OPTI-SAFETY™ Panel

Type:Services
SUBTYPE:Transporter Assays
APPLICATION & SPECIALITY USES:ADME-Toxicology Products and Services
Keywords:DDIRegulatoryTransporters

Our OPTI-SAFETY Panel consists of clinically-relevant transporters that are implicated in diseases and serious adverse drug reactions (ADR). Transporters in the panel can be used to identify potential safety problems, and either eliminate dangerous compounds early in the development process, or mitigate risks by understanding the mechanisms and potential clinical safety issues. We provide customized OPTI-SAFETY Panel research services for rapid screening or comprehensive, mechanistic profiling studies.

Transporter proteins regulate the movement of numerous critical nutrients and signaling molecules, such as amino acids, monosaccharides, bile salts and neurotransmitters. Serious side effects, such as brain excitotoxicity, liver cholestasis, cardiac myopathy and type II diabetes, can be attributed to the 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.

The table below lists transporters that are associated with serious adverse events.

TransporterGenePhysiological/clinical relevanceRelated genetic disorders or adverse effect 
SERTSLC6A4NeurotransmissionHyperthermia, Insomnia, anxiety, nausea
DATSLC6A3NeurotransmissionDrug addiction, parkinsonsim, seizure, dystonia, dyskinesia
NETSLC6A2NeurotransmissionArrhythmia, hypertension, ataxia, constipation, 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