Page last updated: 2024-12-10

calcitriol

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Description

dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5280453
CHEMBL ID846
CHEBI ID17823
CHEBI ID93988
SCHEMBL ID3245
MeSH IDM0003148

Synonyms (189)

Synonym
AC-1859
HY-10002
AB00639957-06
gtpl2779
1alpha,25-dihydroxycholecalciferol
(1alpha,3beta,5z,7e)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol
calcijex
rocaltrol
(1s,3r,5z,7e)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol
calcitriolum
CHEBI:17823 ,
(1s,3r,5z,7e)-9,10-secocholesta-5,7,10-triene-1,3,25-triol
1,25-dhcc
1alpha,25(oh)2d3
1-alpha-25-dihydroxyvitamin d3
(5z,7e)-(1s,3r)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol
decostriol
9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol, (1.alpha.,3.beta,.5z,7e)- & cd4
1,25(oh)2d3 & cd4
cd-2027
1,25-(oh)2-d3
1,25d3
1alpha,25(oh)2-d3
ro-21-5535
vectical
silkis
asentar
rocaltrol (tn)
D00129
calcitriol (jan/usp/inn)
1-alpha,25-dihydroxyvitamin d3
u 49562
topitriol
9,10-seco(5z,7e)-5,7,10(19)-cholestatriene-1alpha,3beta,25-triol
dihydroxyvitamin d3
ro 215535
dn-101
soltriol
1alpha,25-dihydroxyvitamin d
ro 21-5535
cholecalciferol, 1-alpha,25-dihydroxy-
1,25-(oh)2d3
9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol, (1alpha,3beta,5z,7e)-
einecs 250-963-8
1,25-dihydroxycholecaliferol
hsdb 3482
ccris 5522
1,25-dihydroxyvitamin d
(5z,7e)-9,10-secocholesta-5,7,10(19)-triene-1alpha,3beta,25-triol
calcitriolum [inn-latin]
dn 101
1 alpha,25-dihydroxyvitamin d3
IDI1_033757
BSPBIO_001287
1alpha,25-dihydroxyvitamin d3, >=97.0% (hplc)
BCBCMAP01_000160
SPECTRUM5_002061
1,25-dihydroxycholecalciferol
1,25(oh2)d3
(1r,3s,5z)-5-[(2e)-2-[(1r,3as,7ar)-1-[(1r)-5-hydroxy-1,5-dimethyl-hexyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1h-inden-4-ylidene]ethylidene]-4-methylene-cyclohexane-1,3-diol
9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol, (1.alpha.,3.beta,.5z,7e)-
1-alpha,-1,25-dihydroxyvitamin d3
(1r,3s)-5-{2-[(1r,3as,7ar)-1-((r)-5-hydroxy-1,5-dimethyl-hexyl)-7a-methyl-octahydro-inden-4-ylidene]-ethylidene}-4-methylene-cyclohexane-1,3-diol
1.alpha.,25-dihydroxy-26,27-hexadeuterovitamin d3
MLS001424122
(1s,3r,5z,7e)-9,10-seco-5,7,10(19)-cholestatriene-1,3,25-triol
1alpha,25-dihydroxyvitamin d3
calcitriol ,
C01673
1alpha,25-dihydroxyvitamin d3, >=99% (hplc)
MLS000759536
smr000466393
1DB1
cpd000466393
DB00136
(5z,7e)-(1s,3r)-9,10-seco-5,7,10(19)-cholestatriene-1,3,25-triol
1alpha,25-dihydroxyvitamin d3 / 1alpha,25-dihydroxycholecalciferol / calcitriol
LMST03020258
NCGC00161327-01
NCGC00161327-04
vit d
1, 25-(oh)2d3
1,25-dihydroxy vitamin d3
1,25 (oh)2 d3
1 alpha,25 dihydroxyvitamin d3
1,25 dihydroxycholecalciferol
1 alpha,25-dihydroxycholecalciferol
1,25 dihydroxyvitamin d3
d3, 1,25-dihydroxyvitamin
d3, 1 alpha,25-dihydroxyvitamin
HMS2051F06
HMS1989A09
HMS2089N03
bdbm50200182
ro-215535
CHEMBL846 ,
BML2-E03
HMS1791A09
HMS1361A09
nsc749776
nsc-749776
1.alpha.,25-dihydroxycholecalciferol
1.alpha.,25-dihydroxyvitamin d(sub 3)
(5z,10-secocholesta-5,7,10(19)-triene-1.alpha.,3.beta.,25-triol
dihydroxy-vitamin d3
dtxsid5022722 ,
dtxcid002722
BCP9000474
HMS2232D18
AKOS015961898
CCG-101001
panbonis
unii-fxc9231jvh
calcitriol [usan:usp:inn:ban:jan]
fxc9231jvh ,
BCPP000304
calcitriol [jan]
calcitriol [mi]
calcitriol [ep monograph]
calcitriol [usp monograph]
calcitriol [vandf]
calcitriol [usan]
9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol, (1.alpha.,3.beta.,5z,7e)-
calcitriol [hsdb]
calcitriol [mart.]
calcitriol [usp-rs]
calcitriol [who-dd]
calcitriol [inn]
calcitriol [orange book]
1,25-dihydroxycholecalciferol, (1alpha)-
CS-0388
S1466
GMRQFYUYWCNGIN-NKMMMXOESA-N
1alpha 25-dihydroxycholecalciferol
NC00251
SCHEMBL3245
BRD-K27316855-001-06-7
cas number 32222-06-3
toptriol
(1?,3?,5z,7e)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol
(1r,3s,z)-5-(2-((1r,3as,7ar,e)-1-((r)-6-hydroxy-6-methylheptan-2-yl)-7a-methyloctahydro-4h-inden-4-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol
HMS3402A09
(1r,3s,z)-5-((e)-2-((1r,3as,7ar)-1-((r)-6-hydroxy-6-methylheptan-2-yl)-7a-methylhexahydro-1h-inden-4(2h)-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol
1a,25-dihydroxycholecalciferol
AB00639957_07
mfcd00867079
calcitriol, european pharmacopoeia (ep) reference standard
SR-01000759361-4
sr-01000759361
CHEBI:93988
1a,25-dihydroxyvitamin d3
(3b,5z,7e)-9,10-secocholesta-5,7,10(19)-trienetriol
1a,25-(oh)2d3
25-dihydroxycholecalciferol
ro215535
calcitriol; (5z,7e)-9,10-secocholesta-5,7,10(19)-triene-1alpha,3beta,25-triol
(1s,3r,5z,7e,14beta,17alpha)-9,10-secocholesta-5,7,10-triene-1,3,25-triol
'1,25 dihydroxy vitamin d3'
calcitriol (1,25-dihydroxyvitamin d3)
1000873-74-4
C3078
sr-01000946978
SR-01000946978-1
Q139195
BRD-K27316855-001-19-0
9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol, (1a,3b,5z,7e)-
calcitrol 100 microg/ml in acetonitrile
EX-A4435
1 alpha ,25-dihydroxyvitamin d3
STARBLD0021993
(1r,3s,5z)-5-{2-[(1r,3as,4e,7ar)-1-[(2r)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-octahydro-1h-inden-4-ylidene]ethylidene}-4-methylidenecyclohexane-1,3-diol
EN300-22411582
vitamin d3-1alpha,25-dihydroxy (calcitriol)
1,3-cyclohexanediol, 4-methylene-5-[2-[(1r,3as,7ar)-octahydro-1-[(1r)-5-hydroxy-1,5-dimethylhexyl]-7a-methyl-4h-inden-4-ylidene]ethylidene]-, (1r,3s)-
calcitriol (ep monograph)
calcitriol (usp-rs)
calcitriol (mart.)
calcitriolum (inn-latin)
calcitrol
5-(2-(1-(5-hydroxy-1,5-dimethyl-hexyl)-7a-methyl-octahydro-inden-4-ylidene)-ethylidene)-4-methylene-cyclohexane-1,3-diol
calcitriol capsules 0.5 mcg
d05ax03
calcitriol capsules 0.25 mcg
calcitriol (usp monograph)
calcitriol (usan:usp:inn:ban:jan)
1,25(oh)2-d3
calcitriolo
a11cc04
calcitriol 0.25 mcg

Research Excerpts

Overview

Calcitriol is an active product of vitamin D produced by the liver and kidney hydroxylase metabolism with strong physiological activity. It is a rare source of hypercalcemia in solid tumors, especially in gastrointestinal stromal tumors (GIST) Cal citriol has potential to be a simple, economical means of increasing fat graft retention and long-term outcomes.

ExcerptReferenceRelevance
"Calcitriol secretion is a rare source of hypercalcemia in solid tumors, especially in gastrointestinal stromal tumors (GIST)."( Calcitriol-Mediated Hypercalcemia, Somatostatin Receptors Expression and 25-Hydroxyvitamin D
Blanco Molina, MA; Contreras González, MJ; Gálvez-Moreno, MA; González Menchen, A; Guerrero Martínez, MDC; Herrera-Martínez, AD; Herrera-Martínez, Y; Luque, RM; Moreno-Vega, AL; Pedraza-Arévalo, S; Rodrigo Martínez, Á, 2021
)
2.79
"Calcitriol synthesis is a multistep process."( Regulation of 1 and 24 hydroxylation of vitamin D metabolites in the proximal tubule.
Alexander, RT; Beggs, MR; Grimbly, C; Young, K, 2022
)
1.44
"Calcitriol is a nutraceutical essential regulator for host health benefits."( Capric Acid Behaves Agonistic Effect on Calcitriol to Control Inflammatory Mediators in Colon Cancer Cells.
Elsawy, H; Negm, A; Sedky, A, 2022
)
1.71
"Calcitriol is a pleiotropic, safe nutrient with cell-specific influence on viability and metabolic flux."( Active Vitamin D3 (Calcitriol) Increases Adipose Graft Retention in a Xenograft Model.
Amurgis, C; DeSanto, M; Guerrero, D; Gusenoff, JA; Kokai, LE; Lee, P; Loder, S; Olevian, D; Patadji, S; Peter Rubin, J; Stavros, AG; Wang, S, 2023
)
1.96
"Calcitriol has potential to be a simple, economical means of increasing fat graft retention and long-term outcomes."( Active Vitamin D3 (Calcitriol) Increases Adipose Graft Retention in a Xenograft Model.
Amurgis, C; DeSanto, M; Guerrero, D; Gusenoff, JA; Kokai, LE; Lee, P; Loder, S; Olevian, D; Patadji, S; Peter Rubin, J; Stavros, AG; Wang, S, 2023
)
1.96
"Calcitriol is an active product of vitamin D produced by the liver and kidney hydroxylase metabolism with strong physiological activity. "( Economical irregular silica as an effective dispersive solid-phase extraction sorbent for the quantification of calcitriol in soft capsules.
Hou, S; Ji, S; Li, T; Luo, X; Song, H; Wang, X; Zhang, Y, 2021
)
2.28
"As calcitriol is a lipid-soluble molecule, its interaction with DNA and copper would require a "chaperone"-like molecule, which binds the relatively hydrophobic calcitriol and polar DNA."( Calcitriol-induced DNA damage: toward a molecular mechanism of selective cell death.
Hasan, SS; Naseem, I; Rizvi, A, 2013
)
2.35
"Calcitriol is an important drug used for treating osteoporosis, which can be produced from vitamin D3. "( Whole cell bioconversion of vitamin D3 to calcitriol using Pseudonocardia sp. KCTC 1029BP.
Im, JH; Kang, DJ; Kang, JH; Kim, KH, 2015
)
2.12
"Falecalcitriol is a novel vitamin D analog, which has a greater potential to suppress parathyroid hormone (PTH) and a longer half-life. "( Comparison of oral falecalcitriol and intravenous calcitriol in hemodialysis patients with secondary hyperparathyroidism: a randomized, crossover trial.
Ito, H; Kinugasa, E; Ogata, H; Shishido, K; Taguchi, S; Takahashi, J; Takahashi, K; Yamamoto, M, 2009
)
1.22
"Calcitriol is a potent anti-proliferative agent in a wide variety of malignant cell types."( Anti-tumor activity of calcitriol: pre-clinical and clinical studies.
Ahmed, S; Bernardi, RJ; Fakih, M; Hershberger, PA; Johnson, CS; Muindi, J; Trump, DL; Yu, WD, 2004
)
1.36
"Calcitriol seems to be a potent drug with various therapeutic applications, such as regulation of calcium-phosphate homeostasis and treatment of psoriasis, autoimmune diseases, and cancer."( [Biological activity of calcitriol and its new analogues -- potential therapeutic applications].
Jaroszewicz, I; Opolski, A; Pełczyńska, K; Switalska, M, 2005
)
1.36
"Calcitriol is a potent antiproliferative agent against various tumour cells in vitro. "( Correlation between VDR expression and antiproliferative activity of vitamin D3 compounds in combination with cytostatics.
Jaroszewicz, I; Kutner, A; Nevozhay, D; Opolski, A; Pelczynska, M; Switalska, M; Wietrzyk, J; Zabel, M,
)
1.57
"Calcitriol is a potent antiproliferative agent against various tumour cells in vitro. "( Antiproliferative activity of vitamin D compounds in combination with cytostatics.
Jaroszewicz, I; Kutner, A; Maciejewska, M; Opolski, A; Pelczynska, M; Switalska, M,
)
1.57
"Calcitriol is a standard therapy for secondary hyperparathyroidism in chronic renal failure. "( Bone growth during daily or intermittent calcitriol treatment during renal failure with advanced secondary hyperparathyroidism.
He, YZ; Sanchez, CP, 2007
)
2.05
"Calcitriol therapy is a central strategy for the treatment of uremic secondary hyperparathyroidism. "( Alterations in serum phosphate levels predict the long-term response to intravenous calcitriol therapy in dialysis patients with secondary hyperparathyroidism.
Gejyo, F; Hosaka, K; Iino, N; Ito, Y; Kazama, JJ; Maruyama, H; Narita, I; Saito, A; Yamamoto, S, 2008
)
2.01
"Calcitriol is a biologic agent that has activity against multiple solid tumors, including ovarian carcinomas."( Additive inhibition of RL95-2 endometrial carcinoma cell growth by carboplatin and 1,25 dihydroxyvitamin D3.
Cho, YL; Christensen, C; Deppe, G; Lawrence, WD; Malone, JM; Malviya, VK; Saunders, DE; Wappler, NL, 1993
)
1.01
"Calcitriol is a potent differentiation agent that modulates mononuclear phagocyte activation and effector functions."( Monocyte 1 alpha-hydroxylase regulation: induction by inflammatory cytokines and suppression by dexamethasone and uremia toxin.
Gyetko, MR; Hsu, CH; Patel, S; Wilkinson, CC; Young, E, 1993
)
1.01

Effects

Ccitriol has a dose-dependent inhibition on fibroblast proliferation and collagen synthesis. IV calcitriol therapy has a greater suppression of PTH at the 3rd month of the therapy.

Ccitriol has been safely used outside the USA in Europe under the trade name Silkis Ointment for almost a decade in the treatment of psoriasis. It is currently FDA-approved as Vectical Ointments.

ExcerptReferenceRelevance
"Calcitriol has a dose-dependent inhibition on fibroblast proliferation and collagen synthesis and has immunoregulatory activities."( Treatment of linear scleroderma with oral 1,25-dihydroxyvitamin D3 (calcitriol) in seven children.
Elst, EF; Oranje, AP; Van Suijlekom-Smit, LW,
)
1.09
"Calcitriol has a similar effect on kidney distal tubule PMCA activity in vivo but the cellular basis for this effect has not been studied."( Calcitriol upregulates expression and activity of the 1b isoform of the plasma membrane calcium pump in immortalized distal kidney tubular cells.
Dick, IM; Glendenning, P; Prince, RL; Ratajczak, T, 2000
)
2.47
"IV calcitriol therapy has a greater suppression of PTH at the 3rd month of the therapy. "( Comparative effect of oral pulse and intravenous calcitriol treatment in hemodialysis patients: the effect on serum IL-1 and IL-6 levels and bone mineral density.
Akbulut, M; Gönen, S; Gürbilek, M; Tombul, Z; Türk, S; Yeksan, M; Yildiz, A, 2002
)
1.19
"Calcitriol has been revealed to exert neuroprotective effects in ischemic stroke; however, its role and the underlying mechanisms in brain injury induced by ischemia are not well known. "( Calcitriol Ameliorates Brain Injury in the Rat Model of Cerebral Ischemia-Reperfusion Through Nrf2/HO-1 Signalling Axis: An in Silico and in Vivo Study.
Joghataei, MT; Karimian, M; Khassafi, N; Moradi, F; Tameh, AA; Vahidinia, Z; Zare-Dehghanani, Z, 2022
)
3.61
"Calcitriol has potential to be a simple, economical means of increasing fat graft retention and long-term outcomes."( Active Vitamin D3 (Calcitriol) Increases Adipose Graft Retention in a Xenograft Model.
Amurgis, C; DeSanto, M; Guerrero, D; Gusenoff, JA; Kokai, LE; Lee, P; Loder, S; Olevian, D; Patadji, S; Peter Rubin, J; Stavros, AG; Wang, S, 2023
)
1.96
"Calcitriol has antimicrobial activity against H."( Molecular mechanism of calcitriol enhances membrane water permeability.
Cao, Z; Chen, M; Liu, L; Shi, Z; Zhao, L, 2024
)
2.47
"Calcitriol has been shown to lessen skin fibrosis and may be therapeutically beneficial to FAs."( The efficacy and safety of topical rapamycin-calcitriol for facial angiofibromas in patients with tuberous sclerosis complex: a prospective, double-blind, randomized clinical trial.
Chen, PL; Chen, YT; Hong, JB; Liao, YH; Shen, LJ; Wang, SJ, 2020
)
1.54
"Calcitriol has several antineoplastic effects in CRC: it promotes the G1-phase cycle arrest, lowers vascular endothelial growth factor (VEGF) synthesis and acts on tumour stromal fibroblasts to limit cell migration and angiogenesis."( Vitamin D and the insulin-like growth factor system: Implications for colorectal neoplasia.
Ciulei, G; Coste, SC; Cozma, A; Negrean, V; Orasan, OH; Procopciuc, LM, 2020
)
1.28
"Calcitriol has been shown to have enhancing effects on the immune system, the cardiovascular system, the endocrine system, and other metabolic pathways."( Vitamin D: Vitamin or Hormone?
Ellison, DL; Moran, HR, 2021
)
1.34
"Calcitriol has important effects on cellular differentiation and proliferation, as well as on the regulation of the renin gene. "( Calcitriol reduces kidney development disorders in rats provoked by losartan administration during lactation.
Coimbra, TM; Costa, RS; da Silva, CGA; de Almeida, LF; Francescato, HDC, 2017
)
3.34
"Calcitriol has been demonstrated to provide neuroprotection against ischemia/reperfusion (I/R) injury. "( Neuroprotective effect of calcitriol on ischemic/reperfusion injury through the NR3A/CREB pathways in the rat hippocampus.
Fu, J; Gu, J; Pan, X; Ran, R; Xiao, Y; Xue, R; Zhong, H, 2013
)
2.13
"Calcitriol has apparent beneficial effect on acute cellular rejection of liver transplants, which may be associated with increases in the proportion of circulating Treg cells."( Calcitriol reduces the occurrence of acute cellular rejection of liver transplants: a prospective controlled study.
Huang, L; Ling, L; Peng, Z; Qiu, G; Xing, T; Zhong, L, 2013
)
3.28
"Calcitriol has been shown to exert various beneficial cardiovascular effects."( Calcitriol modulates receptor for advanced glycation end products (RAGE) in diabetic hearts.
Chang, CJ; Chen, YJ; Kao, YH; Lee, TI; Lee, TW; Lien, GS, 2014
)
2.57
"Calcitriol has been safely used outside the USA in Europe under the trade name Silkis Ointment for almost a decade in the treatment of psoriasis, and it is currently FDA-approved as Vectical Ointment."( Calcitriol ointment: a review of a topical vitamin D analog for psoriasis.
Feldman, SR; Sigmon, JR; Yentzer, BA, 2009
)
2.52
"Calcitriol has important immunomodulatory properties."( Vitamin D and the adaptive immune system with special emphasis to allergic reactions and allograft rejection.
Koerfer, R; Tenderich, G; Zittermann, A, 2009
)
1.07
"Calcitriol has antitumoural properties."( Calcitriol down-regulates human ether a go-go 1 potassium channel expression in cervical cancer cells.
Avila, E; Barrera, D; Camacho, J; Díaz, L; García-Becerra, R; Halhali, A; Larrea, F; Ordaz-Rosado, D; Rodríguez-Rasgado, JA; Steinmeyer, A; Zügel, U, 2010
)
2.52
"Calcitriol has been shown to inhibit the synthesis and release of certain cytokines, such as RANTES, platelet-derived growth factor, and matrix metalloproteinases, from bronchial smooth muscle cells, thereby leading to decreased lung inflammation and smooth muscle cell proliferation."( The role of vitamin D in asthma.
Casale, TB; Sandhu, MS, 2010
)
1.08
"VD3 (calcitriol) has been identified as a possible adjunct in the treatment of cancer because of its antiproliferative and antitumorigenic properties."( Use of 1,25α dihydroxyvitamin D3 as a cryosensitizing agent in a murine prostate cancer model.
Baust, JG; Baust, JM; Gage, AA; Mouraviev, V; Polascik, TJ; Santucci, KL; Snyder, KK; Van Buskirk, RG, 2011
)
0.82
"Calcitriol has anti-proliferative properties in PCASMCs and these actions are mediated through VDR."( Decreased expression of vitamin D receptors in neointimal lesions following coronary artery angioplasty in atherosclerotic swine.
Agrawal, DK; Agrawal, T; Del Core, MG; Gupta, GK; Hunter, WJ, 2012
)
1.1
"Calcitriol has been associated with calcium homeostasis regulation."( Molecular aspects of vitamin D anticancer activity.
Bohl, L; Liaudat, AC; Picotto, G; Tolosa de Talamoni, N, 2012
)
1.1
"Calcitriol has known anticancer properties on different neoplastic cell lines, but no data are available regarding its activity on tumorigenic pancreatic beta-cells."( Antitumorigenic and antiinsulinogenic effects of calcitriol on insulinoma cells and solid beta-cell tumors.
Adorini, L; Bertuzzi, F; Casorati, M; Cavallaro, U; Christofori, G; Davalli, AM; Fiorina, P; Folli, F; Freschi, M; Galbiati, F; Gregori, S; Polastri, L; Pozza, G; Zerbi, A, 2002
)
1.29
"Calcitriol has been widely used for the treatment of 2HPT."( Effects of calcitriol on parathyroid function and on bone remodelling in secondary hyperparathyroidism.
Costa, AF; dos Reis, LM; Jorgetti, V; Moysés, RM; Ribeiro, MC, 2003
)
1.43
"Calcitriol has been shown to have immunomodulatory effects. "( Reduction of immunosuppressant therapy requirement in heart transplantation by calcitriol.
Briffa, NK; Eisman, JA; Keogh, AM; Sambrook, PN, 2003
)
1.99
"Calcitriol has shown a beneficial effect in scleroderma and morphea during open studies. "( Oral calcitriol: a new therapeutic agent in cutaneous lichen sclerosis.
Balme, B; Chouvet, B; Meunier-Mure, F; Ronger, S; Thomas, L; Viallard, AM, 2003
)
2.28
"Calcitriol ointment has been approved for the treatment of psoriasis in many countries around the world. "( Topical calcitriol is degraded by ultraviolet light.
Gilliard, J; Lebwohl, M; Quijije, J; Rollin, T; Watts, O, 2003
)
2.2
"Calcitriol has been shown to prolong the doubling time of PSA in this context, but near-toxic doses are required."( Pilot study: potential role of vitamin D (Cholecalciferol) in patients with PSA relapse after definitive therapy.
Chander, S; Choo, R; Jamieson, M; Vieth, R; Woo, TC, 2005
)
1.05
"Calcitriol has been implicated as an agent that has neuroprotective effects in various animal models of diseases, possibly by upregulating glial cell line-derived neurotrophic factor (GDNF). "( Calcitriol protection against dopamine loss induced by intracerebroventricular administration of 6-hydroxydopamine.
Cass, WA; Fletcher-Turner, A; Smith, MP; Yurek, DM, 2006
)
3.22
"Calcitriol has traditionally been the most widely used treatment for secondary hyperparathyroidism (SHPT) in uremic patients. "( [A long-term comparative study of calcitriol versus alphacalcidol in patients with secondary hyperparathyroidism on hemodialysis].
Amoedo, ML; Arenas, MD; Egea, JJ; Gil, MT; Millán, I; Muray, S, 2006
)
2.06
"Calcitriol has strong antiproliferative effects in prostate, breast, colorectal, head/neck and lung cancer, as well as lymphoma, leukemia and myeloma model systems."( Vitamin D compounds: clinical development as cancer therapy and prevention agents.
Fakih, M; Johnson, CS; Muindi, J; Trump, DL; Yu, WD,
)
0.85
"Calcitriol has important immunomodulation action and can prolong recipient survival after organ transplantation. "( Calcitriol prolongs recipient survival by inducing expression of zinc-finger protein A20 and inhibiting its downstream gene following rat orthotopic liver transplantation.
Wang, Y; Xie, H; Zhang, A; Zhang, M; Zheng, S, 2006
)
3.22
"Calcitriol has no effect on DHT mediated expression of the three genes."( Regulation of 17beta-hydroxysteroid dehydrogenase type 2, type 4 and type 5 by calcitriol, LXR agonist and 5alpha-dihydrotestosterone in human prostate cancer cells.
Tuohimaa, P; Wang, JH, 2007
)
1.29
"Calcitriol has long been used as the main therapy in renal osteodystrophy, but the efficacy of the oral route is not always as high as expected."( Intraperitoneal calcitriol in infants on peritoneal dialysis.
Azocar, MA; Cano, FJ; Delucchi, MA; Emilfork, M; Guerrero, JL; Lillo, AM; Rodríguez, EE,
)
1.92
"Calcitriol deficit has been described in patients with acute lymphoblast leukemia (ALL). "( Effect of 1,25(OH)2-vitamin D on bone mass in children with acute lymphoblastic leukemia.
Arinoviche, RS; Arriagada, MM; Casanova, DM; Díaz, PR; Fischer, SG; Giadrosich, VR; Milinarsky, AT; Neira, LC; Teresa Torres, MC, 2008
)
1.79
"Calcitriol has been shown to inhibit (i) cell proliferation of renal carcinoma cell lines and of cultured adult human mesangial cells in vitro, and (ii) renal compensatory growth in vivo. "( Inhibition of growth by calcitriol in a proximal tubular cell line (OK).
Orth, S; Reichel, H; Ritz, E; Weih, M; Weinreich, T, 1994
)
2.04
"Calcitriol has recently been shown to be effective against psoriasis. "( Effect of calcitriol on growth, differentiation, chemokine mRNA expression of cultured keratinocytes and on keratinocyte-T cell binding.
Boorsma, DM; Bruynzeel, I; de Haan, P; Sampat, S; Stoof, TJ; van der Raaij, EM; Willemze, R, 1994
)
2.13
"Calcitriol therapy has been documented to reduce PTH levels by shifting the curve to the left and downward."( Different effects of calcitriol and parathyroidectomy on the PTH-calcium curve in dialysis patients with severe hyperparathyroidism.
Colecchia, M; Corradi, B; Cosci, P; Grossi, L; Imbasciati, E; Leopardi, O; Malberti, F; Oldini, C, 1996
)
1.33
"Calcitriol pulse therapy has markedly changed the management of secondary hyperparathyroidism in chronic dialysis patients. "( Ultrasonographic intervention of parathyroid hyperplasia in chronic dialysis patients: a theoretical approach.
Fukagawa, M; Kitaoka, M; Kurokawa, K, 1996
)
1.74
"Calcitriol has been widely used in the management of osteoporosis, but its efficiency is a matter of controversy. "( Comparison of calcitriol treatment with etidronate-calcitriol and calcitonin-calcitriol combinations in Turkish women with postmenopausal osteoporosis: a prospective study.
Bayraktar, M; Gedik, O; Gürlek, A, 1997
)
2.1
"Calcitriol has been shown to cause a shift from Th-1 to Th-2 type reactions when applied locally to the skin."( Effects of calcitriol on eosinophil activity and antibody responses in patients with schistosomiasis.
de Sommers, K; Lizamore, DJ; Snyman, JR; Steinmann, MA, 1997
)
1.41
"Oral calcitriol has been beneficial in the treatment of localized and extensive morphea/scleroderma, but the use of topical calcipotriene has not been reported."( Topical calcipotriene for morphea/linear scleroderma.
Cunningham, BB; Landells, ID; Langman, C; Paller, AS; Sailer, DE, 1998
)
0.76
"Calcitriol has a dose-dependent inhibition on fibroblast proliferation and collagen synthesis and has immunoregulatory activities."( Treatment of linear scleroderma with oral 1,25-dihydroxyvitamin D3 (calcitriol) in seven children.
Elst, EF; Oranje, AP; Van Suijlekom-Smit, LW,
)
1.09
"Calcitriol has a similar effect on kidney distal tubule PMCA activity in vivo but the cellular basis for this effect has not been studied."( Calcitriol upregulates expression and activity of the 1b isoform of the plasma membrane calcium pump in immortalized distal kidney tubular cells.
Dick, IM; Glendenning, P; Prince, RL; Ratajczak, T, 2000
)
2.47
"Calcitriol has shown a benefit in various small uncontrolled studies of ex vivo immune function. "( A placebo-controlled trial to evaluate immunomodulatory effects of paricalcitol.
Ambrosius, WT; Batiuk, TD; Gassensmith, CM; Harezlak, J; Moe, SM; Murphy, CL; Russell, RR; Zekonis, M, 2001
)
1.75
"IV calcitriol therapy has a greater suppression of PTH at the 3rd month of the therapy. "( Comparative effect of oral pulse and intravenous calcitriol treatment in hemodialysis patients: the effect on serum IL-1 and IL-6 levels and bone mineral density.
Akbulut, M; Gönen, S; Gürbilek, M; Tombul, Z; Türk, S; Yeksan, M; Yildiz, A, 2002
)
1.19
"Calcitriol (1,25(OH)2D3) has been shown, under certain conditions, to elicit an in vitro response in adult avian calvarium which may be interpreted as calcium uptake by the bone. "( Vitamin D3 and avian bone in vitro: specificity of effect on Japanese quail calvaria.
Gunasekaran, S; Kenny, AD, 1986
)
1.71

Actions

Calcitriol treatment can increase lumbar BMD and improve balance ability, and these effects become more obvious with prolongation of intervention time. Calcitril may directly suppress osteoblastic activity in patients with secondary hyperparathyroidism when given in large doses.

ExcerptReferenceRelevance
"Calcitriol can inhibit osteoclastogenesis in an inflammatory environment by changing the proportion and function of Th cell subsets. "( Calcitriol inhibits osteoclastogenesis in an inflammatory environment by changing the proportion and function of T helper cell subsets (Th2/Th17).
An, Y; Bi, CS; Chen, FM; Hong, YL; Li, X; Qu, HL; Sun, LJ; Tian, BM, 2020
)
3.44
"Calcitriol tended to increase plasma concentrations of β-hydroxybutyrate and serotonin, but concentrations of glucose, nonesterified fatty acids, and C-telopeptide of type I collagen in plasma did not differ between treatments."( Use of calcitriol to maintain postpartum blood calcium and improve immune function in dairy cows.
Galvão, K; Jeong, KC; Lima, IRP; Lopera, C; Lopes, F; Nelson, CD; Santos, JEP; Sinedino, LDP; Thatcher, WW; Vieira-Neto, A; Zimpel, R, 2017
)
1.63
"Calcitriol could inhibit NF-κB activation and necroptotic pathway."( Calcitriol Ameliorates AngiotensinII-Induced Renal Injury Partly via Upregulating A20.
Gan, H; Xia, Y; Zhao, H, 2017
)
2.62
"Calcitriol treatment can increase lumbar BMD and improve balance ability, and these effects become more obvious with prolongation of intervention time."( Correlations of Serum Hormones and Bone Mineral Density with Fracture and Balance Ability of Postmenopausal Patients and Effects of Calcitriol.
Han, J; Li, J; Li, P; Liu, B; Wang, J; Xu, L; Yang, N, 2018
)
1.41
"Calcitriol did not suppress HBV transcription, cccDNA expression or HBV RNA levels in HepG2.2.15 cells. "( Hepatitis B virus downregulates vitamin D receptor levels in hepatoma cell lines, thereby preventing vitamin D-dependent inhibition of viral transcription and production.
Ben-Ari, Z; Gotlieb, N; Lapidot, Y; Safran, M; Sultan, M; Tachlytski, I, 2018
)
1.92
"Calcitriol promotes vascular calcification through a systemic action rather than through a direct vascular action."( Role of local versus systemic vitamin D receptors in vascular calcification.
Lomashvili, KA; O'Neill, WC; Wang, X, 2014
)
1.85
"Calcitriol could inhibit proliferation of HaCaT at the concentration of 10(-9) -10(-6 ) mol/L."( Calcitriol inhibits keratinocyte proliferation by upregulating leukocyte elastase inhibitor (serpin B1).
Hui, L; Jun, G; Yongxia, Z; Zhili, G, 2014
)
2.57
"Calcitriol can enhance the sensitivity of cancer cells to radiation in vitro. "( Calcitriol does not significantly enhance the efficacy of radiation of human cervical tumors in mice.
Ma, Y; Song, S; Wang, M; Xing, L; Yu, Y; Zhang, F, 2015
)
3.3
"Calcitriol promotes locomotor recovery after SCI by reducing oxidative stress and inhibiting apoptosis, as well as promoting autophagy."( Effects of calcitriol on experimental spinal cord injury in rats.
Chen, DH; Jin, HM; Wang, XY; Wu, K; Xu, HZ; Zhang, XL; Zhou, KL, 2016
)
2.27
"Calcitriol plays an important role in modulating the immune response to viral infections."( Effects of calcitriol (1, 25-dihydroxy-vitamin D3) on the inflammatory response induced by H9N2 influenza virus infection in human lung A549 epithelial cells and in mice.
Chen, Q; Gui, B; He, G; Hu, C; Zhu, C, 2017
)
1.57
"Calcitriol is needed because hypomagnesemia results in decreased production and resistance to the actions of active vitamin D, which leads to the disturbance of intracellular signal transmission."( Primary familial hypomagnesemia syndrome: a new approach in treatment.
Nesibe, A; Sinasi, O, 2012
)
1.1
"Calcitriol may directly suppress osteoblastic activity in patients with secondary hyperparathyroidism when given in large doses to patients undergoing peritoneal dialysis."( Development of adynamic bone in patients with secondary hyperparathyroidism after intermittent calcitriol therapy.
Belin, TR; Chon, Y; Gales, B; Goodman, WG; Ramirez, JA; Salusky, IB; Segre, GV, 1994
)
1.23
"Calcitriol deficits cause increased PTH and, as these two hormones are designed to maintain calcium and phosphorus homeostasis, the PTH increase is initially adaptive."( Benefits of calcitriol therapy and serum phosphorus control in dogs and cats with chronic renal failure. Both are essential to prevent of suppress toxic hyperparathyroidism.
Chew, DJ; Nagode, LA; Podell, M, 1996
)
1.39
"The calcitriol-mediated increase in Na+ uptake appeared to be related to increased tight-junctional or paracellular permeability."( Calcitriol-dependent, paracellular sodium transport in the embryonic chick intestine.
Corradino, RA; Cross, HS; Peterlik, M, 1987
)
2.2
"Calcitriol induced an increase in u-PA mRNA with a marked reduction in PAI-2 mRNA."( Modulation of urokinase-type plasminogen activator and plasminogen activator inhibitor-2 expression by U-937 mononuclear phagocytes. Effects of 1 alpha, 25-dihydroxyvitamin D3 and phorbol ester.
Gyetko, MR; Sitrin, RG; Webb, AC, 1988
)
1

Treatment

Ccitriol treatment after uric acid induction may attenuate kidney injury through upregulation of SOD-1 and downregulation of Collagen-1, TGF-1 gene expression. Treatment repressed renal injury in rat diabetic kidneys and reduced high glucose-induced damage to cultured podocytes.

