has been used as evidence for the following clinical annotations.