Calcilytics: antagonists of the calcium-sensing receptor for the treatment of osteoporosis
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Widler, Leo (2011) Calcilytics: antagonists of the calcium-sensing receptor for the treatment of osteoporosis. Future Medicinal Chemistry, 3 (5). pp. 535-547. ISSN 1756-8919
Abstract
The only bone anabolic agents currently available on the market are based on parathyroid hormone (PTH). Secretion of endogenous PTH is controlled by a calcium sensing receptor (CaSR) at the surface of the parathyroid glands. Antagonists of this receptor (calcilytics) induce the release of the hormone. Provided the effect of the calcilytic is of short duration, a bone anabolic effect should result as well, based on ample experience with exogenous PTH. Although the first calcilytic series became known about ten years ago, the number of different structural types is still small today. This article will outline the quest from hits to potent development candidates of all relevant calcilytic series currrently known. Even after the front-runners unexpectedly failed in the clinic, the approach for an oral alternative to parenteral PTH remains highly attractive.
| Item Type: | Article |
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| Keywords: | calcilytic, calcium sensing receptor antagonist, osteoporosis, parathyroid hormone |
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| Date Deposited: | 13 Oct 2015 13:15 |
| Last Modified: | 13 Oct 2015 13:15 |
| URI: | https://oak.novartis.com/id/eprint/4039 |