ExcerptReferenceRelevance
"Calcitriol treatment attenuated the injury with reducing uric acid and creatinine levels, as well as tubular injury."( Calcitriol Treatment Attenuates Uric Acid-Induced Kidney Injury via Super Oxide Dismutase-1 (SOD-1) Upregulation and Fibrosis Reduction
Arefian, N; Juffrie, M; Perdana Putri, RG; Ratna Sari, DC; Romi, MM; Wahyu Setyaningsih, WA, 2021
)
2.79
"Calcitriol treatment after uric acid induction may attenuate kidney injury through upregulation of SOD-1 and downregulation of Collagen-1 and TGF-1 gene expression."( Calcitriol Treatment Attenuates Uric Acid-Induced Kidney Injury via Super Oxide Dismutase-1 (SOD-1) Upregulation and Fibrosis Reduction
Arefian, N; Juffrie, M; Perdana Putri, RG; Ratna Sari, DC; Romi, MM; Wahyu Setyaningsih, WA, 2021
)
3.51
"Calcitriol treatment repressed renal injury in rat diabetic kidneys and reduced high glucose-induced damage to cultured podocytes."( Vitamin D/vitamin D receptor/Atg16L1 axis maintains podocyte autophagy and survival in diabetic kidney disease.
Shi, L; Song, Z; Xia, Y; Xiao, C; Zha, H; Zhang, Y; Zhu, J, 2022
)
1.44
"Calcitriol treatment did not affect miR-21 levels in HEK-293 cells."( Vitamin D Status, Cardiovascular Risk Profile, and miRNA-21 Levels in Hypertensive Patients: Results of the HYPODD Study.
Abate, V; Buondonno, I; D Amelio, P; D Elia, L; De Filippo, G; Fallo, F; Faraonio, R; Martinelli, F; Muscariello, R; Rebellato, A; Rendina, D; Strazzullo, P; Succoio, M, 2022
)
1.44
"Calcitriol treatment induced cytotoxicity in a dose- and time-dependent manner and caused growth arrest in HeLa cells. "( Calcitriol potentially alters HeLa cell viability via inhibition of autophagy.
Abdulah, R; Gatera, VA; Goenawan, H; Judistiani, RTD; Lesmana, R; Setiabudiawan, B; Setiawan, I; Suardi, D; Supratman, U,
)
3.02
"Calcitriol treatments resulted in a significant fall in iPTH, CTX, PINP and OCN levels and rise FGF-23, with mean (95 % confidence interval) between group differences in iPTH [-27.8 pg/ml; 95 % CI (-42.3 to -13.2); p < 0.001], FGF-23 [30.6 pg/ml; 95 % CI (14.8 to 46.3); p < 0.001], CTX [0.12 μg/l; 95 % CI (-0.19 to -0.06); (p < 0.001) and OCN [-4.03 ng/ml; 95 % CI (-7.8 to -0.27); p = 0.036]."( Impact of treatment with active vitamin D calcitriol on bone turnover markers in people with type 2 diabetes and stage 3 chronic kidney disease.
Ayis, S; Corcillo, A; Fountoulakis, N; Gnudi, L; Karalliedde, J; Maltese, G; Mangelis, A; Panagiotou, A; Stathi, D, 2023
)
1.9
"Calcitriol-treated lipoaspirate demonstrated dose-dependent increases in SVF viability and metabolic reserve during hypoxic stress. "( Active Vitamin D3 (Calcitriol) Increases Adipose Graft Retention in a Xenograft Model.
Amurgis, C; DeSanto, M; Guerrero, D; Gusenoff, JA; Kokai, LE; Lee, P; Loder, S; Olevian, D; Patadji, S; Peter Rubin, J; Stavros, AG; Wang, S, 2023
)
2.68
"Calcitriol-treated MSCs significantly increased the levels of IL-12, TGF-β, and IFN-γ compared to non-treated MSCs groups. "( Effect of Calcitriol Treated Mesenchymal Stem Cells as an Immunomodulation Micro-environment on Allergic Asthma in a Mouse Model.
Ghalavand, M; Gouvarchin Ghaleh, HE; Khafaei, M; Kondori, BJ; Mohammadi-Yeganeh, S; Nodoushan, MM; Paryan, M; Vazifedust, S, 2023
)
2.76
"Calcitriol treatment attenuated FGF23-induced cardiac fibrosis and improved diastolic function via inhibition of transforming growth factor-β signaling."( Fibroblast Growth Factor 23 Exacerbates Cardiac Fibrosis in Deoxycorticosterone Acetate-Salt Mice With Hypertension.
Honda, H; Kato, T; Koiwa, F; Mizobuchi, M; Ogata, H; Saito, T, 2023
)
1.63
"Calcitriol treatment suppressed the expression of genes and proteins implicated in glycolysis (GLUT1, HKII, LDHA), promoted cancer cell apoptosis, and reduced viability and Cyclin D1gene expression in MCM-induced breast cancer cells. "( A High Dose of Calcitriol Inhibits Glycolysis and M2 Macrophage Polarization in the Tumor Microenvironment by Repressing mTOR Activation: in vitro and Molecular Docking Studies.
Al-Harrasi, A; Gollahon, LS; Halim, SA; Hussain, F; Khan, A; Khan, F; Munir, MT; Rahman, MM; Rahman, SM; Santos, JM, 2023
)
2.71
"Calcitriol-treated groups had higher RAS-associated AT2R, MasR, ACE2, and angiopoietin 1-7 (Ang(1-7)) levels in the lungs."( Potential therapeutic implications of calcitriol administration and weight reduction on CD4 T cell dysregulation and renin angiotensin system-associated acute lung injury in septic obese mice.
Chen, KY; Chen, PD; Kuo, TC; Lee, PC; Lin, MT; Wu, JM; Wu, MH; Yang, PJ; Yeh, CL; Yeh, SL, 2023
)
1.9
"The calcitriol treatments did not prevent hyperthermia during the multiple injections of METH, indicating that the protective effects of calcitriol are not due to prevention of METH-induced increases in body temperature."( Calcitriol protects against reductions in striatal serotonin in rats treated with neurotoxic doses of methamphetamine.
Cass, WA; Peters, LE, 2023
)
2.83
"Calcitriol treatment did not alter serum oestradiol concentrations, while 25(OH) D levels significantly decreased in both treated groups."( The effect of calcitriol on the development and implantation capacity of embryos from hyper-stimulated mice.
Bognár, Z; Csabai-Tanics, TJ; Görgey, É; Horváth-Szalai, Z; Mikó, É; Szekeres-Barthó, J, 2023
)
1.99
"Calcitriol as adjunctive treatment can result in beneficial treatment outcomes in M.tb infection by suppressing the inflammatory response and up-regulating the expression of anti-microbial peptides. "( Calcitriol enhances pyrazinamide treatment of murine tuberculosis.
Bao, R; Dai, M; Guo, M; Huang, ZX; Rao, Y; Wang, X; Yu, Q; Zhang, J, 2019
)
3.4
"Calcitriol treatment also decreased production of granzyme, IL-2 and MIP-1β by T cells and increased the transcriptional expression of the inhibitor of NF-kB and the antiviral genes cathelicidin (CAMP) and APOBEC3G in PBMCs from Co-HC."( Vitamin D treatment of peripheral blood mononuclear cells modulated immune activation and reduced susceptibility to HIV-1 infection of CD4+ T lymphocytes.
Aguilar-Jimenez, W; Ball, TB; Gonzalez, SM; Rugeles, MT; Su, RC; Trujillo-Gil, E; Zapata, W, 2019
)
1.24
"Calcitriol-treated group (especially SND2) demonstrated significant lower tubular injury, glomerulosclerosis, and interstitial fibrosis compared to SN."( Calcitriol Ameliorates Kidney Injury Through Reducing Podocytopathy, Tubular Injury, Inflammation and Fibrosis in 5/6 Subtotal Nephrectomy Model in Rats.
Arfian, N; Chairunnisa, N; Debora, J; Leksono, TP; Putri, MW; Reynaldi, GN; Sari, DCR; Simanjuntak, BC; Yunus, J, 2020
)
2.72
"Calcitriol treatment up-regulated VDR and protein tyrosine phosphatase N 2 (PTPN2) expression, down-regulated signal transducers and activators of transcription (STAT3) phosphorylation and thereby facilitating chemotherapy drug Doxorubicin-induced apoptosis in PTC cell lines."( Calcitriol enhances Doxorubicin-induced apoptosis in papillary thyroid carcinoma cells via regulating VDR/PTPN2/p-STAT3 pathway.
Dong, W; He, L; Qin, Y; Sun, W; Wang, Z; Zhang, H; Zhang, P; Zhang, T, 2020
)
2.72
"Calcitriol treatment ameliorated the severity of proteinuria and reduced renal tubular epithelial cells apoptosis in DN rats. "( Calcitriol attenuates renal tubular epithelial cells apoptosis via inhibiting p38MAPK signaling in diabetic nephropathy.
Guo, Y; Xie, X; Yang, Y; Zhang, X; Zhao, Y; Zhou, M, 2020
)
3.44
"Calcitriol treatment attenuates intestinal permeability, reduces bacterial translocation, and enriches potentially beneficial gut microbiota in cirrhotic rats that may enable it as a potential therapeutic agent to prevent cirrhotic complications."( Active Vitamin D
Hou, MC; Hsieh, YC; Huang, YH; Huo, TI; Lee, KC; Lee, PC; Li, CP; Lin, CH; Lin, HC; Yang, UC, 2021
)
2.06
"Calcitriol treatment decreased mitochondrial membrane potential and increased the release of cancer cytochrome C."( Progesterone induces apoptosis by activation of caspase-8 and calcitriol via activation of caspase-9 pathways in ovarian and endometrial cancer cells in vitro.
Casablanca, Y; Maxwell, GL; McGlorthan, L; Paucarmayta, A; Syed, V, 2021
)
1.58
"Calcitriol treatments along with weight loss and diet recommendations decreased the liver enzymes (AST, ALT, and ALP, p < 0.001 for all) and fatty liver indices (HSI, p < 0.01 and APRI, p < 0.001), compared to the baseline. "( The efficacy of calcitriol treatment in non-alcoholic fatty liver patients with different genotypes of vitamin D receptor FokI polymorphism.
Cheraghian, B; Ghanavati, F; Mohammadtaghvaei, N; Seyedian, SS; Yaghooti, H, 2021
)
2.41
"Calcitriol treatment lowered expressions of blood and lung inflammatory mediators at 12 and/or 24 h after CLP."( Intravenous calcitriol administration regulates the renin-angiotensin system and attenuates acute lung injury in obese mice complicated with polymicrobial sepsis.
Chen, KY; Lee, PC; Lin, MT; Su, LH; Wu, JM; Yang, PJ; Yeh, CL; Yeh, SL, 2021
)
1.72
"Calcitriol treatment also resulted in an improvement in renal pathological injury."( Effects of calcitriol on peripheral endothelial progenitor cells and renal renovation in rats with chronic renal failure.
Da, JJ; Dong, R; Sun, ZL; Wan, JX; Yang, X; Yuan, J; Zha, Y, 2021
)
1.73
"The calcitriol treatments significantly increased evoked overflow of DA from the lesioned striatum in both the young adult and middle-aged rats."( Reduced ability of calcitriol to promote augmented dopamine release in the lesioned striatum of aged rats.
Cass, WA; Peters, LE, 2017
)
1.26
"Calcitriol treatment activated VDR protein expression and attenuated neurological deficits in this rat TBI model. "( Induction of the Vitamin D Receptor Attenuates Autophagy Dysfunction-Mediated Cell Death Following Traumatic Brain Injury.
Cui, C; Cui, J; Cui, Y; Gao, J; Jiang, P; Jiang, X; Jin, F; Li, R; Tian, Y; Wang, K, 2017
)
1.9
"Calcitriol treatment can increase lumbar BMD and improve balance ability, and these effects become more obvious with prolongation of intervention time."( Correlations of Serum Hormones and Bone Mineral Density with Fracture and Balance Ability of Postmenopausal Patients and Effects of Calcitriol.
Han, J; Li, J; Li, P; Liu, B; Wang, J; Xu, L; Yang, N, 2018
)
1.41
"Calcitriol treatment yields a considerable decrease in serum sclerostin and significant increase of handgrip strength, and the change in serum sclerostin is regulated by serum PTH and by muscle strength."( Levels of serum sclerostin, FGF-23, and intact parathyroid hormone in postmenopausal women treated with calcitriol.
Chen, M; Cheng, Q; Du, Y; Hong, W; Li, H; Tang, W; Wu, X; Zheng, S, 2018
)
2.14
"Calcitriol treatment increased mRNA expression of triglyceride synthesizing genes DGAT1 and DGAT2 and also lipolytic genes ATGL and CGI-58."( Vitamin D produces a perilipin 2-dependent increase in mitochondrial function in C2C12 myotubes.
Bollinger, LM; Peterson, CA; Schnell, DM; Sullivan, PG; Thomas, DT; Vekaria, HJ; Walton, RG, 2019
)
1.24
"Calcitriol treatment significantly alleviated bone loss, and improved bone microarchitecture and biomechanical properties and also decreased serum glucose and glycated serum protein levels."( 1,25-Dihydroxy vitamin D3 treatment attenuates osteopenia, and improves bone muscle quality in Goto-Kakizaki type 2 diabetes model rats.
Cui, L; Du, M; Lai, W; Li, S; Liang, Y; Liu, Y; Min, Y; Mo, Y; Wang, P; Zhou, L, 2019
)
1.24
"Calcitriol (1 μg/kg) treatment for 7 consecutive days after SCI was compared SCI control and Sham control rat groups."( Immunomodulatory effects of Calcitriol in acute spinal cord injury in rats.
Askarifirouzjaei, H; Fazeli, M; Khajoueinejad, L; Mohammadi, A; Namazi, F; Pourfathollah, AA; Rajaian, H, 2019
)
1.53
"Calcitriol treatment improved the cardiac injury resulting from excessive ISO stimulation, as supported by the suppression of the development of myocardial hypertrophy, interstitial fibrosis, and H2O2 level in heart tissue. "( Cardioprotective effect of calcitriol on myocardial injury induced by isoproterenol in rats.
Cheng, S; Wang, X; Yang, Y; Zhu, Y, 2013
)
2.13
"Calcitriol-treated diabetic hearts also had lesser expressions of p-SMAD2/3 and p-ERK signaling than those of diabetic hearts."( Calcitriol modulates receptor for advanced glycation end products (RAGE) in diabetic hearts.
Chang, CJ; Chen, YJ; Kao, YH; Lee, TI; Lee, TW; Lien, GS, 2014
)
2.57
"The calcitriol treatments also led to increases in postmortem tissue levels of DA in the striatum and substantia nigra."( Calcitriol promotes augmented dopamine release in the lesioned striatum of 6-hydroxydopamine treated rats.
Cass, WA; Fletcher, AM; Peters, LE; Yurek, DM, 2014
)
2.33
"Calcitriol-treated patients had higher cathelicidin (P = 0.04) and IL-10 (P = 0.03) mRNA expression than placebo-treated patients 24 hours after study drug administration."( Randomized controlled trial of calcitriol in severe sepsis.
Donnino, MW; Ginde, AA; Leaf, DE; Raed, A; Waikar, SS, 2014
)
1.41
"Calcitriol treatment began on the day of challenge, and survival assessed for 10 days."( Vitamin D and experimental invasive aspergillosis.
Chen, V; Clemons, KV; Martinez, M; Sirivoranankul, C; Stevens, DA, 2014
)
1.12
"Calcitriol treatment alone significantly decreased TRPM7 protein (↓ to ∼11%), whereas the combination treatment increased both mRNA (1.7×) and protein (6.8×) expression compared with calcitriol alone."( Magnesium Modifies the Impact of Calcitriol Treatment on Vascular Calcification in Experimental Chronic Kidney Disease.
Adams, MA; Barron, H; Holden, RM; Laverty, K; McCabe, KM; Svajger, B; Zelt, JG, 2015
)
1.42
"With calcitriol treatment, oxidative stress was decreased, SOD activity and GSH content were increased and MDA content was decreased. "( Effects of calcitriol on experimental spinal cord injury in rats.
Chen, DH; Jin, HM; Wang, XY; Wu, K; Xu, HZ; Zhang, XL; Zhou, KL, 2016
)
1.34
"Calcitriol treatment resulted in a 60% suppression of PTH levels in animals with CKD."( Calcitriol Suppression of Parathyroid Hormone Fails to Improve Skeletal Properties in an Animal Model of Chronic Kidney Disease.
Allen, MR; Brown, DM; Chen, NX; Hammond, MA; Moe, SM; Newman, CL; Tian, N; Wallace, JM, 2016
)
2.6
"Calcitriol treatment of the TL-1 cell line (model of T-LGLL) led to decreased phospho-Y701 STAT1 and phospho-Y705 STAT3 and increased vitamin D receptor (VDR) levels."( Vitamin D decreases STAT phosphorylation and inflammatory cytokine output in T-LGL leukemia.
Feith, DJ; Kulling, PM; Loughran, TP; Olson, KC; Olson, TL; Rainbow, RJ; Tan, SF, 2017
)
1.18
"Calcitriol treatment of cardiomyocytes induced a concentration-dependent increase in I"( Calcitriol (1,25-dihydroxyvitamin D
Bas, M; Delgado, C; Fernández-Velasco, M; Jesús Larriba, M; Manzanares, E; Martín-Nunes, L; Tamayo, M; Val-Blasco, A, 2017
)
3.34
"Calcitriol treatment prior to and post infection with H9N2 influenza significantly decreased expression of the influenza M gene, IL-6, and IFN-β in A549 cells, but did not affect virus replication. "( Effects of calcitriol (1, 25-dihydroxy-vitamin D3) on the inflammatory response induced by H9N2 influenza virus infection in human lung A549 epithelial cells and in mice.
Chen, Q; Gui, B; He, G; Hu, C; Zhu, C, 2017
)
2.29
"Calcitriol or PRI-2191 treatment caused differentiation of WEHI-3 mouse leukemia cells, but apoptosis of LLC cells."( The influence of 1,25-dihydroxyvitamin D3 and 1,24-dihydroxyvitamin D3 on alphavbeta3 integrin expression in cancer cell lines.
Dabrowska, K; Dzimira, S; Filip, B; Klopotowska, D; Kurzepa, A; Kutner, A; Maciejewska, M; Madej, J; Milczarek, M; Wietrzyk, J, 2008
)
1.07
"calcitriol for the treatment of severe SHPT in our chronic haemodialysis population."( Intravenous calcitriol versus paricalcitol in haemodialysis patients with severe secondary hyperparathyroidism.
Abdul Gafor, AH; Loo, CY; Mohd, R; Norella, KC; Saidin, R; Shah, SA; Zainudin, S, 2009
)
1.45
"Calcitriol pretreatment of the cells elevated their PpIX levels. "( Calcitriol treatment improves methyl aminolaevulinate-based photodynamic therapy in human squamous cell carcinoma A431 cells.
Cicarma, E; Juzeniene, A; Ma, LW; Moan, J; Tuorkey, M, 2009
)
3.24
"calcitriol treatment in the maintenance of normal serum calcium values and renal calcium excretion in children with hypoparathyroidism."( Long-term treatment of 12 children with chronic hypoparathyroidism: a randomized trial comparing synthetic human parathyroid hormone 1-34 versus calcitriol and calcium.
Cutler, GB; Dowdy, K; Peterson, D; Reynolds, J; Sinaii, N; Winer, KK, 2010
)
1.28
"Oral calcitriol treatment could prevent the development of atherosclerosis by changing the function or differentiation of DCs and regulatory T cells. "( Oral administration of an active form of vitamin D3 (calcitriol) decreases atherosclerosis in mice by inducing regulatory T cells and immature dendritic cells with tolerogenic functions.
Hirata, K; Ishida, T; Kita, T; Nakajima, K; Sasaki, N; Shinohara, M; Takeda, M; Yamashita, T, 2010
)
1.12
"Calcitriol-pretreated tumors underwent enhanced apoptotic cell death after ALA-based PDT."( Vitamin D3 enhances the apoptotic response of epithelial tumors to aminolevulinate-based photodynamic therapy.
Anand, S; Hasan, T; Maytin, EV; Wilson, C, 2011
)
1.09
"Calcitriol treatment reduced the levels of urinary miR-155 in patients with SLE."( Expression of miR-146a and miR-155 in the urinary sediment of systemic lupus erythematosus.
Chow, KM; Kwan, BC; Li, EK; Li, PK; Luk, CC; Szeto, CC; Tam, LS; Wang, G, 2012
)
1.1
"Calcitriol treatment reduced actin cytoskeleton reorganization, reduced polarized formation of lamellipodia and reduced colocalization of phosphorylated focal adhesion kinase (p-FAK) with lamellipodia, all consistent with reduced cell ability to move and invade."( The vitamin D receptor regulates rheumatoid arthritis synovial fibroblast invasion and morphology.
Gulko, PS; Laragione, T; Shah, A, 2012
)
1.1
"Calcitriol treatment can reduce proteinuria in patients with DKD without serious adverse events."( An open label, randomized controlled study of oral calcitriol for the treatment of proteinuria in patients with diabetic kidney disease.
Bunnag, S; Krairittichai, U; Mahannopkul, R, 2012
)
2.07
"Calcitriol treatment resulted in 35% reduction of atherosclerosis at the aortic sinus, and in a significant decrease in blood pressure. "( Low-dose calcitriol decreases aortic renin, blood pressure, and atherosclerosis in apoe-null mice.
Entin-Meer, M; Harats, D; Ish-Shalom, M; Kamari, Y; Keren, G; Maysel-Auslender, S; Sack, J; Shaish, A; Stern, N; Tordjman, K; Vechoropoulos, M, 2012
)
2.24
"Calcitriol (C) treatment strategies for secondary hyperparathyroidism remain controversial regarding efficacy and safety. "( Growth in children with chronic renal failure on intermittent versus daily calcitriol.
Ardissino, G; Claris-Appiani, A; Mehls, O; Schmitt, CP; Testa, S, 2003
)
1.99
"Calcitriol treatment increased phosphaturic response to PTH (1-34) (P < 0.05), and there was a negative correlation between phosphaturic response and the PTH levels (P < 0.05)."( Plasma levels of parathyroid hormone (1-84) whole molecule and parathyroid hormone (7-84)-like fragments in pseudohypoparathyroidism type I.
Furukawa, Y; Hatakeyama, Y; Igarashi, T; Mizunashi, K; Sato, Y; Yabuki, S, 2003
)
1.04
"Calcitriol treatment for 6 months significantly increased BMD and reduced serum IL-1 and TNF-alpha concentrations compared with no significant changes in patients treated with calcium alone."( The effects of calcitriol therapy on serum interleukin-1, interleukin-6 and tumour necrosis factor-alpha concentrations in post-menopausal patients with osteoporosis.
Inanir, A; Mermerci, B; Ozoran, K; Tutkak, H,
)
1.21
"Calcitriol treatment did not result in a statistically significant change in the fraction of cells expressing TGFbeta RII, PTEN, or proliferating cell nuclear antigen."( Randomized study of high-dose pulse calcitriol or placebo prior to radical prostatectomy.
Beer, TM; Chin, R; Corless, CL; Garzotto, M; Henner, WD; Lowe, BA; Montalto, MA; Myrthue, A; O'hara, MF, 2004
)
1.32
"Calcitriol treatment produced little or no expression of this approximately 52 kDa band, but markedly increased the expression of a approximately 32 kDa band that was only detected with an antibody directed to the N-terminus of RANKL."( Receptor activator of NF-kappaB ligand protein expression in UMR-106 cells is differentially regulated by parathyroid hormone and calcitriol.
Dossing, DA; Stern, PH, 2005
)
1.25
"Calcitriol treatment of secondary hyperparathyroidism (HPT) in chronic kidney disease (CKD) patients can lead to increased serum calcium and phosphorus, which have been associated as risk factors for vascular calcification. "( 1,25-Dihydroxyvitamin D3 but not cinacalcet HCl (Sensipar/Mimpara) treatment mediates aortic calcification in a rat model of secondary hyperparathyroidism.
Cattley, RC; Colloton, M; Henley, C; Lacey, D; Martin, D; Shatzen, E; Towler, DA, 2005
)
1.77
"Calcitriol-treated rats had moderate to marked aortic calcification, whereas no significant calcification was observed in vehicle- or cinacalcet HCl-only treated groups. "( 1,25-Dihydroxyvitamin D3 but not cinacalcet HCl (Sensipar/Mimpara) treatment mediates aortic calcification in a rat model of secondary hyperparathyroidism.
Cattley, RC; Colloton, M; Henley, C; Lacey, D; Martin, D; Shatzen, E; Towler, DA, 2005
)
1.77
"Calcitriol treatment attenuated PG-mediated functional responses, including the stimulation of prostate cancer cell growth."( Regulation of prostaglandin metabolism by calcitriol attenuates growth stimulation in prostate cancer cells.
Feldman, D; Krishnan, AV; Moreno, J; Nonn, L; Peehl, DM; Swami, S, 2005
)
1.31
"Calcitriol treatment resulted in dose-dependent growth inhibition of LNCaP with approximately 50% growth inhibition at the clinically achievable concentration of 1 nmol/L. "( Effect of calcitriol on prostate-specific antigen in vitro and in humans.
Beer, TM; Eilers, K; Garzotto, M; Janeba, N; Mori, M; Myrthue, A; Park, B; Sauer, D, 2006
)
2.18
"Calcitriol treatment-induced increase in FBPase and decrease in CDDase activities in cancer patient PBM are potential early and sensitive non-hypercalcemia PD measures of calcitriol effects."( Monocyte fructose 1,6-bisphosphatase and cytidine deaminase enzyme activities: potential pharmacodynamic measures of calcitriol effects in cancer patients.
Branch, RA; Johnson, CS; Muindi, JR; Peng, Y; Trump, DL; Wilson, JW, 2007
)
1.99
"Calcitriol treatment decreased the number of fallers and falls. "( An age-related decrease in creatinine clearance is associated with an increase in number of falls in untreated women but not in women receiving calcitriol treatment.
Gallagher, JC; Rapuri, PB; Smith, LM, 2007
)
1.98
"Calcitriol treatment decreases falls in all subjects but especially in elderly women with decreased renal function (<60 ml/min) and frequent fallers."( An age-related decrease in creatinine clearance is associated with an increase in number of falls in untreated women but not in women receiving calcitriol treatment.
Gallagher, JC; Rapuri, PB; Smith, LM, 2007
)
1.98
"The calcitriol treatments did not reduce the hyperthermia associated with multiple injections of METH, indicating that the neuroprotective effects of calcitriol are not due to the prevention of increases in body temperature."( Calcitriol protects against the dopamine- and serotonin-depleting effects of neurotoxic doses of methamphetamine.
Cass, WA; Peters, LE; Smith, MP, 2006
)
2.26
"Calcitriol treatment significantly reduced the number of falls by 50% (OR=0.5, 95% CI: 0.4-0.9, p=0.010) compared to placebo in the low CrCl group."( Falls are associated with decreased renal function and insufficient calcitriol production by the kidney.
Gallagher, JC; Rapuri, P; Smith, L, 2007
)
1.3
"Calcitriol-treatment increased LPS-induced TNFalpha release in MM6 cells but inhibited TNFalpha release from peripheral blood monocytes."( Modulation of monocytic lipopolysaccharide-induced tissue factor expression and tumor necrosis factor alpha release by estrogen and calcitriol.
Angstwurm, MW; Gaertner, R; Vlotides, G,
)
1.06
"Calcitriol-treated animals demonstrated a significant decrease in retinal neovascularization compared with control animals. "( Calcitriol is a potent inhibitor of retinal neovascularization.
Albert, DM; Darjatmoko, SR; Mehraein, F; Scheef, EA; Sheibani, N; Sorenson, CM; Wang, S, 2007
)
3.23
"Calcitriol treatment upregulated the PTH/PTHrP receptor but also increased inhibitors of cell proliferation such as p21(Waf1/Cip1), IGFBP3, and FGFR3."( Bone growth during daily or intermittent calcitriol treatment during renal failure with advanced secondary hyperparathyroidism.
He, YZ; Sanchez, CP, 2007
)
1.33
"Calcitriol-treated uremic rats with acidosis did not develop aortic or soft-tissue calcification, did not increase aortic Pit-1 expression, and had significantly lower mortality."( Metabolic acidosis inhibits soft tissue calcification in uremic rats.
Aguilera-Tejero, E; Lopez, I; Mendoza, FJ; Montes de Oca, A; Perez, J; Rodriguez, M, 2008
)
1.07
"Calcitriol treatment must be closely supervised to prevent hypercalcemia, hyperphosphatemia, and excessive suppression of parathyroid hormone."( Vitamin D therapy in patients receiving dialysis.
Mehls, O; Ritz, E, 1995
)
1.01
"Calcitriol treatment also induced a significant increase in CTR serum levels (P < 0.001) and a significant decrease (P < 0.001) in total parathyroid hormone (PTH)."( Calcitriol effect on natural killer cells from hemodialyzed and normal subjects.
Borrego, F; Martin, A; Peña, J; Quesada, JM; Serrano, I; Solana, R, 1995
)
2.46
"Calcitriol treatment of JB6 Cl41.5a cells for 6 h caused increased secretion of [35S]methionine-labeled OPN, with maximal levels attained after 8 h of treatment."( Calcitriol regulation of osteopontin expression in mouse epidermal cells.
Chang, PL; Prince, CW; Ridall, AL, 1994
)
2.45
"Calcitriol pretreatment (1 microM, 5 days) also decreased the levels of phosphatidyl-inositol, phosphatidylinositol 4-phosphate and phosphatidylinositol 4,5-bisphosphate by 23, 55 and 32%, respectively."( Calcitriol attenuates the thyrotropin-releasing hormone-stimulated inositol phosphate production in clonal rat pituitary (GH4C1) cells.
Haug, E; Sørnes, G; Torjesen, PA, 1993
)
2.45
"Calcitriol treatment of hemodialysis patients with osteitis fibrosa resulted in a significant decrease in PTH throughout the PTH-calcium curve and also reduced the sensitivity (slope) of the PTH-calcium curve."( Parathyroid gland function in chronic renal failure.
Felsenfeld, AJ; Llach, F, 1993
)
1.01
"Calcitriol treatment had no effect on biochemical markers of bone resorption [serum C-terminal telopeptide of type I collagen (ICTP) and fasting urinary excretion of hydroxyproline/creatinine (OHP)]."( Dose-response effect of short-term calcitriol treatment on bone and mineral metabolism in normal males.
Bollerslev, J; Gram, J; Junker, P; Nielsen, HK, 1996
)
1.29
"Calcitriol treatment decreased keratinocyte proliferation, normalized keratinocyte differentiation and decreased immune activation in plaques."( Modulation of epidermal differentiation, tissue inflammation, and T-lymphocyte infilitration in psoriatic plaques by topical calcitriol.
Gilleaudeau, P; Gottlieb, AB; Gottlieb, S; Heftler, N; Kamber, M; Krueger, JG; Lu, I; McLane, JA, 1996
)
1.22
"Calcitriol treatment decreased serum PTH levels and increased the serum calcium and the setpoint (PTHstim); however, the increase in serum calcium was greater than the increase in the setpoint (PTHstim)."( Evidence for both abnormal set point of PTH stimulation by calcium and adaptation to serum calcium in hemodialysis patients with hyperparathyroidism.
Betriu, A; Borrego, MJ; Caravaca, F; Cubero, J; Felsenfeld, AJ; Fernandez, E; Lorenzo, V; Martin-Malo, A; Rodriguez, AP; Rodriguez, M, 1997
)
1.02
"3. Calcitriol treatment should attempt to maintain slightly raised PTH levels."( [Pulsed doses of calcitriol in the treatment of secondary hyperparathyroidism in patients on hemodialysis].
Adamec, M; Petrásek, R; Schück, O; Smrcková, I; Sotorník, I; Tocík, J, 1997
)
1.15
"The calcitriol-pretreated groups demonstrated a significant reduction of apoptosis, with a maximal inhibition seen on day 14."( Reduction of intrafollicular apoptosis in chemotherapy-induced alopecia by topical calcitriol-analogs.
Menrad, A; Paus, R; Schilli, MB, 1998
)
1.01
"Calcitriol treatment significantly lowered serum iPTH levels in group A patients (from 419 +/- 185 to 173 +/- 142 pg/mL, p < 0.0001, delta iPTH: -246 +/- 161 pg/mL); iPTH remained stable in group B patients (delta iPTH: +7.9 +/- 116 pg/mL) with an intergroup significant difference at P < 0.0001."( Long-term effects of small doses of calcitriol in hemodialysis patients with moderate secondary hyperparathyroidism.
Arvanitis, D; Hadjiconstantinou, V; Hadjilouka-Mantaka, A; Noussias, C; Revenas, K; Tzortzis, G; Vlassopoulos, D, 1999
)
1.3
"The calcitriol-treated mice did not have significantly smaller average tumor size (1.26 cm3) than the 16,23-D3-treated mice (P = .35), had significant body weight loss compared with the control animals (calcitriol-treated mice lost 4.03 g) (P =.001), and had a mortality of 90% by the completion of the experiment."( Antineoplastic effect and toxicity of 1,25-dihydroxy-16-ene-23-yne-vitamin D3 in athymic mice with Y-79 human retinoblastoma tumors.
Albert, DM; Darjatmoko, SR; Lindstrom, MJ; Sabet, SJ, 1999
)
0.78
"Calcitriol treatment, either through a reduction in parathyroid hormone (PTH) levels or direct effect on bone, decreases the osteoblast and osteoclast surface and bone formation rate."( Effect of calcitriol and age on recovery from hypocalcemia in hemodialysis patients.
Aljama, P; Almaden, Y; Borrego, MJ; Felsenfeld, AJ; Martin-Malo, A; Rodriguez, M, 1999
)
1.43
"calcitriol treatment period, the observed plasma IPTH concentrations compared with the baseline values were significantly lower (p < 0.01 for A and B group and p < 0.05 for C group) from the sixth month onwards in group A and C and from the third month onwards in group B."( Effective treatment of secondary hyperparathyroidism in hemodialysis patients by titration of intravenous calcitriol dosage.
Balaskas, E; Benos, A; Grekas, D; Kampouris, H; Konstantinou, A; Sioullis, A; Tourkantonis, A, 1999
)
1.24
"Calcitriol treatment abolishes the upregulation of the TSHR number occurring in cells cultivated in the absence of TSH."( Vitamin D: a hormonal regulator of the cAMP signaling pathway.
Berg, JP; Haug, E, 1999
)
1.02
"Calcitriol treatment is used to reduce parathyroid hormone levels in azotemic patients with secondary hyperparathyroidism (HPT). "( The in vitro effect of calcitriol on parathyroid cell proliferation and apoptosis.
Almadén, Y; Campistol, JM; Canalejo, A; Felsenfeld, AJ; Gomez-Villamandos, JC; Ramos, B; Rodríguez, M; Torregrosa, V, 2000
)
2.06
"Calcitriol treatment increased the blood calcium and inorganic phosphorous levels, and reduced the blood PTH level."( Intravenous 1alpha, 25[OH]2 vitamin D3 (calcitriol) pulse therapy for bone lesions in a murine model of chronic cadmium toxicosis.
Hiratsuka, H; Katsuta, O; Kurata, Y; Tsuchitani, M; Umemura, T, 2001
)
1.3
"Calcitriol pretreatment induced a defect in accessory cell function that was evident with fixed monocytes, suggesting a cell-surface-associated mechanism."( Decreased accessory cell function and costimulatory activity by 1,25-dihydroxyvitamin D3-treated monocytes.
Rigby, WF; Waugh, MG, 1992
)
1
"Calcitriol treatment provides a powerful means to reduce PTH concentration in uremic patients that may not be achieved with other methods."( Nephrocalcinosis caused by hyperparathyroidism in progression of renal failure: treatment with calcitriol.
Chew, DJ; Nagode, LA, 1992
)
1.22
"Calcitriol treatment of starved, confluent cultures of MC3T3-E1 cells induced a rapid and transient stimulation of the expression of c-fos, fos-B, c-jun, and jun-B with varying kinetics."( Differential stimulation of fos and jun family members by calcitriol in osteoblastic cells.
Candeliere, GA; Prud'homme, J; St-Arnaud, R, 1991
)
1.25
"Calcitriol-treated cells were morphologically indistinguishable from control cells, while 12-O-tetradecanoylphorbol-13-acetate-treated cells acquired a distinctive morphology."( 1 alpha,25-dihydroxyvitamin D3 stimulates synthesis and secretion of nonphosphorylated osteopontin (secreted phosphoprotein 1) in mouse JB6 epidermal cells.
Chang, PL; Prince, CW, 1991
)
1
"Calcitriol treatment reduced TfR expression by activated T lymphocytes independent of their location in the cell cycle, further suggesting its independence from IL-2-mediated events."( 1,25-Dihydroxyvitamin D3 modulates the effects of interleukin 2 independent of IL-2 receptor binding.
Hamilton, BJ; Rigby, WF; Waugh, MG, 1990
)
1
"Calcitriol treatment was associated with a significant fall in serum phosphorus concentrations and alkaline phosphatase levels as well as with histological evidence of an amelioration of hyperparathyroid changes."( Early therapy of renal bone disease with calcitriol: a prospective double-blind study.
Abrams, SM; Baker, LR; Fanti, P; Faugere, MC; Malluche, HH; Roe, CJ; Subayti, Y, 1989
)
1.26
"In calcitriol pre-treated cells, PMA induced a moderate increase in u-PA mRNA and a marked increase in PAI-2 mRNA."( Modulation of urokinase-type plasminogen activator and plasminogen activator inhibitor-2 expression by U-937 mononuclear phagocytes. Effects of 1 alpha, 25-dihydroxyvitamin D3 and phorbol ester.
Gyetko, MR; Sitrin, RG; Webb, AC, 1988
)
0.79
"Calcitriol treatment did not significantly influence either serum A1 levels or the presence of stainable Al in bone."( Low dose calcitriol versus placebo in patients with predialysis chronic renal failure.
Dahl, E; Nordal, KP, 1988
)
1.41
"Calcitriol treatment of sham-operated rats produced an increase in cancellous and cortical bone mass."( Calcitriol corrects bone loss induced by oophorectomy in rats.
DeLuca, HF; Faugere, MC; Malluche, HH; Okamoto, S, 1986
)
2.44
"Treatment with Calcitriol produced protein carbonyl levels similar to those in the cisplatin-treated and control groups."( Calcitriol potentially alters HeLa cell viability via inhibition of autophagy.
Abdulah, R; Gatera, VA; Goenawan, H; Judistiani, RTD; Lesmana, R; Setiabudiawan, B; Setiawan, I; Suardi, D; Supratman, U,
)
1.91
"Treatment with calcitriol inhibited ovarian cancer cell proliferation, migration, and invasion."( Vitamin D Suppresses Ovarian Cancer Growth and Invasion by Targeting Long Non-Coding RNA CCAT2.
Guo, B; Wang, L; Zhou, S, 2020
)
0.9
"Cows treated with calcitriol excreted more urinary tCa (control = 0.5 vs."( Use of calcitriol to maintain postpartum blood calcium and improve immune function in dairy cows.
Galvão, K; Jeong, KC; Lima, IRP; Lopera, C; Lopes, F; Nelson, CD; Santos, JEP; Sinedino, LDP; Thatcher, WW; Vieira-Neto, A; Zimpel, R, 2017
)
1.23
"Treatment with calcitriol not only reduced proteinuria, but also normalized TRPC6 expression."( The novel role of TRPC6 in vitamin D ameliorating podocyte injury in STZ-induced diabetic rats.
Guo, Y; Song, Z; Zhang, X; Zhou, M, 2015
)
0.76
"Co-treatment with calcitriol (10(-8)M) partially reversed this zoledronate-induced inhibition."( The effect of nitrogen containing bisphosphonates, zoledronate and alendronate, on the production of pro-angiogenic factors by osteoblastic cells.
Edwards, S; Elford, C; Evans, BA; Fogelman, I; Frost, ML; Hampson, G; Ishtiaq, S; Sankaralingam, A, 2015
)
0.74
"Rats treated with calcitriol, especially with the higher dose, exhibited elevated γ-aminobutyric acid (GABA) status."( Neurochemical effects of chronic administration of calcitriol in rats.
Cai, HL; Dang, RL; He, X; Jiang, P; Li, HD; Liu, YP; Tang, MM; Xue, Y; Zhang, LH; Zhu, WY, 2014
)
0.98
"Pretreatment with calcitriol (the active form of vitamin D) reduced cellular injury induced by exposure to catalytic iron."( Protective effects of 1α,25-Dihydroxyvitamin D3 on cultured neural cells exposed to catalytic iron.
Bardelli, C; Molinari, C; Morsanuto, V; Uberti, F, 2016
)
0.76
"Oral treatment with calcitriol reduced Ang-II-induced dissecting AAA formation in apoE(-/-) mice, which was unrelated to systolic blood pressure or plasma cholesterol concentrations. "( Vitamin D Receptor Activation Reduces Angiotensin-II-Induced Dissecting Abdominal Aortic Aneurysm in Apolipoprotein E-Knockout Mice.
Collado, A; Gonzalez-Navarro, H; Hueso, L; Martorell, S; Piqueras, L; Sanz, MJ, 2016
)
0.76
"Treatment with calcitriol for 6 months significantly decreased Th17 cytokine levels compared with the baseline values in another 42 KTRs."( Suppressive Effect of 1α,25-Dihydroxyvitamin D3 on Th17-Immune Responses in Kidney Transplant Recipients With Tacrolimus-Based Immunosuppression.
Cho, ML; Chung, BH; Doh, KC; Kim, BM; Kim, KW; Min, JW; Yang, CW, 2017
)
0.79
"Treatment with calcitriol reduced albuminuria and prevented reduction of capillary density and expansion of interstitium without affecting significant blood pressure and heart weight after perfusion fixation."( Calcitriol ameliorates capillary deficit and fibrosis of the heart in subtotally nephrectomized rats.
Gross, ML; Koleganova, N; Piecha, G; Ritz, E, 2009
)
2.14
"Treatment with calcitriol resulted in growth inhibition in TDEC expressing VDR."( Role of vitamin D receptor in the antiproliferative effects of calcitriol in tumor-derived endothelial cells and tumor angiogenesis in vivo.
Chung, I; Foster, BA; Gillard, BM; Han, G; Johnson, CS; Seshadri, M; Trump, DL; Yu, WD, 2009
)
0.93
"Treatment with calcitriol or tacalcitol inhibits the synthesis of both IL-6 and IL-8 compared to the control group. "( Vitamin D derivatives: calcitriol and tacalcitol inhibits interleukin-6 and interleukin-8 expression in human nasal polyp fibroblast cultures.
Fraczek, M; Krecicki, T; Kubik, P; Kusmierz, D; Latocha, M; Potyka, J; Rostkowska-Nadolska, B; Sliupkas-Dyrda, E; Zatonski, M, 2010
)
1.02
"Treatment with calcitriol resulted in the normalization of biochemical parameters and mean lumbar spine areal bone mineral density z-scores within 3 months, whereas height z-scores increased more gradually."( Short- and long-term outcome of patients with pseudo-vitamin D deficiency rickets treated with calcitriol.
Alos, N; Chabot, G; Edouard, T; Glorieux, FH; Rauch, F; Roughley, P, 2011
)
0.93
"Treatment with calcitriol started in infancy results in short- and long-term correction of all clinical, biochemical, and radiological abnormalities related to PDDR."( Short- and long-term outcome of patients with pseudo-vitamin D deficiency rickets treated with calcitriol.
Alos, N; Chabot, G; Edouard, T; Glorieux, FH; Rauch, F; Roughley, P, 2011
)
0.94
"Treatment with calcitriol produced significantly elevated urinary calcium-to-creatinine ratio."( Persistent hypocalcaemia in a Chinese girl due to a novel de-novo activating mutation of the calcium-sensing receptor gene.
Lam, CW; Tong, CT; Tong, SF; Wong, WC, 2011
)
0.71
"Cotreatment with calcitriol enhanced both modes of TNFalpha-induced death in MCF-7 breast cancer cells."( Vitamin D enhances caspase-dependent and -independent TNFalpha-induced breast cancer cell death: The role of reactive oxygen species and mitochondria.
Koren, R; Liberman, UA; Ravid, A; Weitsman, GE, 2003
)
0.65
"Treatment of calcitriol has a beneficial effect on renal anemia in ESRD patients with SHP."( Improved anemia and reduced erythropoietin need by medical or surgical intervention of secondary hyperparathyroidism in hemodialysis patients.
Huang, CC; Hung, CC; Lin, CL; Yang, CT, 2004
)
0.68
"Treatment with calcitriol was not underway at the time of the biopsy."( 25-hydroxyvitamin D levels and bone histomorphometry in hemodialysis renal osteodystrophy.
Balducci, A; Ballanti, P; Bonucci, E; Coen, G; Manni, M; Mantella, D; Nofroni, I; Sardella, D, 2005
)
0.67
"Treatment with calcitriol induced significant vascular calcification (aortic Ca increased to 4.2+/-1.2 mg/g at day 14 and to 11.4+/-0.7 mg/g at day 56; P<0.05 versus vehicle)."( Calcimimetic R-568 decreases extraosseous calcifications in uremic rats treated with calcitriol.
Aguilera-Tejero, E; Almaden, Y; Lopez, I; Martin, D; Mendoza, FJ; Perez, J; Rodriguez, M, 2006
)
0.9
"Treatment with calcitriol for 8 days resulted in massive medial calcification of the aorta with a 10- to 30-fold increase in the aortic Ca and P content."( Reversibility of calcitriol-induced medial artery calcification in rats with intact renal function.
Aguilera-Tejero, E; Bas, A; Lopez, I; Perez, J; Rodriguez, M, 2006
)
1.01
"Pretreatment with calcitriol (100 nM, 48 h) sensitized HT-29 colon cancer cells to cell death induced by acute exposure to H2O2 or chronic exposure to the H2O2 generating system, glucose/glucose-oxidase."( Calcitriol sensitizes colon cancer cells to H2O2-induced cytotoxicity while inhibiting caspase activation.
Koren, R; Ravid, A; Wacksberg, S; Weitsman, GE, 2006
)
2.1
"Pretreatment with calcitriol, enhanced TNF-induced EGFR-Src dependent ERK activation and tyrosine phosphorylation of the EGFR, but abolished the EGFR-Src independent ERK activation."( Two modes of ERK activation by TNF in keratinocytes: different cellular outcomes and bi-directional modulation by vitamin D.
Koren, R; Miodovnik, M; Ravid, A; Rotem, C; Ziv, E, 2008
)
0.67
"Treatment with calcitriol was associated with a trend toward a lower incidence of dialysis."( Association of activated vitamin D treatment and mortality in chronic kidney disease.
Ahmadzadeh, S; Anderson, JE; Kalantar-Zadeh, K; Kovesdy, CP, 2008
)
0.69
"Treatment with calcitriol, the active form of vitamin D, reduces serum parathyroid hormone (PTH) levels but may result in both hypercalcemia and hyperphosphatemia, increasing the risk of vascular calcification in CKD. "( Emerging role for the vitamin D receptor activator (VDRA), paricalcitol, in the treatment of secondary hyperparathyroidism.
Brancaccio, D; Cozzolino, M, 2008
)
0.7
"Treatment with calcitriol (0.25 to 2 microgram/day) returned all the biochemical values to normal within four months."( Vitamin D dependency: replacement therapy with calcitriol?
Delvin, EE; Glorieux, FH; Marie, PJ; Pettifor, JM, 1981
)
0.86
"Treatment with calcitriol, 1.0 microgram daily, was associated with bone mineral accretion and a diminished incidence of fractures."( Calcitriol deficiency in idiopathic juvenile osteoporosis.
Crawford, AC; Hug, G; Marder, HK; Tsang, RC, 1982
)
2.05
"Treatment with calcitriol (1,25 dihydroxyvitamin D3) induced a dramatic improvement of bone lesions."( Direct effect of calcitriol on the regulation of parathyroid hormone secretion in a case of pseudo-hypoparathyroidism (a 24-month follow-up study).
Audran, M; Basle, MF; Bigorgne, JC; Bregeon, C; Giraud, P; Jallet, P; Rohmer, V, 1995
)
0.97
"Treatment with calcitriol markedly increased the enzyme activity about 20-fold and the mRNA level about six-fold."( Short-term starvation increases calcidiol-24-hydroxylase activity and mRNA level in rat kidney.
Björkhem, I; Hagenfeldt-Pernow, Y; Ohyama, Y; Okuda, K; Sudjana-Sugiaman, E, 1994
)
0.63
"Treatment with calcitriol or its analogue, alfacalcidol often leads to hypercalcaemia, hyperphosphataemia or both in patients which chronic renal failure and advanced secondary hyperparathyroidism. "( Effects of new vitamin D analogues on parathyroid function in chronically uraemic rats with secondary hyperparathyroidism.
Drüeke, TB; Hruby, M; Lacour, B; Mannstadt, M; Schmitt, F; Ureña, P, 1996
)
0.65
"treatment with calcitriol is effective in the treatment of severe secondary HPT."( Long-term effect of intravenous calcitriol on the treatment of severe hyperparathyroidism, parathyroid gland mass and bone mineral density in haemodialysis patients.
Abed, J; Abu-Aisha, H; Al Desouki, M; Al Wakeel, J; Huraib, S; Memon, N, 1997
)
0.92
"Treatment with calcitriol for 12 months followed by calcium for 12 months resulted in similar proximal femoral bone loss to that seen in those patients treated with calcium for 24 months, suggesting calcitriol prophylaxis needs to be continued beyond 12 months."( Effect of calcitriol on bone loss after cardiac or lung transplantation.
Bergin, P; Ebeling, P; Eisman, J; Glanville, A; Henderson, NK; Keogh, A; MacDonald, P; Sambrook, P; Spratt, P, 2000
)
1.05
"Treatment with calcitriol and DHT also results in differences in nuclear matrix protein composition."( In vitro and in vivo effects of vitamin D (calcitriol) administration on the normal neonatal and prepubertal prostate.
Arlotti, J; Dhir, R; Getzenberg, RH; Konety, BR; Leman, E; Vietmeier, B, 2000
)
0.91
"Treatment with calcitriol resulted in a time and dose dependent increase in EGFR mRNA levels in confluent cultures of UMR 106-01 osteoblast-like cells. "( Mechanisms of the regulation of EGF receptor gene expression by calcitriol and parathyroid hormone in UMR 106-01 cells.
Disthabanchong, S; González, EA; Kowalewski, R; Martin, KJ, 2002
)
0.91
"Treatment with calcitriol of isolated cartilage cells derived from epiphyseal growth plates of rachitic chicks results in reduced intracellular calcium concentrations. "( Calcitriol increases Ca2+-ATPase activity.
Edelstein, S; Lidor, C, 1987
)
2.07
"Treatment with calcitriol (0.5-0.75 micrograms/day) increased calcium absorption after 6-12 months to 0.67 +/- 0.02 (P less than 0.001) and, in 29 patients, to 0.66 +/- 0.02 (P less than 0.001) after 24 months."( Effect of long term treatment with calcitriol on calcium absorption and mineral metabolism in postmenopausal osteoporosis.
Nelson, KI; Riggs, BL, 1985
)
0.89

