Drug Discovery Opinion

Iminosugars, where the endocyclic oxygen of sugars is replaced by a basic nitrogen, constitute a class of carbohydrate analogues that has received considerable attention in recent years.

The discovery that the natural product, 1-deoxy nojirimycin, had potent inhibitory properties toward alpha-glucosidases sparked exploration of synthetic approaches to, and biological properties of, the class. This has led to the approval of miglitol (Glyset®) for treatment of type II diabetes and miglustat (Zavesca®) for treatment of type I Gaucher’s disease in patients for whom enzyme replacement therapy is not suitable. More recently, Zavesca® is the first drug to be approved for treatment of progressive neurological manifestations in adult or paediatric patients with Niemann-Pick type C disease.

Subsequent research has identified iminosugars as inhibitors of a broader range of enzymes and the class is providing leads for a variety of diseases including viral infections and tumour metastasis as well as diabetes and lysosomal storage disorders.

A forthcoming meeting, organised by Summit Corporation plc, will cover both historical and future perspectives of iminosugars. Entitled “Iminosugars: Past, Present and Future – Medicines for tomorrow”, the meeting will be held at St John’s College, Oxford (UK) on 28^th June. The full programme and registration details can be found on the Summit website.

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