Unnatural amino acids market research report

RITMIR027: Unnatural Amino Acids – A Market Insight Report, July 2013
© RI Technologies - www.researchimpact.com Sample Page - 1
UNNATURAL AMINO ACIDS MARKET SIZE
Scope of the Study
Unnatural amino acids are increasingly growing in research stature for pharmaceuticals, food and feed
additives, agrochemicals, and other industrial applications. Some amino acids such as isoleucine, threonine,
and hydroxyproline, exhibit second center of asymmetry and hence can exist in four sterioisomeric forms.
The growing importance as pharmaceutical intermediates has led to various methods of enantiomerically
pure preparation. Currently the pharmaceutical industry has more than 40 peptides and there are more
than 100 in a number of clinical phases. Earlier on the pharmaceutical markets did not have too much
interest in peptide research but lately they have developed the interesting peptides which are a result of
the modern day latest technological developments, strategic growth, progress in the areas of formulation
and improved drug delivery technology of peptides. More and more peptide molecules are now being
innovated, and developed by researchers, and studied for their therapeutic properties. These drug
candidates are being clinically investigated for different types of ailments. Based on the present trends, it
may be safely assumed that many biotechnology and pharmaceutical companies will now give more
attention to peptide drugs and research on them. This trend is partly due to the fact that both patients and
physicians are now accepting and acknowledging the benefits from proteinaceous therapeutics. Scientists
have also come up with solutions to the shelf life period of peptide drugs, and delivery problems related to
them.
Though synthetic peptides formed of natural amino acids dominate applications in a wide variety of fields,
it is largely felt that sooner the trend will favor peptides formed of unnatural amino acids. This is because
peptides with novel characteristics are possible only by incorporating unnatural amino acids. The novel
peptides made of unnatural amino acids open the avenue for designing not only small molecule drugs, but
also artificial sweeteners and agrochemicals apart from other applications. Artificial sweeteners are in
demand as alternative to sugar [sucrose] especially by people suffering from diabetes or obesity. Alitame is
an example of artificial sweetener developed from unnatural amino acid (D-alanine). The pyrethroid
insecticide Fluvalinate contains D-valine as a key building block. D-p-Hydroxyphenylglycine is an Important
intermediate for the synthesis of penicillin, cephalosporin-type antibiotics including amoxycillin, celadroxil
and cefatrizin and other semi-synthetic antibiotics. D-Phenylalanine is used in drugs for depression,
attention deficit-hyperactivity disorder (ADHD), Parkinson's disease, chronic pain, alcohol withdrawal
symptoms, osteoarthritis and rheumatoid arthritis. The market for Unnatural amino acid based cancer
pharmaceuticals is increasing at the fastest CAGR of 16.44%, to reach US$ 6.41billion from an estimated
US$ 2.2 billion in 2012.
Though, enormous progress has been achieved in amino acid research, the analytical techniques for
determining a more definite and accurate unnatural amino acids have not been achieved. The development
of successful analytical methods for free and binding unnatural amino acids will show the way to
clarifications in their occurrence and metabolism.
The elucidation of physiological roles of unnatural amino acids will unlock a new field in bioscience and
biotechnology.
This report gives a market insight into the different types of Unnatural Amino Acids (β-Amino Acids, β-

Amino Acid Derivatives, Cyclic Amino Acids & Derivatives, D-Amino Acids, D-Amino Acid Derivatives, DL-
Amino Acids, DL-Amino Acid Derivatives, L-Amino Acid Derivatives and Other ) and their application areas
such as R&D, Pharmaceutical, Food & Feed, Agrochemicals and Other applications.
The study includes estimates and projections for the global Unnatural Amino Acids by type and
applications. Regional Analysis is covered separately for North America (United States and Canada); Europe
(UK, Germany, Switzerland, Italy, The Netherlands, and Rest of Europe; Asia Pacific (China, Japan, India,
South Korea, Australia, and Rest of Asia Pacific); and Rest of World.
Business profiles of 62 major companies are discussed in the report. The report serves as a guide to global
Unnatural Amino Acids industry covering more than 1100 companies that are engaged in Unnatural Amino
Acids R&D, synthesis, discovery, testing and supply of derivatives, products and services. Information
related to industrial activity, corporate developments, research trends, product releases, product
developments, partnerships, collaborations, and mergers and acquisitions is also covered in the report.
Unnatural Amino Acids 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 Competitors
 Consumer Behavioral Patterns
 Other Strategic Business Affecting Data
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.

