LONDON ¿ Chiroscience Group plc reported ¿excellent progress¿ with its matrix metalloproteinase inhibitor (MMP) program, with the lead compound entering initial studies in cancer patients in two U.S. centers, following a successful Phase I program at doses of up to 1,200 milligrams per day. The compound, BMS 275291, is being developed by Bristol-Myers Squibb Co., of New York, which licensed oncology rights to the MMP program in 1998. If the current trials are successful, the compound will move into combined Phase II/III trials.

A second MMP inhibitor, D1927, was also licensed to BMS, but Chiroscience, of Cambridge, said that given the progress with the lead compound and the similarity between the two, rights to D1927 have reverted to Chiroscience for all fields outside oncology. D1927 was well absorbed and well tolerated in initial Phase I trials, and has now moved into repeat-dosing trials. The drug will either be developed for rheumatoid arthritis or the related diseases of psoriasis and inflammatory bowel disease.

Chiroscience said its second-generation MMPs have significant advantages over first-generation compounds. In particular, they do not cause joint pain, the most significant side effect of earlier compounds.

The company said it now has advanced understanding of the underlying cause of joint pain, validating a second animal model which shows a clear difference between its inhibitors and several of the first-generation inhibitors in their potential to cause joint pain.

A further development program of third-generation MMP inhibitors is due to start later this year.

Company Increases Revenue, Cuts Loss

Chiroscience made this disclosure as it released financial results for the year ended February 1999, showing revenues up 57 percent at #41.2 million (US$67 million), from #26.2 million. The net loss fell by 32 percent, to #17.2 million from #23.3 million. Investment in research and development was down to #29.2 million from #36.4 million.

Discussions are still under way to find a marketing partner for Chirocaine, the long-lasting local anesthetic, which was dropped by Zeneca plc as a condition of its merger with Astra AB. Following the FDA granting of approvable status in February 1999, Chiroscience said it hopes to launch in the U.S. later this year, and expects Chirocaine to provide ¿significant income, starting next year.¿

The drug has also been approved in Sweden, and with the European mutual-recognition process, this should lead to further national approvals being granted later this year, with launches in the first half of 2000.

The development costs of Chirocaine have been recovered prior to launch through the #15 million equity investment made by Zeneca, when it took the license in March 1998, and the #10 million in compensation paid when it gave the license back, plus the #3 million paid by Maruishi for the Japanese rights. Zeneca is continuing to bear the full cost of all aspects of the product¿s development.

Chiroscience also reported progress with its PDE IV program, to which Schering-Plough Corp. has all rights. One PDE IV inhibitor, D4396, has completed a number of Phase I studies, and is projected to enter patient trials next year for the treatment of asthma. As a result, Chiroscience said, it has received a milestone payment. n