GPCR Drug targets Market Report by 78398

GPCR DRUG TARGETS MARKET SIZE Scope of the Study G-Protein Coupled Receptors (GPCR) report covers the types of GPCR Families and the various ligands targeting GPCR. The GPCR families covered include Rhodopsin, Secretin, Metabotropic Glutamate and Other. The Ligands targeting GPCRs include Proteins/Peptides, Biogenic Amines, Lipids and Other. The report provides a market analysis of each of the Families and ligands targeting GPCRs by their respective categories. The study includes estimates and projections for the total global GPCR – Drug targets market and also key regional markets that include North America, Europe, Japan, Asia-Pacific (excluding Japan) and Rest of World. Estimates and projections are illustrated graphically. Business profiles of 13 major companies engaged in developing GPCR targeted drugs, GPCR cell lines and GPCR Assays are discussed in the report. The report serves as a guide to global GPCR –Drug Targets industry, covering more than 280 companies that are engaged in the development of GPCR Targeted Drugs, GPCR Assays Information related to recent product releases, Assay developments, partnerships, collaborations, and mergers and acquisitions is also covered in the report. GPCR – Drug Targets report is an ideal research tool providing strategic business intelligence to the corporate sector. This report may help strategists, investors, laboratories, pharmaceutical companies, contract research organizations, biotechnology companies and drug approval authorities in –

 Gauging Competitive Intelligence  Identifying Key Growth Areas and Opportunities  Understanding Geographic Relevance to Product  Knowing Regional Market Sizes and Growth Opportunities and Restraints  Keeping Tab on Emerging Technologies  Equity Analysis  Tapping New Markets Analytics and data presented in this report pertain to several parameters such as –

 Global and Regional Market Sizes, Market Shares, Market Trends  Product (Global and Regional) Market Sizes, Market Shares, Market Trends  Technology Trends  Corporate Intelligence  Key Companies By Sales, Brands, Products  Consumer Behavioral Patterns  Other Strategic Business Affecting Data

RITMIR023: GPCR Drug Targets – A Market Insight Report, July 2013 © RI Technologies - www.researchimpact.com

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Research Methodology RI Technologies publishes business intelligence reports by going through a cycle of diligent research and analysis activity. Research is done using both online and offline resources. The study outline of this report is sketched on the following lines - global market analysis, regional market analysis, product segmentation, global and regional market analysis by product segment, market trends, M&A, R&D, competitive landscape, technology trends, and other key drivers. Current data helps in analyzing the future of the industry and is also helpful for doing market evaluations, and estimating the market size for the future. This report is uniquely researched and the methodology includes:

 Need and Scope of Study  Product Definitions  Segmental Analysis  Regional Analysis  Exclusive Data Analytics  Corporate Intelligence  Feedback Right from concept to final compilation of this report, both primary and secondary research methods are applied. We have provided exclusive feedback forms/pre-release questionnaires for this report to use the information for authentication of our own findings. Secondary research includes government publications, investment research reports, web based surveys, website information of both companies and markets, and other offline resources such as print publications and CDs. Our compilation of easy to navigate PDF reports are essential value addition resources for leading and growing companies.

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II. REPORT SYNOPSIS GPCR There are three major groups of membrane receptors in mammalian cells, namely, GPCRs [G-Protein Coupled Receptors], ion channels, and tyrosine kinases. Among them, GPCRs constitute the largest group regulating almost every aspect of physiology and behavior. They form a link between external agents and physiological events such as : 

Sensory Perception

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Cell Growth &

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Hormonal Regulation

The phenomenon in which external stimuli bring about an expanding cascade of intracellular events culminating in specific cellular responses is called signal transduction. The complex involved in this phenomenon consists of GPCR and G-Protein. This assembly is the most diverse among the cell surface receptors. Future progress may relate discoveries to the development of new medicines. At present the development of drugs is centered on the discovery of chemicals that influence the ability of the ligands to bind with the G-Protein Coupled Receptor or GPCR. This will either accelerate or inhibit the cellular process. In the in-depth studies pertaining to the G-Protein Coupled Receptor family, the role of chemical biology has been significant since the beginning. This is because the majority of the vital group of targets is for improvement in therapeutics. These receptors are defined by a common structural feature which is comprised of seven hydrophobic trans-membrane segments. These proteins are also known as 7 TM, seven trans-membranes or serpentine receptors because in all cases the signaling through heterotrimeric G-Proteins is not exhibited.

