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Seocalcitol (CB1089)
A number of preclinical studies have shown that Vitamin D, or more specifically its biologically active metabolite calcitriol, has anticancer activity in a number of different tumors including prostate, breast, pancreas, colon, skin and brain cancer. Calcitriol has many mechanisms of action in cancer including the ability to inhibit cell proliferation and angiogenesis, and induce differentiation and apoptosis. To date the clinical use of calcitriol has been limited by its adverse effects on calcium metabolism. More specifically, in human testing calcitriol has been shown to elevate serum levels of calcium, resulting in an adverse condition known as hypercalcemia, which can be life-threatening if left untreated.
Seocalcitol (CB1089) is an analog of calcitriol that has been shown, in pre-clinical cancer studies, to be 50-200 times more potent than calcitriol with respect to regulation of cell growth and differentiation. Importantly, pre-clinical studies also indicate that seocalcitol has reduced calcemic activity compared to calcitriol, significantly reducing the incidence of hypercalcemia.
In preclinical models of prostate cancer, CB1089 has been shown to inhibit tumor cell growth more potently than calcitriol (Figure 1).
Figure 1: Effects of CB1089 and Vitamin D (calcitriol) on cell growth in a preclinical model of prostate cancer (LNCaP). Legend: Eth=ethanol control, black bar=CB1089, white bar=calcitriol). (Blutt, Endocrinology, 1997)
Cougar is currently developing seocalcitol (CB1089) for the treatment of hormone refractory prostate cancer.
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Cougar Biotechnology, Inc.
10990 Wilshire Blvd, Suite 1200
Los Angeles, CA 90024
(310) 943-8040 Main
(310) 943-8059 Fax |
