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For example, calcipotriol and 22-oxa calcitriol (OCT) are approved for the treatment of psoriasis

For example, calcipotriol and 22-oxa calcitriol (OCT) are approved for the treatment of psoriasis; paricalcitol, doxercalciferol, and falecalcitriol are approved for secondary hyperparathyroidism (nota bene: OCT and falecalcitriol are approved for use only in Japan). Another analog, 22-oxa-calcitriol (OCT), also promotes differentiation without the calcemia. One example of such an analog with a good dissociation ratio is calcipotriol (DaivonexR), which is clinically used to treat the hyperproliferative skin disease psoriasis. Other vitamin D analogs were clinically approved for the treatment of osteoporosis or secondary hyperparathyroidism. For several conditions such as secondary hyperparathyroidism, psoriasis and osteoporosis, vitamin D analogs are frequently used as a treatment option. A novel vitamin D3 analog, 22-oxa-1,25-dihydroxyvitamin D3, inhibits the growth of human breast cancer in vitro and in vivo without causing hypercalcemia.

For example, calcipotriol and 22-oxa calcitriol (OCT) are approved for the treatment of psoriasis 2The product of claim 3, wherein the once-weekly dosing is about 13 g of 22-oxa-calcitriol. 15. A method of treating hyperparathyroidism comprising utilizing the vessel of claim 21 to administer to a mammal in need thereof an effective amount of the composition contained in the vessel. Examples of compounds suitable for formulations of the present invention include, without limitation, 1,hydroxyvitamin D2, 1 -hydroxyvitamin D4, 1,24-dihydroxyvitamin D4, 1,24-dihydroxyvitamin D2, 1,25-dihydroxyvitamin D3 (calcitriol), 1,25-dihydroxyvitamin D2, 1,25-dihydroxyvitamin D4, 1,24,25-dihydroxyvitamin D2, 1 -hydroxyvitamin D3 (alpha-calcidol), seocalcitol (EB-1089), calcipotriol, 22-oxacalcitriol (maxacalcitol), fluorinated compounds such as falecalcitriol, and 19-nor compounds such as paricalcitol. In a particular example, the drug is calcitriol administered at an oral dose of about 0.5 mcg/kg once a week., Lancet 337:701-702, 1991, treated 19 patients with locally advanced or cutaneous metastatic breast cancer with topical calcipotriol, a Vitamin D analogue. Chugai Pharmaceuticals 22-oxacalcitriol (22-oxa-l,25- (OH)2-D3; (Dovonex) and Tacalcitol, used in the treatment of psoriasis. D molecules are the central focus of this minireview (examples provided in Fig. 2 ). Topically applied vitamin D analogues used in psoriasis (e.g., calcipotriol) were designed to be susceptible to target and liver cell breakdown, making them less likely to cause calcemic side effects should they gain access to the general circulation.

Calcitriol, the most active metabolite of vitamin D, controls parathyroid gland growth and suppresses the synthesis and secretion of parathyroid hormone (PTH). DBP for 22-oxacalcitriol (OCT), an analog of calcitriol for the treatment of secondary hyperparathryoidism, is approximately 300 400 times lower than that of calcitriol and the analog is rapidly cleared from the circulation. 1 -hydroxyvitamin D2 (Hectoral) has recently been approved for oral treatment of secondary hyperparathyroidism. The binding proteins, with blood proteins, and tissue distribution of 22-oxa-1,25 dihydroxyvitamin D3, a noncalcemic analogue of 1,25-dihydroxyvitamin D3 in rats. By Joanna Wietrzyk and Stanislaw Dzimira in Treatment and Vitamin D.

Patent Us20040058895

New Analogs Of Vitamin D3