Toxicity

This study demonstrates that pulse and daily calcitriol are similarly effective and safe for the treatment of mild to moderate secondary hyperparathyroidism in CAPD patients. We conclude that long-term, low-dose IV calcitril is a safe and effective therapy for most hemodialysis patients with secondary hyper parathyroidISM. For postmenopausal women with osteoporosis, calcitrile combined with bisphosphonate therapy can notoriously enhance the clinical therapy effect of sufferers.

ExcerptReferenceRelevance
"Topical application of up to 50 gm of calcipotriol ointment per week was found to be an effective and safe treatment of psoriasis vulgaris."( Efficacy and safety of calcipotriol (MC 903) ointment in psoriasis vulgaris. A randomized, double-blind, right/left comparative, vehicle-controlled study.
Bazex, JA; Beylot, C; Chevrant-Breton, J; Dubertret, L; Jurgensen, HJ; Kalis, B; Meynadier, J; Perussel, M; Souteyrand, P; Wallach, D, 1992
)
0.28
" We conclude that long-term, low-dose IV calcitriol is a safe and effective therapy for most hemodialysis patients with secondary hyperparathyroidism."( Safety and efficacy of long-term treatment of secondary hyperparathyroidism by low-dose intravenous calcitriol.
Moe, SM; Sprague, SM, 1992
)
0.77
" Preexposure of cells to 45 degrees C for 20 min, 4 h earlier, partially prevented the toxic effects of H2O2 particularly in 1,25-(OH)2D3-treated cells, even in the presence of physiological levels of [Ca2+]e."( 1,25-Dihydroxyvitamin D3 increases the toxicity of hydrogen peroxide: the role of calcium and heat shock.
Bonventre, JV; Krane, SM; Polla, BS, 1990
)
0.28
" Therefore, these preliminary findings suggest that orally or topically administered 1,25-(OH)2-D3 may be a safe and effective alternative therapy for the treatment of psoriasis."( A novel approach for the evaluation and treatment of psoriasis. Oral or topical use of 1,25-dihydroxyvitamin D3 can be a safe and effective therapy for psoriasis.
Donovan, L; Holick, MF; Pincus, SH; Smith, EL, 1988
)
0.27
" Preexposure of cells to 45 degrees C for 20 min, 4 h earlier, partially prevented the toxic effects of H2O2 particularly in 1,25-(OH)2D3-treated cells, even in the presence of physiological levels of [Ca2+]e."( 1,25-Dihydroxyvitamin D3 increases the toxicity of hydrogen peroxide in the human monocytic line U937: the role of calcium and heat shock.
Bonventre, JV; Krane, SM; Polla, BS, 1988
)
0.27
" The adverse effect on erythropoiesis appeared related to the degree of the concurrent hypercalcemia, which in turn depends upon the calcium content of the diet."( Adverse effect of 1,25-dihydroxycholecalciferol on erythrocyte precursors in the rat.
Orsatti, MB; Puche, RC, 1986
)
0.27
" We conclude that alpha-calcidol is more toxic than calcitriol in the mouse and suggest that the degree of toxicity is correlated to the degree of hypercalcemia and to the vitamin D metabolite used."( The comparative toxicity of vitamin D metabolites in the weanling mouse.
Cole, DE; Crocker, JF; Hamilton, DC; Muhtadie, SF, 1985
)
0.52
"Short-term treatment with calcipotriol ointment (50 micrograms/g) used in amounts up to about 100 g/wk is moderately efficacious, well-tolerated, and safe in adult patients with various ichthyoses."( Efficacy, tolerability, and safety of calcipotriol ointment in disorders of keratinization. Results of a randomized, double-blind, vehicle-controlled, right/left comparative study.
Axelsen, MB; Esmann, J; Ibsen, HH; Kragballe, K; Sorensen, LH; Steijlen, PM; van de Kerkhof, PC, 1995
)
0.29
" A safe and convenient new treatment modality would be of value to most patients with psoriasis."( Calcipotriene ointment 0.005% for psoriasis: a safety and efficacy study. Calcipotriene Study Group.
Highton, A; Quell, J, 1995
)
0.29
" Only minor treatment-related adverse events were observed."( Calcipotriene ointment 0.005% for psoriasis: a safety and efficacy study. Calcipotriene Study Group.
Highton, A; Quell, J, 1995
)
0.29
" However, the treated cells were more sensitive to a toxic effect of the bacteria."( Apparent killing of Mycobacterium tuberculosis by cytokine-activated human monocytes can be an artefact of a cytotoxic effect on the monocytes.
Andrew, PW; Dhillon, J; Lowrie, DB; O'Brien, L; Warwick-Davies, J, 1994
)
0.29
" This may permit a better evaluation of the pharmacologic and toxic effects not directly associated with the calcium-regulating properties of vitamin D metabolites and analogues."( Toxicity of vitamin D analogues in rats fed diets with standard or low calcium contents.
Binderup, L; Brinck, P; Mortensen, JT, 1993
)
0.29
"1 alpha,25-Dihydroxyvitamin D3 (1 alpha,25(OH)2D3) has recently been reported to exert a toxic effect on both rat and human glioma cell lines."( Cytotoxic effects of 1 alpha,25-dihydroxyvitamin D3 and synthetic vitamin D3 analogues on a glioma cell line.
Baudet, C; Binderup, L; Brachet, P; Chevalier, G; Naveilhan, P; Wion, D, 1996
)
0.29
" The drug did not have any adverse effects on the postnatal development of the offspring such as differentiation, functional development, emotionality, motor ability, learning ability or reproductive performance."( [Reproductive and developmental toxicity studies of calcipotriol (MC903): (4)--A perinatal and postnatal study in rats by subcutaneous administration].
Koike, Y; Konishi, R; Nagata, M; Ono, M; Shirakawa, K; Suzuki, T; Uchiyama, H, 1996
)
0.29
" Topical calcitriol is safe and effective for the treatment of psoriasis."( Efficacy and safety of topical calcitriol (1,25-dihydroxyvitamin d3) for the treatment of psoriasis.
Bhawan, J; Chen, TC; Holick, MF; Pèrez, A; Poche, P; Raab, R; Turner, A, 1996
)
1
" Oral calcitriol is effective and safe for the treatment of psoriasis."( Safety and efficacy of oral calcitriol (1,25-dihydroxyvitamin D3) for the treatment of psoriasis.
Chen, TC; Holick, MF; Perez, A; Raab, R; Turner, A, 1996
)
1.07
" Patients were carefully questioned and observed at each visit for adverse events."( Long-term effectiveness and safety of topical calcipotriene for psoriasis. Calcipotriene Study Group.
Cullen, SI, 1996
)
0.29
" The treatment was well tolerated, with no serious adverse events occurring during the course of the study."( A long-term multicentre assessment of the safety and tolerability of calcitriol ointment in the treatment of chronic plaque psoriasis.
Ashton, P; Langner, A; Van De Kerkhof, PC; Verjans, H, 1996
)
0.53
" Eight patients withdrew from the study (four defaulted, two unacceptable responses, two adverse events)."( Safety and efficacy of calcipotriol ointment (Dovonex) in treating children with psoriasis vulgaris.
Cunliffe, WJ; Darley, CR; Downes, N; Green, CM; Hutchinson, PE; Klaber, MR, 1996
)
0.29
" The incidence of adverse reactions in ipriflavone-treated patients (14."( Efficacy of ipriflavone in established osteoporosis and long-term safety.
Agnusdei, D; Bufalino, L, 1997
)
0.3
" Moreover, 45,000 IU/kg of dietary vitamin A ameliorated the potential toxic effects of feeding high levels of vitamin D3, 25-(OH)D3 and 1,25-(OH)2D3 to young broiler chickens."( The influence of vitamin A on the utilization and amelioration of toxicity of cholecalciferol, 25-hydroxycholecalciferol, and 1,25 dihydroxycholecalciferol in young broiler chickens.
Aburto, A; Britton, WM; Edwards, HM, 1998
)
0.3
"This study demonstrates that pulse and daily calcitriol are similarly effective and safe for the treatment of mild to moderate secondary hyperparathyroidism in CAPD patients despite higher peak levels of 1,25(OH)2-vitamin D with pulse therapy."( Safety and efficacy of pulse and daily calcitriol in patients on CAPD: a randomized trial.
Fineberg, NS; Gannon, FH; Gassensmith, CM; Kraus, MA; Moe, SM; Peacock, M, 1998
)
0.83
" After an overload of vitamin D, DBP-/- mice were unexpectedly less susceptible to hypercalcemia and its toxic effects."( Osteopathy and resistance to vitamin D toxicity in mice null for vitamin D binding protein.
Cooke, NE; Gentile, M; Haddad, JG; Hollis, BW; Liebhaber, SA; Magiera, H; Safadi, FF; Thornton, P, 1999
)
0.3
" Therefore an effective and safe treatment modality is needed."( A pilot study to assess the safety and efficacy of topical calcipotriol treatment in childhood psoriasis.
Park, SB; Suh, DH; Youn, JI,
)
0.13
" There was no difference in the PASI, patient's and investigator's overall assessments and number of adverse events recorded by either group for both the treatment and follow-up phases."( Calcipotriol cream combined with twice weekly broad-band UVB phototherapy: a safe, effective and UVB-sparing antipsoriatric combination treatment. The Canadian Calcipotriol and UVB Study Group.
Bolduc, A; Gilbert, M; Lowson, D; Papp, K; Ramsay, CA; Schwartz, BE, 2000
)
0.31
"Calcipotriol cream + twice weekly broad-band UVB phototherapy is an effective and safe antipsoriatric treatment, resulting in fewer UVB exposures, lower cumulative irradiance and a saving of time."( Calcipotriol cream combined with twice weekly broad-band UVB phototherapy: a safe, effective and UVB-sparing antipsoriatric combination treatment. The Canadian Calcipotriol and UVB Study Group.
Bolduc, A; Gilbert, M; Lowson, D; Papp, K; Ramsay, CA; Schwartz, BE, 2000
)
0.31
" Safety was determined from reports of adverse events and blood chemistry analysis."( The efficacy, safety and tolerance of calcitriol 3 microg/g ointment in the treatment of plaque psoriasis: a comparison with short-contact dithranol.
Hutchinson, PE; Marks, R; White, J, 2000
)
0.58
", 1-100 nM, of 1,25-(OH)(2)D(3) protect cultured dopaminergic neurons against this toxicity, although higher concentrations of this active form of vitamin D have been found to enhance the toxic effect."( Effect of 1,25-dihydroxyvitamin D(3) on cultured mesencephalic dopaminergic neurons to the combined toxicity caused by L-buthionine sulfoximine and 1-methyl-4-phenylpyridine.
Kikuchi, S; Moriwaka, F; Sasaki, H; Shinpo, K; Tashiro, K, 2000
)
0.31
"This article reviews the different treatments currently available for osteoporosis and examines the benefits and adverse events that are associated with each."( Comparative safety of bone remodeling agents with a focus on osteoporosis therapies.
Kleerekoper, M; Schein, JR, 2001
)
0.31
" No serious adverse events were reported: 37 patients (14."( Long-term safety of topical calcitriol 3 microg g(-1) ointment.
Gerritsen, MJ; Langner, A; Van De Kerkhof, PC, 2001
)
0.6
" No adverse local events were observed when calcitriol was applied to animal skin."( Topical calcitriol--studies on local tolerance and systemic safety.
Corroller, M; Rizova, E, 2001
)
1.01
" Treatment was generally well tolerated and there were no serious or unexpected adverse events reported."( Long-term efficacy and safety of tacalcitol ointment in patients with chronic plaque psoriasis.
Berth-Jones, J; Griffiths, CE; Harrison, PV; Hönigsmann, H; Marks, R; Roelandts, R; Schöpf, E; Trompke, C; van de Kerkhof, PC, 2002
)
0.31
"Tacalcitol ointment once daily was demonstrated to be efficacious, safe and well tolerated in the long-term control of plaque psoriasis in patients with up to 20% body surface involvement."( Long-term efficacy and safety of tacalcitol ointment in patients with chronic plaque psoriasis.
Berth-Jones, J; Griffiths, CE; Harrison, PV; Hönigsmann, H; Marks, R; Roelandts, R; Schöpf, E; Trompke, C; van de Kerkhof, PC, 2002
)
0.31
" Safety data showed the frequency of adverse events to be less in the combined formulation groups than in both the calcipotriol group and the vehicle group."( Efficacy and safety of a new combination of calcipotriol and betamethasone dipropionate (once or twice daily) compared to calcipotriol (twice daily) in the treatment of psoriasis vulgaris: a randomized, double-blind, vehicle-controlled clinical trial.
Chu, AC; Garcia-Diez, A; Guenther, L; Kragballe, K; Snellman, E; Springborg, J; Tegner, E; Van de Kerkhof, PC, 2002
)
0.31
" Several clinical trials have demonstrated that calcitriol, the naturally occurring and hormonally active form of vitamin D3, is effective and safe at the dose of 3 microg g(-1) for the treatment of psoriasis affecting the trunk and limbs."( Intra-individual comparison of the cutaneous safety and efficacy of calcitriol 3 microg g(-1) ointment and calcipotriol 50 microg g(-1) ointment on chronic plaque psoriasis localized in facial, hairline, retroauricular or flexural areas.
Czernielewski, J; Dubertret, L; Humbert, P; Janin, A; Lahfa, M; Nicolas, JF; Ortonne, JP; Tonev, SD; Tsankov, N, 2003
)
0.81
" Our purpose is to compare the rates of adverse events associated with different topical psoriasis treatments."( A systematic review of adverse effects associated with topical treatments for psoriasis.
Bruner, CR; Feldman, SR; Fleischer, AB; Ventrapragada, M, 2003
)
0.32
" No significant side effect was seen during the trial."( Effect of oral calcitriol pulse therapy on the lipid, calcium, and glucose homeostasis of hemodialysis-patients: its safety in a combination with oral calcium carbonate.
Khajehdehi, P; Taheri, S, 2003
)
0.67
"Our findings indicate that short-term oral calcitriol pulse therapy in combination with calcium carbonate is safe and beneficial for metabolic abnormalities of HD patients; however, its safety for prolonged therapy is yet to be proved."( Effect of oral calcitriol pulse therapy on the lipid, calcium, and glucose homeostasis of hemodialysis-patients: its safety in a combination with oral calcium carbonate.
Khajehdehi, P; Taheri, S, 2003
)
0.93
"Many efforts have been made to obtain active and less toxic Vitamin D analogs for new clinical applications."( Toxicity and antineoplastic effect of (24R)-1,24-dihydroxyvitamin D3 (PRI-2191).
Dzimira, S; Kuśnierczyk, H; Kutner, A; Madej, J; Opolski, A; Pełczyńska, M; Szelejewski, W; Wietrzyk, J, 2004
)
0.32
" Adverse events were more common in the calcipotriol group than in the clobetasol propionate shampoo group."( Clobetasol propionate shampoo 0.05% and calcipotriol solution 0.005%: a randomized comparison of efficacy and safety in subjects with scalp psoriasis.
Acebes, LO; Arsonnaud, S; Caputo, R; de Waard-van der Spek, FB; Decroix, J; Figueiredo, A; Mrowietz, U; Poncet, M; Reygagne, P, 2005
)
0.33
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
"The calcipotriol/betamethasone dipropionate two-compound product Dovobet/Daivobet/Taclonex(LEO Pharma A/S, Ballerup, Denmark) has been shown to be safe and effective in the treatment of psoriasis for up to 8 weeks."( A 52-week randomized safety study of a calcipotriol/betamethasone dipropionate two-compound product (Dovobet/Daivobet/Taclonex) in the treatment of psoriasis vulgaris.
Austad, J; Barnes, L; Bibby, A; Cambazard, F; de la Brassinne, M; Fleming, C; Heikkilä, H; Jolliffe, D; Kragballe, K; Peyri, J; Svensson, A; Toole, J; Wozel, G, 2006
)
0.33
"Treatment with the two-compound product for up to 52 weeks appears to be safe and well tolerated whether used on its own or alternating every 4 weeks with calcipotriol treatment."( A 52-week randomized safety study of a calcipotriol/betamethasone dipropionate two-compound product (Dovobet/Daivobet/Taclonex) in the treatment of psoriasis vulgaris.
Austad, J; Barnes, L; Bibby, A; Cambazard, F; de la Brassinne, M; Fleming, C; Heikkilä, H; Jolliffe, D; Kragballe, K; Peyri, J; Svensson, A; Toole, J; Wozel, G, 2006
)
0.33
"The calcipotriol/betamethasone dipropionate two-compound product is safe and effective in the short-term treatment of psoriasis."( Efficacy results of a 52-week, randomised, double-blind, safety study of a calcipotriol/betamethasone dipropionate two-compound product (Daivobet/Dovobet/Taclonex) in the treatment of psoriasis vulgaris.
Austad, J; Barnes, L; Bibby, A; Cambazard, F; de la Brassinne, M; Fleming, C; Heikkilä, H; Kragballe, K; Peyri Rey, J; Svensson, A; Toole, J; Williams, Z; Wozel, G, 2006
)
0.33
" Safety evaluations included adverse event reporting, cutaneous safety assessed by the investigator and cutaneous discomfort assessment by the subject (both on a 5-point scale from 0: none, to 4: very severe)."( An investigator-masked comparison of the efficacy and safety of twice daily applications of calcitriol 3 microg/g ointment vs. calcipotriol 50 microg/g ointment in subjects with mild to moderate chronic plaque-type psoriasis.
Andres, P; Briantais, P; Chen, Z; Gu, J; Wang, B; Zhao, G; Zhu, X, 2007
)
0.56
" Fourteen dermatological and treatment-related adverse events were reported with calcipotriol vs."( An investigator-masked comparison of the efficacy and safety of twice daily applications of calcitriol 3 microg/g ointment vs. calcipotriol 50 microg/g ointment in subjects with mild to moderate chronic plaque-type psoriasis.
Andres, P; Briantais, P; Chen, Z; Gu, J; Wang, B; Zhao, G; Zhu, X, 2007
)
0.56
" Both treatments were safe and well tolerated."( Efficacy, safety and quality of life of calcipotriol/betamethasone dipropionate (Dovobet) versus calcipotriol (Daivonex) in the treatment of psoriasis vulgaris: a randomized, multicentre, clinical trial.
Andreassi, L; Ayala, F; Bongiorno, MR; Chimenti, S; Giannetti, A; Lisi, P; Martini, P; Peris, K; Peserico, A; Saraceno, R, 2007
)
0.34
"Active and less toxic vitamin D analogs could be useful for clinical applications."( Toxicity and antitumor activity of the vitamin D analogs PRI-1906 and PRI-1907 in combined treatment with cyclophosphamide in a mouse mammary cancer model.
Filip, B; Kutner, A; Milczarek, M; Nevozhay, D; Wietrzyk, J, 2008
)
0.35
"The LD50 values after five daily subcutaneous (s."( Toxicity and antitumor activity of the vitamin D analogs PRI-1906 and PRI-1907 in combined treatment with cyclophosphamide in a mouse mammary cancer model.
Filip, B; Kutner, A; Milczarek, M; Nevozhay, D; Wietrzyk, J, 2008
)
0.35
" Past policy of the Institute of Medicine has set the tolerable upper intake level (UL) for vitamin D at 50 mug (2000 IU)/d, defining this as "the highest level of daily nutrient intake that is likely to pose no risks of adverse health effects to almost all individuals in the general population."( Vitamin D toxicity, policy, and science.
Vieth, R, 2007
)
0.34
"Effective and safe products are needed for long-term management of scalp psoriasis."( A study of the safety and efficacy of calcipotriol and betamethasone dipropionate scalp formulation in the long-term management of scalp psoriasis.
Bourcier, M; Cambazard, F; Clonier, F; Gupta, G; Kidson, P; Larsen, FG; Luger, TA; Shear, NH, 2008
)
0.35
" Incidences of adverse events possibly associated with long-term corticosteroid use were low in both the two-compound (2."( A study of the safety and efficacy of calcipotriol and betamethasone dipropionate scalp formulation in the long-term management of scalp psoriasis.
Bourcier, M; Cambazard, F; Clonier, F; Gupta, G; Kidson, P; Larsen, FG; Luger, TA; Shear, NH, 2008
)
0.35
" No severe adverse event related to these medications occurred throughout the study."( The efficacy and safety of calcitriol and/or Caltrate D in elderly Chinese women with low bone mass.
Hu, YY; Jiang, Y; Liu, JL; Meng, XW; Tian, JP; Wang, HF; Wang, LH; Weng, SF; Xia, WB; Xing, XP; Xu, T; Yu, W; Zhang, Y; Zhang, ZL; Zhu, GY, 2009
)
0.65
" Secondary efficacy outcomes and adverse events were also evaluated."( Efficacy and safety of calcipotriol plus betamethasone dipropionate scalp formulation compared with calcipotriol scalp solution in the treatment of scalp psoriasis: a randomized controlled trial.
Hoffmann, V; Kragballe, K; Nordin, P; Ortonne, JP; Segaert, S; Tan, J, 2009
)
0.35
" Further evidence of the superiority of the two-compound scalp formulation over the scalp solution was demonstrated through greater improvements in clinical signs and fewer adverse events."( Efficacy and safety of calcipotriol plus betamethasone dipropionate scalp formulation compared with calcipotriol scalp solution in the treatment of scalp psoriasis: a randomized controlled trial.
Hoffmann, V; Kragballe, K; Nordin, P; Ortonne, JP; Segaert, S; Tan, J, 2009
)
0.35
" Serious adverse events (AEs) (reported by 1 participant each unless otherwise noted) included a pretibial skin ulcer (study drug was used only on the upper body), a joint disorder, metrorrhagia (2 participants), heart failure, hospitalization due to arteriosclerosis, breast carcinoma, and an infection (due to a dog bite)."( Calcitriol ointment 3 microg/g is safe and effective over 52 weeks for the treatment of mild to moderate plaque psoriasis.
Andres, P; Briantais, P; Lebwohl, M; Ortonne, JP, 2009
)
1.8
" Calcitriol 3 microg/g ointment has been extensively evaluated for the treatment of chronic plaque-type psoriasis and has been shown to be effective, safe and well-tolerated in a number of short-term and long-term clinical trials."( Efficacy and safety of topical calcitriol 3 microg/g ointment, a new topical therapy for chronic plaque psoriasis.
Kircik, L, 2009
)
1.55
"High-potency topical corticosteroids are very effective for the treatment of psoriasis, but are associated with a number of cutaneous adverse effects."( Calcitriol 3 microg/g ointment: an effective and safe addition to the armamentarium in topical psoriasis therapy.
Abramovits, W, 2009
)
1.8
" Administration of vitamin D receptor (VDR) agonists can ameliorate spontaneous and induced animal models of colitis, but hypercalcemia is a dose-limiting adverse event."( Efficacy of a potent and safe vitamin D receptor agonist for the treatment of inflammatory bowel disease.
Adorini, L; Correale, C; Danese, S; Laverny, G; Nebuloni, M; Penna, G; Vetrano, S, 2010
)
0.36
" No serious adverse effects such as hypoglycemia, liver impairment, or heart failure were observed in any of the patients."( Clinical effectiveness and safety evaluation of long-term pioglitazone treatment for erythropoietin responsiveness and insulin resistance in type 2 diabetic patients on hemodialysis.
Abe, M; Maruyama, N; Maruyama, T; Matsumoto, K; Okada, K; Soma, M, 2010
)
0.36
" These compounds were equally toxic in wild-type and the mutant mice."( 1,25-Dihydroxyvitamin D is not responsible for toxicity caused by vitamin D or 25-hydroxyvitamin D.
Deluca, HF; Plum, LA; Prahl, JM, 2011
)
0.37
" Adverse event incidences were similar between patients with and without prior anti-TNF therapy."( Efficacy and safety of adalimumab in patients with psoriasis previously treated with anti-tumour necrosis factor agents: subanalysis of BELIEVE.
Chimenti, S; Gniadecki, R; Goldblum, O; Kupper, H; Ortonne, JP; Reich, K; Sprøgel, P; Thaçi, D; Unnebrink, K, 2011
)
0.37
" Topical vitamin D, which is used to treat mild-to-moderate psoriasis, has been shown to be safe when used daily for up to 52 weeks."( A multi-center, open-label study to evaluate the safety and efficacy of a sequential treatment regimen of clobetasol propionate 0.05% spray followed by Calcitriol 3 mg/g ointment in the management of plaque psoriasis.
Brodell, RT; Bruce, S; Colón, LE; Gottschalk, RW; Hudson, CP; Johnson, LA; Weiss, JS, 2011
)
0.57
" The sequential treatment regimen was well tolerated with no unexpected adverse events."( A multi-center, open-label study to evaluate the safety and efficacy of a sequential treatment regimen of clobetasol propionate 0.05% spray followed by Calcitriol 3 mg/g ointment in the management of plaque psoriasis.
Brodell, RT; Bruce, S; Colón, LE; Gottschalk, RW; Hudson, CP; Johnson, LA; Weiss, JS, 2011
)
0.57
"05% spray treatment for four weeks immediately followed by an eight-week treatment phase with calcitriol 3 μg/g ointment is efficacious and safe for the management of moderate-to-severe plaque psoriasis."( A multi-center, open-label study to evaluate the safety and efficacy of a sequential treatment regimen of clobetasol propionate 0.05% spray followed by Calcitriol 3 mg/g ointment in the management of plaque psoriasis.
Brodell, RT; Bruce, S; Colón, LE; Gottschalk, RW; Hudson, CP; Johnson, LA; Weiss, JS, 2011
)
0.79
" Dermatologists seek alternative treatments of patients with plaque psoriasis that provide both efficacy and safety while minimizing exposure to high-potency steroids that can have adverse effects following long-term use."( An open-label, multicenter study of the efficacy and safety of an AM/PM treatment regimen with clobetasol propionate spray 0.05% and calcitriol ointment 3 microg/g in the management of plaque psoriasis.
Colón, LE; Gottschalk, R; Hudson, CP; Johnson, LA; Kempers, S; Menter, A; Papp, K; Smith, S; Sofen, H, 2011
)
0.57
" No adverse effects related to the study, including skin irritation, were observed or reported."( Evaluating the efficacy and safety of calcipotriene/betamethasone ointment occluded with a hydrogel patch: a 6-week bilaterally controlled, investigator-blinded trial.
Bhutani, T; Busse, KL; Koo, J; Patel, T, 2011
)
0.37
"The adverse effects of metabolic disorders in obesity have been extensively studied; however, the pathologic effects of hyperphosphatemia or phosphate toxicity in obesity have not been studied in similar depth and detail, chiefly because such an association is thought to be uncommon."( Genetic induction of phosphate toxicity significantly reduces the survival of hypercholesterolemic obese mice.
Kato, S; Ohnishi, M; Razzaque, MS, 2011
)
0.37
" Although highly effective, long-term use of topical steroids can cause adverse side effects."( An open-label, multicenter study of the efficacy and safety of a weekday/weekend treatment regimen with calcitriol ointment 3 microg/g and clobetasol propionate spray 0.05% in the management of plaque psoriasis.
Colón, LE; Gottschalk, R; Hudson, CP; Johnson, LA; Kempers, S; Menter, A; Papp, K; Smith, S; Sofen, H, 2011
)
0.58
" Adverse events (AEs) were recorded throughout the study."( Efficacy and safety of calcipotriene 0.005% foam for the treatment of plaque-type psoriasis: results of two multicenter, randomized, double-blind, vehicle-controlled, phase III clinical trials.
Bruce, S; Brundage, T; Feldman, SR; Grande, K; Kempers, S; Markowitz, O; Matheson, R; Wyres, M, 2012
)
0.38
" Calcipotriene foam was safe with an overall incidence of AEs similar to those experienced in the vehicle foam group."( Efficacy and safety of calcipotriene 0.005% foam for the treatment of plaque-type psoriasis: results of two multicenter, randomized, double-blind, vehicle-controlled, phase III clinical trials.