2. REPORT SYNOPSIS
Unnatural amino acids are increasingly growing in research stature for pharmaceuticals, food and feed
additives, agrochemicals, and other industrial applications. Some amino acids such as isoleucine, threonine,
and hydroxyproline, exhibit second center of asymmetry and hence can exist in four sterioisomeric forms. The
growing importance as pharmaceutical intermediates has led to various methods of enantiomerically pure
preparation. Currently the pharmaceutical industry has more than 40 peptides and there are more than 100
in a number of clinical phases. Earlier on the pharmaceutical markets did not have too much interest in
peptide research but lately they have developed the interesting peptides which are a result of the modern
day latest technological developments, strategic growth, progress in the areas of formulation and improved
drug delivery technology of peptides. More and more peptide molecules are now being innovated, and
developed by researchers, and studied for their therapeutic properties. These drug candidates are being
clinically investigated for different types of ailments. Based on the present trends, it may be safely assumed
that many biotechnology and pharmaceutical companies will now give more attention to peptide drugs and
research on them. This trend is partly due to the fact that both patients and physicians are now accepting and
acknowledging the benefits from proteinaceous therapeutics. Scientists have also come up with solutions to
the shelf life period of peptide drugs, and delivery problems related to them.
This report gives a market insight into the different types of Unnatural Amino Acids (β-Amino Acids, β-
Amino Acid Derivatives, Cyclic Amino Acids & Derivatives, D-Amino Acids, D-Amino Acid Derivatives, DL-
Amino Acids, DL-Amino Acid Derivatives, L-Amino Acid Derivatives and Other ) and their application areas
such as R&D, Pharmaceutical, Food & Feed, Agrochemicals and Other applications.
Segmentation of Unnatural Amino Acids Market
Exhibit 1. Segmentation of Unnatural Amino Acids Market by Type and Application
Type Application
β-Amino Acids Research & Development
β-Amino Acid Derivatives Pharmaceutical
Cyclic Amino Acids & Derivatives Food & Feed
D-Amino Acids Agrochemicals
D-Amino Acid Derivatives
Other (Biomarkers, Biosensors, Biocatalysts, Cosmetics,
etc.)
DL-Amino Acids
DL-Amino Acid Derivatives
L-Amino Acid Derivatives
Other Unnatural amino acids and derivatives
-Amino Acids & Derivatives, Boc protected
Amino Acids, Fmoc Protected Amino Acids, etc.)
© RIT, 2013
Global Unnatural Amino Acids market is projected to reach about US$ XX billion by 2020, from an
estimated US$ XX billion in 2012, growing at a compounded annual growth rate (CAGR) of 14.48%, during
the analysis period 2011-2020.

Many amino acid derivatives are looked upon as effective drugs for the treatment of disorders such as
ulcers, inflammation, liver problems etc. For instance, 4-hydroxyproline is found to be effective in the
prevention of cirrhosis of the liver. Similarly, N-acetyl cysteine methyl ester hydrochloride is found to be
effective in the treatment of bronchitis. Long chain 2-amino alcohols exhibit cytotoxic, immunosuppressive,
and anti-inflammatory properties. Unnatural amino acids also form components of a variety of substances,
of which the bulk is constituted by antibiotics. An antibiotic may accommodate unnatural amino acid in its
side chain, or it can be a peptide containing one or more unnatural amino acids along with the natural
ones.
Both β-amino acids and D-amino acids are constituents of several antibiotics. (3S)-β3-lysine is a β-amino
acid that forms an important constituent of the antibiotics Streptocrocyn and Streptomycin F. β2-tyrosine is
a component of Edeines, which constitute a group of antibiotic peptides. ADDA, chemically known as
(2S,3S,4E,6E,8S,9S)-3-amino-9-methoxy-2,6,8-trimethyl-10-phenyldeca-4,6-dienoic acid, is a β-amino acid
that forms part of the antibiotics such as microcystin, nodularin, and cyanovinfin.
D-amino acids form important components of several semi-synthetic antibiotics. D-lysine and D-cysteine
are found in some of the ß-lactam antibiotics. D-aspartic acid, D-glutamine, D-ornithine, and D-
phenylglycine are unnatural amino acid constituents of the antibiotic Bacitracin-A. D-serine is found in the
antibiotic cycloserine meant for the treatment of tuberculosis. D-valine is a constituent of the antibacterial
compounds Actinomycin D and Valinomycin. D-phenylalanine is a component of Polymyxin, Gramicidin S,
and Tyrocidin A, which are all antibacterial peptides.
Exhibit 2. Unnatural Amino Acids - Global Volume Market Estimations & Predictions (2005-2010) in
Million Metric Tons
Year Volume
2005 XX
2006 XX
2007 XX
2008 XX
2009 XX
2010 XX
CAGR% 11.10
© RIT Figures, 2013
2005 2006 2007 2008 2009 2010
US$ Million

