Aptamers Technology Advances for Men’s Health Issues

Archemix technology is based on the in vitro selection of nucleic acids. In the same way combinatorial chemistry produces millions of compounds that feed the drug discovery pipeline, in vitro selection of nucleic acids yields compounds (nucleic acids) with useful biological activities. Through this process, enormous libraries (up to 1016 unique compounds) are screened to identify individual compounds best suited to a particular application. This method allows Archemix to generate powerful new compounds, Aptamers and RiboReporters™, that meet specific commercial needs.

APTAMERS

Aptamers can be thought of as the nucleic acid antibodies. Archemix’s primary focus is to develop aptamers as a novel source of therapeutics for the treatment of acute and chronic diseases. Like antibodies, aptamers may be also be employed to address critical bottlenecks in the drug discovery process, including target validation and drug screening.

RIBOREPORTER™ SENSORS

RiboReporters™ are unique sensors in that they are able to directly convert molecular recognition into a detectible signal. Archemix is pursuing the use of RiboReporter™ Sensors in a range of applications.

Aptamers are oligonucleotides that bind to molecular targets in a manner conceptually similar to antibodies. Through the SELEX process, aptamers have been identified against numerous target types including growth factors, enzymes, immunoglobulins, receptors, viral proteins and others. The Archemix preclinical portfolio includes aptamers directed to a wide range of validated therapeutic targets (see Examples). Aptamers are similar to therapeutic antibodies, and as such, have a number of desirable characteristics for use as therapeutics, including biological efficacy, high specificity and affinity, and excellent pharmacokinetic properties. In addition, they offer specific competitive advantages such as:

  • aptamers are produced by an entirely in vitro process, which allows for the generation of initial therapeutic leads in as little as two weeks. In vitro selection allows the specificity and affinity of the aptamer to be tightly controlled, including selection against both toxic and non-immunogenic targets.
  • aptamers are able to disrupt protein-protein interactions
  • aptamers as a class have demonstrated little or no immunogenicity or toxicity.
  • aptamer therapeutics can be administered subcutaneously.
  • aptamers are chemically synthesized, allowing for lower cost and easily scaled production.
  • aptamers can be stored at room temperature as lyophilized powders.

 

Archemix and Nuvelo Close Phase Trial for Thrombin Inhibitor

Archemix and Nuvelo Close Phase I Trial for Thrombin Inhibitor, ARC183 – With “Proof of Concept” Achieved, Companies Actively Pursuing an Optimized Second Generation Molecule

By Steven Kingsley

CAMBRIDGE, Mass. and SUNNYVALE, Calif., September 21, 2005 – Archemix Corp. and Nuvelo, Inc. (Nasdaq: NUVO) today announced that they have closed a Phase 1 clinical trial evaluating ARC183 as an anticoagulant for potential use in acute cardiovascular settings such as coronary artery bypass graft (CABG) surgery. Preliminary results from the trial show that administration of ARC183 resulted in a rapid onset of anticoagulation, demonstrated stable, dose-related anticoagulation activity and that the effects of the drug rapidly reversed after administration of the drug infusion ceased. However, the amount of drug needed to achieve the desired anticoagulation for use in CABG surgery resulted in a sub-optimal dosing profile. For that reason, the companies have decided not to pursue development of ARC183, and instead are actively pursuing an optimized second generation molecule.

“This study validated the ability of ARC183 to achieve a rapid onset and offset of anticoagulation,” said Claude Benedict, M.D., Ph.D., head of clinical development at Archemix. “With these insights in hand, we feel we have a solid proof of concept that we are now applying to the development of a more potent second generation molecule.”

The Phase 1 study was an open-label dose-escalation trial designed to evaluate the safety, tolerability, anticoagulation activity and titratability of ARC183 in two cohorts. Dosing has completed in the first cohort, which included 40 healthy volunteers. The second cohort, which was to include 16 patients with coronary artery disease, was closed prior to dosing in all patients due to the decision by both companies to pursue a second generation molecule that could offer superior potency and efficacy than what was being observed with ARC183.