Bruce, S; Brundage, T; Feldman, SR; Grande, K; Kempers, S; Markowitz, O; Matheson, R; Wyres, M, 2012
)
0.38
"005% foam was safe and effective for the treatment of mild to moderate plaque-type psoriasis for up to 8 weeks."( Efficacy and safety of calcipotriene 0.005% foam for the treatment of plaque-type psoriasis: results of two multicenter, randomized, double-blind, vehicle-controlled, phase III clinical trials.
Bruce, S; Brundage, T; Feldman, SR; Grande, K; Kempers, S; Markowitz, O; Matheson, R; Wyres, M, 2012
)
0.38
" Other adverse events were similar between groups."( Randomized controlled trial to compare the efficacy and safety of oral paricalcitol with oral calcitriol in dialysis patients with secondary hyperparathyroidism.
Ching, CH; Ghazali, A; Ghazalli, R; Goh, BL; Goh, HK; Manocha, AB; Mohamad, S; Narayanan, P; Omar, M; Ong, LM; Rahmat, K; Seman, MR; Shaariah, W; Shah, S; Vaithilingam, I, 2013
)
0.61
" The treatment did not cause any serious adverse events, except hypercalcemia grade I, once in 72 administrations."( Evaluation of efficacy, safety and tolerability of high dose-intermittent calcitriol supplementation to advanced intrahepatic cholangiocarcinoma patients--a pilot study.
Bhudhisawasdi, V; Chamadol, N; Chur-in, S; Janeklang, S; Khuntikeo, N; Kukongviriyapan, V; Pairojkul, C; Prawan, A; Pugkhem, A; Sookprasert, A; Vaeteewoottacharn, K; Wongkham, S, 2012
)
0.61
" Mortality was used as an end point to study the toxic effects of calcitriol; the relative risk of mortality in mice injected with saline was evaluated from our previously published animal experiments."( Hydration with saline decreases toxicity of mice injected with calcitriol in preclinical studies.
Albert, DM; Azari, AA; Darjatmoko, SR; Kanavi, MR; Kim, K; Lee, V; Potter, HD, 2013
)
0.87
" Most adverse events (AEs) were mild-moderate severity."( Pooled safety analysis of calcipotriol plus betamethasone dipropionate gel for the treatment of psoriasis on the body and scalp.
Kragballe, K; van de Kerkhof, P, 2014
)
0.4
" Twenty-seven patients (35%) reported a total of 64 adverse events (AEs); most were mild (33/64) or moderate (22/64) in severity and there were no serious AEs."( Safety and efficacy of calcipotriol plus betamethasone dipropionate gel in the treatment of scalp psoriasis in adolescents 12-17 years of age.
Debarre, JM; Gooderham, M; Goodfield, M; Keddy-Grant, J; Kurvits, M; Xu, Z, 2014
)
0.4
"Narrow-band ultraviolet B (NB-UVB) is an effective and safe treatment for vitiligo."( Comparison of efficacy and safety profile of topical calcipotriol ointment in combination with NB-UVB vs. NB-UVB alone in the treatment of vitiligo: a 24-week prospective right-left comparative clinical trial.
Kanwar, AJ; Khullar, G; Parsad, D; Singh, S, 2015
)
0.42
" Calcipotriol produced mild local adverse effects."( Comparison of efficacy and safety profile of topical calcipotriol ointment in combination with NB-UVB vs. NB-UVB alone in the treatment of vitiligo: a 24-week prospective right-left comparative clinical trial.
Kanwar, AJ; Khullar, G; Parsad, D; Singh, S, 2015
)
0.42
" Sixteen patients (52%) experienced a total of 20 adverse events; 19 were considered unrelated to study treatment, 14 were mild, and none were serious or lesional or perilesional on the scalp."( Safety and efficacy of calcipotriene plus betamethasone dipropionate topical suspension in the treatment of extensive scalp psoriasis in adolescents ages 12 to 17 years.
Eichenfield, LF; Ganslandt, C; Kurvits, M; Schlessinger, J,
)
0.13
"Calcipotriol/betamethasone dipropionate combination in a non-alcoholic, lipophilic gel formulation (two-compound gel) has previously been demonstrated as a safe and effective treatment for scalp psoriasis in Caucasian, Hispanic/Latino, and Black/African American populations."( Calcipotriol plus betamethasone dipropionate gel compared with calcipotriol scalp solution in the treatment of scalp psoriasis: a randomized, controlled trial investigating efficacy and safety in a Chinese population.
Cui, P; Facy, P; Gao, T; Ge, M; Gu, J; Hao, F; Kurvits, M; Li, R; Ma, L; Sun, Q; Wang, G; Xu, J; Xu, Z; Yang, H; Yang, Q; Zheng, M, 2016
)
0.43
" The two-compound gel was associated with fewer adverse drug reactions than calcipotriol scalp solution (18."( Calcipotriol plus betamethasone dipropionate gel compared with calcipotriol scalp solution in the treatment of scalp psoriasis: a randomized, controlled trial investigating efficacy and safety in a Chinese population.
Cui, P; Facy, P; Gao, T; Ge, M; Gu, J; Hao, F; Kurvits, M; Li, R; Ma, L; Sun, Q; Wang, G; Xu, J; Xu, Z; Yang, H; Yang, Q; Zheng, M, 2016
)
0.43
" Cholecalciferol substitution was well tolerated without adverse effects."( Efficacy and safety of body weight-adapted oral cholecalciferol substitution in dialysis patients with vitamin D deficiency.
Lhotta, K; Mündle, M; Sprenger-Mähr, H; Zitt, E, 2015
)
0.42
"The study aimed to characterize the short-term safety profile of ZA and identify risk factors for ZA-related adverse events (AEs) in young patients."( Short-Term Safety of Zoledronic Acid in Young Patients With Bone Disorders: An Extensive Institutional Experience.
George, S; Hummel, K; Kaplan, P; Levine, MA; Monk, HM; Weber, DR, 2015
)
0.42
" Safety was monitored by adverse events/calcium homeostasis."( Efficacy and Safety of Calcipotriene Plus Betamethasone Dipropionate Aerosol Foam in Patients With Psoriasis Vulgaris--a Randomized Phase III Study (PSO-FAST).
Bagel, J; Leonardi, C; Olesen, M; Pariser, D; Stein Gold, L; Xu, Z; Yamauchi, P; Østerdal, ML, 2015
)
0.42
" Adverse drug reactions were reported in 10 Cal/BD foam patients (3."( Efficacy and Safety of Calcipotriene Plus Betamethasone Dipropionate Aerosol Foam in Patients With Psoriasis Vulgaris--a Randomized Phase III Study (PSO-FAST).
Bagel, J; Leonardi, C; Olesen, M; Pariser, D; Stein Gold, L; Xu, Z; Yamauchi, P; Østerdal, ML, 2015
)
0.42
"Severe adverse effects of ointment application were not observed in the healthy subjects or oMGD patients."( Clinical safety and efficacy of vitamin D3 analog ointment for treatment of obstructive meibomian gland dysfunction.
Arita, R; Ito, M; Kawashima, M; Tsubota, K, 2017
)
0.46
"Topical eyelid application of an analog of the active form of vitamin D3 was found to be safe as well as to improve the condition of patients with oMGD."( Clinical safety and efficacy of vitamin D3 analog ointment for treatment of obstructive meibomian gland dysfunction.
Arita, R; Ito, M; Kawashima, M; Tsubota, K, 2017
)
0.46
" Treatment-emergent adverse events were reported by 11 (58%) patients in the 25-μg group and 17 (74%) patients in the 50-μg group."( Safety and Efficacy of Recombinant Human Parathyroid Hormone in Adults With Hypoparathyroidism Randomly Assigned to Receive Fixed 25-μg or 50-μg Daily Doses.
Bilezikian, JP; Clarke, BL; Krasner, A; Lee, HM; Mannstadt, M; Rothman, J; Vokes, T, 2017
)
0.46
" During follow-up for a period of 275 person-years, 50 adverse events were recorded."( Parathyroid hormone, calcidiol, calcitriol and adverse events in the acute coronary syndrome.
Castañeda Sancirilo, M; Castillo Moreno, JA; Clavel Ruipérez, G; Consuegra Sánchez, L; García de Guadiana Romualdo, L; García Escribano, I; Jaulent Huertas, L; Martínez Díaz, JJ; Merelo Nicolás, M; Ramos Ruiz, P; Soria Arcos, F; Wasniewski, S, 2018
)
0.76
" The adverse effects (most commonly hyperpigmentation) were noted more frequently on the excimer-treated sides; however, they were well tolerated."( Comparison of effectiveness and safety of excimer lamp vs topical calcipotriol-clobetasol propionate combination in the treatment of palmoplantar psoriasis.
Bishnoi, A; Dogra, S; Narang, T; Thakur, A, 2018
)
0.48
" Treatment-emergent adverse events (AEs) were reported in 48 patients (98."( Safety and Efficacy of 5 Years of Treatment With Recombinant Human Parathyroid Hormone in Adults With Hypoparathyroidism.
Bilezikian, JP; Bone, H; Clarke, BL; Denham, D; Lee, HM; Levine, MA; Mannstadt, M; Peacock, M; Rothman, J; Sherry, N; Shoback, DM; Vokes, TJ; Warren, ML; Watts, NB, 2019
)
0.51
"Psoriasis is commonly treated with topical corticosteroids, oral cytotoxic drugs and biologic agents, which can be associated with significant adverse effects (AEs), high cost and response attenuation."( Efficacy and safety of HAT1 compared with calcipotriol in the treatment of patients with mild to moderate chronic plaque psoriasis: results from an open-label randomized comparative pilot clinical study.
Alex, P; Centola, M; Sutton, C; Sutton, L; Thomas, S; Williams, S; Yesudas, T, 2020
)
0.56
" Safety response criteria included adverse drug reactions [ADRs; any adverse event (AE) possibly or probably related to treatment as determined by the investigator; a primary response criterion] and AEs (a secondary response criterion)."( Safety and efficacy of topical, fixed-dose combination calcipotriene (0.005%) and betamethasone (0.064% as dipropionate) gel in adolescent patients with scalp and body psoriasis: a phase II trial.
Eichenfield, LF; Kurvits, M; Liljedahl, M; Marcoux, D, 2020
)
0.56
"To evaluate whether topical rapamycin-calcitriol combination is an effective and safe treatment for TSC-related FAs."( The efficacy and safety of topical rapamycin-calcitriol for facial angiofibromas in patients with tuberous sclerosis complex: a prospective, double-blind, randomized clinical trial.
Chen, PL; Chen, YT; Hong, JB; Liao, YH; Shen, LJ; Wang, SJ, 2020
)
1.09
"This randomized clinical trial demonstrates that topical rapamycin-calcitriol combination therapy is an effective and safe regimen for TSC-related FAs."( The efficacy and safety of topical rapamycin-calcitriol for facial angiofibromas in patients with tuberous sclerosis complex: a prospective, double-blind, randomized clinical trial.
Chen, PL; Chen, YT; Hong, JB; Liao, YH; Shen, LJ; Wang, SJ, 2020
)
1.05
" Primary objectives included treatment-emergent adverse events (TEAEs) and systemic calcium levels in the overall population, and HPA-axis function, change in calcium excretion and the calcium:creatinine ratio in the HPA-axis cohort."( Safety and efficacy of fixed-dose combination calcipotriol (50 μg/g) and betamethasone dipropionate (0.5 mg/g) cutaneous foam in adolescent patients (aged 12 to <17 years) with plaque psoriasis: results of a phase II, open-label trial.
Abramovits, W; Hoejen, MN; Liljedahl, M; Seyger, M; Teng, J, 2020
)
0.56
"The safety of diclofenac (DIC) use in clinical practice has been questioned because of adverse cardiovascular effects."( Calcitriol Reduces Adverse Effects of Diclofenac on Mitochondrial Function in Isolated Rat Heart Mitochondria.
Atashbar, S; Azizian, S; Khezri, S; Kurdpour, P; Salimi, A; Shaikhgermchi, Z, 2020
)
2
" Cal/BD foam plus apremilast appeared to be safe and well tolerated."( Efficacy and Safety of Calcipotriene 0.005%/Betamethasone Dipropionate 0.064% Foam With Apremilast for Moderate Plaque Psoriasis.
Kircik, LH; Schlesinger, TE; Tanghetti, E, 2020
)
0.56
" Incidence of adverse drug reactions (ADRs) of any type and adverse events (AEs) of concern associated with long-term corticosteroid use on the scalp were evaluated."( Comparison of safety and efficacy between calcipotriol plus betamethasone dipropionate gel and calcipotriol scalp solution as long-term treatment for scalp psoriasis in Chinese patients: a national, multicentre, prospective, randomized, active-controlled
Cao, S; Chen, K; Chen, Y; Cheng, H; Ding, Y; Fang, H; Han, X; He, L; He, Y; Huang, J; Li, M; Li, S; Li, W; Liu, L; Lu, Q; Lu, Y; Pan, W; Wang, J; Yan, G; Zhang, C; Zhang, J; Zheng, M; Zhu, W, 2020
)
0.56
" There was no significant difference in treatment-emergent adverse events (TEAEs) associated with long-term topical corticosteroid use on the scalp (1."( Comparison of safety and efficacy between calcipotriol plus betamethasone dipropionate gel and calcipotriol scalp solution as long-term treatment for scalp psoriasis in Chinese patients: a national, multicentre, prospective, randomized, active-controlled
Cao, S; Chen, K; Chen, Y; Cheng, H; Ding, Y; Fang, H; Han, X; He, L; He, Y; Huang, J; Li, M; Li, S; Li, W; Liu, L; Lu, Q; Lu, Y; Pan, W; Wang, J; Yan, G; Zhang, C; Zhang, J; Zheng, M; Zhu, W, 2020
)
0.56
" Adverse event (AE) monitoring, pharmacokinetics, blinded photographic assessments, and patient self-assessment were evaluated."( A phase I safety study of topical calcitriol (BPM31543) for the prevention of chemotherapy-induced alopecia.
Benaim, E; Berman, B; Dion, H; DiTommaso, N; Goldfarb, SB; Granger, E; Grund, EM; Jimenez, JJ; Lacouture, ME; Luan, S; Narain, NR; Ravipaty, S; Sarangarajan, R; Tanna, N; Thapa, K, 2021
)
0.9
"Out of 23 patients treated with BPM31543, 8 patients experienced at least 1 treatment-related adverse event (AE)."( A phase I safety study of topical calcitriol (BPM31543) for the prevention of chemotherapy-induced alopecia.
Benaim, E; Berman, B; Dion, H; DiTommaso, N; Goldfarb, SB; Granger, E; Grund, EM; Jimenez, JJ; Lacouture, ME; Luan, S; Narain, NR; Ravipaty, S; Sarangarajan, R; Tanna, N; Thapa, K, 2021
)
0.9
"BPM31543 applied topically twice daily to the scalp is safe and well tolerated in patients receiving taxane-based chemotherapy."( A phase I safety study of topical calcitriol (BPM31543) for the prevention of chemotherapy-induced alopecia.
Benaim, E; Berman, B; Dion, H; DiTommaso, N; Goldfarb, SB; Granger, E; Grund, EM; Jimenez, JJ; Lacouture, ME; Luan, S; Narain, NR; Ravipaty, S; Sarangarajan, R; Tanna, N; Thapa, K, 2021
)
0.9
" This superior efficacy was not associated with an increased frequency or severity of adverse events, and there was no evidence for dysregulation of the hypothalamic-pituitary-adrenal axis or calcium homeostasis."( Efficacy and safety of fixed-dose combination calcipotriol/betamethasone dipropionate foam for the treatment of psoriasis.
Paul, C; Romiti, R; Stein Gold, L, 2021
)
0.62
" Only four possible drug-related, non-serious adverse events were reported over the 16-week study, all by the same patient."( Safety and Efficacy of Oral Human Parathyroid Hormone (1-34) in Hypoparathyroidism: An Open-Label Study.
Arbit, E; Blum, M; Burshtein, G; Caraco, Y; Fraser, WD; Galitzer, H; Gershinsky, M; Ish-Shalom, S; Khazen, NS; Raskin, A; Rothner, A; Schwartz, P; Szalat, A; Tang, JC, 2021
)
0.62
"This case suggests calcitriol-mediated hypercalcemia as a novel immune-related adverse event."( Calcitriol-mediated hypercalcemia as an immune-related adverse event in a patient receiving nivolumab and ipilimumab for metastatic renal cell carcinoma, case report.
Issa, M; Johnson, K; Monk, P; Mortazavi, A; Parikh, A; Yang, Y; Yin, M, 2021
)
2.39
"4 and 1 μg/ml) and AlP (20 μg/ml) showed the ability to reduce the toxic effects of AlP."( Calcitriol attenuates the cytotoxicity induced by aluminium phosphide via inhibiting mitochondrial dysfunction and oxidative stress in rat isolated cardiomyocytes.
Hafez, AA; Jamali, Z; Khezri, S; Salimi, A; Samiei, S; Sheikhghaderi, H, 2021
)
2.06
" Efficacy was evaluated based on primary outcome indicators including skin lesion improvement and overall adverse reaction rate."( Clinical efficacy and safety of using calcipotriol-betamethasone compounding agent for psoriasis treatment: a systematic review and meta-analysis.
Ding, H; Dong, S; Feng, J; Li, N; Li, X; Ren, J; Sun, Z; Wang, H; Wang, S; Zhu, Q, 2022
)
0.72
" There was no adverse drug reaction reported with a frequency of >1%, associated with the CAL/BDP PAD-cream."( A pooled analysis of randomized, controlled, phase 3 trials investigating the efficacy and safety of a novel, fixed dose calcipotriene and betamethasone dipropionate cream for the topical treatment of plaque psoriasis.
Augustin, M; Gold, LS; Green, LJ; Pinter, A; Praestegaard, M; Selmer, J, 2022
)
0.72
" Moreover, 40 ng/kg/d calcitriol was not associated with increasing adverse events."( The efficacy and safety of different doses of calcitriol combined with neutral phosphate in X-linked hypophosphatemia: a prospective study.
Chi, Y; Jiajue, R; Jiang, Y; Jin, C; Li, M; Meng, X; Ni, X; Wang, O; Wu, B; Xia, W; Xing, X; Xu, L; Zhang, C; Zhao, Z, 2022
)
1.29
" The experimental results show that for postmenopausal women with osteoporosis, calcitriol combined with bisphosphonate therapy can notoriously enhance the clinical therapy effect of sufferers, with low adverse reactions, and can effectively enhance the bone mineral density and bone density of sufferers."( Clinical Efficacy and Safety Evaluation of Calcitriol Combined with Bisphosphonates in the Therapy of Postmenopausal Osteoporosis: Based on a Retrospective Cohort Study.
Dai, Y; Deng, S; Jing, W; Zhu, J, 2022
)
1.21
" Overall, nine mild non-serious treatment-emergent adverse effects related to all calcipotriol formulations were reported in four subjects, but all recovered at the follow-up visit."( Efficacy and Safety of Water-Free Lipid Formulation System Containing Calcipotriol Against Psoriasis Vulgaris.
Carlsson, A; Holmback, J; Rinwa, P, 2023
)
0.91
"Calcifediol is a safe and efficacious alternative for oral Vitamin D supplementation in young adults."( Efficacy, safety, and dose-response effects of calcifediol supplementation on 25-hydroxyvitamin D, parathyroid hormone, and 1,25-dihydroxyvitamin D levels in healthy adults: An open-label, interventional pilot study.
Bhadada, SK; Das, L; Dutta, P; Holick, MF; Marwaha, RK; Sachdeva, N; Singhmar, S; Thakur, N,
)
0.13

Pharmacokinetics

This article reviews the pharmacokinetic characteristics of calcitriol, paricalcitol, and doxercalciferol. It also provides an overview of the metabolism of vitamin D.

ExcerptReferenceRelevance
" To elucidate this difference, the pharmacokinetic profiles after a single intravenous dose (50 micrograms/kg) of the two compounds to rats were compared."( Calcipotriol (MC 903): pharmacokinetics in rats and biological activities of metabolites. A comparative study with 1,25(OH)2D3.
Binderup, L; Kissmeyer, AM, 1991
)
0.28
" Estrogen replacement therapy (ERT) did not restore POM pharmacokinetic parameters to PRM values."( Menopause: pharmacodynamics and pharmacokinetics.
Benet, LZ; Gustavson, LE,
)
0.13
" Two pharmacokinetic studies (PK1, PK2) were performed 10 days apart, during which the patients received calcitriol after each dialysis."( Pharmacokinetics and efficacy of pulse oral versus intravenous calcitriol in hemodialysis patients.
Levine, BS; Song, M, 1996
)
0.75
" In rat, the pharmacokinetic profile of Seocalcitol (Cmax, AUC, Tmax, T(1/2)) was the same after single and oral administration."( Pharmacokinetics and metabolism of a vitamin D analogue (Seocalcitol) in rat and minipig.
Kissmeyer, AM; Mortensen, JT, 2000
)
0.31
" 1,25-D(3) plasma pharmacokinetic (PK) parameters associated with antitumor activity in experimental animal models are unknown."( Pharmacokinetics of 1alpha,25-dihydroxyvitamin D3 in normal mice after systemic exposure to effective and safe antitumor doses.
Johnson, CS; Modzelewski, RA; Muindi, JR; Peng, Y; Trump, DL, 2004
)
0.32
" The primary objective of this analysis was to determine whether a liquid 1,25-D(3) formulation had a more favorable pharmacokinetic profile."( Pharmacokinetics of liquid calcitriol formulation in advanced solid tumor patients: comparison with caplet formulation.
Johnson, CS; Muindi, JR; Peng, Y; Potter, DM; Trump, DL, 2005
)
0.63
" A dose-proportional increase in peak concentration (C(max)) and area under the concentration curve (AUC) was seen across the full range of DN-101 doses tested."( Pharmacokinetics and tolerability of a single dose of DN-101, a new formulation of calcitriol, in patients with cancer.
Beer, TM; Henner, WD; Javle, M; Lam, GN; Trump, DL; Wong, A, 2005
)
0.55
"To determine, in peripheral blood monocytes (PBM), whether the enzymatic activities of fructose 1,6-bisphosphatase (FBPase), cytidine deaminase (CDDase) and 24-hydroxylase (CYP24), enzymes regulated by calcitriol are useful pharmacodynamic (PD) measures of calcitriol effects in cancer patients."( Monocyte fructose 1,6-bisphosphatase and cytidine deaminase enzyme activities: potential pharmacodynamic measures of calcitriol effects in cancer patients.
Branch, RA; Johnson, CS; Muindi, JR; Peng, Y; Trump, DL; Wilson, JW, 2007
)
0.74
" Pharmacokinetic studies were done for calcitriol and gefitinib."( A phase I pharmacokinetic and pharmacodynamic study of intravenous calcitriol in combination with oral gefitinib in patients with advanced solid tumors.
Bernardi, RJ; Black, JD; Brattain, MG; Creaven, PJ; Fakih, MG; French, R; Hutson, A; Johnson, CS; Muindi, JR; Schwartz, J; Trump, DL, 2007
)
0.85
" The effects of topically applied dermatologic preparations have routinely been assessed by their pharmacodynamic profiles and their concentrations in the skin correlate well with these profiles."( Cutaneous pharmacokinetics of topically applied maxacalcitol ointment and lotion.
Amagishi, H; Hirata, K; Ikeda, Y; Ishihama, Y; Kondo, K; Tokura, Y; Umemura, K, 2008
)
0.35
" From our results, it can offer new opportunities to design and determine individually appropriate therapeutic dosage regimens based on a pharmacokinetic profile and be used for bioequivalence and reevaluation study of generic drug."( Pharmacokinetics of oral calcitriol in healthy human based on the analysis with an enzyme immunoassay.
Jin, SE; Kim, CK; Park, JS, 2009
)
0.66
" The pharmacokinetic properties of synthetic 1,25(OH)2D3 and glycosylated 1,25(OH)2D3 extracted from SG were compared in male rats."( 1,25-Dihydroxyvitamin D3-glycoside of herbal origin exhibits delayed release pharmacokinetics when compared to its synthetic counterpart.
Bachmann, H; Horcajada, MN; Mathis, GA; Offord-Cavin, E; Phothirath, P; Romeis, P, 2013
)
0.39
" To develop an evidence-based clinical algorithm to monitor hypoPT patients treated with recombinant human PTH (rhPTH[1-84]) injected subcutaneously in the thigh, we performed a 24-hour monitoring study of pharmacokinetic and pharmacodynamic effects in a group of 38 patients who had completed a 6-month randomized study on effects of treatment with a fixed rhPTH(1-84) dose of 100 µg/d or similar placebo as an add-on to conventional treatment."( PTH(1-84) replacement therapy in hypoparathyroidism: a randomized controlled trial on pharmacokinetic and dynamic effects after 6 months of treatment.
Amstrup, AK; Kjaer, SG; Mosekilde, L; Rejnmark, L; Rolighed, L; Sikjaer, T, 2013
)
0.39
" Separate pharmacokinetic properties may be associated with distinct TDF toxicities: tenofovir with parathyroid hormone and altered calcium balance and tenofovir diphosphate with hypophosphatemia and FGF23 regulation."( Association of higher plasma vitamin D binding protein and lower free calcitriol levels with tenofovir disoproxil fumarate use and plasma and intracellular tenofovir pharmacokinetics: cause of a functional vitamin D deficiency?
Baker, A; Bethel, J; Flynn, PM; Gordon, CM; Havens, PL; Hazra, R; Kapogiannis, BG; Kiser, JJ; Liu, N; Lujan-Zilbermann, J; Mulligan, K; Pan, CG; Rutledge, B; Stephensen, CB; Van Loan, MD; Wilson, CM; Woodhouse, LR, 2013
)
0.62
" The oral pharmacokinetic properties of 1,25(OH)2D3 of SG origin were established and the subjects were monitored until day 28 for safety reasons."( Human pharmacokinetic profile of 1,25-dihydroxyvitamin D3-glycoside of herbal origin.
Autzen, S; Bachmann, H; Ibanez, R; Mathis, GA; Pokorny, R; Romeis, P; Toggenburger, A, 2014
)
0.4
" The elimination half-life was 17."( Population pharmacokinetic and pharmacodynamic analyses from a 4-month intradose escalation and its subsequent 12-month dose titration studies for a human monoclonal anti-FGF23 antibody (KRN23) in adults with X-linked hypophosphatemia.
Carpenter, TO; Gosselin, NH; Imel, EA; Marier, JF; Peyret, T; Zhang, X, 2016
)
0.43
" Pharmacokinetic analyses were performed after the first and final dose."( Pharmacokinetics of a New Oral Vitamin D Receptor Activator (2-Methylene-19-Nor-(20S)-1α,25-Dihydroxyvitamin D
Bedale, W; Blaser, WJ; Clagett-Dame, M; Coyne, DW; DeLuca, HF; Pandey, R; Plum, LA; Zella, JB; Zhu, JG, 2017
)
0.46
"After the first and final dose, the half-life of DP001 was similar (55."( Pharmacokinetics of a New Oral Vitamin D Receptor Activator (2-Methylene-19-Nor-(20S)-1α,25-Dihydroxyvitamin D
Bedale, W; Blaser, WJ; Clagett-Dame, M; Coyne, DW; DeLuca, HF; Pandey, R; Plum, LA; Zella, JB; Zhu, JG, 2017
)
0.46
"In hemodialysis patients, DP001 has a longer half-life than existing vitamin D therapies and enables control of parathyroid hormone when administered every 2-3 days on the day of dialysis."( Pharmacokinetics of a New Oral Vitamin D Receptor Activator (2-Methylene-19-Nor-(20S)-1α,25-Dihydroxyvitamin D
Bedale, W; Blaser, WJ; Clagett-Dame, M; Coyne, DW; DeLuca, HF; Pandey, R; Plum, LA; Zella, JB; Zhu, JG, 2017
)
0.46
" We previously reported a potent non-secosteroidal VDR modulator (sw-22) with modest anti-tumor activity, which could be due to its undesirable physicochemical and pharmacokinetic properties."( Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
Du, JJ; Han, XL; Hao, MX; Hou, SY; Kang, ZS; Li, YY; Wang, B; Wang, C; Yuan, HL; Zhang, C; Zhou, AW, 2018
)
0.48
" A physiologically-based pharmacokinetic model has been constructed and optimized to match experimental data for multiple QDs: control QDs, QDs conjugated with calcitriol, and QDs conjugated with both calcitriol and SM3 MUC1 antibodies."( A Physiologically-Based Pharmacokinetic Model for Targeting Calcitriol-Conjugated Quantum Dots to Inflammatory Breast Cancer Cells.
Dhurjati, P; Forder, J; Gorky, J; Nohe, A; Schaefer, RJ; Smith, M; van Golen, KL; Wagner, M, 2019
)
0.95
"We developed population pharmacokinetic (PK) and pharmacodynamic (PD) models using a modeling and simulation approach."( Maxacalcitol Pharmacokinetic-Pharmacodynamic Modeling and Simulation for Secondary Hyperparathyroidism in Patients Receiving Maintenance Hemodialysis.
Abe, M; Chen, HH; Fukazawa-Shinotsuka, M; Iida, S; Liu, MC; Saito, T; Terao, K; Wang, IT, 2022
)
0.72

Compound-Compound Interactions

Study evaluated the preliminary efficacy, safety, and impact on quality of life (QoL) of high-dose calcitriol (DN-101) combined with mitoxantrone and glucocorticoids in androgen-independent prostate cancer.