Exhibit 3. Unnatural Amino Acids - Global Volume Market Estimations & Predictions (2011-2020) in
Million Metric Tons
Year Volume
2011 XX
2012 XX
2013 XX
2014 XX
2015 XX
2016 XX
2017 XX
2018 XX
2019 XX
2020 XX
CAGR% 11.10
2011 2012 2013 2014 2015 2016 2017 2018 2019 2020
US$ Million

Exhibit 4. Unnatural Amino Acids - Global Value Market Shares (2008, 2012 & 2020) by Type for D-Amino
Acid Derivatives, L-Amino Acid Derivatives, Cyclic Amino Acid & Derivatives, β-Amino Acid Derivatives, D-
Amino Acids, β-Amino Acids, DL-Amino Acids, DL-Amino Acid Derivatives and Other
Year/
Type
D-Amino
Acid
Derivatives
L-Amino
Acid
Derivatives
Cyclic Amino
Acid &
Derivatives
β-Amino
Acid
Derivatives
D-Amino
Acids
β-Amino
Acids
DL-Amino
Acids
DL-Amino
Acid
Derivatives
Other Total
2008 XX XX XX XX XX XX XX XX XX 100.00
Modern drug discovery research is increasingly experimenting with unnatural amino acids, the non-
proteinogenic amino acids, either natural or chemically synthesized. Their unlimited structural diversity and
versatile applications are being used as chiral building blocks and molecular scaffolds in building
combinatorial libraries. These molecules are powerful ingredients in therapeutic peptidomimetics and are
used as molecular probes which can assimilate the biological systems better. They show improved in vivo
stability, better potency, oral absorption, tissue distribution, and better and selective responses. Unnatural
amino acids are increasingly being used to alter the peptide’s tertiary structure. Drug candidates with side
chain modifications meet and match their biological targets. The pharmaceutical industry accounts for
almost 80% of chiral market revenues.

3. MARKET DYNAMICS
Exhibit 5. Unnatural Amino Acids - Global Value Market Estimations & Predictions (2005-2010) by
Geographic Region for North America, Europe, Asia-Pacific and Rest of World in US$ Million
Year/Region North America Europe Asia - Pacific Rest of World Total
2005 XX XX XX XX XX
2006 XX XX XX XX XX
2007 XX XX XX XX XX
2008 XX XX XX XX XX
2009 XX XX XX XX XX
2010 XX XX XX XX XX
CAGR% XX XX XX XX 14.48
2005 2006 2007 2008 2009 2010
US$ Million
North America Europe Asia - Pacific Rest of World

Exhibit 6. Unnatural Amino Acids - Global Value Market Estimations & Predictions (2011-2020) by
Geographic Region for North America, Europe, Asia-Pacific and Rest of World in US$ Million
Year/Region North America Europe Asia - Pacific Rest of World Total
2011 XX XX XX XX XX
2012 XX XX XX XX XX
2013 XX XX XX XX XX
2014 XX XX XX XX XX
2015 XX XX XX XX XX
2016 XX XX XX XX XX
2017 XX XX XX XX XX
2018 XX XX XX XX XX
2019 XX XX XX XX XX
2020 XX XX XX XX XX
2011 2012 2013 2014 2015 2016 2017 2018 2019 2020
US$ Million

