AIDS TREATMENT NEWS Issue #183, September 17, 1993
John S. James
Cosalane was developed from a chemical known as ATA (aurintricarboxylic acid), which has long been known to have anti-HIV activity. ATA has not been developed as a drug because it is difficult to work with. It is not a single chemical, but a mixture of many different polymers -- and every batch tends to be different. This creates problems for quality control, and makes it almost impossible to get FDA approval for marketing.
The first attempt to overcome this problem was to separate out the smaller molecules (lower molecular weight) in the mixture, to look for a single molecule which could be made uniformly. But, unfortunately, the low molecular weight molecules have the least anti-HIV activity.
Chemists then took one of these low molecular weight components of ATA, and attached it to a steroid molecule (in addition to making other chemical changes). The purpose was to target the substance more effectively to the surface of viruses and of cells. The result, cosalane, has a relatively low molecular weight but works as well as any of the ATA fractions.
Cosalane is believed to inhibit binding of HIV to the cell, and also to inhibit viral entry (the fusion of the virus and the cell, after binding). In laboratory tests, it is active in concentrations of about 3 micromolar (not especially good compared to other drugs), and it must be present continuously to protect the cells. But it has been effective against all strains of HIV-1 and HIV-2 tested, including virus which is resistant to AZT or to the non-nucleoside RT-inhibitor drugs. And plasma concentrations higher than the effective anti-HIV concentration have been achieved in animal studies.
The obstacle now to cosalane's development is making enough for further tests. Only small quantities have been synthesized in laboratories -- not enough to finish animal tests, let alone run a clinical trial. Efforts are now underway to scale up the fairly complex manufacturing process.
Little has been published about cosalane so far, although several papers have appeared about the work with ATA which led up to it. Mark S. Cushman, Ph.D., presented the first technical information at a meeting of the American Chemical Society, August 22-27, 1993. A non-technical article about cosalane appeared in AIDS Weekly, September 6.
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