G-Protein History of G-Proteins G-Proteins form a link between the cell surface receptors and the intracellular events by interacting with GTP. The existence of a link between the GPCR and adenylyl cyclase was suggested by Birnbaumer and Rodbell [1969] and Rodbell et al [1971], and subsequently by Ross and Gilman [1977]. This link was identified as Gs, a heterotrimeric G-Protein. In 1970, in a mutant cell line, lack of response to ligand was observed in spite of the presence of intact ligand receptor and amplifier. This led to the suggestion that an intermediary [G-Protein] is present. The purified intermediary was obtained by Gilman [1980]. The complete pathway was elucidated by Northup [1980] by way of adding the purified G-Protein. Rodbell [1960] suggested the role of GTP in cell signaling. However, the role of GTP was not realized because the preparations meant for analysis were a mixture of cAMP and GTP. It was revealed that upon

RITMIR023: GPCR Drug Targets – A Market Insight Report, July 2013 © RI Technologies - www.researchimpact.com

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hydrolysis of GTP, the G-Proteins directed activation or inhibition of enzymes and ion channels, thus allowing the external agents to regulate the intracellular events. In 1980 Martin Rodbell published a review that paved the way for the identification of G-Protein that reduces cAMP. Gilman could isolate the heterotrimeric G-Protein that elevated the cAMP levels. Rodbell and Gilman shared Nobel Prize in Physiology/Medicine in 1994 for their discovery of G-Proteins and their importance in signal transduction.

Segmentation of GPCR – Drug Targets Exhibit 1. Segmentation of Global GPCR – Drug Targets Market by GPCR Families and by Type of Ligands Targeting GPCR GPCR Families

Ligands Targeting GPCR

Rhodopsin

Peptides or Proteins ^

Secretin

Biogenic Amines

Glutamate

Lipids

Other1

Other2

Other1 Includes Adhesion, and Frizzled/Taste Other2 Includes Amino Acids, Nucleotides, and Cations ^Including Enzymes © RIT, 2013

RITMIR023: GPCR Drug Targets – A Market Insight Report, July 2013 © RI Technologies - www.researchimpact.com

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Global Market Analysis Global market for GPCR - Drug Targets is projected to reach about US$ XX.XX billion by 2020 from an estimated US$ XX.XX billion in 2012, growing at a compounded annual growth rate (CAGR) of XX.XX % during the analysis period 2005-2020. Exhibit 2. GPCR Drug Targets – Global Value Market Estimations and Predictions (2005-2020) in US$ Billion Year

Value

2005

XX.XX

2006

XX.XX

2007

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2008

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2009

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CAGR %

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US$ Billion

2005 2006 2007 2008 2009 2010 2011 2012 2013 2014 2015 2016 2017 2018 2019 2020

RITMIR023: GPCR Drug Targets – A Market Insight Report, July 2013 © RI Technologies - www.researchimpact.com

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III. MARKET DYNAMICS Market Overview Completion of the Human Genome Sequencing researchers has come across many new members of GPCRs Exhibiting physiological functions never known before. These have gained importance in the study of several pharmacology drug-discovery projects because: 

The location of the GPCRs on the cell surface makes them easy targets for the drugs



Present everywhere as they play an important role in almost every system of the human body

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The human genome has hundreds of distinctive GPCRs whose role in the body is yet to be discovered thereby making them potential targets for many drugs

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Because of the large number of physiological functions it is capable of, this receptor family is regarded as a tractable drug target.

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About a quarter of the total prescriptions and drug sales are directed at GPCRs

Of the top 200 best selling drugs on the market, 25% target G-Protein Coupled Receptors (GPCRs), making this class of drug targets one of the most heavily investigated by pharmaceutical companies for drug discovery and development. Because of the large number of physiological functions it is capable of, this receptor family is regarded as a tractable drug target. Thus GPCRs have become the most sought after drug discovery targets by the industry dealing in pharmaceuticals. This has lead to the development of several drugs that have the highest sales in the present market GPCR-targeted drugs have met with success in the past and the potential of GPCR research to be undertaken in the future, together give an indication that these will be the pharmaceutical industry’s main therapeutic drug discovery targets. Nearly half of the naturally targeted receptors interact naturally with Proteins/Peptides. The highest number of non targeted receptors is peptide binding receptors indicating a potential for new drug discovery. The Biogenic Amines binding receptors have the highest number of successfully therapeutically targeted receptors due to their relevance in the treatment of cardiovascular diseases.

