Quick Dips

Immucillins Under Way

Collaboration between Industrial Research and the Albert Einstein College of Medicine (US) has seen the patenting of a new range of immunosuppressive drugs. These could help doctors treat T-cell cancers and certain auto-immune conditions such as arthritis, and prevent the rejection of transplanted organs.

The joint project has also proved the ability of a new method for designing drugs which, in the long term, could see new treatments for illnesses such as malaria, giardia, cryptosporidiosis, psoriasis and African sleeping sickness.

Peter Tyler, an IRL synthetic carbohydrate chemist, worked closely with Professor Vern Schramm of Albert Einstein College to design and make a set of drugs called "Immucillins". These are highly potent enzyme inhibitors which prevent the proliferation of T-cells, part of the white cell complement of blood that makes up the immune system. By stopping T-cells proliferating, ailments caused by an over-active immune system could be treated.

Richard Furneaux, who led IRL's part of the project, says this new way of developing potent enzyme inhibitors is an exciting achievement.

"We can design compounds which are much more potent than anything researchers have had before."

The researchers were able to improve the potency by a factor of one million, so the dosage to treat a condition is tiny.

Biological trials have proved the Immucillins' capabilities, and commercialisation is now being pursued. However, it will be several years at the earliest before doctors are prescribing the drugs, according to Furneaux. Human clinical trials must first be undertaken by a pharmaceutical company.

The team will continue to work on developing more drugs using the pioneering method developed by Schramm for the design of enzyme inhibitors. These compounds are used to control the unwanted enzymic activity in the body which is responsible for the particular disorder.

The first Immucillin was made by a lengthy 21-step process. Furneaux says they originally thought the inhibitor structure proposed by their US counterpart was far too fancy, but as the project progressed the need for completing the full 21 steps was confirmed.

"It really was a Mount Everest of chemistry. Others have done similarly long syntheses in an academic environment, but seldom for true commercial reasons."

The team's latest success has been the development of an abbreviated production route, which makes commercial manufacture more practical.