ExcerptReferenceRelevance
" This investigation was undertaken to determine: (1) the effectiveness of CaCO3 as the sole P binder in combination with low (2."( The effects of calcium carbonate as the sole phosphate binder in combination with low calcium dialysate and calcitriol therapy in chronic hemodialysis patients.
Macon, EJ; Oettinger, CW; Oliver, JC, 1992
)
0.5
"Parathyroid hormone (PTH) alone is known to increase bone mass, but clinical studies of osteoporotic men suggest that when 1,25 dihydroxyvitamin D3 (1,25(OH)2D3) is given in combination with PTH, the effect on bone growth is enhanced."( 1,25 dihydroxyvitamin D3 alone or in combination with parathyroid hormone does not increase bone mass in young rats.
Fonseca, J; Gera, I; Gunness-Hey, M; Hock, JM; Raisz, LG, 1988
)
0.27
"25 micrograms, oestrogens/gestagen alone or combined with 1,25(OH)2D3, and placebo."( Effect of 1,25-dihydroxy-vitamin D3 in itself or combined with hormone treatment in preventing postmenopausal osteoporosis.
Christensen, MS; Christiansen, C; Hagen, C; Rødbro, P; Transbøl, I, 1981
)
0.26
"The effects of the novel vitamin D analogue, EB1089 alone, or in combination with the retinoid, 9-cis retinoic acid (9-cis RA) on indices of apoptosis in MCF-7 breast cancer cells have been examined."( Vitamin D derivatives in combination with 9-cis retinoic acid promote active cell death in breast cancer cells.
Colston, KW; James, SY; Mackay, AG, 1995
)
0.29
" Neopterin secretion was also synergistically enhanced in AML blasts by the action of 1,25(OH)2D3 in combination with IFN but not GM-CSF; secretion was enhanced in AML blasts without concomitant evidence of phenotypic maturation."( Neopterin release by myeloid leukaemic cells can be synergistically augmented by 1,25-dihydroxyvitamin D3 in combination with gamma interferon or granulocyte-macrophage colony stimulating factor.
Coldwell, RD; Kelsey, SM; Makin, HL; Newland, AC; Syndercombe-Court, D, 1994
)
0.29
" GM-CSF and IFN-gamma combined with 1,25(OH)2D3 increased cellular TNF secretion to levels not seen with these agents alone."( Induction of surface tumor necrosis factor (TNF) expression and possible facilitation of surface TNF release from human monocytic cells by granulocyte-macrophage colony-stimulating factor or gamma interferon in combination with 1,25-dihydroxyvitamin D3.
Allen, PD; Kelsey, SM; Macey, MG; Newland, AC; Razak, K, 1993
)
0.29
"Therapies utilizing intermittent human parathyroid hormone(1-34) (hPTH[1-34]) in combination with other agents have recently been proposed as possible anabolic regimens for the treatment of osteoporosis."( Effects of intermittent hPTH(1-34) alone and in combination with 1,25(OH)(2)D(3) or risedronate on endosteal bone remodeling in canine cancellous and cortical bone.
Boyce, RW; Eriksen, EF; Franks, AF; Jankowsky, ML; Paddock, CL, 1996
)
0.29
" We, therefore, evaluated the protective potential of MC1288 (20-epi-1,25-dihydroxyvitamin D3) a nonhypercalcemic analog of 1,25-dihydroxyvitamin D3, both alone and in combination with a short induction course of cyclosporin A, in NOD mice that already have insulitis, as demonstrated in pancreatic biopsies performed 15 days before the start oftherapy."( Prevention of type I diabetes in nonobese diabetic mice by late intervention with nonhypercalcemic analogs of 1,25-dihydroxyvitamin D3 in combination with a short induction course of cyclosporin A.
Bouillon, R; Casteels, KM; Laureys, JM; Mathieu, C; Overbergh, L; Valckx, D; Waer, M, 1998
)
0.3
" We examined the ability of 1,25(OH)2D3 in combination with several anti-cancer drugs to inhibit the proliferation of, and induce differentiation in, human monoblastic leukaemia U937 cells."( Growth inhibition and differentiation induction in human monoblastic leukaemia cells by 1alpha-hydroxyvitamin D derivatives and their enhancement by combination with hydroxyurea.
Honma, Y; Makishima, M; Okabe-Kado, J, 1998
)
0.3
" We used low-dose narrow-band UVB phototherapy, combined with balneotherapy, short-contact anthralin, liquor carbonis detergens and calcipotriol for treatment of psoriatic patients in our day care centre."( Low-dose narrow-band UVB phototherapy combined with topical therapy is effective in psoriasis and does not inhibit systemic T-cell activation.
Bos, JD; de Rie, MA; Out, TA, 1998
)
0.3
" Subsequently, this low-dose irradiation regimen was used in combination with topical medication in 26 psoriatic patients."( Low-dose narrow-band UVB phototherapy combined with topical therapy is effective in psoriasis and does not inhibit systemic T-cell activation.
Bos, JD; de Rie, MA; Out, TA, 1998
)
0.3
"Our data indicate that low-dose narrow-band UVB can be used successfully, in combination with topical treatment, in a day care setting to treat psoriatic patients."( Low-dose narrow-band UVB phototherapy combined with topical therapy is effective in psoriasis and does not inhibit systemic T-cell activation.
Bos, JD; de Rie, MA; Out, TA, 1998
)
0.3
"We examined the ability of four novel 20-epi-vitamin D3 analogs (CB1093, KH1060, KH1266, and CB1267), either alone or in combination with 9-cis retinoic acid (RA) to inhibit colony growth of a human prostate cancer cell line, LNCaP, using soft agar as well as bone marrow stroma."( Novel 20-epi-vitamin D3 analog combined with 9-cis-retinoic acid markedly inhibits colony growth of prostate cancer cells.
Binderup, L; Campbell, MJ; Elstner, E; Heber, D; Koeffler, HP; Munker, R; Said, J; Shintaku, P, 1999
)
0.3
"Calcipotriol has been combined with a number of systemic antipsoriatric treatments, improving efficacy or reducing the systemic treatment required."( Calcipotriol cream combined with twice weekly broad-band UVB phototherapy: a safe, effective and UVB-sparing antipsoriatric combination treatment. The Canadian Calcipotriol and UVB Study Group.
Bolduc, A; Gilbert, M; Lowson, D; Papp, K; Ramsay, CA; Schwartz, BE, 2000
)
0.31
"To assess the efficacy and safety of calcipotriol cream (50 microg/g) combined with twice weekly broad-band UVB and to determine if this treatment would require fewer UVB treatments and lower cumulative UVB irradiance when compared to a standard 3 times weekly broad-band UVB regime in patients with extensive psoriasis."( Calcipotriol cream combined with twice weekly broad-band UVB phototherapy: a safe, effective and UVB-sparing antipsoriatric combination treatment. The Canadian Calcipotriol and UVB Study Group.
Bolduc, A; Gilbert, M; Lowson, D; Papp, K; Ramsay, CA; Schwartz, BE, 2000
)
0.31
" NB4 cells treated with ATRA in combination with 1,25 D(3), a monocytic differentiation inducer, while continuing to reduce NBT also failed to mature into neutrophils or monocytes and again showed features of apoptosis."( All trans retinoic acid induces apoptosis in acute promyelocytic NB4 cells when combined with isoquinolinediol, a poly(ADP-ribose) polymerase inhibitor.
Berry, DM; Meckling-Gill, KA; Williams, K, 2000
)
0.31
"To determine the efficacy of calcitriol 3 microg g-1 ointment in combination with UVB phototherapy in treating plaque psoriasis."( Calcitriol 3 microg g-1 ointment in combination with ultraviolet B phototherapy for the treatment of plaque psoriasis: results of a comparative study.
Altmeyer, P; Christophers, E; Kowalzick, L; Ring, J; Schill, WB; Schöpf, E; Ständer, M; Wolff, HH, 2001
)
2.04
" We tested the growth inhibitory activity of ketoconazole combined with 1,25-dihydroxyvitamin D3 (calcitriol) and with the vitamin D analogue EB 1089 in a preclinical model of prostate cancer."( Preclinical activity of ketoconazole in combination with calcitriol or the vitamin D analogue EB 1089 in prostate cancer cells.
Feldman, D; Hsu, JY; Peehl, DM; Seto, E, 2002
)
0.78
"Clonal assays with primary cultures of human prostatic cancer cells were performed to test anti-proliferative effects of ketoconazole alone or in combination with calcitriol or EB 1089."( Preclinical activity of ketoconazole in combination with calcitriol or the vitamin D analogue EB 1089 in prostate cancer cells.
Feldman, D; Hsu, JY; Peehl, DM; Seto, E, 2002
)
0.76
"To more clearly elucidate the conflicting results that have been obtained after oral calcitriol pulse therapy on lipid, glucose, and calcium levels in hemodialysis (HD) patients, and to determine safety of oral calcitriol pulse therapy in a combination with calcium carbonate."( Effect of oral calcitriol pulse therapy on the lipid, calcium, and glucose homeostasis of hemodialysis-patients: its safety in a combination with oral calcium carbonate.
Khajehdehi, P; Taheri, S, 2003
)
0.9
"Our findings indicate that short-term oral calcitriol pulse therapy in combination with calcium carbonate is safe and beneficial for metabolic abnormalities of HD patients; however, its safety for prolonged therapy is yet to be proved."( Effect of oral calcitriol pulse therapy on the lipid, calcium, and glucose homeostasis of hemodialysis-patients: its safety in a combination with oral calcium carbonate.
Khajehdehi, P; Taheri, S, 2003
)
0.93
"To compare the clinical efficacy, in a half-side manner, of UVB (311 nm) in combination with either calcitriol or dithranol."( Calcitriol vs. dithranol in combination with narrow-band ultraviolet B (311 nm) in psoriasis.
Bröcker, EB; Eggert, AA; Goebeler, M; Hofmann, UB, 2003
)
1.98
" A clinical comparison of UVB (311 nm) in combination with either calcitriol or dithranol revealed no significant therapeutic differences between the regimens."( Calcitriol vs. dithranol in combination with narrow-band ultraviolet B (311 nm) in psoriasis.
Bröcker, EB; Eggert, AA; Goebeler, M; Hofmann, UB, 2003
)
2
"Combination of narrow-band UVB (311 nm) therapy with calcitriol is equally effective as the combination with dithranol for the treatment of psoriasis."( Calcitriol vs. dithranol in combination with narrow-band ultraviolet B (311 nm) in psoriasis.
Bröcker, EB; Eggert, AA; Goebeler, M; Hofmann, UB, 2003
)
2.01
"To determine the effect of exogenous 1,25-dihydroxyvitamin D3 [1,25(OH)2D3] combined with induced parturition on calcium (Ca) metabolism, cows received a single intramuscular injection of 1,25(OH)2D3 and prostaglandin F(2alpha) (PGF(2alpha)) closely before calving."( Calcium metabolism in cows receiving an intramuscular injection of 1,25-dihydroxyvitamin D3 combined with prostaglandin F(2alpha) closely before parturition.
Ayukawa, Y; Lee, I; Naito, Y; Oboshi, K; Yamagishi, N, 2005
)
0.33
" Remarkably, vitiligo lesions treated with calcipotriol initially showed delayed repigmentation compared with control areas; however, there was no therapeutic difference between calcipotriol and placebo, both in combination with UVB311 nm, by the end of the study."( Narrow-band UVB311 nm vs. broad-band UVB therapy in combination with topical calcipotriol vs. placebo in vitiligo.
Bröcker, EB; Hamm, H; Hartmann, A; Hofmann, UB; Lurz, C, 2005
)
0.33
" Applying antiproliferative SRB and MTT assays, we measured the growth inhibitory effects of vitamin D compounds applied alone or in combination with either cisplatin or doxorubicin."( Correlation between VDR expression and antiproliferative activity of vitamin D3 compounds in combination with cytostatics.
Jaroszewicz, I; Kutner, A; Nevozhay, D; Opolski, A; Pelczynska, M; Switalska, M; Wietrzyk, J; Zabel, M,
)
0.13
" In this randomized and comparative study, we investigated the safety and efficacy of narrow band ultraviolet B as monotherapy and in combination with topical calcipotriol in the treatment of generalized vitiligo."( Narrow-band ultraviolet B as monotherapy and in combination with topical calcipotriol in the treatment of vitiligo.
Arca, E; Erbil, AH; Koç, E; Kurumlu, Z; Sezer, E; Taştan, HB, 2006
)
0.33
" For this photo case presentation, Dovobet was used once daily in combination with UVB phototherapy 3 times a week."( Calcipotriol (Dovobet) ointment in combination with UVB therapy for psoriasis treatment.
Rogers, C, 2006
)
0.33
" Applying antiproliferative SRB and MTT assays, the growth inhibitory effects of the vitamin D compounds, applied alone or in combination with either cisplatin or doxorubicin, were measured."( Antiproliferative activity of vitamin D compounds in combination with cytostatics.
Jaroszewicz, I; Kutner, A; Maciejewska, M; Opolski, A; Pelczynska, M; Switalska, M,
)
0.13
" calcitriol can be administered safely in combination with gefitinib."( A phase I pharmacokinetic and pharmacodynamic study of intravenous calcitriol in combination with oral gefitinib in patients with advanced solid tumors.
Bernardi, RJ; Black, JD; Brattain, MG; Creaven, PJ; Fakih, MG; French, R; Hutson, A; Johnson, CS; Muindi, JR; Schwartz, J; Trump, DL, 2007
)
1.49
" Further, since JKF is less calcemic than 1,25D, the data suggest that JKF combined with CA and SB is likely to have a therapeutic advantage over 1,25D-based experimental regimens for myeloid leukemias."( Differentiation-inducing potency of the seco-steroid JK-1624F2-2 can be increased by combination with an antioxidant and a p38MAPK inhibitor which upregulates the JNK pathway.
Danilenko, M; Posner, GH; Studzinski, GP; Zhang, J,
)
0.13
" In the present study, VPA in combination with two differentiating agents, 13-cis retinoic acid and 1,25-dihydroxyvitamin D3, was given to 19 previously untreated patients with MDS or CMML."( Valproic acid combined with 13-cis retinoic acid and 1,25-dihydroxyvitamin D3 in the treatment of patients with myelodysplastic syndromes.
Hallman, H; Honkanen, T; Juvonen, E; Kauppila, M; Koistinen, P; Kutila, A; Mikkola, M; Nyländen, P; Poikonen, E; Rauhala, A; Savolainen, ER; Siitonen, T; Sinisalo, M; Suominen, M; Terävä, V; Timonen, T, 2007
)
0.34
" This study examined the effects of 1,25(OH)2D3 in combination with carnosic acid on monocytic differentiation as well as intracellular reactive oxygen species (ROS) and Ca2+ levels in human leukemia HL-60 cells."( [Enhancement of differentiation induction of HL-60 cells by 1,25-dihydroxyvitamin D3 in combination with carnosic acid].
An, HP; Chen, JJ; Ren, LH, 2008
)
0.35
"Low concentration of 1,25(OH)2D3 combined with 10 micromol/L carnosic acid can produce enhanced differentiation, proliferation inhibition and antioxidant effects of HL-60 cells."( [Enhancement of differentiation induction of HL-60 cells by 1,25-dihydroxyvitamin D3 in combination with carnosic acid].
An, HP; Chen, JJ; Ren, LH, 2008
)
0.35
"To evaluate the preliminary efficacy, safety, and impact on quality of life (QoL) of high-dose calcitriol (DN-101) combined with mitoxantrone and glucocorticoids in androgen-independent prostate cancer (AIPC)."( A phase II study of high-dose calcitriol combined with mitoxantrone and prednisone for androgen-independent prostate cancer.
Beer, TM; Chan, JS; Dehaze, DR; Garzotto, M; Pinski, JK; Quinn, DI; Ryan, CW; Sokoloff, M, 2008
)
0.85
") calcitriol administered in combination with a fixed oral dose of dexamethasone and gefitinib in patients with refractory solid tumors."( A phase I and pharmacokinetics study of intravenous calcitriol in combination with oral dexamethasone and gefitinib in patients with advanced solid tumors.
Christy, R; Engler, KL; Fakih, MG; Johnson, CS; Muindi, JR; Trump, DL, 2009
)
1.32
" The aim of this study was to investigate the possible influence of 1alpha,25-dihydroxyvitamin D(3) (calcitriol) and 1alpha,24(R)-dihydroxyvitamin D(3) (tacalcitol) in monotherapy and in combination with budesonid R (BR) on NP fibroblast proliferation."( Influence of vitamin D(3) analogues in combination with budesonid R on proliferation of nasal polyp fibroblasts.
Fraczek, M; Gawron, W; Latocha, M; Rostkowska-Nadolska, B, 2009
)
0.57
"High-dose, iv calcitriol at a dose of 74 microg weekly in combination with dexamethasone was well tolerated but failed to produce a clinical or PSA response in men with CRPC."( Phase 2 trial of weekly intravenous 1,25 dihydroxy cholecalciferol (calcitriol) in combination with dexamethasone for castration-resistant prostate cancer.
Chadha, MK; Johnson, C; Levine, E; Mashtare, T; Payne, V; Silliman, C; Tian, L; Trump, DL; Wong, M, 2010
)
0.96
" This effect is further accentuated by combination with 5-amino-imidazole-4-carboxamide-1-beta-4-ribofuranoside (AICAR), an activator of AMP-activated protein kinase (AMPK)/acetyl-Co-enzyme A carboxylase (ACC) phosphorylation pathways and an inhibitor of Akt phosphorylation."( Anti-growth effect of 1,25-dihydroxyvitamin D3-3-bromoacetate alone or in combination with 5-amino-imidazole-4-carboxamide-1-beta-4-ribofuranoside in pancreatic cancer cells.
Chadid, S; Deoliveira, R; Eddy, VJ; Persons, KS; Ray, R; Saha, AK, 2010
)
0.36
" The objective of this study was to investigate the effects of 1,25(OH)(2)D(3) and the superagonistic analog CD578 in anaplastic thyroid cancer, alone or in combination with paclitaxel, a taxane, and suberoylanilide hydroxamic acid (SAHA), a potent histone deacetylase inhibitor with promising effects in undifferentiated thyroid cancer."( 1,25-dihydroxyvitamin D3 and a superagonistic analog in combination with paclitaxel or suberoylanilide hydroxamic acid have potent antiproliferative effects on anaplastic thyroid cancer.
Bouillon, R; Clinckspoor, I; Decallonne, B; Korch, C; Mathieu, C; Overbergh, L; Verlinden, L; Verstuyf, A, 2011
)
0.37
"Treatment of plaque-type psoriasis with laser in combination with topical treatment is a safe and effective therapy."( Treatment of plaque-type psoriasis with the 308 nm excimer laser in combination with dithranol or calcipotriol.
Bodendorf, MO; Grunewald, S; Kauer, F; Paasch, U; Rogalski, C; Schetschorke, M; Simon, JC, 2012
)
0.38
"This study aimed to compare the efficacy of targeted microphototherapy alone and in combination with psoralen or calcipotriol in the treatment of plaque-type psoriasis."( Efficacy and safety of non-laser, targeted UVB phototherapy alone and in combination with psoralen gel or calcipotriol ointment in the treatment of localized, chronic, plaque-type psoriasis.
Arca, E; Köse, O; Ozkan, I; Ozmen, I, 2012
)
0.38
"Thirty individuals, affected by plaque-type psoriasis, were treated with targeted narrowband UVB phototherapy alone (Group 1), in combination with psoralen gel (Group 2), or in combination with calcipotriol ointment (Group 3) three times per week based on predetermined minimal erythema doses for 10 weeks."( Efficacy and safety of non-laser, targeted UVB phototherapy alone and in combination with psoralen gel or calcipotriol ointment in the treatment of localized, chronic, plaque-type psoriasis.
Arca, E; Köse, O; Ozkan, I; Ozmen, I, 2012
)
0.38
" We investigated the anti-leukemic effect of low-dose 1,25-dihydroxyvitamin D(3) (1,25(OH)(2)D(3)) in combination with As(2)O(3) on the human AML cell lines HL-60 and K562."( Low-dose 1,25-dihydroxyvitamin D(3) combined with arsenic trioxide synergistically inhibits proliferation of acute myeloid leukemia cells by promoting apoptosis.
Bae, JY; Kim, I; Kim, JW, 2013
)
0.39
"In this 12-week study, patients with moderate to severe psoriasis received twice weekly treatment with XTRAC® Velocity 308-nm excimer laser combined with clobetasol propionate twice daily followed by calitriol ointment twice daily."( Supraerythemogenic excimer laser in combination with clobetasol spray and calcitriol ointment for the treatment of generalized plaque psoriasis: Interim results of an open label pilot study.
Brown, G; Butler, D; Debbaneh, M; Gupta, R; Huynh, M; Koo, JY; Leon, A; Levin, E; Malakouti, M; Wang, E, 2015
)
0.65
"Excimer laser therapy combined with an optimized topical regimen that includes clobetasol spray followed by calictriol ointment appears to be an effective treatment for moderate to severe generalized psoriasis that avoids the risk of serious internal side effects associated with many systemic agents."( Supraerythemogenic excimer laser in combination with clobetasol spray and calcitriol ointment for the treatment of generalized plaque psoriasis: Interim results of an open label pilot study.
Brown, G; Butler, D; Debbaneh, M; Gupta, R; Huynh, M; Koo, JY; Leon, A; Levin, E; Malakouti, M; Wang, E, 2015
)
0.65
"005%) in combination with NB-UVB vs."( Comparison of efficacy and safety profile of topical calcipotriol ointment in combination with NB-UVB vs. NB-UVB alone in the treatment of vitiligo: a 24-week prospective right-left comparative clinical trial.
Kanwar, AJ; Khullar, G; Parsad, D; Singh, S, 2015
)
0.42
" Larger, randomized placebo-controlled trials are required to determine whether addition of calcipotriol has any utility when administered with NB-UVB in the treatment of vitiligo."( Comparison of efficacy and safety profile of topical calcipotriol ointment in combination with NB-UVB vs. NB-UVB alone in the treatment of vitiligo: a 24-week prospective right-left comparative clinical trial.
Kanwar, AJ; Khullar, G; Parsad, D; Singh, S, 2015
)
0.42
" In this 12-week study, patients with moderate to severe psoriasis received twice weekly treatments with a 308-nm excimer laser combined with clobetasol proprionate twice daily for a month followed by calcitriol ointment twice daily for the next month."( An open label pilot study of supraerythemogenic excimer laser in combination with clobetasol spray and calcitriol ointment for the treatment of generalized plaque psoriasis.
Beroukhim, K; Danesh, MJ; Koo, J; Leon, A; Levin, E; Nguyen, CM, 2016
)
0.84
"This study aimed to investigate whether Müllerian inhibiting substance (MIS) in combination with calcitriol modulates proliferation and apoptosis of human ovarian cancer (OCa) cell lines (SKOV3, OVCAR3, and OVCA433) and identify the signaling pathway by which MIS mediates apoptosis."( Anti-Proliferative and Apoptotic Activities of Müllerian Inhibiting Substance Combined with Calcitriol in Ovarian Cancer Cell Lines.
Choi, YS; Han, HD; Jung, YS; Kim, HJ; Kim, JW; Kim, S; Kim, SW; Kim, YT; Nam, EJ; Seo, SK, 2016
)
0.87
"These results, coupled with a much-needed decrease in the toxic side effects of currently employed therapeutic agents, provide a strong rationale for testing the therapeutic potential of MIS, alone or in combination with calcitriol, in the treatment of OCa."( Anti-Proliferative and Apoptotic Activities of Müllerian Inhibiting Substance Combined with Calcitriol in Ovarian Cancer Cell Lines.
Choi, YS; Han, HD; Jung, YS; Kim, HJ; Kim, JW; Kim, S; Kim, SW; Kim, YT; Nam, EJ; Seo, SK, 2016
)
0.84
"The results of our study show that in the treatment of plaque-type psoriasis, topical calcipotriol combined with Spa Rusanda balineotherapy is more effective than topical calcipotriol alone."( Effects of Rusanda Spa balneotherapy combined with calcipotriol on plaque psoriasis.
Golusin, Z; Jovanović, M; Magda, N; Matić, M; Petrović, A; Stojanović, S, 2015
)
0.42
" Here, we investigated the efficacy of calcipotriol, a topical TSLP inducer, in combination with 5-fluorouracil (5-FU) as an immunotherapy for actinic keratosis."( Randomized trial of calcipotriol combined with 5-fluorouracil for skin cancer precursor immunotherapy.
Cornelius, LA; Cunningham, TJ; Demehri, S; Eliane, JP; Kopan, R; Manivasagam, S; Mirzaalian, H; Saavedra, AP; Schaffer, A; Tabacchi, M; Tuchayi, SM; Turkoz, A; Wallendorf, M, 2017
)
0.46
"005% calcipotriol ointment combined with 5% 5-FU cream were compared with Vaseline plus 5-FU for the field treatment of actinic keratosis in a randomized, double-blind clinical trial involving 131 participants."( Randomized trial of calcipotriol combined with 5-fluorouracil for skin cancer precursor immunotherapy.
Cornelius, LA; Cunningham, TJ; Demehri, S; Eliane, JP; Kopan, R; Manivasagam, S; Mirzaalian, H; Saavedra, AP; Schaffer, A; Tabacchi, M; Tuchayi, SM; Turkoz, A; Wallendorf, M, 2017
)
0.46
" In light of the profound and diverse effects of 1,25(OH)₂D₃ reported by in vitro and in vivo studies, we discuss how these effects could support the use of this molecule in combination with "classical" cytotoxic drugs, such as platins and anti-metabolites, for the treatment of solid and hematological tumors."( Effects of 1,25(OH)₂D₃ on Cancer Cells and Potential Applications in Combination with Established and Putative Anti-Cancer Agents.
Abu El Maaty, MA; Wölfl, S, 2017
)
0.46
" The objective of this open label, intraindividual, left right study was to compare two different vitamin D analogues, calcipotriol and tacalcitol, in combination with NBUVB phototherapy in chronic stable plaque psoriasis."( Comparative evaluation of efficacy and safety of calcipotriol versus tacalcitol ointment, both in combination with NBUVB phototherapy in the treatment of stable plaque psoriasis.
Aggarwal, K; Dua, I; Jain, VK, 2017
)
0.46
"5 μg/ml of BV suppressed proliferation of HL-60 cells but had not any effects on their differentiation, whereas in combination with 5 nM of 1,25-(OH)2 VD3, it enhanced antiproliferative and differentiation potency of 1,25-(OH)2 VD3."( Honey bee venom combined with 1,25-dihydroxyvitamin D
Khosravi, Z; Mohseni-Kouchesfahani, H; Nabioni, M; Rahimi, M,
)
0.13
"
 Methods: Thirty SHPT patients were enrolled to receive treatment of cinacalcet combined with low-dose calcitriol, with inclusion criteria as follows: maintenance on MHD>6 months; serum intact parathyroid hormone (iPTH)>600 pg/mL; parathyroid glands with more than 1 nodules by ultrasonography; traditional therapy with no effects."( [Effect of cinacalcet combined with low-dose calcitriol on clinical outcome and bone metabolism in patients with severe secondary hyperparathyroidism].
Chen, X; Liu, H; Wang, C; Yuan, F; Zhou, A, 2017
)
0.93
"To observe the clinical outcome and the effect of bone metabolism of cinacalcet combined with calcitriol in maintenance hemodialysis (MHD) patients with severe secondary hyperparathyroidism (SHPT)."( Effect of Cinacalcet Combined with Calcitriol on the Clinical Outcome and Bone Metabolism in Patients on Hemodialysis with Severe Secondary Hyperparathyroidism.
Chen, X; Li, Z; Liu, H; Wang, C; Yuan, F, 2018
)
0.98
"Cinacalcet combined with low dose calcitriol can improve high calcium, high phosphorus, and high iPTH in MHD patients with severe SHPT and also improve bone metabolism."( Effect of Cinacalcet Combined with Calcitriol on the Clinical Outcome and Bone Metabolism in Patients on Hemodialysis with Severe Secondary Hyperparathyroidism.
Chen, X; Li, Z; Liu, H; Wang, C; Yuan, F, 2018
)
1.04
" Vitamin D compounds have been shown to exert synergistic effects when used in combination with different agents used in anticancer therapies in different cancer models."( Vitamin D derivatives potentiate the anticancer and anti-angiogenic activity of tyrosine kinase inhibitors in combination with cytostatic drugs in an A549 non-small cell lung cancer model.
Filip-Psurska, B; Kutner, A; Maj, E; Milczarek, M; Psurski, M; Wietrzyk, J, 2018
)
0.48
" The present study evaluated the effect of prolactin itself and in combination with estrogen on bone mineral density of female rats."( The effect of prolactin itself and in combination with estrogen on bone mineral density in female rats.
Kasaee, SR; Ranjbar Omrani, GH; Sadeghian, F; Saki, F; Talezadeh, P, 2019
)
0.51
"This study aimed to observe and analyze the effect of calcitriol combined with sevelamer carbonate on serum parathyroid hormone in patients with chronic renal failure."( Effect of calcitriol combined with sevelamer carbonate on serum parathyroid hormone in patients with chronic renal failure.
Liu, Z; Zheng, H, 2020
)
1.21
" Furthermore, when calcitriol was administered alone, the activity of vascular endothelial growth factor decreased in a dose-dependent manner, and when combined with cisplatin, activity was more suppressed."( Calcitriol Combined With Platinum-based Chemotherapy Suppresses Growth and Expression of Vascular Endothelial Growth Factor of SKOV-3 Ovarian Cancer Cells.
Kim, JH; Kim, K; Kim, YB; No, JH; Park, WH; Suh, DH, 2021
)
2.39
"To investigate the clinical efficacy of calcitriol combined with sirolimus in the treatment of chronic primary immune thrombocytopenia (cITP) patients."( [Clinical Study on Calcitriol Combined with Sirolimus in the Treatment of Chronic Primary Immune Thrombocytopenia Patients].
Fan, L; Kang, HY; Li, Q; Liu, J; Tong, CQ; Zhang, B; Zhang, L, 2021
)
1.22
" The control group was treated with oral sirolimus capsule, the observation group was treated with oral calcitriol capsule combined with sirolimus capsule, and the curative effect of the 2 groups was evaluated after continuous treatment for 6 weeks."( [Clinical Study on Calcitriol Combined with Sirolimus in the Treatment of Chronic Primary Immune Thrombocytopenia Patients].
Fan, L; Kang, HY; Li, Q; Liu, J; Tong, CQ; Zhang, B; Zhang, L, 2021
)
1.16
"The present study investigated the clinical efficacy of percutaneous kyphoplasty (PKP) combined with calcitriol and calcium in the treatment of traumatic nonosteoporotic vertebral compression fractures (TNVCFs)."( Clinical Efficacy of Percutaneous Kyphoplasty Combined with Calcitriol and Calcium in the Treatment of Traumatic Nonosteoporotic Vertebral Compression Fractures.
Dai, N; Dai, S; Lu, X; Peng, P; Shi, X; Xu, F; Yang, P, 2022
)
1.18
"PKP combined with calcitriol and calcium medications could significantly relieve pain, alleviate the loss of compressed vertebral height and kyphosis, and improve the spinal function and the life quality of the TNVCF patients."( Clinical Efficacy of Percutaneous Kyphoplasty Combined with Calcitriol and Calcium in the Treatment of Traumatic Nonosteoporotic Vertebral Compression Fractures.
Dai, N; Dai, S; Lu, X; Peng, P; Shi, X; Xu, F; Yang, P, 2022
)
1.3
" This pilot study assesses the effect of twice-weekly maintenance doses of Cal/BD foam after 4 weeks of standard once-daily treatment in combination with apremilast."( The Maintenance Effect of Calcipotriene 0.05% and Betamethasone Dipropionate 0.064% (Cal/BD) Aerosol Foam in Combination With Apremilast.
Kircik, L; Ozyurekoglu, E, 2022
)
0.72
"A retrospective cohort study to explore the clinical efficacy and safety evaluation of calcitriol combined with bisphosphonates in the therapy of postmenopausal osteoporosis is conducted."( Clinical Efficacy and Safety Evaluation of Calcitriol Combined with Bisphosphonates in the Therapy of Postmenopausal Osteoporosis: Based on a Retrospective Cohort Study.
Dai, Y; Deng, S; Jing, W; Zhu, J, 2022
)
1.21
" The objective of this open label intraindividual, left right study was to compare two different vitamin D analogues, calcipotriol and calcitriol, in combination with NBUVB phototherapy in psoriasis."( Comparative evaluation of efficacy and safety of calcipotriol versus calcitriol ointment, both in combination with narrow-band ultraviolet B phototherapy in the treatment of stable plaque psoriasis.
Aggarwal, K; Chakraborty, D, 2023
)
1.35

Bioavailability

Soy increases the bioavailability of endogenous and administered calcitriol, thereby enhancing its anticancer effects and risk of hypercalcemia. In summary, we observed a higher fractional Ca absorption rate in physically active young men compared with sedentary controls.

