in vitro PHARMACOLOGY 2011 CATALOG - Cerep

198 in vitro pharmacology 2011 catalog
❚ Cerep standard profiles
❚ Organ safety profile [270 assays]
full panel (271 assays)
Ref. P26
Suggested testing: 10 µM (n=2)
Q 4 weeks
(Starting on Monday: Compounds
must be received at Cerep France
site on Friday before noon.)
MODULES
Module 1 Ref. P26-m1
Module 2 Ref. P26-m2
Module 3
Module 4
Module 5
Q inquire
Ref. P26-m3
Ref. P26-m4
Ref. P26-m5
This Organ safety profile is inspired from the ICH guidelines S7A: Safety pharmacology studies
for human pharmaceuticals. The ICH S7A is into effect from June 2001 and is applied to new
chemical and biological entities, including biotechnology driven products and may be applied
to marketed pharmaceuticals when appropriate.
Safety pharmacology studies investigate the potential undesirable pharmacodynamic effects
of chemicals or pharmaceutical compounds on vital organs or systems which are essential for
sustaining life. The ICH Safety Expert Working Group has developed a hierarchy of organ
systems with respect to their life supporting functions. The most important functions are those
of the cardiovascular, respiratory or central nervous systems. Drug induced effects on these
systems should be investigated prior to the first administration of substances to humans. Other
organ systems (e.g. the renal or gastrointestinal system), the functions of which can transiently
be disrupted by adverse pharmacodynamic effects without causing irreversible harm, are of
less immediate investigative concern (S. Whitebread et al., (2005), DDT, 10:1421-1433 –
R. Porsolt et al., (2005), Drug. Dev. Res., 64:83-89).
The objective of safety pharmacology studies are: (1) To identify undesirable pharmacodynamic
properties of a substance that may have relevance to its human safety, (2) To evaluate adverse
pharmacodynamic and/or pathophysiological effects of a substance observed in toxicology
and/or clinical studies and (3) To investigate the mechanism of the adverse pharmacodynamic
effects observed and/or suspected. (CPMP/ICH/39/00)
This Organ safety profile (full panel) serves as a complementary tool, to ADME and toxicology
profiling, to select compounds for the in vitro to in vivo transition. It contains 5 modules (Each
module can be purchased separately):
1 Ubiquitous targets (15 assays): Due to their expression in the nucleus, these targets are mainly
involved in the cell cycle.
2 Regulatory-oriented targets (5 assays): These targets, adapted to high throughput screening
mode, are recommended by various regulatory guidelines.
3 Brain panel (221 assays): These targets are expressed in brain.
4 Heart panel (120 assays): These targets are expressed in heart.
5 Lung panel (124 assays): These targets are expressed in lung.
Targets expressed in more than one organ are included in multiple modules.
Rationale for the selection of the most appropriate test systems
Test systems include receptors, ion channels, transporters and enzymes (kinases and others).
Relevant test systems have been selected so that scientifically valid information can be derived.
Assays have been selected according to sensitivity and reproducibility of the test system.
Selected test systems are performed according to standardized processes.
Isoform specific assays as opposed to non-specific assays, have been used when available.
Isoforms have been selected on the basis of their pharmacology behavior (if the same, only
1isoform in the family has been selected).
The Full panel (5 modules/270 assays) is recommended to investigate the potential undesirable
pharmacodynamic effects of a substance on physiological functions.
❚ Comprehensive KINASE profile [218 assays]
Ref. P20
Suggested testing: 10 µM (n=2)
Q 3 weeks
(Starting on Monday: Compounds
must be received at Cerep France
site on Friday before noon.)
The Comprehensive kinase profile is a broad panel containing 218 biochemical kinase assays
taking into consideration the vast diversity of families.
With a 3 week-turnaround time, it allows clients to profile compounds across all major families
in the human kinome (Manning G. et al. (2002) Science, 298: 1912-1934.) and to better
understand the selectivity of their drug candidates.
Our kinases are developed using two technologies: HTRF ® and LANCE ® . A similar process as
both technologies are TR-FRET allows rapid turnaround-time and low cost for our high throughput
selectivity screening.
For list of assays included in standard profiles and updated information:
❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568
New profile Profile/module changed as compared to 2010: please go to www.cerep.com Q Standard turnaround time