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Chemical Compound Review

alfacalcidol     (1R,3S)-5-[2-[(1R,3aR,7aS)- 7a-methyl-1...

Synonyms: ACT06835, 41294-56-8
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Disease relevance of D01518


Psychiatry related information on D01518


High impact information on D01518


Chemical compound and disease context of D01518


Biological context of D01518

  • Although she had been effectively treated since one month postpartum with 1 alpha-hydroxycholecalciferol [1 alpha(OH)D3, alfacalcidol], her mean alkaline phosphatase (EC activity in serum increased to 3680 U/L from a stable value [335 (SD 50) U/L; n = 12] within three weeks, then returned to baseline over the ensuing four months [15].
  • We therefore carried out a prospective study over 18 months to examine the direct effect of high-dose alfacalcidol on erythropoiesis in erythropoietin (rHuEpo)-dependent anaemic patients on HD for more than 6 months with moderate hyperparathyroidism [16].
  • Intravenous alfacalcidol improves insulin resistance in hemodialysis patients [17].
  • Alfacalcidol 1 microg/day fully prevented vertebral bone loss over 3 years in women after the first year of menopause [18].
  • The expanded understanding of the pathogenesis of glucocorticoid- induced osteoporosis with its disturbed calcium homeostasis and the pharmacological effects of alfacalcidol, which counteract such iatrogenic bone loss, contribute to the understanding of its clinical efficacy in this most frequent form of secondary osteoporosis [19].

Anatomical context of D01518

  • ED-71 increased bone mass at the lumbar vertebra to a greater extent than alfacalcidol, while enhancing calcium absorption (indicated by urinary calcium excretion) and decreasing serum PTH levels to the same degree as alfacalcidol [20].
  • Twenty-eight fifth lumbar vertebrae (L-5) were obtained from 10-month-old female rats, comprised of ovariectomized (ovx, n = 6), sham operated (n = 7), and alfacalcidol-treated after ovx (0.1 microg/kg [n = 8] and 0.2 microg/kg [n = 7]) groups [21].
  • RESULTS: Compared with oral daily alfacalcidol, i.v. ibandronate produced significantly superior gains in mean (+/-s.d.) BMD at the lumbar spine (2.2+/-3.1 vs 11.9+/-7.4%; P<0.001), femoral neck (1.3+/-1.8 vs 4.7+/-4.0%; P<0.001) and calcaneus (7.6+/-3.8 vs 15.5+/-10.7%; P<0.0001) after 2 yr [22].
  • The study was performed to clarify the effects of active vitamin D (alfacalcidol) and/or alendronate (ALN) on bone tissue turnover in glucocorticoid (GC)-treated growing minipigs [23].
  • We studied the effect of alfacalcidol on lymphocyte phenotype [24].