“There is a clear need for an anticoagulant with fewer side effects and more predictable dosing than heparin. Heparin, followed by protamine reversal, has significant limitations such as bleeding, heparin-induced thrombocytopenia (HIT), erratic anticoagulant effect and hypotension,” said Steven R. Deitcher, M.D., vice president of medical affairs for Nuvelo. “We are encouraged by the preliminary data from this trial and are optimistic that we will identify a more potent product candidate that meets the high standards that Archemix and Nuvelo have set.”

About the Collaboration
In January 2004, a worldwide collaboration agreement was formed between Archemix and Nuvelo for the development and commercialization of anti-thrombin aptamers. Under the terms of the agreement, Archemix will initially lead development and be responsible for all clinical development activities. Nuvelo will have the option to lead commercialization efforts in which both companies may participate. As part of the transaction, Archemix and Nuvelo will equally share all costs associated with the development and marketing of anti-thrombin aptamers and will have 50/50 ownership of the compound.

About Archemix
Archemix Corp. is a privately-held biopharmaceutical company based in Cambridge, Massachusetts. The company’s mission is to develop aptamers as a class of directed therapeutics for the treatment of human disease. Aptamers are single-stranded nucleic acids that form well-defined three-dimensional shapes, allowing them to bind target molecules in a manner conceptually similar to antibodies. Aptamers combine the optimal characteristics of small molecules and antibodies, including high specificity and affinity, chemical and biological stability and immunogenicity and the ability to target protein-protein interactions. In contrast to monoclonal antibodies, aptamers are chemically synthesized rather than biologically expressed, offering a significant cost advantage. Because of their unique properties and proven efficacy, aptamers are a superior alternative to biologics and small molecules and will be a major class of drugs for the treatment of unmet medical needs.

Archemix’s aptamer expertise is complemented by a dominant patent estate comprised of over 220 issued and 230 pending patents covering the identification, composition and use of therapeutic aptamers. In addition to the company’s core aptamer generation technology, Archemix possesses strong expertise in both preclinical and clinical drug development. Further information about Archemix can be found at http://www.archemix.com.

For further information or to speak with Dr. Errol De Souza, president and chief executive officer, please contact Davia Temin of Temin and Company at 212-588-8788 or news@teminandco.com.

About Nuvelo
Nuvelo, Inc. is dedicated to improving the lives of patients through the discovery, development and commercialization of novel drugs for acute cardiovascular and cancer therapy. Nuvelo’s clinical pipeline includes alfimeprase, a direct acting thrombolytic in Phase 3 trials for the treatment of acute peripheral arterial occlusion (PAO) and catheter occlusion and rNAPc2, an anticoagulant currently in Phase 2 trials that inhibits the factor VIIa and tissue factor complex. Nuvelo recently identified NU206 as a preclinical development candidate from its proprietary research programs and expects to leverage expertise in secreted proteins and antibody discovery to expand its pipeline and create partnering and licensing opportunities.

Information about Nuvelo is available at our website at www.nuvelo.com or by phoning 408-215-4000.

This press release contains “forward-looking statements” regarding the progress and potential therapeutic benefits of Archemix’s and Nuvelo’s collaborative research and development programs. These statements are hereby identified as “forward-looking statements” for purposes of the safe harbor provided by the Private Securities Litigation Reform Act of 1995. Such statements are based on our management’s current expectations and involve risks and uncertainties. Actual results and performance could differ materially from those projected in the forward looking statements as a result of many factors, including, without limitation, uncertainties relating to drug discovery; clinical development processes; enrollment rates for patients in our clinical trials; changes in relationships with strategic partners and dependence upon strategic partners for the performance of critical activities under collaborative agreements; the impact of competitive products and technological changes; uncertainties relating to patent protection and uncertainties relating to our ability to obtain funding. These and other factors are identified and described in more detail in Nuvelo filings with the SEC, including without limitation Nuvelo’s recent annual report on Form 10-K for the year ended December 31, 2004 and subsequent filings. We disclaim any intent or obligation to update these forward-looking statements.

