Optivia’s Opti-Safety™ Transporter Services Panel is comprised of clinically relevant transporters that are implicated in diseases and serious adverse drug reactions (ADR). Studying these transporters can help you identify potential safety problems and eliminate dangerous compounds early, or help you better mitigate the risk by understanding the mechanism and potential clinical safety issues. Optivia offers a wide range of services for the Opti- Safety™ Panel, ranging from low-cost, rapid screening to comprehensive, mechanistic profiling studies.
Transporter proteins regulate the trafficking and distribution of numerous critical nutrients and signaling molecules, such as amino acids, monosaccharides, bile salts and neurotransmitters. Some serious drug side effects, such as brain excitotoxicity, liver cholestasis, cardiac myopathy and type II diabetes can be attributed to unexpected modulation of transporters by pharmaceuticals, leading to expensive clinical failures and drug withdrawals. To help reduce safety-related attrition rates, it is important to evaluate a compound’s effect on transporters that are important modulators of key physiological processes.
Please contact us for more information on the Opti-Safety™ Panel and how Optivia can help enhance your safety studies.
Safety Transporters Associated With Serious Adverse Effects
|Transporter||Gene||Physiological/clinical relevance||Related genetic disorders or adverse effect|
|SERT||SLC6A4||Neurotransmission||Hyperthermia, Insomnia, anxiety, nausea|
|DAT||SLC6A3||Neurotransmission||Drug addiction, parkinsonsim, seizure, dystonia, dyskinesia|
|NET||SLC6A2||Neurotransmission||Arrhythmia, hypertension, ataxia, costipation, abuse potential|
|EAAT1||SLC1A3||Neurotransmission||Alzheimer's disease, Huntington's disease, epilepsy, cerebellar ataxia type 7, schizophrenia, excitotoxicity|
|EAAT2||SLC1A2||Neurotransmission||amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, epilepsy, ischemia, schizophrenia, excitotoxicity|
|EAAT3||SLC1A1||Neurotransmission||Huntington's disease, epilepsy, ischemia, Alzheimer's disease, Niemann-Pick disease, obsessive-compulsive disorder,excitotoxicity|
|xCT||SLC7A11||Glutathione synthesis||Neurodegeneration, oxidative glutamate toxicity|
|BSEP||ABCB11||Bile salt secretion||PFIC 2, mixed cholestatic hepatitis, drug induced liver injury (DILI)|
|OATP1B1||SLCO1B1||Statin DDI||Myopathy, rhabdomyolysis|
|ASBT||SLC10A2||bile salt transport||hypertriglycerimaemia, constipation, cholestatic liver diseases, NASH, primary bile acid malabsorption|
|OCTN2||SLC22A5||Fatty acid oxidation||Muscle fatigue, mental retardation, cardiac deficiencies|
|THTR1||SLC19A2||Thiamine transport||Thiamine-responsive megaloblastic anemia syndrome|
|THTR2||SLC19A3||Thiamine transport||Wernicke's encephalopathy, biotin-responsive basal ganglia disease|
Safety Transporter Resources