Part I.
Pharmacogenes code for medication transporters.
Medication transporters are responsible for moving drugs in and out of target tissues, regulating drug exposure to metabolic enzymes and eventually to elimination pathways.
An example of a medication transporter is SLCO1B1 which is predominantly located in liver cells.
Lipid lowering statin medications rely on SLCO1B1 for uptake into liver cells - where they exert their effects to lower total and LDL cholesterol - and subsequently undergo metabolism and elimination.
SLCO1B1 genetic variations are associated with reduced statin uptake by liver cells and delayed metabolism and elimination.
Patients with decreased or minimal to no transporter function likely experience reduced efficacy and are at greater risk for developing statin-associated musculoskeletal symptoms (SAMS), as well as more serious adverse effects such as myopathy and rhabdomyolysis.
Preemptive pharmacogenetic (PGx) testing, via a simple cheek swab, can determine if genetic variations of transporters such as SLCO1B1 are present. These results can be used to guide the selection of medication that is more likely to offer benefit and less likely to cause harm.
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