Drug intelligence / Profile preview

digoxin + furosemide + metformin + rosuvastatin

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

digoxin + furosemide + metformin + rosuvastatin is a non-branded combination of four generic drugs used jointly in pharmacokinetic studies to assess transporter-mediated drug–drug interactions. - **Digoxin** is a cardiac glycoside, primarily an inhibitor of *Na⁺/K⁺-ATPase*, used for heart failure and atrial fibrillation. - **Furosemide** is a loop diuretic that inhibits *sodium-potassium-chloride symporter* in the thick ascending limb of the loop of Henle, treating edema and hypertension. - **Metformin** is a biguanide antihyperglycemic agent, inhibiting hepatic glucose production (via *AMP-activated protein kinase activation*) and increasing insulin sensitivity, for type 2 diabetes. - **Rosuvastatin** is an HMG-CoA reductase inhibitor (statin), reducing cholesterol synthesis and increasing hepatic LDL receptors, for hypercholesterolemia and cardiovascular risk reduction. This cocktail is primarily employed as a probe set in clinical research for drug transporter interactions, especially for P-glycoprotein (P-gp, digoxin), OAT1/OAT3 (furosemide), OCT2/MATE1/MATE2-K (metformin), and OATP1B1/OATP1B3/BCRP (rosuvastatin)[1][5]. Notably, metformin and, to a lesser extent, furosemide, increase the systemic exposure of rosuvastatin when administered together, mostly through transporter-mediated mechanisms[1]. This four-drug combination is not a commercial product and is used specifically for clinical pharmacology and drug development research.

Other names
Digoxin, Furosemide, Metformin, and Rosuvastatin CocktailDigoxin + Furosemide + Metformin + Rosuvastatin
02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)SLC47A1 (Multidrug and toxin extrusion transporter 1)AMPK (Adenosine monophosphate–activated protein kinase)ABCG2 (Breast cancer resistance protein)OAT1 (Organic anion transporter 1)ABCB1 (P-glycoprotein)SLCO1B3 (Organic anion transporting polypeptide 1B3)SLC22A8 (Organic anion transporter 3)OCT2 (Organic cation transporter 2)SGLT2 (Sodium-glucose cotransporter protein subunit 2)MATE2-K (Multidrug and toxin extrusion protein 2)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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