BioWorld International Correspondent

PARIS - The CEO of NicOx SA, Michele Garufi, unveiled an "aggressive development plan" for 2001, saying the company would have four drugs in Phase II clinical trials and another two in Phase I by the end of this year, and that two more lead compounds would have entered clinical development.

At a conference in Paris last week, at which Nobel Prize-winner Louis Ignarro, a member of NicOx's scientific advisory board, outlined the merits of nitric oxide-releasing therapeutics for treating conditions such as atherosclerosis, the vascular complications of diabetes, chronic inflammatory disease, certain cancers, urinary incontinence and even erectile dysfunction. Garufi claimed that NicOx had "achieved what we promised investors at the time of our IPO in November 1999."

The company's "ambitious objectives for 2001" include the completion of Phase II trials of its NO-releasing flurbiprofen derivative HCT 1026, which is being tested in three indications - urinary incontinence, osteoporosis and dermatological disorders. A Phase II trial of HCT 1026 in Paget's disease has just been completed in the UK, and the company expects to have the results available "quite soon."

In addition, Garufi said he expected HCT 3012 to "move into full Phase II development very soon." HCT 3102 is an NO-releasing derivative of the nonsteroidal anti-inflammatory drug (NSAID) naproxen that is being co-developed with AstraZeneca for the treatment of pain and inflammation.

NicOx will have another two drugs in Phase II trials by the end of 2001. One is NCX 4016, an NO-releasing aspirin derivative, which has been in Phase I trials for cardiovascular disease since early 2000. Describing it as "one of the most exciting products we have in development," Garufi explained that in Phase II it would be tested in the primary indication of restenosis. The other is NCX 1022, an NO-releasing hydrocortisone derivative for the treatment of psoriasis, which was one of three compounds that entered Phase I clinical trials in December. The other two are NCX 701, an NO-releasing derivative of paracetamol for the treatment of pain, and NCX 1015, an NO-releasing prednisolone derivative for inflammatory bowel disease.

NCX 701 is being developed under a fast-track program that is due to see it in Phase Ib trials by the third quarter of this year. Initial trials had already established proof of principle for it as a potent analgesic, said Garufi. The other compound that is due to be in Phase I trials by the end of 2001 is NCX 1020, which is being developed for the treatment of asthma. Two more compounds in preclinical development could reach the Phase I stage by year end: NCX 1000, for liver and biliary diseases, and another asthma drug, NCX 950.

In addition, NicOx said it has six promising drug candidates in its research pipeline, two of which will be selected for taking into clinical development during the course of this year. They are likely to be NCX 2216, an NO-releasing NSAID with anti-oxidant properties being developed for neuroinflammation that has demonstrated promising potential for the treatment of Alzheimer's disease, and one of two NO-releasing NSAIDS being developed for the treatment of cancer, NCX 4050 and NCX 1102.

Also in the pipeline are NCX 2111, another NO-NSAID with anti-oxidant properties designed to treat urinary incontinence, an NO-5-ASA for the treatment of IBD, and an NO-releasing heparin being developed as an antithrombotic.

Looking ahead, Garufi confirmed that "our business development plan still provides for the first drug to be on the market by 2004." It would probably be NCX 3012, he said, which AstraZeneca was planning to file for regulatory approval in the fourth quarter of 2003. The company could thus achieve its objective of breaking even that year, but that would depend on whether the product was launched in October or December. Garufi added that NicOx was still negotiating to get a royalty rate of "at least 12 percent from AstraZeneca."

Garufi concluded by saying NicOx would shortly be transferring its corporate headquarters into larger premises at Sophia-Antipolis, in the south of France. Furthermore, in March the company's U.S. subsidiary, NicOx Inc., which was incorporated late last year, will be moving into offices in Princeton, N.J., while this summer the company will be opening a new laboratory in Milan, Italy. NicOx's work force grew from 21 to 33 in 2000 and is due to reach 55 by the end of this year.