A New 1,25 Dihydroxy Vitamin D Analog with Strong Bone Anabolic Activity in OVX Rats with Little or no Bone Resorptive Activity.
basic_science · Level V
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- Record sourced from PubMed, PMID 31369169.
- Also identified by DOI 10.1002/jbmr.3838.
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Abstract
A new 1α,25-dihydroxy vitamin D<sub>3</sub> analog (2-methylene-22(E)-(24R)-22-dehydro-1α,24,25-trihydroxy-19-norvitamin D<sub>3</sub> or WT-51) has been tested as a possible therapeutic for osteoporosis. It is 1/10th as active as 1,25(OH)<sub>2</sub> D<sub>3</sub> in binding affinity for the vitamin D receptor but is at least 200 times more active than 1,25(OH)<sub>2</sub> D<sub>3</sub> and equal to that of 2MD (2-methylene-19-nor-(20S)-1α,25(OH)<sub>2</sub> D<sub>3</sub> , an analog previously tested in postmenopausal women), in supporting bone formation by isolated osteoblasts in culture. However, in contrast to 2MD, it is virtually inactive on bone resorption in vivo. WT-51 markedly increased bone mass (lumbar and femur) in ovariectomized (OVX) female rats. Further, bone strength tested by the three-point bending system is significantly increased by WT-51. Thus, WT-51 is an attractive candidate for the treatment of postmenopausal osteoporosis. © 2019 American Society for Bone and Mineral Research.
Medical subject headings
- Bone Density
- Bone Resorption