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Therapeutic Targets

API currently has projects ongoing in seven therapeutic areas, of which the Estrogen program is the most advanced.

  • Estrogen Project: API designed an estrogen (PDC-7) using its estrogen pharmacophore. PDC-7 was predicted to be more active than the natural hormone estradiol. Synthesized by Magellan Laboratories, PDC-7 was tested in classical in vivo estrogen assays at an independent institution and was found to be 2-3 times more potent than estradiol, thereby providing validation of the technology. PDC-7 was a poor binder to the estrogen receptor (approximately 15%) relative to estradiol (100%) and thus would not have been selected as a candidate based upon protein receptor based technology. API has submitted a patent application on PDC-7 for use in estrogen responsive targets including hormone replacement therapy (HRT), Alzheimer's disease, stroke and contraception.
  • Neuroprotection Project: The goal of this project is to identify compounds that may be useful in Alzheimer's disease and stroke. Initial in vitro biological testing in one assay system has been completed and results demonstrate that one of API's compounds is neuroprotective.
  • Oncology Project: A novel class of compounds designed using API's technology has recently been shown to inhibit the growth of breast cancer cells in vitro. The activity of these compounds correlates with the direct binding of the drugs to DNA. The experiments were conducted independently and were recently published providing further validation of the technology. One of the compounds is 7 times more potent in these assays than tamoxifen, a leading drug used in the treatment of breast cancer.
  • Sedative Project: A sedative pharmacophore has been created as well as a sedative search engine. In initial phases of in silico testing, benchmark studies indicate that the search engine is effective in identifying known sedatives. Candidate structures are being evaluated for further development. Computer databases of other CNS drugs (e.g., antidepressants) are also being constructed
  • Diabetes/Anti-Obesity Project: API has developed pharmacophores and associated search engines for certain oral anti-diabetic drugs. API is also currently evaluating confidential and structural data on novel compounds that lower glucose and lipid levels in vivo.
  • Impotence Project: API has recently developed a search engine for vasodilators that are known to have activity in erectile dysfunction. The search engine has been effective in capturing various compounds known to have vasodilator effects. Initial data suggest it may be possible to develop a oral drug having beneficial effects for the treatment of impotence as well as diabetes, a well known cause of erectile dysfunction.
  • Additional Targets: API has created a Cardiovascular Disease project as recent research has indicated that API's technology may be applicable to the development of certain cardiac drugs. A search engine for cardiac drugs has been constructed. In light of the events of September 11, API has also created an antibiotic search engine for compounds like Cipro that are effective against Anthrax. Promising leads have been identified including compounds with structures unrelated to Cipro or other fluoroquinolones.
  • Thursday November 20 17:37 CST


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