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Aphios Awarded STTR Grant from NCI for Nanosomal Formulation of Novel, Nontoxic Vitamin D Analog for HormoneRefractory Prostate Cancer

September 18, 2007 - Aphios Corporation today announced that Aphios and its university collaborator Boston University Medical School were awarded a Phase I Small Business Technology Transfer Grant (STTR) from the National Cancer Institue (NCI) to develop a novel, nontoxic Vitamin D analog for hormone-refractory prostate cancer.

The new molecular entity (NME) being developed, APH-M109, is an analog of the naturally occurring Vitamin D hormone that is very toxic at therapeutic concentrations. APH-M109 is designed to covalently link the bioactive hormone inside the ligand-binding pocket of the nuclear Vitamin D receptor (VDR), which will significantly reduce catabolic degradation. As a result, less compound will be required to have an anti-tumor effect resulting in reduced toxicity. In vitro studies have shown that APH-M109 has strong anti-proliferative effects on several human prostate cancer cells. Additionally, it induced apoptosis in these cells. Furthermore, through in vivo studies, APH-M109 produced strong anti-tumor effect in athymic nude mice with hormone refractory prostate cancer at a dose approximately 10 times less than the parent vitamin D hormone without significant toxicity.

Phospholipid nanosomes are being used to encapsulate in order to further APH-M109’s translational potential as a therapeutic agent for prostate cancer. Phospholipid nanosomes are small, uniform liposomes. Phospholipid nanosomes will prolong APH-M109 circulation time, further reduce any systemic toxicity and enhance its therapeutic index. Phospholipid nanosomes will be manufactured utilizing proprietary green nanotechnologies (US, Japanese and International Patents).

Prostate cancer is the most prevalent cancer among men; and the second leading cause of cancer death among men in the US. According to the NCI, there are approximately 1.7 million men living in the US with a diagnosis of prostate cancer. Approximately 230,000 new cases of prostate cancer will be diagnosed and 29,000 men will die of the disease each year in the US. Although prostate cancer mostly affects elderly men, the number of younger men with prostatic carcinoma is significant. In addition, general increase in longevity has further emphasized the need for effective treatment of prostate cancer, especially for prostate cancers that are androgen-insensitive and metastatic.

Aphios Corporation has an exclusive license to APH-M109 (US Patent Pending) from Boston University Medical School. Aphios Corporation (www.aphios.com) is a biopharmaceutical company that is developing enabling technology platforms and enhanced therapeutic products for the prevention and treatment of certain cancers, infectious diseases and CNS disorders.


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