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BioPortfolio | HTStec | GPCR Screening & Profiling Trends 2008

GPCR Screening & Profiling Trends 2008

HTStec's GPCR Screening & Profiling Trends 2008 report was published on 15 August 2008. This 57 page report summarizes the results of HTStec’s third global Pharma and Biotech web-based benchmarking survey on GPCR screening & profiling carried out in July 2008. The objectives of this study were to better understand: 1) recent changes in GPCR assay metrics; 2) to comprehensively document current practices and technology preferences for GPCR primary screening and compound profiling; and 3) to understand future user requirements, particularly with respect to the need for outsourced services. The report is based on 68 responses from 42 different companies/organizations.

Executive Summary

o This market report summarizes the results of HTStec's third industry-wide global Pharma and Biotech web-based benchmarking survey on GPCR screening and profiling carried out in July 2008.

o The study was initiated by HTStec to meet the specific needs, interests and focus of the survey sponsors. The main objectives were to better understand: 1) recent changes in GPCR assay metrics; 2) to comprehensively document current practices and technology preferences for GPCR primary screening and compound profiling; and 3) to understand future user requirements, particularly with respect to the need for outsourced services. The aim was to compile a reference document on GPCR screening and profiling metrics, which could be directly compared relative to HTStec's 2006 report. Equal emphasis was given to soliciting opinion from Pharma and Biotech market segments in both North America and Europe. In addition some feedback from academic screening centers was also obtained.

o The survey looked at in house and outsourced GPCR primary screening and compound profiling, as practiced today (2008) and predicted for the future (2010). Specifically the following were investigated: the proportion of GPCR screens that are cell-based and orphan receptors; use of different methods for assaying GPCR activation; preferred GPCR assay readout technology and supplier for primary screening and compound profiling; number of GPCR primary screens and compound profiling screens; number of receptors screened and profiled; number of wells per screen and profile; GPCR compound profiling approach and company organization of these activities; level of interest in outsourcing; methods of assaying GPCR activation that respondents wish to access by outsourcing; most trusted providers of outsourced GPCR assay services; decision making criteria in selecting an outsourced GPCR assay service provider; in house and outsourced budgets for primary screening and compound profiling; budget breakdown; number of FTE's supporting GPCR primary screening and compound profiling; average costs paid per well; total number of GPCR wells per lab per year; interest in GPCR label free assays, HCS/HCA approaches and multiplexed formats; and where GPCR assay service providers should focus their efforts in the future.

o The main questionnaire consisted of 29 multi-choice questions, focused mainly on assay preferences, data point and budget metrics, and 1 open-ended question. In addition, there were 7 questions related solely to survey demographics.

o The survey collected 68 responses (56 complete and 12 partially filled out) from 42 different organizations. Responses were geographically split - 50% North America, 46% Europe, 3% Asia (Excluding Japan) and 1% Rest of World.

o Survey respondents were drawn from persons and groups actively involved in GPCR screening, GPCR profiling and the outsourcing of GPCR testing and assay services to fee-for-service providers.

o Respondents came from 36 Large Pharma; 19 Small/Medium Pharma & All Biotech; 11 University, Research Institute or Government Labs; 1 Contract Research Organisation and 1 Agrochemical Company. The majority (88%) of survey respondents had a senior job role or position which was in descending order either: section/group leader; senior scientist/researcher; director; principal investigator; department head; lab manager; professor/assistant professor; and vice president.

o Survey respondents represented: 21 labs with multiple drug discovery roles; 19 primary screening (HTS) labs; 10 assay development labs; 6 hit-to-lead (lead optimization) labs; 3 other labs; 2 basic research labs; 2 life science research labs; 2 compound profiling labs; 1 leads-to-candidate (ADME Tox/preclinical research) lab; 1 secondary screening lab; and 1 therapeutic area (target identification/validation) lab.

o Survey results were expressed as an average of all survey respondents. In addition, the data was fully reanalyzed after sub-division into the following 4 survey groups: 1) Large Pharma; 2) Medium/Small Pharma & All Biotech; 3) Europe; and 4) North America.

o 73% of GPCR primary screens were cell-based and 11% were orphan receptors in 2008.

o Most respondents have organised their GPCR primary screening and compound profiling activities to be undertaken by the same group and individuals. The median total number of FTE's allocated to support both in house GPCR primary screening and compound profiling was 5 in 2008.

o The current (2008) relative use of different methods for the study of GPCR activation was: 36% Gq-Coupled - Ca2+ Flux/Mobilization Assays; 19% Gs/Gi-Coupled - Second Messenger Assays; 14% G-Protein Dependent - Functional Assays; 12% G-Protein Independent - Binding Assays; 12% G-Protein Independent - Functional Assays; and 7% Gq-Coupled - Second Messenger Assays.