Associations of D01518 with other chemical compounds


Gene context of D01518


Analytical, diagnostic and therapeutic context of D01518


  1. Treatment of advanced myelodysplastic syndrome with alfacalcidol. Mehta, A.B., Kumaran, T.O., Marsh, G.W., McCarthy, D.M. Lancet (1984) [Pubmed]
  2. Screening for subclinical osteomalacia in the elderly: normal ranges or pragmatism? Hosking, D.J., Campbell, G.A., Kemm, J.R., Cotton, R.E., Knight, M.E., Berryman, R., Boyd, R.V. Lancet (1983) [Pubmed]
  3. Alfacalcidol inhibits bone resorption and stimulates formation in an ovariectomized rat model of osteoporosis: distinct actions from estrogen. Shiraishi, A., Takeda, S., Masaki, T., Higuchi, Y., Uchiyama, Y., Kubodera, N., Sato, K., Ikeda, K., Nakamura, T., Matsumoto, T., Ogata, E. J. Bone Miner. Res. (2000) [Pubmed]
  4. Prevention of metabolic bone disease in the pre-end-stage renal disease setting. Coburn, J.W., Elangovan, L. J. Am. Soc. Nephrol. (1998) [Pubmed]
  5. Intermittent intravenous ibandronate injections reduce vertebral fracture risk in corticosteroid-induced osteoporosis: results from a long-term comparative study. Ringe, J.D., Dorst, A., Faber, H., Ibach, K., Sorenson, F. Osteoporosis international : a journal established as result of cooperation between the European Foundation for Osteoporosis and the National Osteoporosis Foundation of the USA. (2003) [Pubmed]
  6. Dementia in Idiopathic hypoparathyroidism. Rapid efficacy of alfacalcidol. Mateo, D., Giménez-Roldán, S. Arch. Neurol. (1982) [Pubmed]
  7. Superiority of alfacalcidol over plain vitamin D in the treatment of glucocorticoid-induced osteoporosis. Ringe, J.D., Dorst, A., Faber, H., Schacht, E., Rahlfs, V.W. Rheumatol. Int. (2004) [Pubmed]
  8. Sustained haematological response to high-dose oral alfacalcidol in patients with myelodysplastic syndromes. Kelsey, S.M., Newland, A.C., Cunningham, J., Makin, H.L., Coldwell, R.D., Mills, M.J., Grant, I.R. Lancet (1992) [Pubmed]
  9. Comparative efficacy of hormone replacement therapy, etidronate, calcitonin, alfacalcidol, and vitamin K in postmenopausal women with osteoporosis: The Yamaguchi Osteoporosis Prevention Study. Ishida, Y., Kawai, S. Am. J. Med. (2004) [Pubmed]
  10. Vitamin D hormone inhibits osteoclastogenesis in vivo by decreasing the pool of osteoclast precursors in bone marrow. Shibata, T., Shira-Ishi, A., Sato, T., Masaki, T., Masuda, A., Hishiya, A., Ishikura, N., Higashi, S., Uchida, Y., Saito, M.O., Ito, M., Ogata, E., Watanabe, K., Ikeda, K. J. Bone Miner. Res. (2002) [Pubmed]
  11. Lower risk for cardiovascular mortality in oral 1alpha-hydroxy vitamin D3 users in a haemodialysis population. Shoji, T., Shinohara, K., Kimoto, E., Emoto, M., Tahara, H., Koyama, H., Inaba, M., Fukumoto, S., Ishimura, E., Miki, T., Tabata, T., Nishizawa, Y. Nephrol. Dial. Transplant. (2004) [Pubmed]
  12. Plasma oxalate in patients receiving continuous ambulatory peritoneal dialysis. Tomson, C.R., Channon, S.M., Parkinson, I.S., Owen, J.P., Ward, M.K., Simpson, J.M., Laker, M.F. Nephrol. Dial. Transplant. (1988) [Pubmed]
  13. Redifferentiation therapy in brain tumors: long-lasting complete regression of glioblastomas and an anaplastic astrocytoma under long term 1-alpha-hydroxycholecalciferol. Trouillas, P., Honnorat, J., Bret, P., Jouvet, A., Gerard, J.P. J. Neurooncol. (2001) [Pubmed]
  14. Alendronate or alfacalcidol in glucocorticoid-induced osteoporosis. de Nijs, R.N., Jacobs, J.W., Lems, W.F., Laan, R.F., Algra, A., Huisman, A.M., Buskens, E., de Laet, C.E., Oostveen, A.C., Geusens, P.P., Bruyn, G.A., Dijkmans, B.A., Bijlsma, J.W. N. Engl. J. Med. (2006) [Pubmed]
  15. Transient hyperphosphatasemia in a child with autosomal recessive vitamin D dependency. Cole, D.E. Clin. Chem. (1986) [Pubmed]
  16. High-dose alfacalcidol improves anaemia in patients on haemodialysis. Albitar, S., Genin, R., Fen-Chong, M., Serveaux, M.O., Schohn, D., Chuet, C. Nephrol. Dial. Transplant. (1997) [Pubmed]
  17. Intravenous alfacalcidol improves insulin resistance in hemodialysis patients. Günal, A.I., Celiker, H., Celebi, H., Ustündağ, B., Günal, S.Y. Clin. Nephrol. (1997) [Pubmed]
  18. Importance of alfacalcidol in clinical conditions characterized by high rate of bone loss. Reginster, J.Y., Lecart, M.P., Richy, F. The Journal of rheumatology. Supplement. (2005) [Pubmed]
