Target intelligence / Profile preview

Solute carrier family 22 member 5 (OCTN2)

Target
OCTN2
Molecular classification
Transporter, Solute carrier family, Membrane protein, Organic cation transporter
01

Overview

Solute carrier family 22 member 5 (OCTN2) is a widely expressed membrane transporter responsible for the high-affinity, sodium-dependent uptake of L-carnitine and various organic cations across cell membranes[1][2][3][4][6]. Critical for fatty acid oxidation and energy production, especially in muscle, heart, and kidney, OCTN2 maintains cellular and systemic carnitine homeostasis by mediating intestinal absorption and renal reabsorption of carnitine[1][4][6]. Mutations in SLC22A5 cause primary systemic carnitine deficiency, a condition marked by muscle weakness, cardiomyopathy, hypoglycemia, and other metabolic symptoms[3][4][6]. OCTN2 is also polyspecific, transporting diverse drugs and zwitterions, and plays a role in drug disposition and potential drug-drug or drug-nutrient interactions[1][2][3]. Therapeutically, monitoring and targeting OCTN2 holds importance in metabolic diseases, while drug-induced inhibition of its function poses risks for secondary carnitine deficiency and rhabdomyolysis[2][4][6].

Other names
Organic cation/carnitine transporter 2Carnitine transporter (CTT)Carnitine transporter 1 (CT1)CDSPHigh-affinity sodium-dependent carnitine cotransporterOrganic cation transporter 5Novel organic cation transporter 2S22A5_HUMANSCDSolute carrier family 22 (organic cation transporter), member 5
02

Mechanism of action

Competitive inhibition of carnitine uptake, Blockade of organic cation transport, Drug-induced reduction of cellular or systemic carnitine levels

03

Biological functions

L-carnitine transportFatty acid metabolismCellular energy productionDrug transport and dispositionRenal reabsorption of L-carnitineIntestinal absorption of carnitineRegulation of cellular carnitine levels
04

Disease associations

Primary systemic carnitine deficiencyCardiomyopathySkeletal myopathyCrohn’s diseaseMetabolic disordersRhabdomyolysis (secondary to drug-induced carnitine deficiency)Heart failureHypoglycemia
05

Safety considerations

Risk of systemic carnitine deficiencyMetabolic decompensation (hypoketotic hypoglycemia, hepatic encephalopathy, muscle weakness)Cardiomyopathy and heart failureDrug-drug interactions leading to unintended carnitine depletionRhabdomyolysis with certain drug combinations
06

Interacting drugs

Tetraethylammonium (TEA)

11 more in the full profile.

07

Biomarkers

Plasma/serum carnitine level (diagnosis and monitoring of carnitine deficiency)Urinary carnitine excretionSLC22A5 gene mutation screening (primary carnitine deficiency risk)

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