Exhibit 7. Unnatural Amino Acids - Global Value Market Estimations & Predictions (2005 - 2010) by
Application for R&D, Pharmaceuticals, Food & Feed, Agrochemicals and Other in US$ Million
Year/Application Research & Development Pharmaceuticals Food & Feed Agrochemical Other Total
2005 XX XX XX XX XX XX
CAGR% XX XX XX XX XX 14.48
2005 2006 2007 2008 2009 2010
US$ Million
Research& Development Pharmaceuticals Food & Feed Agrochemical Other

Exhibit 8. Unnatural Amino Acids - Global Value Market Estimations & Predictions (2011 - 2020) by
Application for R&D, Pharmaceuticals, Food & Feed, Agrochemicals and Other in US$ Million
Year/Application Research & Development Pharmaceutical Food & Feed Agrochemical Other Total
CAGR% XX XX XX XX XX 14.48
2011 2012 2013 2014 2015 2016 2017 2018 2019 2020
US$ Million
Research& Development Pharmaceutical Food & Feed Agrochemical Other

Exhibit 9. Unnatural Amino Acids by Disease Treatment - Global Value Market Estimations and
Predictions (2005-2010) in US$ Million for Neurological Disorders, Cardiovascular, Diabetes, Arthritis,
Cancer and Other
Year/Disease Neurological Disorders Cardiovascular Diabetes Arthritis Cancer Other Total
2005 XX XX XX XX XX XX XX
CAGR% XX XX XX XX XX XX 15.54
2005 2006 2007 2008 2009 2010
US$ Million
NeurologicalDisorders Cardiovascular Diabetes Arthritis Cancer Other

Exhibit 10. Unnatural Amino Acids by Disease Treatment - Global Value Market Estimations and
Predictions (2011-2020) in US$ Million for Neurological Disorders, Cardiovascular, Diabetes,
Arthritis, Cancer and Other
Year/Disease Neurological Disorders Cardiovascular Diabetes Arthritis Cancer Other Total
CAGR% XX XX XX XX XX XX 15.54
2011 2012 2013 2014 2015 2016 2017 2018 2019 2020
US$ Million
NeurologicalDisorders Cardiovascular Diabetes Arthritis Cancer Other

Currently the pharmaceutical industry has more than 40 peptides and there are more than 100 in a number
of clinical phases. Earlier on the pharmaceutical markets did not have too much interest in peptide research
but lately they have developed the interesting peptides which are a result of the modern day latest
technological developments, strategic growth, progress in the areas of formulation and improved drug
delivery technology of peptides. So there are eight new peptide drugs which have been introduced into the
pharmaceutical industry of late. These eight new drugs would have been previously portrayed as being
difficult to produce on a large-scale that is required by the pharmaceutical industry. It is because of the
latest technological progress that the production of these drugs has been possible. Conventional as well as
contemporary methods have been used for the production of these new peptide drugs. The latest
achievements along with the conventional advantages of the peptides like high biological activity, low
toxicity and high specificity have made the pharmaceutical companies to focus more on peptide based
substances. In this way these potential next generation of peptide drugs could help treat a number of grave
diseases.
Pharmaceutical Intermediates Market Driven by Drug Development and
Consolidations
Unlike the chemical industry, the Pharmaceutical Intermediates industry is influenced by customer
requirements and products for specific applications. Major challenging area in the intermediates market is
drug development, which is the major driving force. Once the intermediate is developed it has huge
potential applications. Pharmaceutical Intermediate companies are expected to be well equipped with
latest technology and sophisticated equipment for the production, in order for pharmaceutical companies
to concentrate on drug development and marketing. With the ongoing consolidations in the global pharma
industry, pharmaceutical intermediate manufacturers have to rethink about their production strategies due
to significant shrinking customer base. Mergers and acquisitions are common strategies for growing
companies and this is set to have an indirect impact on the pharmaceutical intermediates market.
Overview of Peptide Therapeutics Market
Most of the major pharmaceutical companies have gradually expanded their peptide drug base thus
contributing to the robust growth of peptide drugs specifically due to enormous progress in synthesis
technology, availability of firm support materials, purification techniques, and drug delivery methodologies.
The Good Manufacturing Practices (GMP) peptide market continued to expand in spite of worldwide
economic slowdown as fresh peptide drug candidates emerged from researches and instituted therapeutic
peptide projects progressed. The requirement of peptides for research however arose at a slightly slower
rate, specifically for peptide libraries that have applications in screening drugs, validating targets, epitope
mapping and study of structure-activities.
Manufacturers of research-grade peptides in the Western countries are facing stiff competition from the
emergent Eastern country manufacturers as the latter are able to offer peptides at lower rates on account
of low operating costs. Specifically, Indian and Chinese producers are in advantageous position to provide
research peptides in the fast emerging Asian market. Some manufacturers based in Western countries are
also installing satellite facilities in Eastern regions to compete.

