Licensed from Boston Univ Med School, canidate showed antitumor effect in mice with the hormone-refractory version.

Aphios obtained a Phase I Small Business Technology Transfer Grant (STTR) from the NCI to develop a nontoxic vitamin D analog for hormone-refractory prostate cancer. Aphios has an exclusive license to this compound, APH-M109, from Boston University Medical School.

APH-M109 is designed to covalently link the bioactive hormone inside the ligand-binding pocket of the nuclear vitamin D receptor, which will significantly reduce catabolic degradation, the companies explain. As a result, less compound will be required to have an antitumor effect resulting in reduced toxicity, they add.

In vitro studies have reportedly shown that APH-M109 has strong antiproliferative effects on several human prostate cancer cells and induces apoptosis in these cells. In in vivo experiments, the compound produced antitumor 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, the partners say.

Phospholipid nanosomes, small, uniform liposomes, are being used for the delivery of APH-M109. They are said to prolong APH-M109 circulation time, further reduce any systemic toxicity, and enhance its therapeutic index.

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