SAFETY ASSESSMENT with ROBUST HUMAN TARGET EXPRESSION DATA
Understanding the safety risks associated with drug targets is essential for understanding whether undesired side effects may derail a drug discovery & development program. Therefore, knowledge of where your target of interest is expressed across human tissue and organ systems supports both the validation of that target as relevant for a particular therapeutic approach and provides information as to where unexpected or undesired expression may be. BioIVT’s XPRESSWAY® Profile Safety Package provides these data for 46 drug targets that are known to be associated with drug safety issues.
BioIVT XPRESSWAY Sample-Report
What is an XPRESSWAY Profile?
- An XPRESSWAY profile consists of quantitative gene expression for a single target in 72 different human tissues from 3 different donors (216 samples in total). The tissue cohort was chosen to represent the major organ systems of the body and includes many sub-dissected regions of key organ systems. All the tissues are defined as pathologically normal by certified pathologists.
XPRESSWAY Profile Safety Package Helps Understand Off-Target Risk
- As part of the drug development process NCEs are regularly screened against this panel of targets to identify off-target binding. Correlation of these screening data with the target expression patterns provided by XPRESSWAY Profile Safety Package enable better understanding of the potential for side effect liability.
- Improved go/no-go decisions for lead optimization and candidate selection can then be made based on the known pharmacokinetics and distribution of your NCE.
XPRESSWAY PROFILE SAFETY PACKAGE Benefits
- Better understand and mitigate development risk by understanding biological context of screening data
- Expression data generated by a rigorous, highly controlled qRT-PCR method that has been used to generate consistent and reliable data over many years, with excellent assay performance and full data heritage
- Immediate access to tailored data package, supported by over 2,300 profiles for additional targets
- Robust data can be used with confidence to interpret screening results
Data are provided in the format of PDF report containing the relevant information regarding the target gene, data and donor details for the 46 specific genes. The raw data for the target gene and GAPDH, together with the donor details, are also provided in Excel format to enable the data to be presented in any format required by the client.
Gene Profiles included in XPRESSWAY PROFILE SAFETY PACKAGE:
GPCR – 5HT1A & 5HT1B receptors, 5HT2A & 5HT2B receptors, Adenosine A2A receptor, Alpha1a & alpha2a adrenoceptors, Beta1 & beta2 adrenoceptors, Cannabinoid CB1 & CB2 receptors, Cholecystokinin CCK1 receptor, Dopamine D1 & D2S receptors, Endothelin receptor, Histamine H1 & H2 receptors, Muscarinic M1, M2 & M3 receptors, Delta, kappa, & mu opioid receptors, Vasopressin V1A receptor
Ion Channel – 5HT3A receptor, Cav 1.2 L type Ca2+ channel, GABAA channel, Glutamate NMDA channel, Nicotinic alpha2/beta4 acetylcholine, K+ channel: hERG, Kv 4.3, Kir2.1, KCHiP2, Na+ channel Nav1.5
Enzyme – Acetylcholinesterase, COX1 & COX2, Lck tyrosine kinase, MAO-A, PDE3A phosphodiesterase, PDE4D2 phosphodiesterase
Transporter – Dopamine transporter, Norepinephrine transporter, Serotonin transporter
Hormone Receptor – Androgen receptor, Glucocorticoid receptor
Tissues included by Organ System
Cardiovascular – Heart: left atrium & ventricle, Blood Vessels: coronary, mesenteric, cerebral, pulmonary, renal, Choroid plexus
Hemolymphoid – Spleen, Tonsil
Urinary – Kidney: cortex, medulla & pelvis, Ureter, Bladder, Bladder trigone
Reproductive – Female: Ovary, Fallopian tube, Uterus myometrium, & Uterus cervix; Male: Prostate, Vas deferens, & Testis
Gastrointestinal – Esophagus, Stomach: fundus, body, antrum, & pyloric canal; Intestine: duodenum, jejunum, ileum, cecum, colon, & rectum; Gallbladder, Pancreas, Liver
Respiratory – Trachea, Lung, Primary & tertiary bronchus
Adipose – Omental (ileum)
Endocrine – Adrenal, pineal, pituitary, & thyroid glands
Blood – Mononuclear cell
Nervous System – Cerebellum, Hippocampus, Locus ceruleus, Medulla oblongata, Amygdala, Caudate, Hypothalamus anterior & posterior, Cortex: cingulate anterior & posterior, frontal lateral & medial, occipital, parietal, & temporal; Nucleus accumbens, Substantia nigra, Dorsal raphe nucleus, Spinal cord, Dorsal root ganglia (DRG)
Integumental – Foreskin, Breast tissue
Musculoskeletal – Skeletal muscle
The XPRESSWAY Profile Safety package is provided in both digital and print formats, containing the following for all 46 gene profiles:
- One quick reference print booklet to quickly determine expression pattern
- Gene expression data (raw data and interpolated gene copy number), SwissProt name and description
- Nucleotide accession number
- Sequences of forward primer, reverse primer and probe
- Full donor details for all human tissues used
Over 2300 existing profiles are immediately available and new profiles rapidly generated on request.
Creation of Custom Reports based on client need is also available.