What medications are processed by SLCO1B1?

What medications are processed by SLCO1B1?

The gene organic anion transporting polypeptide 1B1 (OATP1B1, also known as SLCO1B1) encodes the transmembrane protein OATP1B1, which transports anionic drugs such as statins, irinotecan, rifampin, repaglinide and methotrexate.

What is the SLCO1B1 gene?

The SLCO1B1 gene provides instructions for making a protein called organic anion transporting polypeptide 1B1, or OATP1B1. This protein is found in liver cells; it transports compounds from the blood into the liver so that they can be cleared from the body.

What does SLCO1B1 decreased function mean?

Having SLCO1B1 decreased function means that you may have reduced transport of certain medications into the liver for processing and removal from the body. This may lead to slightly higher than normal medication levels in the body, or have no noticeable effects.

What is SLCO1B1 drug transport?

SLCO1B1 (solute carrier organic anion transporter family member 1B1) is a drug transporter that helps the body get rid of certain medicines through the liver. There are many medications that may be affected by SLCO1B1. There are many variations or genetic differences in the gene for SLCO1B1.

What are OATP1B1 inhibitors?

Clinical significance Therapeutically important drugs such as cyclosporine, gemfibrozil, some statins, antibiotics, and antiretroviral drugs are recognized clinical inhibitors of OATP1B1.

What is statin induced myopathy?

Statin-associated myopathy or myalgia is a well-known side effect of lipid-lowering agents. Usually, after discontinuation of the drug, symptoms alleviate and patients may be re-challenged with another statin. However, in rare cases, symptoms of myalgia do not subside after statins are discontinued.

What is OATP1B1 substrate?

Known substrates of OATP1B1 and OATP1B3 include statins, repaglinide, olmesartan, enalapril, valsartan, several xenobiotic glucuronide metabolites, as well as a host of cytotoxic chemotherapeutic agents, including the taxanes paclitaxel and docetaxel, the platinum-based drug cisplatin, and methotrexate.

What is OATP2B1?

OATP2B1 is a ubiquitously expressed uptake transporter with broad substrate specificity. It transports mostly anionic organic endo- and xenobiotics, and its activity appears to be pH-dependent.

What drugs inhibit CYP450?

Severe toxicity can result if CYP450 enzyme–inhibiting drugs are added to the following medications: atypical antipsychotics, benzodiazepines, cyclosporine (Sandimmune), statins, or warfarin (Coumadin).

Are there any statin studies for SLCO1B1 genotype?

Peyser et al 12 have performed the first prospective randomized SLCO1B1 genotype-guided study for statin reinitiation. Although they failed to show that genotyping improved statin adherence, they did show that genotyping led to a greater number of patients reinitiated on statins and meaningful improvements in LDL-C levels.

Are there different versions of the SLCO1B1 gene?

There are different SLCO1B1 gene versions, or variants, and each has a different effect on how well simvastatin is metabolized in the body. Some variants result in normal function while others function only at an intermediate or low level.

When do you get your SLCO1B1 results?

Patients in the usual care arm received their SLCO1B1 results at the end of the 8-month study period. Test results and statin dosing recommendations were returned to primary care providers within the electronic health record with minimal disruption to the clinical workflow.

Is the SLCO1B1 gene code for CT genoytpe?

Patients at Intermediate Risk for myopathy carry one copy of a variant in SLCO1B1 that results in a low-functioning SLCO1B1 protein. The gene product is coded by the *5 variant, which may also be expressed as the heterozygous ‘CT’ genoytpe.