GPCR-Drug Targets Global market for GPCR - Drug Targets is projected to reach about US$ XX.XX billion by 2020 from an estimated US$ XX.XX billion in 2012, growing at a CAGR of XX.XX % during the analysis period 2005-2020. North America is estimated as the largest market for GPCR - Drug Targets in 2012 with a share of XX.XX % valued at US$ XX.XX billion and is projected to reach US$ XX.XX billion by 2020 to retain its position with a share of XX.XX %.

RITMIR023: GPCR Drug Targets – A Market Insight Report, July 2013 © RI Technologies - www.researchimpact.com

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Europe is projected to be the second largest (XX.XX % market share in 2020). Asia-Pacific is projected to be the fastest growing (XX.XX % during 2005-2020) market. In 2012, the market for Europe and Asia-Pacific is estimated at US$ XX.XX billion and US$ XX.XX billion respectively. Exhibit 3. GPCR - Drug Targets -Global Value Market Estimations & Predictions (2005 -2020) by Geographic Region for North America, Europe, Japan, Asia-Pacific^ and Rest of World in US$ Billion Year /Region

North America

Europe

Japan

Asia-Pacific

Rest of World

Total

2005

XX.XX

2006

XX.XX

2007

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2008

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2009

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2011

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2012

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CAGR%

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US$ Billion

2005

2006

2007

North America

2008

2009

2010

Europe

2011

2012 Japan

2013

2014

2015

2016

2017

Asia-Pacific

RITMIR023: GPCR Drug Targets – A Market Insight Report, July 2013 © RI Technologies - www.researchimpact.com

2018

2019

2020

Rest of World

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Exhibit 4. GPCR - Drug Targets - Global Value Market Shares (2010, 2015 & 2020) by Geographic Region for North America, Europe, Japan, Asia-Pacific^ and Rest of World Year /Region

North America

Europe

Japan

Asia-Pacific

Rest of World

Total

2010

XX.XX

100.00

2015

XX.XX

100.00

2020

XX.XX

100.00

THE OUTLOOK Global market for GPCR - Drug Targets is projected to grow at more than XX.XX % compounded annually from 2005 through 2020. North America, the leading market (XX.XX % of global market share in 2010) for GPCR - Drug Targets presently is projected to retain the leading position during the analysis period with its share dropping to XX.XX % by 2020. Asia-Pacific is the fastest growing (XX.XX % during 2005-2020) market for GPCR - Drug Targets. Asia-Pacific is followed by Japan in terms of growth rate with a CAGR of XX.XX %. GPCRs together with G-Proteins are known to have a very important role in physiology and diseases including diseases of the sense organs, digestive tract, endocrine system, and respiratory system and their processes. GPCRs are known to be attractive drug targets for several reasons. Firstly the location of the GPCRs on the cell surface makes them easy targets for the drugs. In addition, GPCRs are generally present everywhere as they play an important role in almost every system of the human body. As the human genome project is completed unknown functions of many of the genes expressing into GPCRs can be unraveled and thereby making them potential drug targets proteins in drug development. Molecular Devices Corporation’s Transfluor technology is used for detecting compounds activity against orphan or known GPCR targets. It is used to screen for G-Protein Coupled Receptors (GPCRs) ligands and other potential drugs that regulate GPCRs. 7TM Pharma, Arena Pharmaceuticals are world leaders in discovery and development of GPCR Targeted drugs. The GPCR targeted drugs which now account for XX.XX % of the pharmaceutical market is expected to increase nearly XX.XX % by 2020.