ExcerptReferenceRelevance
" The binding and bioavailability of vitamin D metabolites thus might be altered by mono- and polyunsaturated but not by saturated fatty acids."( Polyunsaturated fatty acids decrease the apparent affinity of vitamin D metabolites for human vitamin D-binding protein.
Bouillon, R; Convents, R; Van Baelen, H; Xiang, DZ, 1992
)
0.28
" The potential value of alternative modes of calcitriol administration for the control of secondary hyperparathyroidism is discussed as well as the differences in the bioavailability of sterol according to the different routes for calcitriol administration."( Renal bone disease in pediatric patients receiving treatment with maintenance peritoneal dialysis.
Goodman, WG; Salusky, IB, 1991
)
0.54
"Calcium bioavailability was defined as either retention of 45Ca in tibias (Experiment 1) or retention of 47Ca in carcasses (Experiment 2)."( Lactose, calcium source and age affect calcium bioavailability in rats.
Buchowski, MS; Miller, DD, 1991
)
0.28
" 1,25(OH)2D3 was less potent because of diminished bioavailability due to self induction of its presystemic metabolism and inactivation."( Tracer kinetics and actions of oral and intraperitoneal 1,25-dihydroxyvitamin D3 administration in rats.
Balfe, JW; Kooh, SW; Rawlins, M; Tinmouth, WW; Vieth, R, 1990
)
0.28
" To examine potential mechanisms for this difference, the bioavailability of calcitriol was evaluated after single oral (PO), IV, and IP doses of 60 ng/kg in each of six adolescent patients with osteitis fibrosa undergoing continuous ambulatory peritoneal dialysis (CAPD) or continuous cycling peritoneal dialysis (CCPD)."( Pharmacokinetics of calcitriol in continuous ambulatory and cycling peritoneal dialysis patients.
Adams, JS; Coburn, JW; Fine, RN; Goodman, WG; Holloway, M; Horst, R; Kim, L; Norris, KC; Salusky, IB; Segre, GV, 1990
)
0.83
" In untreated uremic rats, the glucose absorption rate was lower than in sham-operated rats."( Effect of 1,25-dihydroxyvitamin D3 on intestinal glucose absorption in uremic rats.
Fujita, Y; Inagaki, O; Inoue, S; Mori, H; Nagasaka, H; Syono, T, 1989
)
0.28
" The average rate of absorption of 1,25-dihydroxyvitamin D3 [1,25(OH)2D3] was two- and fivefold higher than that of 25-hydroxyvitamin D3 [25(OH)D3] and vitamin D3 (D3), respectively."( Intestinal metabolism and portal venous transport of 1,25(OH)2D3, 25(OH)D3, and vitamin D3 in the rat.
Baylink, DJ; Lau, KH; McDonald, GB; Schy, AL; Wergedal, JE, 1985
)
0.27
"7 pg/ml (mean +/- SD) in normal volunteers after administration of 1 alpha-hydroxyvitamin D, while values of intestinal calcium absorption rate were 61."( Evidence that factors other than 1,25 dihydroxyvitamin D may play a role in augmenting intestinal calcium absorption in patients with primary hyperparathyroidism.
Aoki, J; Dokoh, S; Fukunaga, M; Hino, M; Morita, R; Shigeno, C; Torizuka, K; Yamamoto, I, 1986
)
0.27
" 1,25(OH)2D3 is well absorbed into the systemic circulation, raises ionized calcium levels, and leads to a marked suppression of PTH."( The effects of intraperitoneal calcitriol on calcium and parathyroid hormone.
Delmez, JA; Dougan, CS; Gearing, BK; Rapp, N; Rothstein, M; Slatopolsky, E; Windus, DW, 1987
)
0.56
" The hepatic uptake of 1,25-dihydroxyvitamin D3 is discussed in relation to its systemic bioavailability following intravenous or oral administration as well as in relation to the hepatic uptake of other vitamin D sterols; it is postulated that the hepatic uptake of vitamin D sterols does not seem to be mediated by specific receptors on the liver plasma membrane; it seems, however, that the hepatic uptake of vitamin D sterols may be inversely related to their relative affinity for the circulating carrier, the vitamin D binding protein."( Uptake of the hormone 1,25-dihydroxyvitamin D3 by the dog liver.
Gascon-Barré, M; Huet, PM; Vallières, S, 1986
)
0.27
" At low luminal concentrations, under conditions where calcium is transported predominantly by active processes, the calcium absorption rate was reduced though not abolished in hyperthyroid patients (16 +/- 4 (SE) mumol/h ."( The defect of intestinal calcium transport in hyperthyroidism and its response to therapy.
Keck, E; Krüskemper, HL; Peerenboom, H; Strohmeyer, G, 1984
)
0.27
" They act by modifying Ca bioavailability and perhaps brush-border permeability."( [Intestinal absorption of calcium and its regulation. Tissue, membrane and molecular events].
Bellaton, C; Pansu, D; Roche, C, 1984
)
0.27
" If betamethasone was administered for 10 days and then stopped 4-13 days before these parameters were measured, a compensatory increase was found in 1-hydroxylase activity while the Ca absorption rate attained control values in all but the 4 day group in which it was still significantly depressed."( The effect of betamethasone on duodenal calcium absorption and 1,25-dihydroxy vitamin D3 production in the chick.
Blahos, J; Care, AD; Sommerville, BA, 1983
)
0.27
" Thirty-centimeter segments of jejunum were perfused with test solutions containing varying concentrations of phosphate; phosphate absorption rate and electrical potential difference were measured."( Absorption of phosphate in the jejunum of patients with chronic renal failure before and after correction of vitamin D deficiency.
Davis, GR; Fordtran, JS; Krejs, GJ; Pak, CY; Parker, TF; Zerwekh, JE, 1983
)
0.27
" The net calcium absorption rate from a Thirty-Vella loop of jejunum increased with increasing intraluminal Ca concentration and was increased by the addition of 1 alpha-hydroxy-cholecalciferol (3 micrograms/l) to the loop fluid."( Effects of dietary phosphorus and calcium on the intestinal absorption of Ca in sheep.
Abdel-Hafeez, HM; Care, AD; Mañas-Almendros, M; Marshall, DH; Ross, R, 1982
)
0.26
" In rachitic chicks, the rate of absorption of 203Pb was greater in the distal than in the proximal segments of the intestine; after cholecalciferol repletion, the degree of absorption in al segments was similar, indicting the order of cholecalciferol effectiveness as duodenum greater than or equal to jejunum greater than ileum."( Effect of vitamin D on the intestinal absorption of 203Pb and 47Ca in chicks.
Mykkänen, HM; Wasserman, RH, 1982
)
0.26
"5, or 1 mg supplemental Cu/kg) was used to investigate the effect of microbial phytase at 600 U/kg and 1,25-dihydroxycholecalciferol [1,25-(OH)2D3] at 10 micrograms/kg on Cu bioavailability from dehulled soybean meal (SBM) and cottonseed meal (CSM)."( Effect of microbial phytase and 1,25-dihydroxycholecalciferol on dietary copper utilization in chicks.
Aoyagi, S; Baker, DH, 1995
)
0.29
" The fractional absorption of 45Ca and Sr at 6h (FA360) and the absorption rate as a function of time were calculated by deconvolution."( Stable strontium absorption as a measure of intestinal calcium absorption: comparison with the double-radiotracer calcium absorption test.
Blumsohn, A; Eastell, R; Morris, B, 1994
)
0.29
" Other sugars thought to be poorly absorbed in the small intestine (xylitol, lactobionate, arabinose, raffinose, pyroglutamate, sorbitol, gluconate and raftilose) stimulated Ca absorption to an identical extent as lactulose."( Intestinal calcium absorption in rats is stimulated by dietary lactulose and other resistant sugars.
Antille, S; Binacua, C; Brommage, R; Carrié, AL, 1993
)
0.29
"Because intravenous (iv) calcitriol has greater bioavailability than oral calcitriol, it may be more efficacious in suppressing parathyroid hormone (PTH) secretion."( Pharmacokinetics and efficacy of pulse oral versus intravenous calcitriol in hemodialysis patients.
Levine, BS; Song, M, 1996
)
0.84
" The differential therapeutic effects in the epidermal and dermal skin compartments may be due to a reduced bioavailability of calcipotriol in the dermal compartment."( Biologic effects of topical calcipotriol (MC 903) treatment in psoriatic skin.
Bahmer, FA; Baum, HP; Kerber, A; Müller, SM; Reichrath, J, 1997
)
0.3
" The culture model we describe should prove useful in defining the role of CYP3A4 in limiting the oral bioavailability of many xenobiotics."( Expression of enzymatically active CYP3A4 by Caco-2 cells grown on extracellular matrix-coated permeable supports in the presence of 1alpha,25-dihydroxyvitamin D3.
Fisher, JM; Lown, KS; Paine, MF; Schmiedlin-Ren, P; Thummel, KE; Watkins, PB, 1997
)
0.3
" This yielded the estimated fraction of the dose circulating at 1 hr, which then was converted into a fractional absorption rate from our previously published equation."( Modification and validation of a single-isotope radiocalcium absorption test.
Clifton, PM; Horowitz, M; Morris, HA; Need, AG; Nordin, BE; Scopacasa, F; Wishart, JM, 1998
)
0.3
" Those children are likely to have suboptimal bioavailability of vitamin D, which might hamper their achievement of an adequate peak bone mass."( Seasonal deficiency of vitamin D in children: a potential target for osteoporosis-preventing strategies?
Amado, JA; Docio, S; González-Macías, J; Olmos, JM; Pérez, A; Riancho, JA, 1998
)
0.3
" Young chicks were used to evaluate the efficacy of 2 new vitamin D3 analogs relative to 1 alpha-hydroxycholecalciferol (1 alpha-OH D3) for their ability to improve the bioavailability of phytate-bound phosphorus (P) when added to P-deficient maize-soyabean meal diets that were superadequate in cholecalciferol."( Activity of various hydroxylated vitamin D3 analogs for improving phosphorus utilisation in chicks receiving diets adequate in vitamin D3.
Baker, DH; Biehl, RR; Deluca, HF, 1998
)
0.3
"Insulin-like growth factor binding proteins (IGFBPs) modulate the actions and bioavailability of insulin-like growth factors (IGFs), however, their regulation in vivo is incompletely understood."( Effects of growth hormone treatment on serum levels of insulin-like growth factors (IGFs) and IGF binding proteins 1-4 in postmenopausal women.
Blum, WF; Brixen, K; Flyvbjerg, A; Kassem, M; Mosekilde, L, 1998
)
0.3
" This increased rate of absorption was not found at concentrations of calcium that result in diffusional calcium absorption."( A characterization of vitamin D-independent intestinal calcium absorption in the osteopetrotic (op/op) mouse.
DeLuca, HF; McCary, LC; Staun, M, 1999
)
0.3
" In summary, we observed a higher fractional Ca absorption rate in physically active young men compared with sedentary controls which is probably mediated by calcitriol."( Exercise-trained young men have higher calcium absorption rates and plasma calcitriol levels compared with age-matched sedentary controls.
Danz, A; Dimitriou, T; Jantzen, S; Klein, K; Platen, P; Sabatschus, O; Scheld, K; Stehle, P; Zittermann, A, 2000
)
0.73
"The authors hypothesized that estrogen treatment or vitamin D status may affect the bioavailability of two common calcium supplements differently."( Effect of estrogen treatment and vitamin D status on differing bioavailabilities of calcium carbonate and calcium citrate.
Adams-Huet, B; Heller, HJ; Poindexter, JR, 2002
)
0.31
"We determined the bioavailability of calcium from 3 different sources: orange juice fortified with calcium-citrate malate, skim milk, and a calcium carbonate supplement."( Relative bioavailability of calcium-rich dietary sources in the elderly.
Martini, L; Wood, RJ, 2002
)
0.31
" This finding suggests that the calcium bioavailability from the 3 sources was equivalent."( Relative bioavailability of calcium-rich dietary sources in the elderly.
Martini, L; Wood, RJ, 2002
)
0.31
"In elderly subjects, the calcium bioavailability of the 3 high-calcium dietary sources tested was equivalent, during both the acute postprandial and longer-term periods."( Relative bioavailability of calcium-rich dietary sources in the elderly.
Martini, L; Wood, RJ, 2002
)
0.31
" In spite of this promising activity, a broad therapeutic application of vitamin D metabolites and analogs is still restricted because of their poor bioavailability and their hypercalcemic actions."( Induction of apoptosis by vitamin D metabolites and analogs in a glioma cell line.
Edling, C; Elias, J; Lachmann, B; Marian, B; Noe, CR; Rolf, SH; Schuster, I, 2003
)
0.32
" Such a formulation may provide convenience and enhanced activity compared with separate applications, but it is essential that the biological activity and bioavailability of either active agent is not adversely affected by the other component."( Bioavailability of betamethasone dipropionate when combined with calcipotriol.
Traulsen, J, 2004
)
0.32
"His study was designed to determine whether the bioavailability of the corticosteroid component of Daivobet was equivalent to that in a corticosteroid-only formulation (Diprosone, Schering-Plough Laboratories, France)."( Bioavailability of betamethasone dipropionate when combined with calcipotriol.
Traulsen, J, 2004
)
0.32
" The bioavailability after oral administration of seocalcitol dissolved in medium chain triglyceride (MCT), long chain triglyceride (LCT), and a reference formulation containing propylene glycol (PG) was studied in vivo in rats."( Bioavailability of seocalcitol I: Relating solubility in biorelevant media with oral bioavailability in rats--effect of medium and long chain triglycerides.
Grove, M; Müllertz, A; Nielsen, JL; Pedersen, GP, 2005
)
0.33
" In this study, we assessed the cutaneous bioavailability of topically applied maxacalcitol ointment in vivo by tape stripping."( In vivo assessment of the cutaneous bioavailability of topically applied maxacalcitol.
Hirata, K; Ikeda, Y; Kano, S; Kondo, K; Takahara, J; Umemura, K; Yanagihara, H, 2005
)
0.33
"Intermittent administration allows substantial dose escalation of calcitriol but limited bioavailability of the commercially available formulations at high doses is limiting."( Pharmacokinetics and tolerability of a single dose of DN-101, a new formulation of calcitriol, in patients with cancer.
Beer, TM; Henner, WD; Javle, M; Lam, GN; Trump, DL; Wong, A, 2005
)
0.79
" Optimal administration of vitamin D analogues is only just being achieved with high-dose intermittent administration overcoming bioavailability and hypercalcemia problems and combination therapy with cytotoxic agents (taxols and cisplatins), antiresorptive agents (bisphosphonates), or cytochrome P450 inhibitors being attempted."( Promise of vitamin D analogues in the treatment of hyperproliferative conditions.
Jones, G; Masuda, S, 2006
)
0.33
" The industrial usefulness of the developed SMEDDS was evaluated with regard to bioavailability and chemical stability using the vitamin D analogue, seocalcitol, as model compound."( Bioavailability of seocalcitol II: development and characterisation of self-microemulsifying drug delivery systems (SMEDDS) for oral administration containing medium and long chain triglycerides.
Grove, M; Müllertz, A; Nielsen, JL; Pedersen, GP, 2006
)
0.33
"The bioavailability of seocalcitol from two lipid-based formulations and a propylene glycol (PG) solution was studied in minipigs in the fasted and fed state."( Bioavailability of seocalcitol III. Administration of lipid-based formulations to minipigs in the fasted and fed state.
Grove, M; Müllertz, A; Nielsen, JL; Pedersen, GP, 2007
)
0.34
" FLL could enhance the apparent Ca absorption rate and reduce Ca excretion, via its actions on modulating the levels of calciotropic hormones and CaBPs expression."( Improvement of Ca balance by Fructus Ligustri Lucidi extract in aged female rats.
Che, CT; Lai, WP; Leung, PC; Wong, MS; Zhang, Y, 2008
)
0.35
"FLL significantly reduced fecal Ca excretion and induced apparent Ca absorption rate in rats fed with MCD and HCD."( Improvement of Ca balance by Fructus Ligustri Lucidi extract in aged female rats.
Che, CT; Lai, WP; Leung, PC; Wong, MS; Zhang, Y, 2008
)
0.35
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
" To predict the clinical efficacy of the lotion, we investigated the cutaneous bioavailability of topically applied lotion and compared this with that of its ointment formulation in healthy subjects."( Cutaneous pharmacokinetics of topically applied maxacalcitol ointment and lotion.
Amagishi, H; Hirata, K; Ikeda, Y; Ishihama, Y; Kondo, K; Tokura, Y; Umemura, K, 2008
)
0.35
"In conclusion, we observed that assessment of cutaneous bioavailability by using tape stripping was reproducible."( Cutaneous pharmacokinetics of topically applied maxacalcitol ointment and lotion.
Amagishi, H; Hirata, K; Ikeda, Y; Ishihama, Y; Kondo, K; Tokura, Y; Umemura, K, 2008
)
0.35
" Our results imply that coingestion of IMA-contaminated food and CYP3A4- or CYP1A1-metabolizable drugs or chemicals could lead to drug bioavailability modulation or toxicological interactions, with possible adverse effects for human health."( CYP1A1 induction and CYP3A4 inhibition by the fungicide imazalil in the human intestinal Caco-2 cells-comparison with other conazole pesticides.
Dupont, I; Jassogne, C; Larondelle, Y; McAlister, D; Muller, M; Pussemier, L; Ribonnet, L; Schneider, YJ; Scippo, ML; Sergent, T; van der Heiden, E, 2009
)
0.35
" In this study, we investigated the methylation status of genes regulating vitamin D bioavailability and activity in the placenta."( Placenta-specific methylation of the vitamin D 24-hydroxylase gene: implications for feedback autoregulation of active vitamin D levels at the fetomaternal interface.
Beck, S; Craig, JM; Dimitriadis, E; Down, T; Evain-Brion, D; Fournier, T; Manuelpillai, U; Morley, R; Ng, HK; Novakovic, B; Rakyan, V; Saffery, R; Sibson, M, 2009
)
0.35
" In vivo, these effects could result in reduced activation of procarcinogens and/or in drug bioavailability limitation."( CYP1A1 and CYP3A4 modulation by dietary flavonoids in human intestinal Caco-2 cells.
Dupont, I; Larondelle, Y; Pussemier, L; Schneider, YJ; Scippo, ML; Sergent, T; Van der Heiden, E, 2009
)
0.35
" This study evaluated the bioavailability of DN101, a concentrated oral calcitriol formulation specifically developed for anticancer applications."( Oral bioavailability of DN101, a concentrated formulation of calcitriol, in tumor-bearing dogs.
Bailey, DB; Johnson, CS; Muindi, JR; Rassnick, KM; Trump, DL, 2011
)
0.84
" Calcitriol oral bioavailability was highly variable among dogs (mean ± SEM, 71 ± 12."( Oral bioavailability of DN101, a concentrated formulation of calcitriol, in tumor-bearing dogs.
Bailey, DB; Johnson, CS; Muindi, JR; Rassnick, KM; Trump, DL, 2011
)
1.52
"This study demonstrates that a high-dose formulation of calcitriol has a moderate bioavailability in dogs, but inter-individual variability in PK parameters is similar to that observed in people."( Oral bioavailability of DN101, a concentrated formulation of calcitriol, in tumor-bearing dogs.
Bailey, DB; Johnson, CS; Muindi, JR; Rassnick, KM; Trump, DL, 2011
)
0.86
" We investigated the effects of lanthanum carbonate and sevelamer carbonate on the bioavailability of oral calcitriol."( The effect of sevelamer carbonate and lanthanum carbonate on the pharmacokinetics of oral calcitriol.
Hossack, S; Martin, P; Pierce, D; Poole, L; Robinson, A; Smyth, M; Van Heusen, H, 2011
)
0.8
"02 × 10(-6)cm/s, thus ruling out the role of efflux pathways in poor oral bioavailability of curcumin."( Identification of permeability-related hurdles in oral delivery of curcumin using the Caco-2 cell model.
Bansal, AK; Pawar, YB; Wahlang, B, 2011
)
0.37
"Vitamin D binding protein (DBP) plays a key role in the bioavailability of active 1,25-dihydroxyvitamin D (1,25(OH)(2)D) and its precursor 25-hydroxyvitamin D (25OHD), but accurate analysis of DBP-bound and free 25OHD and 1,25(OH)(2)D is difficult."( Vitamin D binding protein and monocyte response to 25-hydroxyvitamin D and 1,25-dihydroxyvitamin D: analysis by mathematical modeling.
Adams, JS; Chun, RF; Hewison, M; Peercy, BE, 2012
)
0.38
" Hepatic biotransformation of 1α,25(OH)(2)D(3) by cytochrome P450 (P450) enzymes could be an important determinant of bioavailability in serum and tissues."( Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
Adomat, H; Deb, S; Guns, ES; Pandey, M, 2012
)
0.38
"Soy increases the bioavailability of endogenous and administered calcitriol, thereby enhancing its anticancer effects and risk of hypercalcemia."( Combination of calcitriol and dietary soy exhibits enhanced anticancer activity and increased hypercalcemic toxicity in a mouse xenograft model of prostate cancer.
Feldman, D; Krishnan, AV; Swami, S; Wang, JY, 2012
)
0.97
" The current data highlight the potential application of VDR-based treatment regimes as a means to limit the bioavailability of growth-promoting androgens within the tumor microenvironment."( Regulation of CYP3A4 and CYP3A5 expression and modulation of "intracrine" metabolism of androgens in prostate cells by liganded vitamin D receptor.
Campbell, MJ; Doherty, D; Maguire, O; Martin, P; McClean, S; Owen, A; Pollock, C; Smyth, T; Thompson, P, 2012
)
0.38
" Since astemizole improves calcitriol bioavailability and activity, decreased calcitriol dosing is advised for conjoint administration."( Astemizole synergizes calcitriol antiproliferative activity by inhibiting CYP24A1 and upregulating VDR: a novel approach for breast cancer therapy.
Avila, E; Barrera, D; Camacho, J; Díaz, L; Gamboa-Domínguez, A; García-Becerra, R; García-Quiroz, J; Halhali, A; Larrea, F; Medina-Franco, H; Ordaz-Rosado, D; Rivas-Suárez, M; Rodríguez, P; Santos, N, 2012
)
0.99
" The over expression of CYP24A1 in cancer cells may be a factor affecting 1,25(OH)2D3 bioavailability and anti-proliferative activity pre-clinically and clinically."( 24-Hydroxylase in cancer: impact on vitamin D-based anticancer therapeutics.
Hershberger, PA; Johnson, CS; Luo, W; Trump, DL, 2013
)
0.39
"Insulin-like growth factor (IGF) binding protein-3 (IGFBP-3) is a secreted glycoprotein that reduces the bioavailability of IGFs."( Insulin-like growth factor binding protein-3 modulates osteoblast differentiation via interaction with vitamin D receptor.
Fu, S; Jin, D; Lei, L; Li, J; Mei, G; Wang, G; Yu, B; Zhou, J, 2013
)
0.39
" The results suggested a 1,25(OH)2D3 bioavailability of approximately 15%."( The efficacy of a standardised product from dried leaves of Solanum glaucophyllum as source of 1,25-dihydroxycholecalciferol for poultry.
Autzen, S; Bachmann, H; Frey, U; McCormack, H; Rambeck, W; Wehr, U; Whitehead, CC, 2013
)
0.39
" Here, we report that VDR mutant mice are characterized by lower bioavailability of the vasodilator nitric oxide (NO) due to reduced expression of the key NO synthesizing enzyme, endothelial NO synthase, leading to endothelial dysfunction, increased arterial stiffness, increased aortic impedance, structural remodeling of the aorta, and impaired systolic and diastolic heart function at later ages, independent of changes in the renin-angiotensin system."( Vitamin D is a regulator of endothelial nitric oxide synthase and arterial stiffness in mice.
Ambrisko, TD; Andrukhova, O; Erben, RG; Heppelmann, MS; Kuebler, WM; Markovic, M; Riesen, SC; Slavic, S; Zeitz, U, 2014
)
0.4
" Hepatic and intestinal biotransformation of 1α,25(OH)2D3 and modifiers of metabolic capacity could be important determinants of bioavailability in serum and tissues."( Ginsenoside-mediated blockade of 1α,25-dihydroxyvitamin D3 inactivation in human liver and intestine in vitro.
Adomat, H; Chin, MY; Deb, S; Guns, ES, 2014
)
0.4
"In the present study, a method was developed for determining the alimentary tract Ca absorption capacity of ruminant animals by measuring the absorption rate of Sr after the administration of an oral dose of strontium chloride acting as a tracer analogue of Ca."( In vivo measurement of the absorption of strontium in the rumen and small intestine of sheep as an index of calcium absorption capacity.
Fraser, DR; Hyde, ML, 2014
)
0.4
"The bioavailability of orally administered therapies are often significantly limited in the human intestine by the metabolic activities of cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp)."( Simultaneous evaluation of human CYP3A4 and ABCB1 induction by reporter assay in LS174T cells, stably expressing their reporter genes.
Inami, K; Kumagai, T; Nagata, K; Sasaki, T, 2015
)
0.42
" Moreover calcitriol strongly synergizes with itraconazole (ITZ) in Smo inhibition, which did not result from elevated calcitriol bioavailability due to ITZ-mediated 24-hydroxylase inhibition but rather from a direct interaction of the compounds at the level of Smo."( A Functional and Putative Physiological Role of Calcitriol in Patched1/Smoothened Interaction.
Adamski, J; Dittmann, K; Hahn, H; Linder, B; Uhmann, A; Weber, S, 2015
)
1.08
" Importantly, the total area under the plasma concentration-time curve from time zero to time infinity (AUC), peak plasma concentration (Cmax) and extent of absolute oral bioavailability (F) of adefovir after oral administration of adefovir dipivoxil were significantly higher in 1,25(OH)2D3-treated rats than in control rats."( Effects of 1α,25-Dihydroxyvitamin D3 on Intestinal Absorption and Disposition of Adefovir Dipivoxil and Its Metabolite, Adefovir, in Rats.
Choi, MK; Kim, SB; Maeng, HJ; Son, JH; Yoon, IS, 2015
)
0.42
" Moreover, the alcohol-free aerosol foam formulation allows a higher penetration of the active ingredients into the skin, resulting in enhanced bioavailability and, consequently, in better clinical outcomes than other products with the same components."( Back to the future: a new topical approach for mild-to-moderate psoriasis.
Calzavara Pinton, P; Cicchetti, A; Cristaudo, A; Girolomoni, G, 2018
)
0.48
" This enhanced penetration improves local bioavailability and, consequently, Cal/BD aerosol foam therapy is associated with improved clinical outcomes if compared with other products with the same components."( Calcipotriene plus betamethasone dipropionate in aerosol foam formulation: will this effective treatment for mild-to-moderate psoriasis change clinical practice?
Giacomelli, L; Giovene, GL, 2018
)
0.48
" Genetic variants of these vitamin D metabolizing genes may alter the bioavailability of\ vitamin D, and hence modulate the risk of breast cancer."( Molecular Mechanism of Cancer Susceptibility Associated with Fok1 Single Nucleotide Polymorphism of VDR in Relation to\ Breast Cancer
Arif, JM; Bhatt, MLB; Dhasmana, A; Lohani, M; Raza, S, 2019
)
0.51
" However, its poor bioavailability restricts its clinical application."( Gemini Curcumin Suppresses Proliferation of Ovarian Cancer OVCAR-3 Cells via Induction of Apoptosis.
Azeez, HJ; Babaei, E; Ghaderi, S; Hussen, BM; Mahdavi, M, 2021
)
0.62
" When applied, Cal/BD foam forms a supersaturated solution on the skin, increasing the penetration and bioavailability of Cal and BD."( Early efficacy and safety data with fixed-dose combination calcipotriol/betamethasone dipropionate foam attributed to mechanism of absorption and steroid potency.
Iversen, L; Koo, J; Tada, Y, 2021
)
0.62

Dosage Studied

Daily and intermittent dosing of calcitriol will decrease plasma parathyroid hormone concentration in normal cats and cats with chronic renal failure without causing ionized hypercalcemia. Initiation of calcium carbonate and Vitamin D3 Tablets, Calcitriol Soft Capsules, and Potassium aspartate and Magnesium Aspartate Tablets were prescribed.

