Identify potential liability issues in early stages of drug discovery
Toxicity and clinical safety are one of the leading causes of drug candidate failure in preclinical and clinical testing stage, and also the major reason for the withdrawal of approved drugs from the market. For example, hepatotoxicity and cardiotoxicity result in the most severe problems in drug development and are often the cause of drug withdrawals. To reduce attrition of drug candidates during clinical development, toxicology and risk assessment should be an integrated part of the early drug discovery process.
WuXi Biology offers comprehensive services at the target and cellular level to assess drug safety profiles in the discovery process. With our expertise and cutting-edge technologies, we will provide high quality and cost-effective data with fast turnaround. Applying these assays to your drug discovery and development programs will help to avoid costly late-stage failures.
Off-target Profiling
WuXi Biology Mini Safety Panel | WuXi Mini 44
A primary safety panel, which is designed to identify compounds with the highest risk because it contains targets associated with the most serious ADRs. This panel is recommended for use early in drug discovery stage for early hazard identification.
The 44 selected targets are recommended by four major pharmaceutical companies (Bowes J. et al. Nat Rev Drug Discov. 2012), including 24 GPCRs, 8 ion channels, 7 enzymes, 3 monoamine transporters and 2 nuclear hormone receptors.
GPCRs
Adenosine receptor
Adrenergic receptors
Alpha1A
Cannabinoid receptor
Cholecystokinin receptor
Dopamine receptors
Endothelin receptor
Histamine receptor
5-Hydroxytryptamine receptor
Muscarinic receptor
Opioid receptor
Vasopressin receptor
Channels
Ca2+Channel
K+Channel
Na+channel
Serotonin
Nicotinic
Glutamate
Transporters and NR
Transporter DAT / 5HTT / NET
Steroid Nuclear Receptors
Enzymes
Protein-Tyrosine Kinase -CTK
Phosphodiesterase
Cyclooxygenase
Monoamine & NRT Synthesis & Metabolism
WuXi Biology Second Safety Panel | WuXi Extra 54
A panel of additional 54 targets. This more extensive panel contains such targets that have the combination of either low-hit-rate/high-risk ADRs or high-hit-rate/ lower-risk ADRs. This panel is ideal for broad characterization of a limited number of compounds for lead selection, provides data to drive SAR for lead optimization.
The 54 selected targets include 26 GPCRs, 5 ion channels, 18 enzymes, 3 nuclear hormone receptors and 2 transmembrane targets.
GPCRs
5-Hydroxytryptamine receptor
Adenosine receptor
Adrenoceptor
Bradykinin receptor
Cholecystokinin receptor
Dopamine receptor
PGE2 receptor
Platelet-Activating Factor
Endothelin receptor
Histamine receptor
Muscarinic receptor
Tachykinin receptor
Vasopressin receptor
Channels
ATP-sensitive inward rectifier potassium channel
Cav1.2 (L-type) Rat Calcium Ion Channel
Glutamate ( Non-Selective) Rat Ion Channel
NR
Estrogen receptor
Peroxisome proliferator activated receptor gamma
Progesterone receptor
Transmembrane (Other)
Sigma receptor
Enzymes
Angiotensin converting enzyme
Cholinesterase
Serine/threonine-protein kinase
Serine protease
Monoamine oxidase
Histone Deacetylase
INSR Tyrosine kinase
Rho-associated protein kinase
Vascular Endothelial Growth Factor Receptor
Phosphodiesterase
WuXi Biology Full Panel | WuXi 98
The combination of WuXi Mini 44 and WuXi Extra 54.