4. PRODUCT TECHNOLOGY RESEARCH
The Emergence of Chiral Drugs
Chiral technology has made tremendous progress so much so that it can now be developed with ease. This
has been made easier with the increase in chiral analytical techniques that are capable of differentiating
between enantiomers either during development of the drug or while monitoring its results in the body.
Despite the fact that chiral drugs have been in use much before the arrival of modern medicine, it is only
now that chiral drugs in the pharmaceutical industry has gained so much attention. This is largely due to
the understanding that enantiomers often show different bioactivity and metabolic fates. In addition there
is also a commercial reason where pharmaceutical companies have the chance to extend patent coverage
after expiry of patents on racemic drugs. This can take place through the development of the chiral switch
enantiomers with suitable bioactivity.
The usual protocol on drug design and development involves making the isomer mixtures first after which
the preferred isomer is selected. Recently there have been many developments in medicinal chemistry that
makes use of automated rapid synthesis. This is based on connecting building blocks in a particular manner
and this is combined with automated bioscreening for therapeutic activity and selectivity determination.
Information gathered must be exact to validate the use of single isomers.
Synthesis of Unnatural Amino Acids
In principle, an unnatural amino acid can be produced by procedures such as replacement of hydrogen by
fluorine in a ring structure, or phenyl by another resonant ring system, or one kind of heterocyclic ring by
another one, or a remnant from the framework of an amino acid by another remnant of one that is
analogous in shape and size. Practically all the advantageous amino acid analogues have earlier existed as
close structural isomers of amino acids that occur naturally.
So far, no efficient analogs of proline, glutamic acid, aspartic acid, alanine, threonine, cysteine, serine or
glycine have been accounted for. Probably, the biological sites that are involved in these amino acids are
governed by particular size and shape of molecule when compared to amino acids of larger size. Some of
the alterations that are performed for the production of anti-metabolites from the larger sized amino acids
are not tenable with smaller sized amino acids. This is because the resultant compounds lack appreciable
stability as in the case of fluoroglycine or substitution of sulfur for –CH2 within the molecular framework of
glutamic acid or threonine. In this regard, the non-existence of proline analog is intriguing, though the
occurrence of azetidine-2-carboxylic acid is worth mentioning. Most of the amino acid analogues could be
conceived as anti-tumor, antiviral or antimicrobial. The amino acid analogues are regularly subjected to
screening to find the possibility of anti metabolite activity to counteract bacteria. These experiments are all
documented in detail and are useful for those who want to study the effect of analogues on proliferating
bacteria.

Peptide Synthesis
Exhibit 11. Peptide Synthesis – Global Value Market Estimations and Predictions (2005 - 2010) in US$
Million for North America, Europe, Asia-Pacific and Rest of World
Year/Region North America Europe Asia-Pacific Rest of World Total
2005 XX XX XX XX XX
2006 XX XX XX XX XX
2007 XX XX XX XX XX
2008 XX XX XX XX XX
2009 XX XX XX XX XX
2010 XX XX XX XX XX
2005 2006 2007 2008 2009 2010
US$ Million