ExcerptRelevanceReference
" Rats dosed with 1 alpha,25-dihydroxy-[3 alpha-3H]vitamin D3 and 1 alpha,25-dihydroxy[26,27-14C]vitamin D3 produced compounds with a high 3H/14C ratio."( Isolation and characterization of 1 alpha-hydroxy-23-carboxytetranorvitamin D: a major metabolite of 1,25-dihydroxyvitamin D3.
DeLuca, HF; Esvelt, RP; Schnoes, HK, 1979
)
0.26
" The rather weak effect of 3 on serum calcium levels in normal mice at a dosage of 500 micrograms/kg (intravenous administration) indicates that the essential importance of the 21-methyl moiety may lie in its effect on the regulation of calcium metabolism."( Synthetic studies of vitamin D analogues. X. Synthesis and biological activities of 1 alpha,25-dihydroxy-21-norvitamin D3.
Kawanishi, T; Kubodera, N; Matsumoto, M; Miyamoto, K; Mori, T; Ohkawa, H, 1992
)
0.28
" The sCT dose-response curves showed a higher cAMP production from 10(-9) M to 10(-7) M of sCT in the presence of 500 pg/ml TGF-beta than in control cultures."( Transforming growth factor-beta enhances calcitonin-induced cyclic AMP production and the number of calcitonin receptors in long-term cultures of human umbilical cord blood monocytes in the presence of 1,25-dihydroxycholecalciferol.
Bouizar, Z; De Vernejoul, MC; Jullienne, A; Mbalaviele, G; Orcel, P, 1992
)
0.28
" The results suggest that wide spacing of oral 'pulse' doses of calcitriol can achieve favourable modification of the PTH/iCa relationship, and that dosing interval and dose size, rather than route of administration, may be the major determinants of the previously reported superiority of intravenous over daily oral calcitriol regimens."( 'Pulse' oral calcitriol in uraemic patients: rapid modification of parathyroid response to calcium.
Almond, MK; Beer, JC; Cunningham, J; Evans, SJ; Kwan, JT; Noonan, K, 1992
)
0.89
"3 mM NaB, the dosage of F6-1,25-(OH)2D3 required to inhibit cell growth and colony formation and to induce cell differentiation was significantly reduced."( Effect of hexafluoro-1,25-dihydroxyvitamin D3 and sodium butyrate combination on differentiation and proliferation of HL-60 leukemia cells.
Eguchi, T; Ikekawa, N; Saijo, N; Tanaka, Y; Yoshida, M,
)
0.13
" Dose-response curves indicated that at physiological concentrations (10(-9) M) 1 alpha,25(OH)2D3 was mitogenic, whereas at higher concentrations (10(-8) M) it promotes differentiation."( The human prostatic carcinoma cell line LNCaP expresses biologically active, specific receptors for 1 alpha,25-dihydroxyvitamin D3.
Ferrara, JA; Hedlund, TE; Lucia, MS; Miller, GJ; Pfister, S; Stapleton, GE; Upadhya, P, 1992
)
0.28
" Dynamic tests of parathyroid function by EDTA infusion and an oral calcium load revealed a sigmoidal relationship between serum PTH and calcium levels, and that parathyroid surgery induced considerable changes in both the position and slope of the dose-response curve."( Dynamics of parathyroid hormone release and serum calcium regulation after surgery for primary hyperparathyroidism.
Akerström, G; Graf, W; Ljunghall, S; Rastad, J; Wide, L,
)
0.13
" The observation that heterozygous girls appear to respond better than hemizygous boys to calcitriol and Pi therapy provides evidence for a gene dosage effect in the expression of this X-linked dominant disorder."( X-linked hypophosphatemic rickets: a study (with literature review) of linear growth response to calcitriol and phosphate therapy.
Boniface, AM; Petersen, DJ; Rupich, RC; Schranck, FW; Whyte, MP, 1992
)
0.72
"We measured changes in serum insulin-like growth factor-1 (IGF-1), calcitriol, parathyroid hormone (PTH), thyroid hormones, insulin, and plasma glucagon in response to seven days of treatment with a pharmacological dosage of recombinant human growth hormone (r-hGH) (0."( Effects of short-term growth hormone treatment on PTH, calcitriol, thyroid hormones, insulin and glucagon.
Bouillon, R; Brixen, K; Flyvbjerg, A; Mosekilde, L; Nielsen, HK, 1992
)
0.77
"We have determined the dose-response of 1,25-dihydroxyvitamin D-3 (1,25-(OH)2D3) on the intracellular free calcium-ion concentration ([Ca2+]i) in the osteoblastic osteosarcoma cells, ROS 17/2."( Lead inhibits 1,25-dihydroxyvitamin D-3 regulation of calcium metabolism in osteoblastic osteosarcoma cells (ROS 17/2.8).
Gupta, RK; Rosen, JF; Schanne, FA, 1992
)
0.28
" At the high infusion rate, treatment was discontinued after 1-2 days of dosing due to pronounced adverse clinical signs such as extensive vomitings, apathy, ataxia, and muscle spasms."( Hypocalcemia induced by foscarnet (Foscavir) infusion in dogs.
Lundström, J; Nordgren, T; Ryrfeldt, A, 1992
)
0.28
" Dose-response studies of vitamin D3 derivatives showed that 1 alpha,25(OH)2D3 was the most potent in inhibiting neutral lipid synthesis in PA6 cells, followed by 1 alpha-hydroxyvitamin D3, 25-hydroxyvitamin D3, and 24R,25-dihydroxyvitamin D3, in that order."( 1 alpha,25-dihydroxyvitamin D3 modulation in lipid metabolism in established bone marrow-derived stromal cells, MC3T3-G2/PA6.
Hasegawa, K; Shinki, T; Shionome, M; Suda, T; Takahashi, N, 1992
)
0.28
" In contrast to conventional dosing regimens, low-dose IV therapy does not necessitate the use of aluminum-containing phosphate binders and/or a low-calcium dialysate bath."( Safety and efficacy of long-term treatment of secondary hyperparathyroidism by low-dose intravenous calcitriol.
Moe, SM; Sprague, SM, 1992
)
0.5
" The author concludes the following: (1) some hypoparathyroid women show a significant and symptomatic decline in serum calcium at the time of menses; (2) serum calcium values obtained at the time of menses may not be a reliable guide to adjusting medication dosage for hypoparathyroidism; and (3) further investigation will be needed to determine the mechanism of the decline in serum calcium values and whether the effect of estrogens on serum calcitriol might be altered in the absence of the parathyroid glands."( Case report: hypoparathyroidism with menses-associated hypocalcemia.
Mallette, LE, 1992
)
0.45
" We also determined the severity of nephrocalcinosis (on a scale of 0 to 4, with 0 indicating no abnormalities and 4 stone formation) with renal ultrasonography and whether it could be related to the dosage of phosphate or vitamin D or to other factors."( Effects of therapy in X-linked hypophosphatemic rickets.
Cowell, CT; Howard, NJ; Lam, A; Silink, M; Simpson, JM; Verge, CF, 1991
)
0.28
" The dose-response relation was studied at 6h."( [In vitro effects of 1,25-dihydroxycholecalciferol on alkaline phosphatase and gamma-glutamyltransferase activity in hypophysectomized rats].
Do, TX; Girault, A; Planchenault, P; Prelot, M, 1990
)
0.28
" A dose-response study showed that with 24 h preincubation, 5, 3, and 1 microgram/ml of GN inhibited 81, 62, and 0% of PTH-induced calcium release."( Gallium nitrate inhibits bone resorption and collagen synthesis in neonatal mouse calvariae.
Lakatos, P; Mong, S; Stern, PH, 1991
)
0.28
" There was a gradual reduction of ANF release as the dosage of calcitriol increased from 1 ng to 10 ng."( The effect of calcitriol on atrial natriuretic factor release from isolated atrium.
Halabe, A; Sutton, RA; Wong, EF; Wong, NL, 1991
)
0.88
" Serum from MC903 or 1,25(OH)2D3 dosed rats (i."( Calcipotriol (MC 903): pharmacokinetics in rats and biological activities of metabolites. A comparative study with 1,25(OH)2D3.
Binderup, L; Kissmeyer, AM, 1991
)
0.28
"3 nM 1,25(OH)2D3, a 60-fold higher dosage than was required for the half maximal stimulation of BGP synthesis in these cells."( Induction of matrix Gla protein synthesis during prolonged 1,25-dihydroxyvitamin D3 treatment of osteosarcoma cells.
Fraser, JD; Price, PA, 1990
)
0.28
" In Exp I, a high dosage of 1,25 (OH)2D3 raised the hCa level to over 8 mg/dl within 12 hours; formation of a new mineralizing front and remineralization of the dentin were observed."( [Appositional rate of incisor dentin and hematic calcium level in rats. Application of time marking method using lead acetate].
Matsumoto, S, 1990
)
0.28
" Any dosage modifications that may need to be made rely totally on established communication between the centers, the DCC, and the Core Pharmacy."( Masking procedure, randomization and stratification, and compliance monitoring in the Growth Failure in Children with Renal Diseases Study.
Boyle, RM; Chan, JC; Coppedge, SH; Shasky, DA, 1990
)
0.28
" An increase in reactivity occurred as early as 10 min after dosing of the chicks with 1,25(OH)2D3."( Reactivity of sulfhydryl groups in the brush-border membranes of chick duodena is increased by 1,25-dihydroxycholecalciferol.
Mykkanen, HM; Wasserman, RH, 1990
)
0.28
" True absorption was calculated after dosing cows intravenously with 45Ca and 32P to measure endogenous fecal losses."( True absorption of calcium and phosphorus from alfalfa and corn silage when fed to lactating cows.
Belo, AT; Belyea, RL; Goff, JP; Martz, FA; Weiss, MF, 1990
)
0.28
" Mitochondria isolated from skeletal muscle of vitamin D-deficient chicks and chicks dosed with 1,25(OH)2D3 for 3 or 7 days (50 ng/day) were employed."( In vitro calcium transport properties of skeletal muscle mitochondria from vitamin D-deficient and 1,25-dihydroxy-vitamin D3-treated chicks.
Boland, RL; Selles, J, 1990
)
0.28
"We treated a hypoparathyroid woman with calcitriol during pregnancy and did not reduce the dosage after delivery."( Hypercalcemia in a calcitriol-treated hypoparathyroid woman during lactation.
Beguin, EA; Caplan, RH, 1990
)
0.88
" We found that the maturational effects of the lymphokine or 1,25[OH]2D3 were accompanied by a marked reduction in the PGE2-induced increase in cellular content of adenosine 3':5'-cyclic monophosphate (cAMP) and a shift in the dose-response curve consistent with a decrease in PGE2 receptor number or binding affinity."( The adenosine 3':5'-cyclic monophosphate response to prostaglandin E2 is altered in U937 cells in association with maturational events induced by activated T lymphocytes and 1,25-dihydroxyvitamin D3.
Amento, EP; Goldring, SR; Krane, SM; Roelke, MS, 1986
)
0.27
" These observations suggest that the culture density and dose-response relationship must be carefully defined in in vitro studies utilizing osteogenic cell culture systems."( Cell density-dependent vitamin D effects on calcium accumulation in rat osteogenic sarcoma cells (ROS 17/2).
Avioli, LV; Birge, SJ; Kim, YS; Miller, R, 1987
)
0.27
" Pretreatment of ROS cells for 2 days with the glucocorticoid triamcinolone acetonide (TRM), shifted the dose-response curve for PKA activation by PTH upward compared to the control value."( Glucocorticoids and 1,25-dihydroxyvitamin D3 regulate parathyroid hormone stimulation of adenosine 3',5'-monophosphate-dependent protein kinase in rat osteosarcoma cells.
Catherwood, BD; Lorang, MT; Rubin, JE; Titus, L, 1988
)
0.27
" The initial dosage was 300 mg intravenously daily."( Treatment of tumor hypercalcemia with clodronate.
Scharla, SH; Ziegler, R, 1989
)
0.28
"In order to further test the validity of the vesicular transport model of 1,25-dihydroxyvitamin D3 (1,25(OH)2D3)-stimulated intestinal calcium absorption, dose-response studies were undertaken."( 1,25-Dihydroxyvitamin D3-mediated vesicular calcium transport in intestine: dose-response studies.
Nemere, I; Norman, AW, 1989
)
0.28
" In contrast to previous studies, the present investigation does not provide evidence of clinical efficacy for the drug at that dosage and with the vehicle that was used."( A double-blind study of topical 1 alpha,25-dihydroxyvitamin D3 in psoriasis.
Czarnetzki, BM; van Bokhoven, M; van de Kerkhof, PC; Zultak, M, 1989
)
0.28
" The serum calcitriol levels initially rose markedly in all experimental rabbits in proportion to infused dosage and peaked at 3 days."( Serum calcitriol and parathyroid hormone levels following prolonged infusion of calcitriol in vitamin D replete and depleted rabbits.
Long, JF; Nagode, LA; Steinmeyer, CL; Thornton, DJ, 1989
)
1.15
" Because CsA has a dose-related systemic toxicity, there is a need for approaches by which the dosage of CsA could be reduced while maintaining the required immunosuppression."( Potentiation of immunosuppressive effects of cyclosporin A by 1 alpha,25-dihydroxyvitamin D3.
Fass, D; Gupta, S; Shimizu, M; Vayuvegula, B, 1989
)
0.28
" However, calcitriol was 5-fold more potent for HL-60 cells cultured in SFM than those cultured in 10% SCM as indicated by shifts in dose-response curves for induction of CL responsiveness and lysozyme activity."( Induction of monocytic differentiation by calcitriol (1,25-dihydroxyvitamin D3) in the human promyelocytic leukemic cell line (HL-60) in serum-free medium.
Dunlap, BE; Lee, Y; Mellon, WS, 1987
)
0.94
" The dose-response curve was bell-shaped, and at 10(-6) M 1,25-(OH)2D3 even suppressed PRL production to about 75% of controls."( A permissive role for extracellular Ca2+ in regulation of prolactin production by 1,25-dihydroxyvitamin D3 in GH3 pituitary cells.
Bjøro, T; Gautvik, KM; Haug, E, 1987
)
0.27
" Only the daily dosage of 250,000 IU caused significant increases of concentrations of vitamin D or 25-hydroxyvitamin D in plasma."( Effects of dietary vitamin D3 on concentrations of vitamin D and its metabolites in blood plasma and milk of dairy cows.
Beitz, DC; Horst, RL; Littledike, ET; McDermott, CM, 1985
)
0.27
" Each action exhibited a different dose-response pattern, implying that different levels of control are required for each individual response."( The effects of 1,25-dihydroxyvitamin D3 and dexamethasone on rat osteoblast-like primary cell cultures: receptor occupancy and functional expression patterns for three different bioresponses.
Cabrales, S; Chen, TL; Feldman, D; Hauschka, PV, 1986
)
0.27
" The effect of vitamin D metabolites was estimated on 3 experimental animals applying a daily dosage of 600."( [Effect of bile on intestinal calcium and vitamin D absorption. Animal experiment studies in swine].
Braun, F, 1986
)
0.27
" The dose-response curve was biphasic for all compounds studied; for 1,25(OH)2D3 initial stimulation of transport was detected at only 30 pM [the plasma concentration of 1,25(OH)2D3 is normally 125 pM] while maximal stimulation was 154% above control at a concentration of 650 pM."( Biological activity of vitamin D metabolites and analogs: dose-response study of 45Ca transport in an isolated chick duodenum perfusion system.
Norman, AW; Yoshimoto, Y, 1986
)
0.27
" The dose-response profiles for two additional bioresponses in these cells, namely induction of 24-hydroxylase and inhibition of 1 alpha-hydroxylase activity, were comparable to those for CaBP induction."( 1,25-Dihydroxyvitamin D3 induces the synthesis of vitamin D-dependent calcium-binding protein in cultured chick kidney cells.
Clemens, TL; Craviso, GL; Garrett, KP, 1987
)
0.27
" When the chicks were dosed with [3H]calcitriol, significantly lower concentrations of the sterol were detected in the duodena of EHDP-treated birds."( The effect of disodium ethane-1-hydroxy-1,1-diphosphonate on the metabolism of calcitriol in chicks.
Edelstein, S; Lidor, C; Meyer, MS; Wasserman, RH, 1987
)
0.77
" Time-course and dose-response evaluations of the 1,25-(OH)2D3 effect revealed that the decrease in [14C]choline incorporation was seen within 12 h of incubation and occurred with as little as 10(-9) M, respectively."( Effect of 1,25-dihydroxyvitamin D3 on phospholipid metabolism in cultured bovine parathyroid cells.
Morrissey, J; Ritter, C; Slatopolsky, E; Sugimoto, T, 1988
)
0.27
" Serum calcium and ionized calcium concentrations increased in the treatment group, and the calcitriol dosage had to be reduced in 8 patients at least once because of hypercalcemia."( Low dose calcitriol versus placebo in patients with predialysis chronic renal failure.
Dahl, E; Nordal, KP, 1988
)
0.91
" While T3 alone had no effect on calcium uptake by gut segments cultured on d 20 of embryonic development, the thyroid hormone amplified the effect of 1,25-(OH)2D3 on calcium transport and effectively shifted the dose-response curve to lower 1,25-(OH)2D3 concentrations."( Calcium and inorganic phosphate transport in embryonic chick intestine: triiodothyronine enhances the genomic action of 1,25-dihydroxycholecalciferol.
Cross, HS; Peterlik, M, 1988
)
0.27
" The maximum concentration of calbindin and its mRNA found after dosing vitamin D-deficient chicks with dihydroxyvitamin D3 (1,25-(OH)2D3) is less than 5% of that found with vitamin D dosing."( Relationship between the levels of calbindin synthesis and calbindin mRNA in chick intestine. Quantitation of calbindin mRNA.
Lane, SM; Lawson, DE; Mayel-Afshar, S, 1988
)
0.27
" The 2-fold purpose of this study was 1) to develop a practical method for quantitating DHT2 after oral dosing in normal subjects, and 2) to assess changes in serum DHT2 levels and calcium and phosphorus metabolism after DHT2 administration for 8 days."( Serum dihydrotachysterol levels and biological action in normal man.
Bikle, DD; Norman, ME; Taylor, A, 1988
)
0.27
"25-dihydroxyvitamin-D3 at dosage of 16."( [Effect of treatment with 1,25-dihydroxyvitamin D3 in children with chronic renal insufficiency].
Crespo Hernández, M; del Molino Anta, A; Málaga Guerrero, S; Rey Galaán, C; Riaño Galán, I; Santos Rodríguez, F, 1987
)
0.27
" For each stimulator tested, the dose-response relationships for the stimulation of resorption and the inhibition of collagen synthesis were found to coincide."( Simultaneous measurement of bone resorption and collagen synthesis in neonatal mouse calvaria.
Hefley, TJ; Krieger, NS; Stern, PH, 1986
)
0.27
" When HT-39 cells were grown in medium containing different calcium levels and dosed with 10 nM 1,25-(OH)2D3, we found that the inhibitory action of 1,25-(OH)2D3 was modified."( Calcium antagonizes 1,25-dihydroxyvitamin D3 inhibition of breast cancer cell proliferation.
Arnold, AJ; Simpson, RU, 1986
)
0.27
" Treatment at this dosage could be made in the early stages of predialysis CRF without need of close and continuous monitoring of serum biochemical parameters."( Treatment of secondary hyperparathyroidism of predialysis chronic renal failure with low doses of 1,25(OH)2D3: humoral and histomorphometric results.
Ballanti, P; Bonucci, E; Cinotti, GA; Coen, G; Della Rocca, C; Donato, G; Landi, A; Massimetti, C; Mazzaferro, S; Smacchi, A, 1986
)
0.27
" This reduction of 1,25-dihydroxyvitamin D was dependent on the dose of 25,26-dihydroxyvitamin D3 administered since a 5 micrograms/day dosing regimen failed to alter serum 1,25-dihydroxyvitamin D levels."( Administration of pharmacological amounts of 25(s),26-dihydroxyvitamin D3 reduces serum 1,25-dihydroxyvitamin D3 levels in rats.
Harvey, JA; Pak, CY; Zerwekh, JE, 1987
)
0.27
" The effects of increases of calcitriol dosage and modifications of calciuria with hydrochlorothiazide were systematically examined."( Hypercalciuria associated with long-term administration of calcitriol (1,25-dihydroxyvitamin D3). Action of hydrochlorothiazide.
Chan, JC; Santos, F; Smith, MJ, 1986
)
0.81
" Due to the wider therapeutic dosage range, this compound might be of clinical value."( Biological activity of fluorine-substituted 1,25-dihydroxyvitamin D3 in rats, in chicken and in Japanese quails.
Rambeck, WA; Weiser, H; Zucker, H, 1986
)
0.27
"5 nM 1,25-(OH)2D3, progressive inhibition of Ca transport was observed, yielding a biphasic dose-response curve."( Hypercalcemia inhibits the rapid stimulatory effect on calcium transport in perfused duodena from normal chicks mediated in vitro by 1,25-dihydroxyvitamin D3.
Nemere, I; Norman, AW; Yoshimoto, Y, 1986
)
0.27
" 24,25-Dihydroxycholecalciferol and 25-hydroxycholecalciferol (25(OH)D3) also stimulated transfer, although dose-response curves were less effective than for 1,25(OH)2D3."( Vitamin D metabolites stimulate phosphatidylcholine transfer to renal brush-border membranes.
Hagerty, D; Hruska, KA; Huskey, M; Kurnik, BR, 1986
)
0.27
" We studied the efficacy of chloroquine in two patients with sarcoidosis who were unable to tolerate the dosage of corticosteroids required to control hypercalciuria and prevent the formation of renal stones."( The effects of chloroquine on serum 1,25-dihydroxyvitamin D and calcium metabolism in sarcoidosis.
Cohanim, M; Jones, G; Lohnes, D; O'Leary, TJ; Yendt, ER; Yip, A, 1986
)
0.27
" Renal function was most severely affected in cows treated with 24,24-F2-dihydroxycholecalciferol and was evident even at the 100-micrograms dosage level."( Bone resorption, renal function and mineral status in cows treated with 1,25-dihydroxycholecalciferol and its 24-fluoro analogues.
Boris, A; Goff, JP; Horst, RL; Littledike, ET; Uskokovic, MR, 1986
)
0.27
"The deleterious effects of corticosteroids (CS) on bone are well known, but probably differ depending on duration and dosage of CS therapy."( Bone metabolism during methylprednisolone pulse therapy in rheumatoid arthritis.
Bijlsma, JW; Duursma, SA; Huber-Bruning, O, 1986
)
0.27
" Blunted calciuric response to low doses of calcitriol is compatible with an altered dose-response relationship."( Calciuric response to 1,25-(OH)2D3 in early renal failure.
Cremer, B; Klooker, P; Lübbers, E; Ritz, E; Schmidt-Gayk, H, 1985
)
0.53
" The Mi AR evaluated by double tetracycline labeling was enhanced at all dosage levels."( Contrasting effects of 1,25-dihydroxyvitamin D3 on bone matrix and mineral appositional rates in the mouse.
Garba, MT; Hott, M; Marie, PJ, 1985
)
0.27
"5 mg/day of prednisolone on the amount of calcium deposited in the kidney of rats dosed with either 500 ng/d or 2000 ng/day of 1-alpha OHD2 or 1-alpha OHD3."( The effect of prednisolone on kidney calcification in vitamin D-treated rats.
Lindgren, U; Sjöden, G, 1985
)
0.27
" Using labeled material it was shown that the dosing levels of 1,25(OH)2D3 employed ensured a higher than normal plasma concentration of that metabolite over the period between doses."( Histological observations on the failure of rachitic rat bones to respond to 1,25/OH)2D3.
Gallagher, JA; Lawson, DE, 1980
)
0.26
" A dose-response study after intramuscular 1,25(OH)(2)D(3) injection yielded a hyperbolic curve with an apparent plateau at 70% receptor occupancy, corresponding to 5 nmol 1,25(OH)(2)D(3) injected."( Effect of vitamin D status on the equilibrium between occupied and unoccupied 1,25-dihydroxyvitamin D intestinal receptors in the chick.
Bishop, JE; Hunziker, W; Norman, AW; Walters, MR, 1982
)
0.26
" 24-Keto-1,25-dihydroxyvitamin D3 is present in vivo in the plasma and small intestinal mucosa of rats fed a stock diet, receiving no exogenous 1,25-dihydroxyvitamin D3, and in the plasma and small intestinal mucosa of rats dosed chronically with 1,25-dihydroxyvitamin D3."( Intestinal synthesis of 24-keto-1,25-dihydroxyvitamin D3. A metabolite formed in vivo with high affinity for the vitamin D cytosolic receptor.
Horst, RL; Napoli, JL; Pramanik, BC; Reinhardt, TA; Royal, PM, 1983
)
0.27
" However, IFN-gamma dose-response studies using both HL-60 cells and a nondifferentiation variant of HL-60 cells (HL-60 blast) clearly show that induction of transcription and expression of HLA-D gene products by IFN-gamma can be uncoupled from expression of other monocyte-macrophage characteristics."( Gamma-interferon induces expression of the HLA-D antigens on normal and leukemic human myeloid cells.
Billing, R; Bohman, R; Koeffler, HP; Ranyard, J; Yelton, L, 1984
)
0.27
" A dose-response inhibition of the response of serum 25-OHD to vitamin D by 1,25(OH)2D3 was demonstrated in two of the normal subjects."( Evidence that 1,25-dihydroxyvitamin D3 inhibits the hepatic production of 25-hydroxyvitamin D in man.
Bell, NH; Shaw, S; Turner, RT, 1984
)
0.27
" Calcium transport rates could be partially restored by in vivo administration of 1,25-dihydroxyvitamin D-3 at a dosage which did not affect vesicular calcium uptake in control animals."( Calcium and glucose uptake in rat small intestinal brush-border membrane vesicles. Modulation by exogenous hypercortisolism and 1,25-dihydroxyvitamin D-3.
Birkenhäger, JC; Braun, HJ; De Jonge, HR, 1984
)
0.27
" A similar profile of metabolites was observed on high-pressure-liquid-chromatographic analysis of an extract from the kidneys of rats dosed intravenously with 1,25-dihydroxy[3H]cholecalciferol."( Production of C-24- and C-23-oxidized metabolites of 1,25-dihydroxycholecalciferol by cultured kidney cells (LLC PK1) and their presence in kidney in vivo.
Martin, CA; Napoli, JL, 1984
)
0.27
" (23S)-1,23,25-Trihydroxyvitamin D3 had no intestinal calcium absorptive or bone calcium resorptive activity when dosed to vitamin D deficient rats at levels up to 500 ng."( (23S)-1,23,25-Trihydroxyvitamin D3: its biologic activity and role in 1 alpha,25-dihydroxyvitamin D3 26,23-lactone biosynthesis.
Baggiolini, EG; Engstrom, GW; Horst, RL; Napoli, JL; Uskoković, MR; Wovkulich, PM, 1984
)
0.27
"24-Keto-1,23,25-trihydroxyvitamin D3 has been identified as a major 1,25-dihydroxyvitamin D3 metabolite, produced by intestinal mucosa cells isolated from rats dosed chronically with 1,25-dihydroxyvitamin D3."( C(24)- and C(23)-oxidation, converging pathways of intestinal 1,25-dihydroxyvitamin D3 metabolism: identification of 24-keto-1,23,25-trihydroxyvitamin D3.
Horst, RL; Napoli, JL, 1983
)
0.27
" During treatment with 1,25-dihydroxy vitamin D3 progressive reduction in dosage was required in the majority of patients because of hypercalcaemia, which was rapidly corrected by stopping treatment for a few days."( Long-term effects of 1,25-dihydroxy vitamin D3 and 24,25-dihydroxy vitamin D3 in renal osteodystrophy.
Adami, S; Catto, GR; Edward, N; Fraser, RA; Muirhead, N; O'Riordan, JL; Sandler, LM, 1982
)
0.26
"Six patients with Paget disease of bone were treated with a 6-mo course of disodium-ethane-1-hydroxy-1, 1-diphosphate (EHDP) at a dosage of 5 mg/kg/day (one patient) or 20 mg/kg/day (five patients)."( An apparent 1,25-dihydroxyvitamin D-independent stimulation of intestinal calcium absorption in patients with Paget disease of bone during a short-term diphosphonate therapy.
Norman, DA; Pak, CY; Zerwekh, JE, 1981
)
0.26
"5mM-Ca2+ (food-deprived) for rats dosed with 1,25-dihydroxycholecalciferol."( Oxygen-dependent 1,25-dihydroxycholecalciferol-induced calcium ion transport in rat intestine.
DeLuca, HF; Kabakoff, B; Kendrick, NC, 1981
)
0.26
"6% of 3545 treatment days and was readily controlled by adjusting the dosage of 1,25-(OH)2D3."( X-linked hypophosphatemia: effect of calcitriol on renal handling of phosphate, serum phosphate, and bone mineralization.
Cole, DE; Costa, T; Delvin, EE; Glorieux, FH; Marie, PJ; Nogrady, B; Reade, TM; Scriver, CR, 1981
)
0.54
" Chronic dosing of vitamin D-deficient rats with 1,25-dihydroxyvitamin D3 caused a 4-fold increase in skin 7-dehydrocholesterol content."( 1,25-Dihydroxyvitamin D3 stimulated increase of 7,8-didehydrocholesterol levels in rat skin.
DeLuca, HF; Esvelt, RP; Sar, M; Stumpf, WE; Wichmann, JK; Yoshizawa, S; Zurcher, J, 1980
)
0.26
" With the 1 alpha-hydroxylated derivatives, initial dosage of 2 to 6 micrograms daily was required to achieve optimal healing rates by comparison with other responses."( Calcitriol dosage in osteomalacia, hypoparathyroidism and attempted treatment of myositis ossificans progressiva.
Stamp, TC, 1981
)
1.71
" A single dose of 1,25(OH)2D3 significantly increased calcium transport in the hypophysectomized (Hx) rats treated with bGH but not in the Hx rats who did not receive bGH, unless the dosage of 2,25(OH)2D3 was increased to 500 p moles."( The relationship of growth hormone to 1,25-dihydroxyvitamin D3 in intestinal calcium transport.
Aloia, JF; Yeh, JK, 1981
)
0.26
" All other medications except vitamin D2 were continued at their pretreatment dosage levels throughout the study."( Effects of 1,25-dihydroxyvitamin-D3 on renal function, mineral balance, and growth in children with severe chronic renal failure.
Chan, JC; Kodroff, MB; Landwehr, DM, 1981
)
0.26
" When chicks, fed a high strontium diet to inhibit endogenous 1,25 (OH)2 vitamin D3 production and intestinal calcium transport, were dosed with the extract or synthetic 1,25 (OH)2D345Ca absorption from the duodenum in vivo was stimulated, whereas vitamin D3 was ineffective."( Evidence for aqueous soluble vitamin D-like substances in the calcinogenic plant, Tristetum flavescens.
Levack, VM; Morris, KM, 1982
)
0.26
" Concomitantly, epiphyseal, endosteal, and periosteal bone mineralization were improved in correlation with both the dosage of 1,25-(OH)2D3 and the serum phosphorus level."( Healing of bone lesions with 1,25-dihydroxyvitamin D3 in the young X-linked hypophosphatemic male mouse.
Glorieux, FH; Marie, PJ; Travers, R, 1982
)
0.26
" The remaining hypocalcemic occurrences responded to an increase in the dosage of 1,25-(OH)2D3."( 1,25-dihydroxyvitamin D3-treated hypoparathyroidism: 35 patients years in 10 children.
DeLuca, HF; Markowitz, ME; Rosen, JF; Smith, C, 1982
)
0.26
" Using a 5-min preincubation and a 15-min incubation, a dose-response curve for 1,25-dihydroxyvitamin D3 shows 6 pmol to be the lowest dose to give a significant response and 60 pmol to be the level at which the maximal response is reached."( 1,25-Dihydroxyvitamin C3-stimulated active uptake of phosphate by rat jejunum.
DeLuca, HF; Kabakoff, B; Kendrick, NC, 1982
)
0.26
" Four- to five-week-old vitamin D-deficient cockerels were dosed intraperitoneally with 1 microgram of 1,25-dihydroxyvitamin D3 [1,25-(OH)2D3] alone 15 hr before sacrifice or in combination with 1, 3, or 5 mg of cortisol 24 and 48 hr before sacrifice."( Decreased intestinal calcium absorption in vivo and normal brush border membrane vesicle calcium uptake in cortisol-treated chickens: evidence for dissociation of calcium absorption from brush border vesicle uptake.
Bollman, S; Kumar, R; Shultz, TD, 1982
)
0.26
" At equimolar dosage 1,25-dihydroxycholecalciferol had a potent stimulatory effect on bone resorption."( Suppressive effects of 24,25-dihydroxycholecalciferol on bone resorption induced by acute bilateral nephrectomy in rats.
Balsan, S; Bourdeau, A; Cournot-Witmer, G; Fischer, JA; Heynen, G; Pavlovitch, JH, 1981
)
0.26
" In conclusion, patients with severe HPTH respond very well to IV calcitriol, provided that dosing of calcitriol is commensurate to PTH levels, and hyperphosphatemia is kept under control."( The importance of dosing intravenous calcitriol in dialysis patients with severe hyperparathyroidism.
Cerezo, S; Hervas, J; Llach, F, 1995
)
0.8
"We report four cases of chronic plaque psoriasis that developed in patients who used UV-B phototherapy for a substantial period without ill effects and in whom photosensitivity reactions within psoriatic plaques developed after calcipotriene ointment was added, without changes in their UV-B dosage or frequency of treatment."( Photosensitivity associated with combined UV-B and calcipotriene therapy.
McKenna, KE; Stern, RS, 1995
)
0.29
" Although initial, uncontrolled clinical trials suggested the superiority of intravenous calcitriol treatment, more recent controlled investigations have shown that different routes (oral versus intravenous), frequency (daily versus intermittent) and dosing (physiologic versus pharmacologic) of calcitriol administration are equivalent."( Oral versus intravenous calcitriol: is the route of administration really important?
Indridason, OS; Quarles, LD, 1995
)
0.82
" During treatment PTH (1-84) normalized with high dosage of calcitriol in spite of low or subnormal levels of serum calcium, and subsequently increased for each reduction of calcitriol dosage despite normal calcium levels."( Direct effect of calcitriol on the regulation of parathyroid hormone secretion in a case of pseudo-hypoparathyroidism (a 24-month follow-up study).
Audran, M; Basle, MF; Bigorgne, JC; Bregeon, C; Giraud, P; Jallet, P; Rohmer, V, 1995
)
0.87
" TPA also shifted the dose-response curve of 1,25-(OH)2D3 to the left, so that 1,25-(OH)2D3 was effective at a concentration as low as 1 nM."( Effects of 1,25-dihydroxyvitamin D3 and phorbol ester on 25-hydroxyvitamin D3 24-hydroxylase cytochrome P450 messenger ribonucleic acid levels in primary cultures of rat renal cells.
Armbrecht, HJ; Boltz, MA; Chen, ML, 1993
)
0.29
" Dose-response studies of Cmpds C, V, HM (10(-7)-10(-11)M) showed that in serumless culture conditions, transactivation of the VDRE-CAT was similar; however, in the presence of serum, Cmpd C at 10(-9)M had 20-fold less activity than analogs V and HM."( Potent vitamin D3 analogs: their abilities to enhance transactivation and to bind to the vitamin D3 response element.
Imai, Y; Koeffler, HP; Pike, JW, 1995
)
0.29
"7 mmol/l, but a decrease in calcitriol dosage resulted in a decrease to within normal limits within one day."( [Calcitriol administration during pregnancy in a partial DiGeorge anomaly].
Dörr, HG; Hensen, J; Höper, K; Kändler, C; Kruse, K; Pavel, M; Wildt, L, 1994
)
1.49
" This dosage made it possible to correct the low calcium concentrations (2."( [Vitamin D and pubertal maturation. Value and tolerance of vitamin D supplementation during the winter season].
Chalas, J; Delaveyne, R; Garabédian, M; Odièvre, M; Rehel, P; Zeghoud, F, 1995
)
0.29
" Dose-response studies showed that KH 1060 was the most potent analogue, because it was able to induce differentiation in all seven breast cancer cell lines (measured by lipid staining) and to suppress more than 50% clonal proliferation (ED50) at 10(-10) M in all cell lines, except MDA-MB-436 and BT-20."( 20-epi-vitamin D3 analogues: a novel class of potent inhibitors of proliferation and inducers of differentiation of human breast cancer cell lines.
Binderup, L; de Vos, S; Elstner, E; Heber, D; Koeffler, HP; Linker-Israeli, M; Said, J; Shintaku, IP; Umiel, T; Uskokovic, M, 1995
)
0.29
" Whereas the dose-response relations for the effects of both compounds on 24-OHase mRNA were similar, OCT was slightly more potent than 1,25(OH)2D3 in stimulating 24-OHase activity in both tissues."( Induction of vitamin D 24-hydroxylase messenger RNA and activity by 22-oxacalcitriol in mouse kidney and duodenum. Possible role in decrease of plasma 1 alpha,25-dihydroxyvitamin D3.
Akeno, N; Horiuchi, N; Kimura, S; Saikatsu, S, 1994
)
0.52
" Active Ca transport was increased in both spontaneously hypertensive rats (SHR) and in normotensive control WKY rats 5 h after calcitriol dosing of either 60 and 600 ng per rat."( Duodenal calcium binding protein and active calcium transport in rats: are they functionally related?
Aymard, P; Banide, H; Chabanis, S; Drüeke, T; Duchambon, P; Hanrotel, C; Kubrusly, M; Lacour, B, 1994
)
0.49
"Twice-daily dosing of calcipotriene was compared with its vehicle, for up to 8 weeks, in a double-blind study of 277 patients at 10 study centers in the United States."( Calcipotriene ointment 0.005% for psoriasis: a safety and efficacy study. Calcipotriene Study Group.
Highton, A; Quell, J, 1995
)
0.29
" Dose-response curves with measurable ranges applicable to biological specimens were obtained for 1 alpha,25-dihydroxyvitamin D3, 1 alpha,25-dihydroxyvitamin D2, (24R)-1 alpha,24,25-trihydroxyvitamin D3, (23S,25R)-1 alpha,25-dihydroxyvitamin D3 26,23-lactone, and 22-oxacalcitriol by the radioimmunoassay system using this improved antibody."( Production of a group-specific antibody to 1 alpha,25-dihydroxyvitamin D and its derivatives having the 1 alpha,3 beta-dihydroxylated A-ring structure.
Kobayashi, N; Shimada, K; Shiomura, K; Tabata, Y; Takagi, K; Takama, A, 1994
)
0.47
"We performed dosing experiments to evaluate the bone mass increasing action of a novel, synthetic vitamin D derivative, 2 beta-(3-hydroxypropoxy)-1 alpha,25(OH)2D3 (ED-71), in normal and estrogen-deficient rats."( A novel synthetic vitamin D analogue, 2 beta-(3-hydroxypropoxy)1 alpha, 25-dihydroxyvitamin D3 (ED-71), increases bone mass by stimulating the bone formation in normal and ovariectomized rats.
Higuchi, Y; Nakamura, T; Nishii, Y; Sato, K; Suzuki, K; Tsurukami, H, 1994
)
0.29
" The effects of exogenous T on suppression of spermatogenesis in 19 healthy men were recently compared, using a T dosage of 200 mg im/week for 20 weeks."( Metabolic and behavioral effects of high-dose, exogenous testosterone in healthy men.
Bagatell, CJ; Bremner, WJ; Heiman, JR; Matsumoto, AM; Rivier, JE, 1994
)
0.29
"0 months of control observations and were randomly assigned to a treatment period; 82 completed the treatment period of at least 6 months while receiving a calcitriol dosage (mean +/- SD) of 17."( A prospective, double-blind study of growth failure in children with chronic renal insufficiency and the effectiveness of treatment with calcitriol versus dihydrotachysterol. The Growth Failure in Children with Renal Diseases Investigators.
Abitbol, CL; Boineau, FG; Chan, JC; Chinchilli, VM; Friedman, AL; Lum, GM; McEnery, PT; Roy, S; Ruley, EJ; Strife, CF, 1994
)
0.69
" The control group received calcium carbonate (maximal dosage of 1 g x 3)."( 24,25-dihydroxy vitamin D3 treatment inhibits parathyroid-stimulated adenylate cyclase in iliac crest biopsies from uremic patients.
Aarseth, HP; Ganss, R; Gautvik, KM; Gordeladze, JO; Haug, E; Mortensen, BM,
)
0.13
" In dose-response experiments, specific [3H]MeTRH binding increased with 1,25-(OH)2D3 concentration and reached a maximum at 10 nmol/l."( 1,25-Dihydroxyvitamin D3-induced upregulation of the thyrotropin-releasing hormone receptor in clonal rat pituitary GH3 cells.
Atley, LM; Lefroy, N; Wark, JD, 1995
)
0.29
" Vascular perfusion with a range of 1,25-(OH)2D3 concentrations yielded an apparent biphasic dose-response curve."( Apparent nonnuclear regulation of intestinal phosphate transport: effects of 1,25-dihydroxyvitamin D3,24,25-dihydroxyvitamin D3, and 25-hydroxyvitamin D3.
Nemere, I, 1996
)
0.29
" No changes in parameters of reproductive performance were seen in any dosed groups."( [Reproductive and developmental toxicity studies of calcipotriol (MC903): (1)--A fertility study in rats by subcutaneous administration].
Koike, Y; Konishi, R; Nagata, M; Ono, M; Shirakawa, K; Suzuki, T; Uchiyama, H, 1996
)
0.29
