Global Market of GPCR Screening & Profiling Trends 2013

2013-08-30
Published : Aug-2013

This market report summarizes the results of HTStec’s 5th industry-wide global web-based benchmarking survey on GPCR screening and profiling carried out in August 2013. The survey was initiated by HTStec as part of its tracking of life science marketplaces. The questionnaire was compiled to meet the needs, requirements and interests of the GPCR vendor community. The objectives were to comprehensively document current practices and preferences in GPCR primary screening and compound profiling, and to understand future user requirements, particularly with respect to the need for new assays, approaches and the use of outsourced services. The aim was to compile a reference document on GPCR screening and profiling metrics, which could be directly compared with HTStec’s previous reports (the last one on GPCRs was published in October 2010). Equal emphasis was given to soliciting opinion from Pharma, Biotech and Academic Research market segments in both North America and Europe.

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The survey looked at both in house and outsourced GPCR primary screening and compound profiling, as practiced today (2013) and in some cases as predicted for the future (2015). Specifically the following were investigated: whether the number of GPCR primary screening targets or programs under investigation is changing; the proportion of GPCR screens that are cell-based and orphan receptors; use of different methods for assaying GPCR activation; preferred assay readout technology and supplier for GPCR screening; proportion of GPCR Ca2+ flux assays that are fluorescence-based; number of GPCR primary screens and wells per screen; approach to GPCR profiling; preferred assay readout technology and supplier for GPCR profiling; size of in house profiling panels and total wells profiled in house per year; how receptor panels are chosen; level of interest in outsourcing; methods of assaying GPCR activation that respondents wish to access by outsourcing; type of GPCR panels most interested to access at a fee-for-service provider; typical sizes of outsourced GPCR profiling panels used and total wells profiled per year at a fee-for-service providers; most trusted and most used providers of outsourced GPCR assay services; in house and outsourced budgets for GPCR screening and profiling; the breakdown of in house budgets; average costs paid per well for GPCR screening and profiling; level of interest in new assays/approaches for GPCR screening and profiling; suitability of available tools for new assays/approaches for GPCR screening and profiling; the proportion of GPCR assays that are made using primary cell lines and stem cell derived phenotypes; main barriers to the implementation of a new GPCR screening technology; where a GPCR reagent developer or assay fee-for-service provider should focus their efforts in the future; preferred way of sourcing GPCR expressing cell lines and the factors that drive decision making when sourcing; and any unmet needs in GPCR screening & profiling today.

The main questionnaire consisted of 30 multi-choice questions and 1 open-ended question. In addition, there were 7 questions related solely to survey demographics. The survey collected 96 validated responses, of these 66% provided comprehensive input. Survey responses were geographically split: 61% North America; 27% Europe; 7% Asia (excluding Japan); and 5% Japan. Survey respondents were drawn from persons or groups involved in GPCR primary screening and compound profiling in house and the outsourcing of GPCR testing to fee-for-service providers. Respondents came from 21 Large Pharma; 21 University; 17 Biotech; 12 Medium-Small Pharma; 9 Hospital/Clinic/Medical School; 6 Research Institute; 5 Academic Screening Center; 4 Government Laboratory; and 1 Other.

Most survey respondents had a senior job role or position which was in descending order: 17 senior scientists/researchers; 17 principal investigators; 13 research scientists; 13 professors/assistant professors; 8 directors; 7 section/group leaders; 7 department heads; 1 graduate/PhD student; 1 vice president; and 1 outsourcing manager.

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Respondents main group activities were: 27 basic research; 23 a combination of drug discovery roles; 11 assay development; 10 primary screening (HTS); 8 applied research; 7 hits-to-leads (lead optimization); 6 therapeutic areas; 2 secondary screening; and 2 compound profiling. Survey results were expressed as an average of all survey respondents. In addition, where appropriate the data was fully reanalyzed after sub-division into the following 5 survey groups: 1) Pharma; 2) Biotech; 3) Academic Research; 4) Europe; and 5) North America.

