Details of Drug-Drug Interaction
| Drug General Information (ID: DDIHFEC2Y4) | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Drug Name | Rosuvastatin | Drug Info | Gemfibrozil | Drug Info | |||||
| Drug Type | Small molecule | Small molecule | |||||||
| Therapeutic Class | Statins/Antihyperlipidemic Agents | Antihyperammonia Agents | |||||||
| Structure | |||||||||
| Mechanism of Rosuvastatin-Gemfibrozil Interaction (Severity Level: Major) | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Transporter inhibition Click to Show/Hide Mechanism Graph | |||||||||
 |
|||||||||
| Drug Name | Rosuvastatin | Gemfibrozil | |||||||
| Mechanism | OATP2B1 substrate | OATP2B1 inhibitor | |||||||
| Key Mechanism Factor 1 | |||||||||
| Factor Name | Organic anion transporter B |
×
Structure
Sequence
MGPRIGPAGEVPQVPDKETKATMGTENTPGGKASPDPQDVRPSVFHNIKLFVLCHSLLQLAQLMISGYLKSSISTVEKRFGLSSQTSGLLASFNEVGNTALIVFVSYFGSRVHRPRMIGYGAILVALAGLLMTLPHFISEPYRYDNTSPEDMPQDFKASLCLPTTSAPASAPSNGNCSSYTETQHLSVVGIMFVAQTLLGVGGVPIQPFGISYIDDFAHNSNSPLYLGILFAVTMMGPGLAFGLGSLMLRLYVDINQMPEGGISLTIKDPRWVGAWWLGFLIAAGAVALAAIPYFFFPKEMPKEKRELQFRRKVLAVTDSPARKGKDSPSKQSPGESTKKQDGLVQIAPNLTVIQFIKVFPRVLLQTLRHPIFLLVVLSQVCLSSMAAGMAIFLPKFLERQFSITASYANLLIGCLSFPSVIVGIVVGGVLVKRLHLGPVGCGALCLLGMLLCLFFSLPLFFIGCSSHQIAGITHQTSAHPGLELSPSCMEACSCPLDGFNPVCDPSTRVEYITPCHAGCSSWVVQDALDNSQVFYTNCSCVVEGNPVLAGSCDSTCSHLVVPFLLLVSLGSALACLTHTPSFMLILRGVKKEDKTLAVGIQFMFLRILAWMPSPVIHGSAIDTTCVHWALSCGRRAVCRYYNNDLLRNRFIGLQFFFKTGSVICFALVLAVLRQQDKEARTKESRSSPAVEQQLLVSGPGKKPEDSRV
|
|||||||
| Gene Name | OATP2B1 | ||||||||
| Uniprot ID | SO2B1_HUMAN | ||||||||
| KEGG Pathway | hsa:11309 | ||||||||
| Protein Family | Organo anion transporter (TC 2.A.60) family | ||||||||
| Protein Function |
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Click to Show/Hide
|
||||||||
| Mechanism Description |
|
||||||||
| Recommended Action | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Management | Concurrent use of rosuvastatin and gemfibrozil should generally be avoided unless the benefit of further alterations in lipid levels is anticipated to outweigh the potential risks. Addition of fibrates to HMG-CoA reductase inhibitor therapy typically provides little additional reduction in LDL cholesterol, but further reductions of triglycerides and increases in HDL cholesterol may be attained. The daily dosage of rosuvastatin should not exceed 10 mg when used in combination with gemfibrozil. Patients should be advised to promptly report any unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever. Therapy should be discontinued if creatine kinase is markedly elevated in the absence of strenuous exercise or if myopathy is otherwise suspected or diagnosed. | ||||||||