AnorMED Inc announced the first clinical proof of principle for CXCR4, a chemokine receptor, as a new target in the treatment of HIV. Results presented demonstrate that AnorMED's first CXCR4 inhibitor, AMD-3100, completely eliminated a specific strain of HIV in 9/19 patients and that this activity is dose-dependent. AnorMED leads in the development of CXCR4 inhibitors, having the only small molecule candidate in the clinic to date and preclinical studies on an entirely new series of orally administrable compounds targeting this receptor near completion.

In order to enter and infect cells, HIV must bind to either the CXCR4 (X4) or CCR5 (R5) chemokine receptor. Different strains of HIV prefer one receptor or the other. Therefore blocking both the X4 and R5 receptors can prevent the relevant HIV strains from entering and infecting the target cells. An infected individual may contain different levels of both X4 and R5 using strains. AMD-3100 and the Company's new compounds target the X4-using HIV strains.

The new clinical data was generated from a retrospective analysis of AnorMED's HIV Phase Ib/IIa clinical trial of AMD-3100. Using a genetic analysis tool, blood samples from patients in the trial were tested for the presence of X4-using strains of HIV. At the start of the study 19 of 40 patients had varying amounts of both X4 and R5. By the end of the study AMD-3100 eliminated X4 using HIV in 9 of the 19 patients. It was determined that the one patient who had nearly a one log drop in viral load by study end was entirely X4 at the beginning of the study. Furthermore, results indicated that the ability of AMD-3100 to completely eliminate CXCR4-using variants of HIV was dose-dependent.

The Phase Ib/IIa trial was closed in May 2001 due to adverse effects believed to be related to the specific structure of AMD-3100 when administered as a continuous intravenous infusion over 10 days. AnorMED has developed new X4 inhibitors that are structurally different from AMD-3100 and can be administered as a pill. The Company plans to select a new candidate from its chemokine inhibitor program by year end and will also continue with the development of new HIV drug candidates targeting the CCR5 chemokine receptor. Preclinical studies on a number of new compounds for HIV as well as rheumatoid arthritis, asthma and cancer are ongoing and additional work in the identification and optimization of new CXCR4 compounds continues.

AnorMED's core strength involves the application of chemistry, biochemistry and biology to the discovery and development of small molecule therapeutics for the treatment of diseases including inflammation, cancer and HIV. AnorMED's late stage clinical products include: Foznol, exclusively licensed to Shire Pharmaceuticals Group plc, which is on track for a US filing and European market approval by mid-year 2002; AMD-473, a new platinum based anticancer agent, in ongoing Phase II trials; AMD-3100, a potential new agent for stem cell transplant in cancer patients currently in a Phase I trial, and Apomate, a radiopharmaceutical used in the diagnosis of abdominal cancer and other diseases, which employs a technology licensed to NASI by AnorMED.