The median number of GPCR primary screening targets/programs under investigation in 2013 was 3. 70% of GPCR primary screens were cell-based and 17% were orphan receptors in 2013. In 2013 the relative use of different methods used to study GPCR activation was: 24% binding assays; 16% cAMP or cGMP assays; 13% Ca2+ flux/mobilization assays; 12% β-arrestin recruitment or receptor internalization; and 11% reporter gene assays. All other methods had less than 10% use. The preferred GPCR readout technologies and suppliers for GPCR activation assays used in both primary screening and compound profiling were as follows: binding assays – radiometric from PerkinElmer; β-arrestin recruitment or receptor internalization – chemiluminescence from DiscoveRx; label-free cellular changes & translocation – label-free readout from Corning; GTP

γS – radiometric from PerkinElmer; reporter gene assays – glow luminescence from Promega ; Ca2+ flux/mobilization assays – fluorescence intensity from Molecular Devices; IP3 or IP1 – TR-FRET from Cisbio; cAMP or cGMP Assays – TR-FRET from Cisbio; ERK phosphorylation assays – TR-FRET from PerkinElmer; and other phenotypic readouts – various readouts and suppliers. 44% of all GPCR Ca2+ flux/mobilization assays were fluorescence-based in 2013.

Median in house 2013 GPCR screening metrics were: 3 primary screens/year and 10K-25K wells/screen. The preferred approach to GPCR profiling was to profile selected lead compounds only in house. Median in house 2013 GPCR profiling metrics were: 2 to 3 new receptors added to the panel per year; a total of 6 to 10 receptors per panel; and 5K-10K wells profiled per year. Respondents did not have a preferred way of choosing panels when running GPCR compound profiles.

42% of respondents might outsource GPCR primary screening versus 57% might outsource GPCR compound profiling today (2013). Most want to access primary screening using β-arrestin recruitment or receptor internalization methods and compound profiling using binding assays methods. The types of GPCR panels respondents were most interested in accessing for outsourced compound profiling today (2013) were those that included all known GPCRs available. The median outsourced 2013 GPCR profiling metrics were: 6 to 10 receptors/profile and 1K-15K wells profiled per year.

PerkinElmer, Life Technologies and Cerep were ranked the most trusted and most used outsourced GPCR fee-for-service providers. Although no provider stood out way above all others. The median GPCR primary screening budget allocations in 2013 were $10K-$25K/lab in house and $5K-$10K/lab outsourced. The biggest expenditure was on bulk reagents & pre-packaged assay kits.

The median GPCR compound profiling budget allocations in 2013 were $10K-$25K/lab in house and lt;$5K/lab outsourced. The biggest expenditure was on bulk reagents & pre-packaged assay kits. The median cost/well for GPCR primary screening in 2013 was $0.35-$0.50/well both in house & outsourced.

The median cost per well for GPCR compound profiling in 2013 was $0.35-$0.5/well in house versus $0.50-$0.75/well outsourced. Functional selectivity was rated the assay/approach for GPCR primary screening and compound profiling that respondents had most interest in using/evaluating. Receptor internalization and trafficking was the assay/approach for GPCR primary screening and compound profiling where the suitability of currently available tools was rated most effective.

24% of GPCR assays were made using primary cells and 6% using stem cell derived phenotypes in 2013. Instrumentation/technology costs were the most significant barrier to new GPCR technology adoption. Receptor internalization and trafficking was rated as the area where respondents thought GPCR reagent developers should focus their efforts going forward. Offer screening services in more biologically relevant cellular backgrounds was rated as the area where respondents thought GPCR fee-for service providers should focus their efforts going forward.

Most respondents prefer to source GPCR expressing cell lines by making them in house. Cost and time were ranked the most important factors when making/sourcing GPCR expressing cell lines. Feedback on some unmet needs that exist today in GPCR screening and profiling were documented. Several bottom-up models were developed around the respondent’s annual budgets to estimate the global markets for GPCR screening and profiling. In 2013 these markets were estimated to be as follows: in house GPCR primary screening reagents – $144M; in house GPCR compound profiling reagents – $28M; outsourced GPCR primary screening – $20M; and outsourced GPCR compound profiling – $24M. The market was segmented by organization and geography. CAGR estimates for 2015 were made for the market segments.

The full report provides the data, details of the breakdown of the responses for each question, its segmentation and the estimates for the future (2015). It also highlights some interesting differences, particularly between Pharma versus the other survey groups.

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