Release issued 15th September 2000

From the symposium Nimesulide: a multifactorial approach to inflammation and pain, held on 17 July in Florence (Italy) in occasion of the VII World Conference on Clinical Pharmacology and Therapeutics (CPT 2000) and chaired by Prof. Rainsford and Prof. Velo, nimesulide the first COX-2 inhibitor to enter the market - emerged as a NSAID endowed by a strong analgesic activity. The pharmacological basis of this activity and the rationale of the use of Nimesulide in a pathologic condition, like dysmenorrhoea, in which a very quick effect is needed, have been dealt with at the above symposium.

It is already known that COX-2 is only one of the mediators involved in inflammation and pain. Professor Alan Bennett, from the Guy's, King's and St. Thomas' Medical School in London (U.K.), showed several other mediators which are related to inflammation and pain: i.e. superoxide anions from neutrophils, histamine, cytokine TNFa and proteolytic enzymes. Nimesulide is the only NSAID able to affect all these substances. This results in significant anti-inflammatory and analgesic activities.

Innovative data were presented by Professor Desmond Fitzgerald, Director of the Department of Clinical Pharmacology at the Royal College of Surgeons in Dublin (Ireland). Based on recent findings which have shown that COX-2 is expressed in neuronal cells of the spinal cord following a peripheral injury, Fitzgerald and his group demonstrated that Nimesulide was able to inhibit COX-2 in neuronal cells and to reduce pain in subjects who underwent major surgical interventions (such as thoracotomy), reducing the daily dose of morphine. This effect did not occur with the comparative drug, ibuprofen, a non COX-2 selective NSAID. These evidences support the hypothesis that the reduction of COX-2 in neuronal cells produced by nimesulide might explain its ability to reduce pain at central level.

Professor Giorgio Sandrini, Head of the Centre for Adaptive Disorders and Headache of the Pavia University (Italy), by using a special technique for provoking pain, came to the hypothesis of a central analgesic effect of Nimesulide through a spinal-supraspinal mechanism. This analgesic activity seems to depend on the inhibition of COX-2 and also of nitric oxide produced by Nimesulide .

Another interesting finding emerging from the study is the rapidity of the onset of analgesic effect (15 minutes), as confirmation of previous evidences which were reviewed and newly analysed by Professor Martii Pulkkinen, from the Department of Obstetrics and Gynaecology at the Turku University in Finland. He underlined that Nimesulide, unlike other NSAIDs, is able to reduce intrauterine contractility in dysmenorrhoic women. This effect converts the uterus from pathological to physiological condition, with a significant reduction of pain and consequent improvement of patients' quality of life. The faster onset of action in comparison with other NSAIDs emerged once again . In the light of these evidences, it seems that a rationale for the use of nimesulide in the treatment of dysmenorrhoea does exist.

Professor Fabio Facchinetti, from Modena University and co-ordinator of a group of investigators from various Universities and Hospital Centres in Italy, confirmed the clinical benefits of Nimesulide in this pathology through a double-blind study versus diclofenac involving 304 women. Nimesulide resulted to be as effective as diclofenac in reducing pain, but its analgesic activity consistently with the data from Sandrini and Pulkkinen presented hereby - was already evident within the first half hour after administration.

As a matter of fact, Nimesulide came once again on to the scene of the international scientific world during the recent VII World Conference on Clinical Pharmacology and Therapeutics (July 2000, Florence, Italy ). In fact, the symposium fully dedicated to this drug has evidenced that this COX-2 selective NSAID clearly differentiates from both conventional NSAIDs and new COX-2 inhibitors thanks to its peculiar modes of action and to its clinical profile. In particular, its analgesic properties have been highlighted and explained with its ability in inhibiting COX-2 in spinal cord. Additional pharmacological activities at the basis of its clinical efficacy in dysmenorrhoea were presented. The faster onset of the Nimesulide's analgesic activity, compared with other NSAIDs, was also underlined.

According to Fitzgerald, one of the speakers, once again Nimesulide is a selective COX-2 inhibitor that has provided valuable insight into the role of COX-2 in disease.

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