  19. The therapeutic effects of alfacalcidol on bone strength, muscle metabolism and prevention of falls and fractures. Schacht, E., Richy, F., Reginster, J.Y. Journal of musculoskeletal & neuronal interactions. (2005) [Pubmed]
  20. ED-71, a vitamin D analog, is a more potent inhibitor of bone resorption than alfacalcidol in an estrogen-deficient rat model of osteoporosis. Uchiyama, Y., HiguchI, Y., Takeda, S., Masaki, T., Shira-Ishi, A., Sato, K., Kubodera, N., Ikeda, K., Ogata, E. Bone (2002) [Pubmed]
  21. Contribution of trabecular and cortical components to the mechanical properties of bone and their regulating parameters. Ito, M., Nishida, A., Koga, A., Ikeda, S., Shiraishi, A., Uetani, M., Hayashi, K., Nakamura, T. Bone (2002) [Pubmed]
  22. Three-monthly ibandronate bolus injection offers favourable tolerability and sustained efficacy advantage over two years in established corticosteroid-induced osteoporosis. Ringe, J.D., Dorst, A., Faber, H., Ibach, K., Preuss, J. Rheumatology (Oxford, England) (2003) [Pubmed]
  23. Modulation of bone turnover by alfacalcidol and/or alendronate does not prevent glucocorticoid-induced osteoporosis in growing minipigs. Akahoshi, S., Sakai, A., Arita, S., Ikeda, S., Morishita, Y., Tsutsumi, H., Ito, M., Shiraishi, A., Nakamura, T. J. Bone Miner. Metab. (2005) [Pubmed]
  24. Effect of intravenous alfacalcidol on lymphocyte phenotyping in hemodialysis patients. Huraib, S., Tanimu, D., Abu-Romeh, S., al-Khairy, K., Quadri, K., al-Ghamdi, G., Iqbal, A. Am. J. Kidney Dis. (1998) [Pubmed]
  25. Alendronate treatment of established primary osteoporosis in men: results of a 2-year prospective study. Ringe, J.D., Faber, H., Dorst, A. J. Clin. Endocrinol. Metab. (2001) [Pubmed]
  26. A comparison of the effects of alfacalcidol treatment and vitamin D2 supplementation on calcium absorption in elderly women with vertebral fractures. Francis, R.M., Boyle, I.T., Moniz, C., Sutcliffe, A.M., Davis, B.S., Beastall, G.H., Cowan, R.A., Downes, N. Osteoporosis international : a journal established as result of cooperation between the European Foundation for Osteoporosis and the National Osteoporosis Foundation of the USA. (1996) [Pubmed]
  27. Controlled trial of falecalcitriol versus alfacalcidol in suppression of parathyroid hormone in hemodialysis patients with secondary hyperparathyroidism. Akiba, T., Marumo, F., Owada, A., Kurihara, S., Inoue, A., Chida, Y., Ando, R., Shinoda, T., Ishida, Y., Ohashi, Y. Am. J. Kidney Dis. (1998) [Pubmed]
  28. Vitamin D analogs versus native vitamin D in preventing bone loss and osteoporosis-related fractures: a comparative meta-analysis. Richy, F., Schacht, E., Bruyere, O., Ethgen, O., Gourlay, M., Reginster, J.Y. Calcif. Tissue Int. (2005) [Pubmed]
  29. Prevention of osteopenia induced with a gonadotropin-releasing hormone agonist in rats. Sakamoto, S., Sassa, S., Mitamura, T., Kudo, H., Suzuki, S., Yoshimura, S., Zhou, Y., Kikuchi, T., Shinoda, H. Calcif. Tissue Int. (1999) [Pubmed]
  30. The influence of Coenzyme Q10 on total serum calcium concentration in two patients with Kearns-Sayre Syndrome and hypoparathyroidism. Papadimitriou, A., Hadjigeorgiou, G.M., Divari, R., Papagalanis, N., Comi, G., Bresolin, N. Neuromuscul. Disord. (1996) [Pubmed]
  31. D-hormone analog alfacalcidol: an update on its role in post-menopausal osteoporosis and rheumatoid arthritis management. Richy, F., Deroisy, R., Lecart, M.P., Hanssens, L., Mawet, A., Reginster, J.Y. Aging clinical and experimental research. (2005) [Pubmed]
  32. A comparison of oral and intravenous alfacalcidol in the treatment of uremic hyperparathyroidism. Lee, W.T., Padayachi, K., Collins, J.F., Cundy, T. J. Am. Soc. Nephrol. (1994) [Pubmed]
  33. Supplementation with Alfacalcidol increases protein intake and serum albumin concentration in patients undergoing hemodialysis with hpoalbumineamia. Yonemura, K., Sugiura, T., Yamashita, F., Matsushima, H., Hishida, A. Blood Purif. (2004) [Pubmed]
  34. Hypercalcemia during pulse vitamin D3 therapy in CAPD patients treated with low calcium dialysate: the role of the decreasing serum parathyroid hormone level. Chagnac, A., Ori, Y., Weinstein, T., Zevin, D., Korzets, A., Hirsh, J., Edelstein, S., Gafter, U. J. Am. Soc. Nephrol. (1997) [Pubmed]
  35. Preventing bone loss in renal transplant recipients with vitamin D. El-Agroudy, A.E., El-Husseini, A.A., El-Sayed, M., Ghoneim, M.A. J. Am. Soc. Nephrol. (2003) [Pubmed]
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