Exhibit 12. Peptide Synthesis – Global Value Market Estimations and Predictions (2011 - 2020) in US$
Million for North America, Europe, Asia-Pacific and Rest of World
2011 XX XX XX XX XX
2012 XX XX XX XX XX
2013 XX XX XX XX XX
2014 XX XX XX XX XX
2015 XX XX XX XX XX
2016 XX XX XX XX XX
2017 XX XX XX XX XX
2018 XX XX XX XX XX
2019 XX XX XX XX XX
2020 XX XX XX XX XX
2011 2012 2013 2014 2015 2016 2017 2018 2019 2020
US$ Million

Exhibit 13. Unnatural Amino Acids in Pharmaceutical Applications – Global Market Analysis by Region
(2005--2010) for North America, Europe, Asia-Pacific and Rest of World
2005 XX XX XX XX XX
2006 XX XX XX XX XX
2007 XX XX XX XX XX
2008 XX XX XX XX XX
2009 XX XX XX XX XX
2010 XX XX XX XX XX
CAGR% XX XX XX XX XX
2005 2006 2007 2008 2009 2010
US$ Million

Exhibit 14. Unnatural Amino Acids in Pharmaceutical Applications – Global Market Analysis by Region
(2011--2020) for North America, Europe, Asia-Pacific and Rest of World
2011 XX XX XX XX XX
2012 XX XX XX XX XX
2013 XX XX XX XX XX
2014 XX XX XX XX XX
2015 XX XX XX XX XX
2016 XX XX XX XX XX
2017 XX XX XX XX XX
2018 XX XX XX XX XX
2019 XX XX XX XX XX
2020 XX XX XX XX XX
CAGR% XX XX XX XX XX
Beta-Lactam (β-lactam) antibiotics are a broad class of antibiotics whose molecule has a β-lactam ring at
the centre (nucleus). They include a wide class of antibiotics such as penicillin derivatives, cephalosporins,
monobactams, carbapenems, and β-lactamase inhibitors β-lactam antibiotics are used for the prevention
and the treatment of bacterial infections.
2011 2012 2013 2014 2015 2016 2017 2018 2019 2020
US$ Million

Treatment of Other Disorders
Fertility problems
Nafarelin contains the unnatural amino acid D-2-Naphthylalanine as a constituent. This drug is a GnRH
agonist. Nafarelin can be used in the treatment of estrogen-dependent conditions
like endometriosis or uterine fibroids, to treat central precocious puberty, and also to control ovarian
stimulation in IVF. It is normally delivered via a nasal spray. Nafarelin acetate is marketed by Searle unit of
Pfizer under the brand name Synarel.
Cetrorelix is another drug meant for correcting the problems of uterine fibroids and endometriosis in
women. It is also useful in the treatment of hypertrophy of prostate gland in men. This drug is a
decapeptide consisting of D-amino acids. Its chemical composition is acetyl-D-3-(2´-naphtyl)-alanine- D-4-
chlorophenylalanine-D-3-(3´-pyridyl)- alanine-L-serine-L-tyrosine-D-citruline-L- leucine-L-arginine-L-proline-
D- alanine-amide. This drug is marketed worldwide in the name of Cetrotide by Merck for using in IVF. But
in Japan the market right for this drug is held by Shionogi and Nippon Kayaku in Japan.
Acyline and its Potential as a Contraceptive Medicine
Acyline is considered as one of the most popular and potential GnRH antagonists used as a contraceptive
and reproductive drug in human beings. Acyline is a peptide and was first successfully synthesized and
patented by the Salk Institute for Biological Studies financially supported by NICHD. Some of the major
structural changes have been incorporated in GnRH by replacing the natural amino acids with the unnatural
amino acids. The best example in this regard is the replacement of D-amino acids in the place of unnatural
L-amino acids. Scientists have been involved in carrying out intensive studies using Acyline. The early
clinical results on administering a dose of 300 ug / kg in male human being have indicated a reduction in
testosterone levels for two weeks without any visible side effects.
Exhibit 15. Therapeutic Products Containing Unnatural Amino Acids
Drugs /Compound Unnatural Amino Acids Indication Trade Name(s)
Nateglinide D-Phenylalanine
Derivatives
Type 2 diabetes Starlix
L-DOPA D- Phenylalanine Parkinson's Disease and Dopamine-
responsive dystonia (DRD)
Levodopa; Sinemet, Parcopa,
Atamet, Stalevo, Madopar,
Prolopa
Enalapril L-Homophenylalanine, D-
serine
Hypertension and some types of
chronic heart failure
VASOTEC, Renitec
Octreotide D-Tryptophan treatment of acromegaly, the treatment
of diarrhea and flushing episodes
associated with carcinoid syndrome,
and treatment of diarrhea in patients
with vasoactive intestinal peptide-
secreting tumors (VIPomas).
Sandostatin
Leuprolide D-Leucine Prostate & Breast Cancer Viadur, Eligard, Lupron
More………