Aptamer Therapeutics: A New Frontier in Drug Development

Aptamer Therapeutics: A New Frontier in Drug Development

Article by Steven Kingsley

Archemix is the biopharmaceutical company leading the development of aptamers as a new class of directed therapeutics for the prevention and treatment of chronic and acute disease.

Archemix believes the unique properties of aptamers hold extraordinary potential in the fast-breaking world of drug discovery and development. Because of their unequaled specificity for their molecular targets, aptamers provide a promising alternative to conventional therapeutic approaches. Aptamers can be used in a wide range of disease areas, including many of those currently addressed by protein-based therapeutics. Aptamers demonstrate little to no immunogenicity or toxicity, and can be produced quickly and economically.

With a portfolio of over 300 patents and patent applications, Archemix holds the key to the development of aptamer technology and its implications for the pharmaceutical industry. We are committed to using our expertise to aggressively pursue drug discovery and development for the benefit of all.

Archemix Announces Milestone Achievement

Archemix Announces Milestone Achievement with Candidate Selection
by Eyetech as Part of Broad Collaboration to Discover and Develop Therapeutic Aptamers for Ophthalmology

 CAMBRIDGE, Mass., June 22 /PRNewswire/ — Archemix Corp. announced today
that Eyetech Pharmaceuticals, Inc. has formally selected and nominated its
first pre-clinical candidate pursuant to the parties’ collaboration agreement,
which was signed in 2004.

The pre-clinical candidate selected by Eyetech is an aptamer directed
against the target Platelet Derived Growth Factor-B (PDGF-B) for potential use
in neovascular age-related macular degeneration (neovascular AMD). In addition
to uses as a single agent, pre-clinical studies have also demonstrated that
aptamers directed against PDGF-B may provide additional benefit when used in
combination with Macugen(R) (pegaptanib sodium injection) for neovascular AMD.
In conjunction with this milestone, Archemix received an undisclosed payment
from Eyetech.

“Eyetech is pleased to announce that a candidate has been selected,”
stated Dr. David Guyer, Chief Executive Officer of Eyetech Pharmaceuticals.
“The speed with which we were able to select this candidate is indicative of
the quality of our collaboration and the science behind it. We view this
selection as an important step in building and deepening our product pipeline.
The use of combination therapy may represent the future direction of
ophthalmic treatment, and the opportunity to test an anti-PDGF aptamer with
Macugen places us on the cutting edge of this potential new paradigm of
treatment.”

“For Archemix, this candidate milestone demonstrates the value of our
expertise in therapeutic aptamers and our commitment to this collaboration,”
stated Dr. Errol De Souza, President and Chief Executive Officer of Archemix.
“The selection of a development candidate in less than one year after the
agreement was signed shows that our proprietary selection methods and know-how
translate into rapid discovery of high quality drug candidates. We look
forward to Eyetech using their extensive expertise to develop this and other
candidates that come out of this collaboration.”

Eyetech’s compound Macugen is being marketed with Pfizer Inc for the
treatment of all types of the neovascular AMD, the leading cause of
irreversible vision loss in developed countries in people over 60 years of
age. In addition, Eyetech and Pfizer are conducting a Phase 2 clinical trial
for the use of Macugen for the treatment of diabetic macular edema (DME), a
leading cause of blindness in younger people. Macugen is also being studied
for other indications including retinal vein occlusion.

About Aptamers
Aptamers are single-stranded nucleic acids that form well-defined three-dimensional shapes,
binding target molecules in a manner conceptually similar
to antibodies. Aptamers have a number of desirable characteristics for use as
therapeutics, including clinically demonstrated biological efficacy, high
specificity and affinity, and excellent pharmacokinetic properties.

