Corporate Banner
Satellite Banner
Medicinal Chemistry
Scientific Community
 
Become a Member | Sign in
Home>News>This Article
  News
Return

Seven Steps to ‘Billion Dollar’ Drugs

Published: Tuesday, August 21, 2012
Last Updated: Tuesday, August 21, 2012
Bookmark and Share
The methodology described should make it easier to discover new biologically active prostaglandin analogues.

A highly efficient method for making prostaglandins - natural, hormone-like chemicals that have pharmaceutical applications - is reported by University of Bristol scientists this week in Nature.

Some synthetic analogues of prostaglandin are ‘billion dollar’ drugs; the prostaglandin analogue latanoprost, which is used to treat glaucoma and ocular hypertension, generates approximately $1.6 billion in sales each year.

Prostaglandins are some of the most important molecules in biology and medicine as they regulate a broad range of activities in the body, including blood circulation, digestion and reproduction.

The breadth of biological activity, coupled with their challenging molecular architecture has made prostaglandins popular targets in synthesis for over 40 years.

However, since these molecules cannot be isolated from natural sources in sufficient quantities, they have to be synthesized, but routes are lengthy.

For example, the current synthesis of latanoprost requires 20 steps and uses the methodology and strategy developed by E. J. Corey, a giant in the area of synthesis (he was awarded the Nobel Prize in Chemistry, in 1990 "for his development of the theory and methodology of organic synthesis").

Until now, despite huge synthetic effort in industry and academia, advances in the synthesis of prostaglandins since Corey’s contributions have been limited.

Professor Varinder Aggarwal, who led the research at the University’s School of Chemistry, and colleagues now report a concise synthesis of prostaglandin PGF2a, which relies on the use of an organocatalyst, a small organic molecule, to catalyze a key step in the process.

The key step not only produces a key intermediate, but it also does so with exquisite control over relative and absolute stereochemistry.

The new process uses a new disconnection which has enabled them to complete the synthesis in just seven steps. It should be possible to modify the authors’ synthetic route to obtain other known prostaglandin-based drugs, e.g. latanaprost in a more cost-effective manner and to make it easier to discover new biologically active prostaglandin analogues.

In a follow-up patent, the authors have described the application of this technology to a simple synthesis of prostaglandin-based drugs, e.g. latanoprost and bimataprost.

The methodology should now make it easier to discover new biologically active prostaglandin analogues. It is a major advance and represents a step change in the synthesis of this important class of compounds.

Professor Aggarwal said: "Despite the long syntheses and the resulting huge effort that is required for the preparation of these molecules, they are still used in the clinic, because of their important biological activity.

"Being able to make complex pharmaceuticals in a shorter number of steps and therefore more effectively, would mean that many more people could be treated for the same cost."


Further Information

Join For Free

Access to this exclusive content is for Technology Networks Premium members only.

Join Technology Networks Premium for free access to:

  • Exclusive articles
  • Presentations from international conferences
  • Over 2,900+ scientific posters on ePosters
  • More than 4,200+ scientific videos on LabTube
  • 35 community eNewsletters


Sign In



Forgotten your details? Click Here
If you are not a member you can join here

*Please note: By logging into TechnologyNetworks.com you agree to accept the use of cookies. To find out more about the cookies we use and how to delete them, see our privacy policy.

Related Content

Alzheimer’s to Benefit from Landmark MRC-AstraZeneca Compound Collaboration
A study to investigate Alzheimer’s disease led by scientists at the University of Bristol has been awarded funding by the Medical Research Council (MRC).
Tuesday, November 06, 2012
Scientific News
Spero Therapeutics Announces $30 Million Series B Preferred Financing
Company has announced financing of $30 million to support development of novel therapies to treat gram-negative bacterial infections.
Keeping Tumor Growth at Bay
Engineers at Washington University in St. Louis found a way to keep a cancerous tumor from growing by using nanoparticles of the main ingredient in common antacid tablets.
Future of Medicine Could be Found in a Tiny Crystal Ball
A Drexel University materials scientist has discovered a way to grow a crystal ball in a lab. Not the kind that soothsayers use to predict the future, but a microscopic version that could be used to encapsulate medication in a way that would allow it to deliver its curative payload more effectively inside the body.
Improving Delivery of Poorly Soluble Drugs Using Nanoparticles
A technology that could forever change the delivery of drugs is undergoing evaluation by the Technology Evaluation Consortium™ (TEC). Developed by researchers at Northeastern University, the technology is capable of creating nanoparticle structures that could deliver drugs into the bloodstream orally – despite the fact that they are normally poorly soluble.
Faster Drug Discovery?
Startup develops more cost-effective test for assessing how cells respond to chemicals.
New Mechanism of Antitumor Action Identified
A team of UAB researchers and collaborators from the Catalan biotech company Ability Pharmaceuticals (UAB Research Park), have described a new mechanism of anti-tumour action, identified during the study and development of the new drug ABTL0812.
Nanoparticles Deliver Tumor Suppressors to Damaged Livers
UT Southwestern Medical Center chemists have successfully used synthetic nanoparticles to deliver tumor-suppressing therapies to diseased livers with cancer, an important hurdle scientists have been struggling to conquer.
Experimental Combination Surprises with Anti-HIV Effectiveness
A compound developed to protect the nervous system from HIV surprised researchers by augmenting the effectiveness of an investigational antiretroviral drug beyond anything expected.
A New Type of Anticancer Agent
Success in the development of a ?-tubulin specific inhibitor.
Nanoparticles Proven Effective Against Antibiotic-Resistant “Superbugs”
In the ever-escalating evolutionary battle with drug-resistant bacteria, humans may soon have a leg up thanks to adaptive, light-activated nanotherapy developed by researchers at the University of Colorado Boulder.
SELECTBIO

Skyscraper Banner
Go to LabTube
Go to eposters
 
Access to the latest scientific news
Exclusive articles
Upload and share your posters on ePosters
Latest presentations and webinars
View a library of 1,800+ scientific and medical posters
2,900+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
4,200+ scientific videos
Close
Premium CrownJOIN TECHNOLOGY NETWORKS PREMIUM FOR FREE!