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Take home messages from the ITC papers. The potential for drug-drug interactions DDIs involving membrane transporters has become an area of intense regulatory review over the past seven years. Regulatory Guidance for Drug Interaction Studies.


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Try out PMC Labs and tell us what you think. Learn More. The renal organic cation transport system mediates the tubular secretion of cationic compounds including drugs, toxins and endogenous metabolites into urine. Recently, substrate specificity, transcription mechanisms, structure, polymorphisms, in vivo contributions and clinical outcomes on MATE have been investigated intensively.

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Drugs that are eliminated by the MATE1 transporter, a multidrug and toxin extrusion transporter located in the apical membrane in the kidney and liver that is encoded by the SLC47A1 gene. Drugs Drug Drug Description Cephalexin A first generation cephalosporin used to treat certain susceptible bacterial infections.

Mate 1 substrates

Acyclovir A guanosine analog used to treat herpes simplex, varicella zoster, herpes zoster. N-methylnicotinamide N-methylnicotinamide is an experimental drug with no approved indication.

Metformin A biguanide drug used in conjunction with diet and exercise for glycemic control in type 2 diabetes mellitus and used off-label for insulin resistance in polycystic ovary syndrome PCOS. Cefradine A first-generation cephalosporin antibiotic used in the treatment of bacterial infections of the respiratory and urinary tracts and of the skin and soft tissues. Estrone sulfate An estrogen used as monotherapy or in several combination hormone replacement products for managing menopause symptoms and hormone disorders.

Importance of the multidrug and toxin extrusion mate/slc47a family to pharmacokinetics, pharmacodynamics/toxicodynamics and pharmacogenomics

Ganciclovir A DNA polymerase inhibitor used to treat cytomegalovirus and herpetic keratitis of the eye. Tetraethylammonium Tetraethylammonium is an experimental drug with no approved indication. Guanidine A strong organic base used to treat muscle weakness and fatigue associated with the myasthenic complications of Eaton-Lambert syndrome. Procainamide A medication used to treat life threatening ventricular arrhythmias.

Topotecan An antineoplastic agent used to treat ovarian cancer, small cell lung cancer, or cervical cancer.

Levofloxacin A fluoroquinolone antibiotic used to treat infections caused by susceptible bacteria of the upper respiratory tract, skin and skin structures, urinary tract, and prostate, as well as for post-exposure treatment of inhaled anthrax and the plague. Ciprofloxacin A second generation fluoroquinolone used to treat various susceptible bacterial infections. Tipiracil A thymidine phosphorylase inhibitor used as an adjunct treatment of adult patients with certain types of gastric or colorectal malignancies.

Solriamfetol Solriamfetol is indicated for treatment of daytime sleepiness associated with obstructive sleep apnea and narcolepsy, but is not a treatment for the underlying airway obstruction in apnea patients[FDA Label][A,A]. Relebactam A beta-lactamase inhibitor used to prevent hydrolysis of beta-lactam antibiotics, leading to increased effectiveness.

Nadolol A non-selective beta-adrenergic antagonist used for the management of arrhythmias, angina pectoris, and hypertension. Flecainide A class Ic antiarrhythmic agent used to manage atrial fibrillation and paroxysmal supraventricular tachycardias PSVT.

Emtricitabine A nucleoside reverse transcriptase inhibitor used for the treatment and prophylaxis of HIV. Trimethoprim An antifolate antibiotic often used in combination with sulfamethoxazole to treat a of infections, including those of the urinary tract, respiratory tract, and gastrointestinal tract.

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Sulpiride A selective D2 dopamine receptor antagonist indicated to treat chronic and acute schizophrenia. Fosdenopterin An exogenous form of cyclic pyranopterin monophosphate cPMP used as a replacement substrate in patients with molybdenum cofactor deficiency MoCD type A. Amisulpride A dopamine D2 receptor antagonist used in the treatment of acute and chronic schizophrenia, and in the prevention and treatment of postoperative nausea and vomiting in adults.

Glycopyrronium An anticholinergic agent used to treat hyperhidrosis, severe drooling, COPD, used with other medications to treat ulcers, and used in anesthesia. A biguanide drug used in conjunction with diet and exercise for glycemic control in type 2 diabetes mellitus and used off-label for insulin resistance in polycystic ovary syndrome PCOS. A first-generation cephalosporin antibiotic used in the treatment of bacterial infections of the respiratory and urinary tracts and of the skin and soft tissues.

An estrogen used as monotherapy or in several combination hormone replacement products for managing menopause symptoms and hormone disorders.

A strong organic base used to treat muscle weakness and fatigue associated with the myasthenic complications of Eaton-Lambert syndrome. An antineoplastic agent used to treat ovarian cancer, small cell lung cancer, or cervical cancer.

Introduction

A fluoroquinolone antibiotic used to treat infections caused by susceptible bacteria of the upper respiratory tract, skin and skin structures, urinary tract, and prostate, as well as for post-exposure treatment of inhaled anthrax and the plague. A thymidine phosphorylase inhibitor used as an adjunct treatment of adult patients with certain types of gastric or colorectal malignancies. Solriamfetol is indicated for treatment of daytime sleepiness associated with obstructive sleep apnea and narcolepsy, but is not a treatment for the underlying airway obstruction in apnea patients[FDA Label][A,A].

A beta-lactamase inhibitor used to prevent hydrolysis of beta-lactam antibiotics, leading to increased effectiveness.

A non-selective beta-adrenergic antagonist used for the management of arrhythmias, angina pectoris, and hypertension. A class Ic antiarrhythmic agent used to manage atrial fibrillation and paroxysmal supraventricular tachycardias PSVT.

An antifolate antibiotic often used in combination with sulfamethoxazole to treat a of infections, including those of the urinary tract, respiratory tract, and gastrointestinal tract. An exogenous form of cyclic pyranopterin monophosphate cPMP used as a replacement substrate in patients with molybdenum cofactor deficiency MoCD type A.

A dopamine D2 receptor antagonist used in the treatment of acute and chronic schizophrenia, and in the prevention and treatment of postoperative nausea and vomiting in adults.

An anticholinergic agent used to treat hyperhidrosis, severe drooling, COPD, used with other medications to treat ulcers, and used in anesthesia. Electron transfer flavoprotein-ubiquinone oxidoreductase, mitochondrial. Solute carrier organic anion transporter family member 4C1. Solute carrier organic anion transporter family member 1A2.