About Archemix
Archemix Corp. is a privately held biopharmaceutical company based in
Cambridge, Massachusetts. The company’s mission is to develop aptamers as a
class of directed therapeutics for the treatment of human disease. Because of
their unique properties and proven efficacy, aptamers are a superior
alternative to biologics and small molecules and will be a major class of
drugs for the treatment of unmet medical needs.

Archemix’s aptamer expertise is complemented by a dominant patent estate
comprised of over 220 issued and 230 pending patents covering the
identification, composition and use of therapeutic aptamers. In addition to
the company’s core aptamer generation technology, Archemix possesses strong
expertise in both pre-clinical and clinical drug development. Further
information about Archemix can be found at http://www.archemix.com.

For further information or to speak with Dr. Errol De Souza, please
contact Davia Temin of Temin and Company at 212-588-8788 or
news@teminandco.com.

Boston Scientific Chief Financial Officer, Lawrence C. Best, Joins Archemix Corp. Board of Directors

Boston Scientific Chief Financial Officer, Lawrence C. Best,
Joins Archemix Corp. Board of Directors

 CAMBRIDGE, MA April 26, 2005 Archemix Corp., the privately-held
biopharmaceutical company focused on discovering and developing aptamer-based
therapeutics, announced today that Lawrence C. Best has been appointed to the
Companys Board of Directors.  In addition to his responsibilities as a
Board member, Mr. Best qualifies as an Audit Committee Financial Expert in
accordance with Regulation S-K 401(h) and the rules implementing Section 407 of
the Sarbanes-Oxley Act.

Mr. Best currently serves as Executive
Vice President and Chief Financial Officer of Boston Scientific Corporation. He
brings more than 30 years of financial experience to Archemix.  Prior to
his work with Boston Scientific, Mr. Best was a partner in the accounting firm
of Ernst & Young, where he specialized in serving multinational companies in
the high technology and life sciences fields. He served a two-year fellowship at
the Securities and Exchange Commission from 1979 to 1981 and a one-year term as
a White House-appointed Presidential Exchange Executive in Washington. Mr. Best is also a Director and Audit
Committee Financial Expert for Biogen Idec and Haemonetics Corporation.

We are
privileged to have someone of Larrys experience and knowledge join our Board,
commented Dr. Errol De Souza, Chief Executive Officer of Archemix. “Larry brings
an impressive record of financial expertise and strategic management and has
been a key member of the Boston Scientific executive team that is credited with
building one of the foremost companies in the medical device industry.
Dr. De Souza also stated that filling the role of financial expert is an
important step for Archemix as we continue to evolve our Board to meet the
requirements of a public company.

Archemix is at an exciting stage of its development,
said Mr. Best. The Companys aptamers have the potential to bring forth a new
class of therapeutics for the treatment of acute and chronic diseases. I look
forward to contributing to Archemix as the company strives to meet its strategic
initiatives and develops its portfolio of aptamer therapeutics.

About Aptamers

Aptamers
are single-stranded nucleic acids that form well-defined three-dimensional
shapes, allowing them to bind to target molecules in a manner that is
conceptually similar to antibodies. Aptamers combine the optimal characteristics
of small molecules and antibodies, including high specificity and affinity,
chemical and biological stability, low toxicity and immunogenicity and the
ability to target protein-protein interactions. In contrast to monoclonal
antibodies, aptamers are chemically synthesized rather than biologically
expressed, offering a significant cost advantage. As therapeutic agents,
aptamers have demonstrated clinical biological efficacy and have excellent,
tunable pharmacokinetic properties.

About Archemix
Corp.

Archemix
Corp. is a privately-held biopharmaceutical company based in
Cambridge, Massachusetts. The company’s
mission is to develop aptamers as a class of directed therapeutics for the
treatment of human disease. Because of their unique properties and proven
efficacy, aptamers are a superior alternative to biologics and small molecules
and will be a major class of drugs for the treatment of unmet medical needs.