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IV. PRODUCT/TECHNOLOGY RESEARCH Much prior to the understanding of molecular and biochemical activities of GPCRs, the use of natural products were in vogue. These products were opium, ergot and belladonna. They were extracted from various plant sources to obtain pharmacological effects at targets that were unknown at that time for the treatment of a host of illnesses. It was only in the advent of the 20th century that the concept of receptors was first presented by Paul Ehrlich. He proposed that drug substances had the ability to interact with discrete chemoreceptors and generate pharmacological effects. The description of the activity of compounds at receptors which were later recognized as GPCRs came to be known through the studies of eminent pharmacologists like James Black, R.P.Ahlquist, Otto Loewi and Henry Dale. This lead to the formulation of rational drug design basis. The beginning of molecular biological approaches resulted in the recognition of the GPCR superfamily of about 750 genes. These comprise approximately 1% of the genome. There is still working remaining on the elucidation of the functions and endogenous ligands of a high quantity of these receptors, known as orphan GPCRs. Drug discovery had a significant impact from the cloning of GPCRs. This led to the recognition of proteins and genes of those receptors in a biomolecular perspective. These receptors were earlier described pharmacologically. An example of this is those for biogenic amines. The additional iso-form subtypes of these receptors, and new, formerly uncharacterized GPCRs whose functions are only presently being unraveled and for which drugs are being developed. The GPCRs can be grouped into four families which have sequence similarity as their foundation. The largest of the three is Family A which is illustrated by the Rhodopsin receptor. Many members of Family A, share similar sequence motifs. The sequence motifs are namely, seventh transmembrane NPXXY domains and the third transmembrane DRY. The Family A is comprised of about 350 olfactory GPCRs. This includes approximately 90% of total GPCRs and about 70% of non- olfactory GPCRs. Family A is illustrated by the biogenic amine, peptide, nucleotide, prostanoidreceptors and others. . Examples of biogenic amines are histaminergic, dopaminergic, muscarinic and adrenergic. Examples of biogenic peptides are angiotensin II and opioid. Family B is grouped as per the structural similarity to the Secretin receptor. The structural authentication of Family B is a large extracellular N-terminal domain. This domain is comprised of about 40 orphan GPCRs and 25 liganded. The members of Family B are illustrated by the gonadotropin- and calcitonin-releasing hormone receptors.

GPCR Tractability: Current Therapeutics Pharmaceutical companies have historically looked upon these cell surface receptors as enticing drug targets. Above 30% of all prescription drugs are known to be directed at lesser than 50 known receptors. There is one distinct characteristic of this receptor family because of which it is regarded as a tractable drug target. This is because of the large number of physiological functions it is capable of.

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Those are the functions which include homeostatic mechanisms, central nervous system function and the growth that is regulated per the activation of GPCRs that is brought about by their endogenous ligands. The homeostatic mechanisms comprise of metabolic, gastrointestinal and cardiovascular processes. The characteristic of this receptor helps in the provision of a high quantity of potentially selective targets. The dysregulation of these pathways many a time results in pathophysiological consequences that can be improved by selective antagonists. These antagonists help to reverse those disease states which are caused by excessive stimulation of the concerned GPCR. On a converse basis it is seen that selective agonists stimulate GPCR pathways which are found to be hypo functioning, which results in the reversal of a disease process physiologically. The finding of naturally occurring mutant GPCRs in humans has highlighted the role played by GPCRs in various disease states. These naturally occurring mutant GPCRs in humans add to pathologic conditions. This is achieved through the utilization of transgenic animals that have their genes knocked out or knocked in, to permit a deeper comprehension of the in vivo phenotype of the GPCR. This takes into account genes that are liganded as well as the orphan GPCRs. There is one more main viewpoint of the tractability of GPCRs as drug targets. This is the capability for designing small molecules with selectivity and potency of a high order. This potency is the outcome of the specificity in the primary structures of the binding sites found in other GPCRs selected from isoforms and families. And those chosen from selective localization of the targeted GPCR in tissues that are accountable for the regulation of the targeted physiological function. These characteristics will be dealt with in more detail subsequently, starting with a short overview of the popularity presently being enjoyed by GPCRs as targets for drugs used by human beings as on date. Exhibit 5. GPCR Targeted Cancer Drugs Trade Name/ Generic Name

Company

GPCR Target

Indication

Zoladex / Goserelin

AstraZeneca plc (UK)

GnRH Receptors

Prostate Cancer

Flomax /Tamsulosin Hydrochloride

Boehringer Ingelheim GmbH (Germany)

β1-adrenergic

BPH

Lupron / Leuprolide

Takeda Pharmaceutical Co., Ltd. (Japan)

GnRH

2005 US$ 1004 Million

2006 US$ 1008 Million

€ 1020 Million

¥ 62.4 Billion

Prostate Cancer

2007

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Research – As Good as the Methodology is! RITMIR023: GPCR Drug Targets – A Market Insight Report, July 2013 © RI Technologies - www.researchimpact.com

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

Gauging Competitive Intelligence



Identifying Key Growth Areas and Opportunities



Understanding Geographic Relevance to Product



Knowing Regional Market Sizes and Growth Opportunities and Restraints



Keeping Tab on Emerging Technologies



Equity Analysis



Tapping New Markets

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