Alitame
Alitame is a food additive and an artificial strong sweeter, having 2000 times higher sweetness than
sucrose. Its N- terminal end is substituted with tetramethylthietanyl-amine moiety. It is a dipeptide
composed of L-aspartic acid and D-alanine. Production of alitame involves multiple steps among two
intermediate substances - (S)-[2,5-dioxo- (4-thiazolidine)] acetic acid and (R)-2-amino-N- (2,2,4,4-
tetramethyl-3-thietanyl) propanamide.
Exhibit 16. Global Market for Alitame (2009-2020) in US$ million
Year/Country China Australia RoW Total
2009 XX XX XX XX
2010 XX XX XX XX
2011 XX XX XX XX
2012 XX XX XX XX
2013 XX XX XX XX
2014 XX XX XX XX
2015 XX XX XX XX
2016 XX XX XX XX
2017 XX XX XX XX
2018 XX XX XX XX
2019 XX XX XX XX
2020 XX XX XX XX
CAGR% XX XX XX XX
2009 2010 2011 2012 2013 2014 2015 2016 2017 2018 2019 2020
US$ Million
China Australia RoW

Fluvalinate
Tau-fluvalinate earlier known as “Fluvalinate,” a racemic fluvalinate range, originally included four
diastereoisomers. In 1994, the product gained its name tau-fluvalinate which included only two
insecticidally active diastereoisomers. Wellmark International, the manufacturer of tau-fluvalinate
emphasized much on the partially resolved version instead of racemic fluvalinate registration. Fluvalinate is
a type of artificial pyrethroid. This compound is made from D-Valine, a D- Amino acid.
UNNATURAL AMINO ACIDS – MARKET OUTLOOK
There are certain therapeutic areas that have unmet medical needs. One of them pertains to the disorders
associated with CNS. Another area of interest will be the development of novel drugs and vaccines against
viral diseases like AIDS, swine flu, avian flu, and so on. HIV infection is pandemic with 33.4 million people
living with this disease as per the latest statistics taken in 2008. Of these South Saharan Africa alone
accounts for 22.4 million, and next comes South East Asia with HIV affected people amounting to 3.8
million. Enfuvirtide [T-20] was approved by FDA for treatment of AIDS and marketed by Trimeris and Roche
in the trade name of Fuzeon. This is a short peptide. Development of anti-HIV peptide drugs is one of the
attractive areas open for companies keen on plunging into the pharmaceutical market.
Development of selective peptide receptor ligands with orally administered drug properties has progressed
rapidly in the past decade. However, the prime problem is devising of proper structure for decisive balance
of optimal pharmacological (e.g. receptor binding) and optimal pharmaceutical properties (e.g. membrane
permeability and metabolic stability). Non-natural amino acids are accepted major tool to prepare peptide
ligand mimetics with superior biological activity and proteolytic resistance.
Unnatural Amino Acids market is a rapidly growing market in the intermediates sector. Majority of the
products utilizing these compounds are pharmaceutical intermediates (β-Lactam Antibiotics). Asia-Pacific
region is acquiring lead position in global pharmaceuticals market with the balance gradually shifting from
the US and Europe to Asia-Pacific. With high growths in China, India and Singapore, the region is becoming
the largest global pharmaceuticals market. International pharmaceutical companies are setting up facilities
in the region and the regional pharmaceutical companies are acquiring international market share.
…………………………………………………………..
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 Equity Analysis
 Tapping New Markets
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Unnatural amino acids market research report

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Unnatural amino acids market research report