Archemix’s aptamer expertise is complemented by a
dominant patent estate comprised of over 220 issued and 230 pending patents
covering the identification, composition and use of therapeutic aptamers. In
addition to the company’s core aptamer generation technology, Archemix possesses
strong expertise in both preclinical and clinical drug development. Further
information about Archemix can be found at
http://www.archemix.com.
 

Archemix Names Page

Archemix Names Page
Bouchard Senior Vice President of Preclinical Drug Discovery and Development

 CAMBRIDGE, Mass., Nov. 4 /PRNewswire/ — Archemix Corp., the privately-held
biopharmaceutical company discovering and developing aptamer therapeutics,
announced today the appointment of Dr. Page Bouchard as Senior Vice President of
Preclinical Drug Discovery and Development. Dr. Bouchard will have
responsibility for directing the Company’s preclinical pharmacology, drug
metabolism and pharmacokinetics and drug safety efforts.

“Page has extensive experience in the area of preclinical drug discovery and
development and will lead this important multifunctional area at Archemix,” said
Dr. Errol De Souza, President and Chief Executive Officer of Archemix. “Page
possesses the unique combination of scientific experience and leadership skills
necessary to move our rapidly expanding pipeline of therapeutic aptamer leads
into clinical development. We are delighted to have Page as a part of our team
and look forward to his contributions to the development of aptamer therapeutic
products and the generation of shareholder value.”

“Archemix is at an exciting stage of its development,” commented Dr. Bouchard.
“The company’s aptamer technology has the potential to bring forth an entirely
new class of therapeutics for the treatment of acute and chronic diseases. I
look forward to leveraging my experience with both biotherapeutics and small
molecule drug candidates to this new class of therapeutics. The efficient
integration of preclinical and clinical development activities with novel
technology, rigorous science and focused strategic planning will lead to
significant product opportunities.”

Prior to joining Archemix, Dr. Bouchard was Vice President, Drug Safety
Evaluation at Millennium Pharmaceuticals. In this position, Dr. Bouchard led the
preclinical Drug Safety and Pathology organization, leading development projects
to critical clinical and regulatory milestones. Prior to joining Millennium, Dr.
Bouchard was Assistant Vice President of Pathology at Wyeth-Ayerst, heading the
discovery support pathology, toxicologic pathology, clinical pathology and
toxicogenomics efforts.

Dr. Bouchard received a bachelor’s degree from Wesleyan University and a D.V.M.
from Tufts University Veterinary School. He trained in veterinary pathology at
Cornell Veterinary School and is board certified in veterinary pathology by the
American College of Veterinary Pathologists.

About Aptamers

Aptamers are single-stranded nucleic acids that form well-defined
three-dimensional shapes, allowing them to bind to target molecules in a manner
that is conceptually similar to antibodies. Aptamers combine the optimal
characteristics of small molecules and antibodies, including high specificity
and affinity, chemical and biological stability, low toxicity and immunogenicity
and the ability to target protein-protein interactions. In contrast to
monoclonal antibodies, aptamers are chemically synthesized rather than
biologically expressed, offering a significant cost advantage. As therapeutic
agents, aptamers have demonstrated clinical biological efficacy and have
excellent, tunable pharmacokinetic properties.

About Archemix Corp.

Archemix Corp. is a privately-held biopharmaceutical company based in Cambridge,
Massachusetts. The company’s mission is to develop aptamers as a class of
directed therapeutics for the treatment of human disease. Because of their
unique properties and proven efficacy, aptamers are a superior alternative to
biologics and small molecules and will be a major class of drugs for the
treatment of unmet medical needs.

Archemix’s aptamer expertise is complemented by a dominant patent estate
comprised of over 180 issued and 220 pending patents covering the
identification, composition and use of therapeutic aptamers. In addition to the
company’s core aptamer generation technology, Archemix possesses strong
expertise in both preclinical and clinical drug development. Further information
about Archemix can be found at http://www.archemix.com/.

For further information or to speak with Dr. Errol De Souza or Dr. Page
Bouchard, please contact Davia Temin of Temin and Company at (212) 588-8788 or
news@teminandco.com.