A short cut to billion dollar drugs

Sep 20, 2012
A short cut to billion dollar drugs

(Phys.org)—Scientists have found a highly efficient method of making hormone-based drugs which could generate billions of sales for the pharmaceutical industry.

Organic chemists from the University of Bristol, whose work was recently published in Nature, have perfected a quicker way of making which would mean many more people could be treated for a range of illnesses for the same cost.

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

Some synthetic analogues of prostaglandin are 'billion dollar' drugs. The prostaglandin analogue latanoprost, for example, which is used to treat and ocular hypertension, generates approximately $1.6 billion in sales each year.

Prostaglandins have been popular targets in synthesis for the last forty years because of their breadth of and their challenging . However, since these molecules cannot be isolated from in sufficient quantities, they have to be synthesised, but process is lengthy.  For example, the current synthesis of latanoprost requires twenty steps. Until now, despite huge synthetic effort in industry and academia, advances in the synthesis of prostaglandins have been limited.

Professor Varinder Aggarwal, who led the research funded jointly by the Engineering and Physical Sciences Research Council and the European Research Council, now reports a concise synthesis of prostaglandin PGF2a, which relies on the use of an organocatalyst, a small , to catalyse a key step in the process. The new process has enabled them to complete the synthesis in just seven steps.

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, from the University's School of Chemistry, 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."

Explore further: Scientists sweep cells apart for use in medical research

More information: doi:10.1038/nature11411

Related Stories

Seven steps to 'billion dollar' drugs

Aug 15, 2012

(Phys.org) -- 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 synthe ...

Building blocks of the future

Apr 06, 2010

(PhysOrg.com) -- Professor Varinder Aggarwal is no ordinary builder. He and his team in the School of Chemistry have just discovered a new technique that could hasten the development of new drugs for today’s ...

New way of synthesizing organic chemicals mimics nature

Jul 15, 2011

Organic chemists have found a new way of synthesizing multiple complex organic molecules that until now have needed to be synthesized using time-consuming methods. The new strategy, which mimics natural biosynthesis methods, ...

Recommended for you

'Global positioning' for molecules

Dec 19, 2014

In everyday life, the global positioning system (GPS) can be employed to reliably determine the momentary location of one en route to the desired destination. Scientists from the Institute of Physical and ...

User comments : 0

Please sign in to add a comment. Registration is free, and takes less than a minute. Read more

Click here to reset your password.
Sign in to get notified via email when new comments are made.