Drug Metabolism & Transporters

Drug Transporter

TRİlaç Taşıyıcısı
Also known as:Membrane transporter · Transporter protein

A membrane protein that moves drugs across cell membranes, either into cells (uptake) or out of them (efflux), and thereby influences absorption, distribution and elimination.

In depth

Drug transporters belong mainly to two superfamilies: ATP-binding cassette (ABC) efflux pumps such as P-glycoprotein (ABCB1), BCRP (ABCG2) and the MRPs, and solute carrier (SLC) transporters such as OATP1B1/1B3, OAT1/3, OCT1/2 and MATE1/2-K. They are expressed in the intestine, liver and kidney and at blood–tissue barriers such as the blood–brain barrier.

Transporters determine tissue exposure, hepatic uptake and renal tubular secretion, and are sites of drug interactions and pharmacogenetic variation. Regulatory guidance recommends that new drugs be evaluated as substrates and inhibitors of the key transporters.

Clinical pearl

Transporter inhibition can raise drug levels without any CYP involvement: ciclosporin inhibits OATP1B1 and increases statin exposure, and trimethoprim or cimetidine reduces renal secretion of metformin and creatinine.

Example drugs

Digoxin Rosuvastatin Metformin Methotrexate
TRIn Turkish

İlaç Taşıyıcısı

İlaçları hücre zarları boyunca hücre içine (alım) veya hücre dışına (dışa atım) taşıyarak absorpsiyonu, dağılımı ve eliminasyonu etkileyen bir membran proteinidir.

İlaç taşıyıcıları başlıca iki süper aileye ayrılır: P-glikoprotein (ABCB1), BCRP (ABCG2) ve MRP'ler gibi ATP bağlayıcı kaset (ABC) dışa atım pompaları ile OATP1B1/1B3, OAT1/3, OCT1/2 ve MATE1/2-K gibi solüt taşıyıcı (SLC) ailesi üyeleri. Bağırsak, karaciğer ve böbrekte ve kan–beyin bariyeri gibi kan–doku bariyerlerinde eksprese edilirler.

Taşıyıcılar doku maruziyetini, hepatik alımı ve renal tübüler sekresyonu belirler; ilaç etkileşimlerinin ve farmakogenetik değişkenliğin önemli bir kaynağıdır. Düzenleyici kılavuzlar yeni ilaçların başlıca taşıyıcıların substratı ve inhibitörü olarak değerlendirilmesini önerir.

Taşıyıcı inhibisyonu CYP'den bağımsız olarak ilaç düzeylerini yükseltebilir: siklosporin OATP1B1'i inhibe ederek statin maruziyetini artırır; trimetoprim veya simetidin ise metformin ve kreatininin renal sekresyonunu azaltır.

Diğer adları:Membran taşıyıcısı · Taşıyıcı protein
Updated 24.09.2026 0 views Educational reference — verify against current sources before clinical use.

Read next

P-glycoproteinP-glikoprotein

An ATP-dependent efflux transporter (ABCB1, MDR1) that pumps a wide range of drugs out of cells, limiting their intestinal absorption and brain entry and promoting their biliary and renal excretion.

 OATP1B1OATP1B1

An organic anion-transporting polypeptide, encoded by the SLCO1B1 gene, that mediates uptake of many drugs and endogenous compounds from blood into hepatocytes across the sinusoidal (basolateral) membrane.

 Blood–Brain BarrierKan–Beyin Bariyeri

A selective barrier formed by brain capillary endothelial cells joined by tight junctions and supported by pericytes and astrocyte end-feet, which restricts the passage of drugs and solutes from blood into the central nervous system.

 Renal ClearanceRenal Klirens

The component of total clearance attributable to the kidneys: the volume of plasma cleared of drug by urinary excretion per unit time.

 Pharmacokinetic InteractionFarmakokinetik Etkileşim

An interaction in which one drug alters the absorption, distribution, metabolism or excretion of another, so that the concentrations of the affected drug change rather than its concentration–effect relationship.

 BioavailabilityBiyoyararlanım

The fraction of an administered dose that reaches the systemic circulation unchanged, and the rate at which it does so; by definition, bioavailability is 1 (100%) for an intravenous dose.