Safety Pharmacology has recently emerged as an important component in the discovery and development pathway of a wide range of pharmaceutical and chemical products. The goal of drug development is advancing novel drugs that provide true health benefits by optimizing efficacy with minimal or no adverse effects. Prior to approving a drug for clinical trials, the TGA/FDA and other regulatory agencies require a core battery for safety pharmacology studies in which the effects of a test article on vital functions of the central nervous system, cardiovascular system and respiratory system are evaluated.

hERG K+ Ion Channel Assay

hERG (Human Ether-a-go-go Related Gene) testing for drug candidates is a crucial component of the drug development process as an estimated 25–40% of all lead compounds show some degree of hERG related toxicity. As a result, regulatory agencies including FDA and EMEA require hERG/Kr pre-clinical safety data as part of any investigational new drug submission. RDDT Laboratories offers fast and reliable results between hERG channels and drug candidates through our GLP compliant and non-GLP assays.

Format	hERG Fast Patch Duo	hERG Fast Patch Quattro	hERG SAR Optimization	GLP hERG Assay
	This service includes Solubility Testing Drug Degradation Security Vehicle and Positive Controls Representative Current Traces Study Plan and Report in CTD Format	Assay Features Solubility Testing Drug Degradation Security Vehicle and Positive Controls Representative Current Traces Study Plan and Report in CTD Format IC50 value determination	This service includes Solubility Testing Drug Degradation Security Vehicle and Positive Controls Representative Current Traces Study Plan and Report in CTD Format Detailed IC50 value and SAR Characteristics	Assay Features Solubility Testing Drug Degradation Security Vehicle and Positive Controls Representative Current Traces Study Plan and Report in CTD Format Study according to GLP Principles ICH S7A/B
Relevance	Discovery Safety Screen Fast & High Content	Discovery Safety Screen IC50 value determination	Discovery Safety Screen Structure Activity Relationship	Discovery Safety Screen GLP Format
Target Gene	KCNH2	KCNH2	KCNH2	KCNH2
Source	Human	Human	Human	Human
Accession Sequence	UO4270	UO4270	UO4270	UO4270
Genomic Context	Chromosome 7, Location &q35–q36	Chromosome 7, Location &q35–q36	Chromosome 7, Location &q35–q36	Chromosome 7, Location &q35–q36
Test System	HEK or CHO ChanClone Cell Line	HEK or CHO ChanClone Cell Line	HEK or CHO ChanClone Cell Line	HEK or CHO ChanClone Cell Line
Technology	Patch-clamp whole cell Configuration	Patch-clamp whole cell Configuration	Patch-clamp whole cell Configuration	Patch-clamp whole cell Configuration
Test Item Application	FastSolution Exchange	FastSolution Exchange	FastSolution Exchange	FastSolution Exchange
Assay Temperature	Room temperature	Room temperature	Room temperature or 37°C	Room temperature
No. of Concentrations	2	4	4	4
Number of Replicates	N=2 cells	N=2 cells	N=3 cells	N=3 cells
Data point Number	4 per Test Item	8 per Test Item	12 per Test Item	18 per Test Item
Positive Control	E-4031 or Dofetilide (n=1 cell, included)	E-4031 or Dofetilide (n=1 cell, included)	E-4031 or Dofetilide (n=2 cells, included)	E-4031 or Dofetilide (n=3 cells, ANOVA & Dunnett)
Positive Control	DMSO or Ethanol (n=1 cell, included)	DMSO or Ethanol (n=1 cell, included)	DMSO or Ethanol (n=2 cells, included)	DMSO or Ethanol (n=3 cells, ANOVA & Dunnett)
Compound Quantity	2–5mg or 100μl stock solution 1000x	2–5mg or 100μl stock solution 1000x	10mg or 200μl stock solution	10mg
Storage Conditions	-80°C/-20°C/4°C/RT	-80°C/-20°C/4°C/RT	-80°C/-20°C/4°C/RT	-80°C/-20°C/4°C/RT
Turnaround Time	2 weeks per Drug Cluster (50 molecules)	4 weeks per Drug Cluster (50 molecules)	6 weeks per Drug Cluster (50 molecules)	2 weeks per Drug (Draft GLP Study Report)