Safety Transporters – Opti-Safety™ Panel

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

TransporterGenePhysiological/clinical relevanceRelated genetic disorders or adverse effect 
SERTSLC6A4NeurotransmissionHyperthermia, Insomnia, anxiety, nausea
DATSLC6A3NeurotransmissionDrug addiction, parkinsonsim, seizure, dystonia, dyskinesia
NETSLC6A2NeurotransmissionArrhythmia, hypertension, ataxia, costipation, abuse potential
EAAT1SLC1A3NeurotransmissionAlzheimer's disease, Huntington's disease, epilepsy, cerebellar ataxia type 7, schizophrenia, excitotoxicity
EAAT2SLC1A2Neurotransmissionamyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, epilepsy, ischemia, schizophrenia, excitotoxicity
EAAT3SLC1A1NeurotransmissionHuntington's disease, epilepsy, ischemia, Alzheimer's disease, Niemann-Pick disease, obsessive-compulsive disorder,excitotoxicity
xCTSLC7A11Glutathione synthesisNeurodegeneration, oxidative glutamate toxicity
BSEPABCB11Bile salt secretionPFIC 2, mixed cholestatic hepatitis, drug induced liver injury (DILI)
MRP2ABCC2Bilirubin secretionHyperbilirubinemia
OATP1B1SLCO1B1Statin DDIMyopathy, rhabdomyolysis
ASBTSLC10A2bile salt transporthypertriglycerimaemia, constipation, cholestatic liver diseases, NASH, primary bile acid malabsorption
OCTN2SLC22A5Fatty acid oxidationMuscle fatigue, mental retardation, cardiac deficiencies
THTR1SLC19A2Thiamine transportThiamine-responsive megaloblastic anemia syndrome
THTR2SLC19A3Thiamine transportWernicke's encephalopathy, biotin-responsive basal ganglia disease

Safety Transporter Resources

Reducing safety-related drug attrition: the use of in vitro pharmacological profiling

The ABCs of membrane transporters in health and disease (SLC series): Introduction

Drug transporters in drug efficacy and toxicity

Role of organic cation transporters in drug-induced toxicity

Glutamate Transporters in Neurologic Disease

The Role of the Sodium-Taurocholate Co-transporting Polypeptide (NTCP) and of the Bile Salt Export Pump (BSEP) in Physiology and Pathophysiology of Bile Formation

Beyond the ITC White Paper: emerging sciences in drug transporters and opportunities for drug development

Bioparadigm SLC transporter database