o The preferred primary screening readout technologies and suppliers were: 1) G-Protein Independent - Binding Assays was Radiometric with SPA/LEADseeker from GE Healthcare; 2) G-Protein Independent Functional Assays was EFC with chemiluminescent readout from DiscoveRx; 3) G-Protein Dependent Functional Assays was Glow Luminescence from Invitrogen; 4) Gq-Coupled - Ca2+ Flux/Mobilization Assays was FLIPR & Reporter Gene Assays from MDS Analytical Technologies; 5) Gq-Coupled - Second Messenger Assays was TR-FRET from Cisbio; and 5) Gs/Gi-Coupled - Second Messenger Assays was TR-FRET from Cisbio.

o In 2008 the following median screening metrics were obtained: 5 GPCR primary screens per lab, 8 receptors screened, and 250K-500K wells per primary screen.

o The median GPCR primary screening budget allocations in 2008 were $250K-$500K per lab in house and none per lab outsourced. On average respondents allocated ~50% of their in house GPCR primary screening budget to external reagent purchases (i.e. bulk reagents & pre-packaged assay kits).

o The median cost per well for GPCR primary screening in 2008 was $0.10-$0.25 per well in house versus $1-$1.50 per well outsourced. The median total number of wells per year in 2008 for GPCR primary screening was 1 million - I.5 million in house versus none outsourced.

o The preferred approach to GPCR compound profiling was a combination of in house and outsourced panels for selected lead compounds.

o The preferred compound profiling readout technologies and suppliers were: 1) G-Protein Independent - Binding Assays was Radiometric Filter Binding from PerkinElmer; 2) G-Protein Independent Functional Assays was Label Free-Impedance-Based from MDS Analytical Technologies; 3) G-Protein Dependent Functional Assays was FRET from Invitrogen; 4) Gq-Coupled - Ca2+ Flux/Mobilization Assays was FLIPR & Reporter Gene Assays from MDS Analytical Technologies; 5) Gq-Coupled - Second Messenger Assays was TR-FRET from Cisbio; and 5) Gs/Gi-Coupled - Second Messenger Assays was TR-FRET from Cisbio.

o In 2008 the following median profiling metrics were obtained: 5 GPCR profiling screens per lab, 8 receptors profiled, and 1K-5K wells per profiling screen.

o The median GPCR compound profiling budget allocations in 2008 were $25K-$50K per lab in house and $25K-$50K per lab outsourced. On average respondents allocated ~50% of their in house GPCR profiling budget to external reagent purchases (i.e. bulk reagents & pre-packaged assay kits).

o The median cost per well for GPCR compound profiling in 2008 was $0.25-$0.35 per well in house versus $5-$10 per well outsourced. The median total number wells per year in 2008 for GPCR compound profiling was 2.5K-5K in house versus 1K-2.5K outsourced.

o Active outsourcing of a significant amount of GPCR testing (>25% of total undertaken) today (2008) was limited to only 2% of respondents for primary screening and 19% of respondents for compound profiling. Interest in outsourcing is expected to increase by 2010. Respondents ranked G-Protein Independent - Functional Assays as the method of GPCR primary screening and compound profiling that they most wanted to access by outsourcing.

o Cerep was rated the fee-for-service GPCR outsourcing supplier most trusted to provide rapid turnaround and reliable results. With data quality ranked the most important decision making criteria in their selection of an outsourced GPCR assay service supplier.

o There was considerable interest in new GPCR assay technology approaches with 22% of respondents having implemented label free, 16% HCS/HCA, and 7% multiplexed assays for screening and profiling.

o Lowering the price and improved data quality were the areas where respondents thought GPCR fee-for-service providers should focus their efforts going forward.

o Respondent's feedback on the unmet needs that exist today in GPCR screening and profiling and related services are documented.

o Several bottom-up models were developed to estimate the global pharma and biotech market for GPCR screening and profiling. The GPCR primary screening reagent market was estimated to be around $250 million in 2008. The in house GPCR compound profiling reagent market was estimated to be around $40 million in 2008. The GPCR compound profiling market for outsourced services was estimated to be around $60 million in 2008. Estimates for 2010 were made and growth rates determined for 4 market segments: 1) Large Pharma; 2) Medium/Small Pharma & All Biotech; 3) Europe; and 4) North America.

o The value of the full report is in the survey group analysis where several interesting differences between the 4 survey groups and the average of all survey respondents are documented.

Format PDF August 2008

Table of Contents
Price: $2,475.00 / €1,654.29

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