" After six months the therapy was progressively reduced to physiological dosage with optimal metabolic control."( [Vitamin D-dependent type-1 rickets: diagnosis and treatment of a further case].
Bini, R; Pela, I; Seracini, D,
)
0.13
" However, while the incidence of TD in birds dosed with 1,25(OH)2D3 was lower (10%) than in control chicks (55%), RO 23-7553 was ineffective (50%)."( In vivo and in vitro effect of 1,25-dihydroxyvitamin D3 and 1,25-dihydroxy-16-ene-23-yne-vitamin D3 on the proliferation and differentiation of avian chondrocytes: their role in tibial dyschondroplasia.
Farquharson, C; Loveridge, N; Rennie, JS; Whitehead, CC, 1996
)
0.29
" Although initial uncontrolled clinical trials suggested the superiority of intravenous calcitriol treatment, more recent controlled investigations show that different routes (oral versus intravenous), frequency (daily versus intermittent), and dosing (physiological versus pharmacological) of calcitriol administration are clinically equivalent."( Calcitriol administration in end-stage renal disease: intravenous or oral?
Indridason, OS; Quarles, LD, 1996
)
1.96
" Initiation of calcitriol therapy late in severe HPT and inappropriate dosing of calcitriol are common causes of inadequate use of calcitriol."( Guidelines for dosing of intravenous calcitriol in dialysis patients with hyperparathyroidism.
Fernandez, E; Llach, F, 1996
)
0.92
" The availability of a parenteral formulation of calcitriol, and new information regarding alternative routes of administration and regimens employing oral pulse dosing have renewed interest in calcitriol for the management of uremic secondary HPT."( Calcitriol in the management of secondary hyperparathyroidism of renal failure.
Daisley-Kydd, RE; Mason, NA,
)
1.83
"At predefined dosage schedules, all three compounds significantly decreased plasma immunoreactive PTH levels (except EB1213 at low dose)."( Effects of new vitamin D analogues on parathyroid function in chronically uraemic rats with secondary hyperparathyroidism.
Drüeke, TB; Hruby, M; Lacour, B; Mannstadt, M; Schmitt, F; Ureña, P, 1996
)
0.29
" However, more prolonged administration to uraemic rats of calcitriol analogues with slightly modified dosage schedules and of calcitriol with lower non-hypercalcaemic dose is required for an optimal comparison before considering clinical trials."( Effects of new vitamin D analogues on parathyroid function in chronically uraemic rats with secondary hyperparathyroidism.
Drüeke, TB; Hruby, M; Lacour, B; Mannstadt, M; Schmitt, F; Ureña, P, 1996
)
0.54
" Dose-response curves generated after oral and subcutaneous administration of 1 alpha,24(OH)2D2, calcitriol, and calcipotriol to normal rats indicated that 1 alpha,24(OH)2D2 increases serum and urine calcium to a much lesser extent than calcitriol, and to a slightly greater extent than calcipotriol."( Pharmacokinetics and systemic effect on calcium homeostasis of 1 alpha,24-dihydroxyvitamin D2 in rats. Comparison with 1 alpha,25-dihydroxyvitamin D2, calcitriol, and calcipotriol.
Bishop, CW; Knutson, JC; LeVan, LW; Valliere, CR, 1997
)
0.71
" The purpose of the study was to determine the dose-response effects of olestra on fat-soluble vitamins and selected water-soluble micronutrients."( Olestra dose response on fat-soluble and water-soluble nutrients in the pig.
Berry, DA; Cooper, DA; King, D; Kiorpes, AL; Peters, JC; Spendel, VA, 1997
)
0.3
" A dose-response analysis showed that a 10(-6) M concentration of this vitamin consistently induced a maximal accumulation of 7-fold over the control cells."( Growth inhibition of human breast cancer cells by 1,25-dihydroxyvitamin D3 is accompanied by induction of apolipoprotein D expression.
Alvarez, S; Binderup, L; López-Boado, YS; López-Otín, C; Puente, XS; Tolivia, J, 1997
)
0.3
"Oral pulse dosing of calcitriol has been proposed as an alternative to intravenous administration in the treatment of renal osteodystrophy."( Pulse dose oral calcitriol therapy for renal osteodystrophy: literature review and practice recommendations.
Dahl, NV; Foote, EF, 1997
)
0.96
" These results were achieved by a lower drug dosage of vitamin D3 and at lower trough blood levels of 1,25(OH)2D3 as compared to those of oral One-Alpha."( Comparison of the efficacy of two injectable forms of vitamin D3 and oral one-alpha in treatment of secondary hyperparathyroidism in patients on maintenance hemodialysis.
al-Mohannadi, S; el-Reshaid, K; el-Reshaid, W; Sivanandan, R; Sugathan, T, 1997
)
0.3
" Unfortunately there is no general accepted recommendation for the dosage and intervals of the oral calcitriol pulse therapy."( [Oral calcitriol pulse therapy in hemodialysis patients. Effects on histomorphometry of bone in renal hyperparathyroidism].
Abendroth, K; Humbsch, K; Sperschneider, H, 1997
)
0.99
" [3H]Thymidine incorporation displayed a bell-shaped dose-response curve in both strains."( LNCaP prostatic adenocarcinoma cells derived from low and high passage numbers display divergent responses not only to androgens but also to retinoids.
Esquenet, M; Heyns, W; Swinnen, JV; Verhoeven, G, 1997
)
0.3
" Fibroblast responsiveness to 1,25(OH)2D3, assessed by induction of 24-hydroxylase mRNA, was similar between BB and bb cell types in dose-response experiments."( Vitamin D receptor gene polymorphisms: analysis of ligand binding and hormone responsiveness in cultured skin fibroblasts.
Eccleshall, TR; Feldman, D; Gross, C; Malloy, PJ; Musiol, IM, 1998
)
0.3
" Dose-response studies indicated that the synergistic stimulation of 45Ca release from neonatal mouse calvariae by glucocorticoids and PTH could be elicited at glucocorticoid concentrations of 10(-8) to 10(-6) mol/l and at PTH concentrations of 10(-11) to 10(-9) mol/l."( Differential effects of glucocorticoids on bone resorption in neonatal mouse calvariae stimulated by peptide and steroid-like hormones.
Conaway, HH; Grigorie, D; Lerner, UH, 1997
)
0.3
"These results underline the usefulness of the association of calcipotriol and cyclosporine in order to decrease the total dosage of cyclosporine."( Calcipotriol improves the efficacy of cyclosporine in the treatment of psoriasis vulgaris.
Kokelj, F; Plozzer, C; Torsello, P, 1998
)
0.3
" The objective of this study was to evaluate key measures of calcium metabolism in patients with psoriasis under supervised dosing conditions in a vehicle-controlled study."( Evaluating the safety of calcipotriene 30 g per day in patients with psoriasis: a parallel group, vehicle-controlled study.
Blum, R; Epinette, WW; Schwartzel, E; Siskin, S, 1998
)
0.3
" Dose-response clonogenic studies showed that each of these analogs had more potent antiproliferative activities against the cancer cells than 1,25(OH)2D3, and 1,25-(OH)2-16,23Z-diene-26,27-bishomo-19-nor-D3 (Ro 27-2014) was the most potent analog [10-fold increased activity compared to 1,25(OH)2D3]."( 19-nor-26,27-bishomo-vitamin D3 analogs: a unique class of potent inhibitors of proliferation of prostate, breast, and hematopoietic cancer cells.
Koeffler, HP; Koike, M; Koshizuka, K; Kubota, T; Miyoshi, I; Uskokovic, M, 1998
)
0.3
" The dosage of both drugs was adjusted to maintain the initial serum calcium levels, and the relative change (%change) of serum biochemical parameters were compared."( Controlled trial of falecalcitriol versus alfacalcidol in suppression of parathyroid hormone in hemodialysis patients with secondary hyperparathyroidism.
Akiba, T; Ando, R; Chida, Y; Inoue, A; Ishida, Y; Kurihara, S; Marumo, F; Ohashi, Y; Owada, A; Shinoda, T, 1998
)
0.61
" To assess calcium absorption over a wide physiological range of plasma 1,25(OH)2D, in a dose-response study we altered plasma 1,25(OH)2D by continuous infusion of 1,25(OH)2D (at 0, 4, or 14 ng/100 g BW/day) for 9 days."( Intestinal calcium absorption in the aged rat: evidence of intestinal resistance to 1,25(OH)2 vitamin D.
Bruns, ME; Cashman, K; Deluca, HF; Fleet, JC; Wood, RJ, 1998
)
0.3
" Dose-response curves were non-monotonic passing a maximum at low dosages."( Low-molecular-weight hormonal factors that affect head formation in Hydra.
Bartsch, C; Bartsch, H; Bayer, E; Maidonis, I; Müller, WA, 1998
)
0.3
"We determined the quantitative relationships between graded oral dosing with vitamin D3, 25(OH)D3, and 1,25(OH)2D3 for short treatment periods and changes in circulating levels of these substances."( Vitamin D and its major metabolites: serum levels after graded oral dosing in healthy men.
Barger-Lux, MJ; Chen, TC; Dowell, S; Heaney, RP; Holick, MF, 1998
)
0.3
" In the dosed groups, radioactivity was detected locally in the metaphysis, the modeling site in bones."( Distribution and metabolism of F6-1,25(OH)2 vitamin D3 and 1,25(OH)2 vitamin D3 in the bones of rats dosed with tritium-labeled compounds.
Kanamaru, H; Komuro, S; Nakatsuka, I; Yoshitake, A, 1998
)
0.3
" An increased osteoblast-like cell activity on sintered HA surfaces in the presence of different TGF-beta dosage suggested that sintering of HA surfaces may play an important role in governing cellular response."( Effect of transforming growth factor-beta on osteoblast cells cultured on 3 different hydroxyapatite surfaces.
Carnes, DL; Ong, JL; Sogal, A,
)
0.13
" Under basolateral sink conditions and low apical MDZ dosing concentration (1-8 microM), the first-pass extraction ratio was found to be approximately 15%."( First-pass midazolam metabolism catalyzed by 1alpha,25-dihydroxy vitamin D3-modified Caco-2 cell monolayers.
Calamia, JC; Fisher, JM; Kunze, KL; Schmiedlin-Ren, P; Shen, DD; Thummel, KE; Watkins, PB; Wrighton, SA, 1999
)
0.3
" In experiment 2, a dose-response study of the effects of E2 therapy on calcium absorption in OVX C57BL mice was carried out."( Ovariectomized murine model of postmenopausal calcium malabsorption.
Chen, C; Kalu, DN, 1999
)
0.3
" Compared with the interaction of VDR with RXR or GRIP-1, the differentiation dose-response most closely correlated to the ligand-dependent recruitment of the DRIP coactivator complex to VDR and to the ability of the receptor to activate transcription in a cell-free system."( 20-Epi analogues of 1,25-dihydroxyvitamin D3 are highly potent inducers of DRIP coactivator complex binding to the vitamin D3 receptor.
Freedman, LP; Yang, W, 1999
)
0.3
" The 765 patients who received the minimum effective dosage for more than 6 months made up the 'treatment group'."( Treatment with active vitamin D metabolites and concurrent treatments in the prevention of hip fractures: a retrospective study.
Endo, N; Imura, K; Ishii, Y; Mashiba, T; Nishida, S; Takahashi, HE; Takano, Y; Tanizawa, T, 1999
)
0.3
" Hormone dose-response relationships for translocation and for transactivation were similar."( Hormone-dependent translocation of vitamin D receptors is linked to transactivation.
Barsony, J; Racz, A, 1999
)
0.3
" Furthermore, codosing of 1,25(OH)(2)D(3) and 9-cis-retinoids resulted in higher circulating concentrations of 9-cis-RA and 9,13-di-cis-RA when compared to rats dosed with 9-cis-retinoids alone."( 1,25-Dihydroxyvitamin D(3) and 9-cis-retinoids are synergistic regulators of 24-hydroxylase activity in the rat and 1, 25-dihydroxyvitamin D(3) alters retinoic acid metabolism in vivo.
Horst, RL; Koszewski, NJ; Omdahl, J; Reinhardt, TA, 1999
)
0.3
" calcitriol dosage according to the severity of HPTH is an effective and safe treatment of HPTH in chronic hemodialysis patients."( Effective treatment of secondary hyperparathyroidism in hemodialysis patients by titration of intravenous calcitriol dosage.
Balaskas, E; Benos, A; Grekas, D; Kampouris, H; Konstantinou, A; Sioullis, A; Tourkantonis, A, 1999
)
1.43
" We also measured serum intact parathyroid hormone before and 48 hours after dosing as an index for efficacy."( Chronotherapy of high-dose 1,25-dihydroxyvitamin D3 in hemodialysis patients with secondary hyperparathyroidism: a single-dose study.
Fujimura, A; Kawaguchi, A; Ohmori, M; Saito, T; Sugimoto, K; Tsuruoka, S, 1999
)
0.3
" However, the area under concentration-time curve from zero to 48 hours [AUC(0-48)] and peak concentration of these variables were markedly lower after dosing at 8 PM."( Chronotherapy of high-dose 1,25-dihydroxyvitamin D3 in hemodialysis patients with secondary hyperparathyroidism: a single-dose study.
Fujimura, A; Kawaguchi, A; Ohmori, M; Saito, T; Sugimoto, K; Tsuruoka, S, 1999
)
0.3
"The administration of vitamin D3 at night may reduce the occurrence of hypercalcemia and hyperphosphatemia in patients with secondary hyperparathyroidism, whereas the pharmacokinetics and intact parathyroid hormone-lowering effect of the drug does not vary with dosing time."( Chronotherapy of high-dose 1,25-dihydroxyvitamin D3 in hemodialysis patients with secondary hyperparathyroidism: a single-dose study.
Fujimura, A; Kawaguchi, A; Ohmori, M; Saito, T; Sugimoto, K; Tsuruoka, S, 1999
)
0.3
" The rats were dosed orally with each sterol for 7 days at a rate of 1 ng/g body weight/day."( Comparison of the relative effects of 1,24-dihydroxyvitamin D(2) [1, 24-(OH)(2)D(2)], 1,24-dihydroxyvitamin D(3) [1,24-(OH)(2)D(3)], and 1,25-dihydroxyvitamin D(3) [1,25-(OH)(2)D(3)] on selected vitamin D-regulated events in the rat.
Bishop, C; Horst, R; Knutson, J; Koszewski, N; Prapong, S; Reinhardt, T, 2000
)
0.31
" Control of hyperphosphatemia, maintenance of normocalcemia, and appropriate dosing of vitamin D analogues can prevent HPT in many cases."( Current medical management of secondary hyperparathyroidism.
Llach, F; Yudd, M, 2000
)
0.31
" Calcitriol dosing was similar in both groups (3-6 micrograms per week in three divided doses)."( Pulse oral versus pulse intraperitoneal calcitriol: a comparison of efficacy in the treatment of hyperparathyroidism and renal osteodystrophy in peritoneal dialysis patients.
Arora, N; Gadallah, MF; Moles, K; Ramdeen, G; Schaeffer-Pautz, A; Torres, C, 2000
)
1.48
" Clonogenic survival studies indicate that EB 1089 shifts the dose-response curve for sensitivity to adriamycin by approximately six-fold in p53 wild-type MCF-7 cells; comparative studies in MCF-7 cells with a temperature-sensitive dominant negative p53 mutation show less than a two-fold shift in adriamycin sensitivity in the presence of EB 1089."( The vitamin D3 analog EB 1089 enhances the antiproliferative and apoptotic effects of adriamycin in MCF-7 breast tumor cells.
Chaudhry, M; Gewirtz, DA; Gupta, M; Reardon, D; Sundaram, S, 2000
)
0.31
"We have recently reported that the degree of hypercalcemia as an adverse effect induced by a single large-dose of active vitamin D3 varied with its dosing time without alteration in therapeutic effect for secondary hyperparathyroidism in patients with chronic renal failure."( Contribution of diet to the dosing time-dependent change of vitamin D3-induced hypercalcemia in rats.
Fujimura, A; Sugimoto, K; Tsuruoka, S, 2000
)
0.31
"Administration of 1,25(OH)2D3 as a continuous hepatic arterial infusion allows a high dosage to be administered without inducing hypercalcemia."( A phase one study of the hepatic arterial administration of 1,25-dihydroxyvitamin D3 for liver cancers.
Ahkter, J; Finlay, IG; Morris, DL; Stewart, GJ, 2001
)
0.31
" An in vivo metabolism study in rats dosed with a physiological dose of 1alpha,25-dihydroxy-[26,27-3H]vitamin D3 confirmed the absence of 26-hydroxylation of the hormone."( 26-Hydroxylation of 1alpha,25-dihydroxyvitamin D3 does not occur under physiological conditions.
DeLuca, HF; Endres, B, 2001
)
0.31
"Weekly dosing of oral calcitriol permitted substantial dose escalation with minimal toxicity."( A Phase I trial of pulse calcitriol in patients with refractory malignancies: pulse dosing permits substantial dose escalation.
Beer, TM; Henner, WD; Munar, M, 2001
)
0.93
" When the dosage was increased in one study, there was a higher incidence of hypercalcemia."( Prevention of metabolic bone disease in the pre-end-stage renal disease setting.
Coburn, JW; Elangovan, L, 1998
)
0.3
" The mean number of sessions and the cumulative UVA dosage for initial and complete repigmentation were calculated."( Is the efficacy of psoralen plus ultraviolet A therapy for vitiligo enhanced by concurrent topical calcipotriol? A placebo-controlled double-blind study.
Alpsoy, E; Cetin, L; Ermis, O; Yilmaz, E, 2001
)
0.31
" Weekly calcitriol dosing is associated with minimal toxicity and permits substantial dose escalation over the daily schedule."( Weekly high-dose calcitriol and docetaxel in advanced prostate cancer.
Beer, TM; Garzotto, M; Henner, WD; Hough, KM; Lowe, BA, 2001
)
1.08
" Subsequent dosing was based on iPTH, calcium, and phosphorus determinations."( Paricalcitol in dialysis patients with calcitriol-resistant secondary hyperparathyroidism.
Llach, F; Yudd, M, 2001
)
0.58
" Furthermore, in separate trials, calcipotriol combination therapy reduced the dosage of acitretin required to achieve clearance of psoriasis and the duration of PUVA and dosage of UVA phototherapy, potentially improving the benefit/risk ratio for these other antipsoriatic treatments."( Calcipotriol ointment. A review of its use in the management of psoriasis.
Dunn, CJ; Goa, KL; Scott, LJ, 2001
)
0.31
" In addition, calcipotriol ointment proved beneficial in combination with other topical, phototherapy or systemic antipsoriatic treatments, reducing the dosage and/or duration of some of these treatments and potentially improving their benefit/risk ratio."( Calcipotriol ointment. A review of its use in the management of psoriasis.
Dunn, CJ; Goa, KL; Scott, LJ, 2001
)
0.31
" 1,25(OH)(2)D(3) induction of vitamin D receptors and the CaMBP-Ds was similar with respect to dose-response and time course."( 1,25-Dihydroxyvitamin D-stimulated calmodulin binding proteins: a sustained effect on distal tubules.
Siaw, EK; Walters, MR, 2002
)
0.31
"Although the PTH-suppressive effect of intravenous calcitriol has already been demonstrated by various studies, the precise dose-response to calcitriol has not been fully determined for uremic secondary hyperparathyroidism (2HPT)."( Clinical effect of intravenous calcitriol administration on secondary hyperparathyroidism. A double-blind study among 4 doses.
Akiba, T; Akizawa, T; Arakawa, M; Koshikawa, S; Kurokawa, K; Marumo, F; Morii, H; Ogata, E; Ohashi, Y; Sakai, O; Seino, Y; Suzuki, M; Tsukamoto, Y, 2002
)
0.85
" In the second stage, which begins at the first instance of DLT, a two-parameter logistic dose-response model estimates the MTD from the DLT experience of all patients."( Adaptive dose finding for phase I clinical trials of drugs used for chemotherapy of cancer.
Potter, DM, 2002
)
0.31
" Group A received FAE tablets (Fumaderm) with an increasing daily dosage from 105 to 1,075 mg + ointment vehicle."( Topical calcipotriol plus oral fumaric acid is more effective and faster acting than oral fumaric acid monotherapy in the treatment of severe chronic plaque psoriasis vulgaris.
Altmeyer, P; Christophers, E; Gollnick, H; Kaufmann, R; Pavel, S; Ring, J; Ziegler, J, 2002
)
0.31
" Both isolated enterocytes and the perfused duodenal loop system exhibited apparent biphasic dose-response curves for 1,25(OH)2D3-stimulated 32P uptake and transport, and inhibition of stimulation by 24,25(OH)2D3."( 1,25(OH)2D3-mediated phosphate uptake in isolated chick intestinal cells: effect of 24,25(OH)2D3, signal transduction activators, and age.
Nemere, I; Zhao, B, 2002
)
0.31
"Little attention is given to accurate dosage of topical medication which is a potential source of side-effects and treatment failure."( The importance of accurate dosage of topical agents: a method of estimating involved area and application to calcipotriol treatment failures.
Hutchinson, PE; Osborne, JE, 2002
)
0.31
" Dosing was 5X/week for five weeks."( Vitamin D analogs, a new treatment for retinoblastoma: The first Ellsworth Lecture.
Albert, DM; Audo, I; Gamm, DM; Lindstrom, MJ; Nickells, RW; Schlamp, CL; Zimbric, ML, 2002
)
0.31
" Patients were divided according PTH into 4 groups and calcitriol was dosed accordingly."( [Calcitriol dose optimization in the treatment of secondary hyperparathyroidism during dialysis. Results at 6 months].
Cannata Andía, JB; Fernández Martín, JL; Hervás Sánchez, J; Rodríguez García, M; Ruiz de Castañeda, J, 2002
)
1.47
" These results suggest that OCT is a highly effective drug for the suppression of PTH levels in 2HPT, and is an overall safe drug if the dosage is adjusted for serum Ca and intact-PTH levels."( Long-term effect of 1,25-dihydroxy-22-oxavitamin D(3) on secondary hyperparathyroidism in haemodialysis patients. One-year administration study.
Akiba, T; Akizawa, T; Kurokawa, K; Nishizawa, Y; Ogata, E; Ohashi, Y; Slatopolsky, E; Suzuki, M, 2002
)
0.31
"Treatment of hyperparathyroidism includes the use of 1,25-dihydroxy-vitamin D3 (1,25D3) to suppress parathyroid hormone (PTH), but dosing of 1,25D3 is limited by the development of hypercalcemia and a high calcium x phosphorus (Ca x P) product because of gut absorption of calcium and phosphorus and enhanced bone resorption."( Differential effects of acute administration of 19-Nor-1,25-dihydroxy-vitamin D2 and 1,25-dihydroxy-vitamin D3 on serum calcium and phosphorus in hemodialysis patients.
Ahya, SN; Coyne, DW; Giles, K; Grieff, M; Norwood, K; Slatopolsky, E, 2002
)
0.31
" Three controlled clinical trials have demonstrated that the addition of calcipotriene ointment to systemic antipsoriatic treatment with MTX, acitretin, and cyclosporine increases the therapeutic efficacy compared with systemic therapy alone and minimizes side effects by either reducing the dosage or duration of treatment."( Vitamin D and systemic therapy.
van de Kerkhof, P, 2002
)
0.31
" The cell lines were incubated with EB 1089, a synthetic analogue vitamin of D(3), in dose-response studies."( Vitamin D receptor is expressed in pancreatic cancer cells and a vitamin D3 analogue decreases cell number.
Albrechtsson, E; Axelson, J; Höglund, M; Jonsson, T; Möller, S; Ohlsson, B, 2003
)
0.32
" While their less calcemic properties make higher dosing safer, their specificity to recruit co-activator molecules to the transcriptional pre-initiation complex could compensate for reduced 1,25(OH)2D3/VDR by potentiating VDR-transactivation/transrepression of genes critical for normal PTH synthesis and parathyroid cell growth."( Vitamin D receptor: mechanisms for vitamin D resistance in renal failure.
Dusso, AS, 2003
)
0.32
" Two thirds of patients, labeled "noncompliants," showed one or more violation in the dosage regimen."( Advantages of adjusting the initial dose of intravenous calcitriol according to PTH levels.
Cannata-Andía, JB; de Castañeda, JR; Fernández-Martín, JL; Hervás-Sánchez, J; Rodríguez-García, M, 2003
)
0.57
" Therefore, the calcitriol dosage should be small and then adjusted according to the degree of SH."( [Role of diet in the management of osteodystrophy during progressive renal insufficiency].
Martínez, I; Montenegro, J; Muñoz, RI; Ocharán, J; Saracho, R, 2003
)
0.66
"6 times higher at 6, 24, and 48 h postdosing than after dosing with [1beta-3H] 1alpha,25(OH)2 vitamin D3."( Disposition and metabolism of F6-1alpha,25(OH)2 vitamin D3 and 1alpha,25(OH)2 vitamin D3 in the parathyroid glands of rats dosed with tritium-labeled compounds.
Kanamaru, H; Komuro, S; Sato, M, 2003
)
0.32
" In order to compare the efficacy of different dosing schedules of Seocalcitol, rats were treated either 6 times weekly (1 microg/kg) or by intermittent dosing to achieve the same total weekly dose."( Effects of Seocalcitol (EB1089) on nitrosomethyl urea-induced rat mammary tumors.
Binderup, L; Bramm, E; Colston, KW; Hamberg, KJ; Pirianov, G, 2003
)
0.32
" Comparison of dose-response curves for ion transport and kinase activities in 7-week chicks suggested that PKC mediates phosphate transport while PKA mediates calcium transport."( Effect of growth and maturation on membrane-initiated actions of 1,25-dihydroxyvitamin D3-II: calcium transport, receptor kinetics, and signal transduction in intestine of female chickens.
Larsson, B; Nemere, I, 2003
)
0.32
" This limitation has been overcome with intermittent dosing of calcitriol."( Development of weekly high-dose calcitriol based therapy for prostate cancer.
Beer, TM,
)
0.65
" Such concentrations are not achievable in patients when calcitriol is dosed daily due to predictable hypercalcemia and hypercalcuria; however, phase I trials have demonstrated that intermittent dosing allows substantial dose escalation and has produced potentially therapeutic peak calcitriol concentrations."( Calcitriol in cancer treatment: from the lab to the clinic.
Beer, TM; Myrthue, A, 2004
)
2.01
"After each recipient was treated with 1,25-(OH)2D3 at a dosage of (0."( Role of 1,25-dihydroxyvitamin D3 in preventing acute rejection of allograft following rat orthotopic liver transplantation.
Jia, CK; Wang, Y; Zhang, AB; Zheng, SS, 2004
)
0.32
" In this study, the chronopharmacological effect of 22-oxacalcitriol, a newly developed active vitamin D3 analogue with less calcemic activity, was evaluated by a single and repeated dosing of the drug in aged SHRSP."( Chronopharmacology of oxacalcitriol in rat model of osteoporosis.
Fujimura, A; Tsuruoka, S; Wakaumi, M; Yamamoto, H, 2004
)
0.87
" Due to the cumbersome dosing schedule and the lack of significant activity observed, Phase II trials of this regimen are not planned."( High-dose calcitriol, zoledronate, and dexamethasone for the treatment of progressive prostate carcinoma.
Curley, T; Delacruz, A; Diani, M; Fallon, M; Fleisher, M; Flombaum, C; Kelly, WK; Morris, MJ; Scher, HI; Schwartz, L; Slovin, S; Smaletz, O; Solit, D; Zhu, A, 2004
)
0.73
" Group B included 33 patients treated with the same cyclosporin dosage plus, for the same time, topical application of calcipotriol cream twice a day."( Nail psoriasis: combined therapy with systemic cyclosporin and topical calcipotriol.
Amerio, P; Cerritelli, L; Feliciani, C; Forleo, P; Proietto, G; Tulli, A; Zampetti, A,
)
0.13
" In this study, the chronopharmacological effect of 22-oxacalcitriol (OCT), a newly developed active vitaminD3 analogue with less calcemic activity, was evaluated by a single and repeated dosing of the drug."( Chronopharmacology of oxacalcitriol in 5/6 nephrectomized rats.
Ando, H; Fujimura, A; Ning, W; Nishiki, K; Tsuruoka, S; Wakaumi, M; Yamamoto, H, 2004
)
0.87
"The dose-response relationships and the safety of administering 22-oxacalcitriol (OCT) to patients with secondary hyperparathyroidism (2HPT) under regular three-times-weekly hemodialysis (HD) were evaluated by double-blind parallel group design."( Dose-response study of 22-oxacalcitriol in patients with secondary hyperparathyroidism.
Akiba, T; Akizawa, T; Kurokawa, K; Nishizawa, Y; Ogata, E; Ohashi, Y; Slatopolsky, E; Suzuki, M, 2004
)
0.85
"We investigated the effects of long-term (6-week) treatment with 1,25(OH)2D3, at a non-hypercalcemic dosage (0."( Systemic cardiovascular disease in uremic rats induced by 1,25(OH)2D3.
Eggert, B; Godes, M; Haffner, D; Hocher, B; König, K; Müller, D; Nissel, R; Querfeld, U; Richter, CM; Schwarz, J; Simon, K, 2005
)
0.33
" We found no changes in blood pressure, although there was a trend toward a reduced dosage of antihypertensive drugs."( Effect of parathyroidectomy on renal graft function.
Ceballos, M; Garcia, A; Garcia, T; González, P; Mazuecos, A; Rivero, M, 2005
)
0.33
" 1,25-(OH)2D3 rapidly stimulated PHF release with enhanced sensitivity in SHR versus WKY cultures indicated by a leftward shift in the dose-response curve, whereas 24,25-dihydroxyvitamin D3 (24,25-(OH)2D3) had the converse effect."( Regulation of parathyroid hypertensive factor secretion by vitamin D3 analogs in parathyroid cells derived from spontaneously hypertensive rats.
Benishin, CG; Nemere, I; Sutherland, SK, 2005
)
0.33
" ASCENT builds on phase I work showing that weekly dosing allows substantial dose-escalation of calcitriol, the natural ligand for the vitamin D receptor, and on phase II work that suggested that adding weekly high-dose 'pulse' calcitriol may enhance the activity of weekly docetaxel in patients with AIPC."( ASCENT: the androgen-independent prostate cancer study of calcitriol enhancing taxotere.
Beer, TM, 2005
)
0.79
" Dose-response curves demonstrated that as little as 1pM 1,25(OH)2D3 significantly inhibited chemotaxis enhancement."( Selective inhibition of the C5a chemotactic cofactor function of the vitamin D binding protein by 1,25(OH)2 vitamin D3.
DiMartino, SJ; Kew, RR; Shah, AB; Trujillo, G, 2006
)
0.33
" Our data show that ED at a dosage that suppresses bone metabolism markedly inhibits vascular calcification in rats with renal failure."( Effect of etidronate on aortic calcification and bone metabolism in calcitriol-treated rats with subtotal nephrectomy.
Aizawa, S; Hashiba, H; Kogo, H; Suzuki, Y; Tamura, H; Tamura, K, 2005
)
0.56
"Review of current and new procedures to estimate the body surface area, to calculate the most adequate quantity of medication to be prescribed, to instruct patients and to assess the individual dosing procedures of topical treatments."( The right dose in the right place: an overview of current prescription, instruction and application modalities for topical psoriasis treatments.
Aractingi, S; Ortonne, JP; Savary, J, 2005
)
0.33
" Dosing devices, such as a spatula, may help patients to dose their daily topical treatment, avoiding over- and underdosing of the medication."( The right dose in the right place: an overview of current prescription, instruction and application modalities for topical psoriasis treatments.
Aractingi, S; Ortonne, JP; Savary, J, 2005
)
0.33
"A correct evaluation of the lesions sizes, a precise calculation of the treatments quantity to be prescribed, clear instructions and treatment-specific individual dosing devices may help to achieve higher patient compliance and treatment success."( The right dose in the right place: an overview of current prescription, instruction and application modalities for topical psoriasis treatments.
Aractingi, S; Ortonne, JP; Savary, J, 2005
)
0.33
" The objective of the present study was to evaluate the stability of physiological activities of CT and OCT in PD bags and to determine the CT or OCT dosage for intraperitoneal (IP) administration."( Pharmacokinetics of calcitriol and maxacalcitol administered into peritoneal dialysate bags in peritoneal dialysis patients.
Fukui, M; Hamada, C; Hayashi, K; Inaba, M; Io, H; Maeda, K; Ro, Y; Shou, I; Tomino, Y,
)
0.45
"If peritoneal administration of vitamin D derivatives is contemplated, it is important to select the composition of PD bag resins, type of vitamin D analog, and time lag to use when deciding the dosage of injectable vitamin D preparations, such as OCT or CT, for IP administration to PD patients."( Pharmacokinetics of calcitriol and maxacalcitol administered into peritoneal dialysate bags in peritoneal dialysis patients.
Fukui, M; Hamada, C; Hayashi, K; Inaba, M; Io, H; Maeda, K; Ro, Y; Shou, I; Tomino, Y,
)
0.45
"Retired female rats obtained from Sprague-Dawley were ovariectomized, and were either dosed with vehicle or 2MD at 5-7 ng/kg body weight each day."( 2MD, a new anabolic agent for osteoporosis treatment.
Binkley, NC; Clagett-Dame, M; DeLuca, HF; Fitzpatrick, LA; Ma, X; Plum, LA; Zella, JB, 2006
)
0.33
" This combination not only provides earlier pigmentation with lower total UVB dosage and less adverse UVB effects, but also reduces the duration and cost of treatment as well."( Combination of narrow band UVB and topical calcipotriol for the treatment of vitiligo.
Aydin, F; Canturk, MT; Goktas, EO; Senturk, N; Turanli, AY, 2006
)
0.33
" Cows receiving 25-OH D3 or DCAD+25-OH D3 were dosed with 125 mg of 25-OH D3 6 d before slaughter."( Effects of 25-hydroxyvitamin D3 and manipulated dietary cation-anion difference on the tenderness of beef from cull native Korean cows.
Cho, YM; Choi, H; Hwang, IH; Kim, YK; Myung, KH, 2006
)
0.33
" Dosing was at intervals of at least two weeks in a 5x5 Latin square design."( Dose response to vaginal administration of 1,25-dihydroxyvitamin D3 to cows.
Koiwa, M; Naito, Y; Okura, N; Yamagishi, N, 2007
)
0.34
" Despite multiple dosage alterations in the phosphate and calcitriol therapy, the patient had recurrent tertiary HPT and another kidney stone (treated by lithotripsy)."( Tertiary hyperparathyroidism attributable to long-term oral phosphate therapy.
McHenry, CR; Mostafavi, K; Murphy, TA,
)
0.38
"Long-term follow-up of patients with tertiary HPT is critical, with careful dosage adjustments in phosphate and vitamin D therapy and monitoring of serum levels of phosphorus, calcium, and parathyroid hormone."( Tertiary hyperparathyroidism attributable to long-term oral phosphate therapy.
McHenry, CR; Mostafavi, K; Murphy, TA,
)
0.13
" In addition to screening potential antipsoriatic substances, the PPT can help answer other questions (frequency of use, dose-response relationship)."( [Is the psoriasis plaque test still relevant in the age of biologicals?].
Wozel, G, 2006
)
0.33
" Initial studies tested daily dosing of calcitriol and showed that substantial dose escalation was not feasible due to hypercalciuria and/or hypercalcemia."( Calcitriol in the treatment of prostate cancer.
Beer, TM; Myrthue, A,
)
1.84
" Data suggest that dosing should be gauged according to degree of SHPT."( Paricalcitol versus calcitriol treatment for hyperparathyroidism in pediatric hemodialysis patients.
Abitbol, CL; Chandar, J; Nwobi, O; Seeherunvong, W; Strauss, J; Zilleruelo, G, 2006
)
0.66
"At the dosage used, calcitriol has a modest effect on residual pancreatic beta-cell function and only temporarily reduces the insulin dose."( The effects of calcitriol and nicotinamide on residual pancreatic beta-cell function in patients with recent-onset Type 1 diabetes (IMDIAB XI).
Anguissola, GB; Bizzarri, C; Cavallo, MG; Crinò, A; Di Stasio, E; Guglielmi, C; Manfrini, S; Matteoli, MC; Patera, IP; Pitocco, D; Pozzilli, P; Spera, S; Suraci, C; Visalli, N, 2006
)
1.01
" Few controlled dose-response studies are available on the effects of high P intake in man."( High phosphorus intakes acutely and negatively affect Ca and bone metabolism in a dose-dependent manner in healthy young females.
Kärkkäinen, MU; Kemi, VE; Lamberg-Allardt, CJ, 2006
)
0.33
"A lymph cannulated conscious rat model was dosed orally with (3)H-seocalcitol dissolved in either LCT or PG."( Bioavailability of seocalcitol IV: evaluation of lymphatic transport in conscious rats.
Grove, M; Müllertz, A; Nielsen, JL; Pedersen, GP, 2006
)
0.33
"05) higher recovery of the dosed (3)H-seocalcitol was found in the intestinal lymph upon administration of the LCT solution (1."( Bioavailability of seocalcitol IV: evaluation of lymphatic transport in conscious rats.
Grove, M; Müllertz, A; Nielsen, JL; Pedersen, GP, 2006
)
0.33
" Uremic patients, however, suffer from severe deprivation of biological vitamin D effects, that puts them in need of highly dosed vitamin D in order to both ameliorate their bone status and to preserve their general and cardiovascular health."( Therapy of secondary hyperparathyroidism to date: vitamin D analogs, calcimimetics or both?
Cannella, G; Messa, P,
)
0.13
" (2005) Clin Cancer Res 11:7794-7799] were eligible for this continuation weekly dosing study."( Phase I study of weekly DN-101, a new formulation of calcitriol, in patients with cancer.
Beer, TM; Garzotto, M; Henner, WD; Javle, MM; Johnson, CS; Lam, GN; Ryan, CW; Trump, DL; Wong, A, 2007
)
0.59
" PK parameters following repeat dosing were comparable to those for the initial dose (n = 4)."( Phase I study of weekly DN-101, a new formulation of calcitriol, in patients with cancer.
Beer, TM; Garzotto, M; Henner, WD; Javle, MM; Johnson, CS; Lam, GN; Ryan, CW; Trump, DL; Wong, A, 2007
)
0.59
"To investigate the contribution of intestinal calcium (Ca) absorption to 1,25-dihydroxyvitamin D(3) (1,25(OH) (2)D(3))-induced Ca action, we assessed parameters related to Ca metabolism after a single dosing of 1,25(OH)(2)D (3) in the total parenteral nutrition (TPN) solution or 5% D-mannitol (MAN) solution treatment with rats."( Contribution of intestinal calcium absorption to 1,25-dihydroxyvitamin D3-induced calcium action in the total parenteral nutrition rat.
Asanuma, K; Chiba, S; Komatsu, S; Sakurai, T; Takai, R, 2006
)
0.33
" Induction of 24-hydroxylase mRNA levels by 1,25 dihydroxyvitamin D(3) [1,25(OH)(2) D(3)] injection was significantly reduced in the duodenum and kidney of HT mice in both time-course and dose-response experiments."( Intestinal resistance to 1,25 dihydroxyvitamin D in mice heterozygous for the vitamin D receptor knockout allele.
Fleet, JC; Song, Y, 2007
)
0.34
" Dose-response studies indicated a biphasic curve with optimal stimulation at 300 pM 1,25(OH)(2)D(3) and inhibition at 600 pM seco-steroid."( Phosphate uptake in chick kidney cells: effects of 1,25(OH)2D3 and 24,25(OH)2D3.
Khanal, RC; Nemere, I; Smith, NM, 2007
)
0.34
"Daily and intermittent dosing of calcitriol will decrease plasma parathyroid hormone concentration in normal cats and cats with chronic renal failure without causing ionized hypercalcemia."( Comparison of the effects of daily and intermittent-dose calcitriol on serum parathyroid hormone and ionized calcium concentrations in normal cats and cats with chronic renal failure.
Chew, DJ; DiBartola, SP; Drost, WT; Hostutler, RA; Nagode, LA; Rajala-Schultz, PJ; Schenck, PA,
)
0.66
" Potential reasons for lack of apparent effect include small sample size, insufficient duration of study, insufficient dosage of calcitriol, problems with formulation or administration of calcitriol, and variable gastrointestinal absorption of calcitriol."( Comparison of the effects of daily and intermittent-dose calcitriol on serum parathyroid hormone and ionized calcium concentrations in normal cats and cats with chronic renal failure.
Chew, DJ; DiBartola, SP; Drost, WT; Hostutler, RA; Nagode, LA; Rajala-Schultz, PJ; Schenck, PA,
)
0.58
" Interestingly, although 1,25(OH)(2)D(3) alone did not increase expression of the 1,25D(3)-MARRS promoter-reporter, co-treatment of transfected IEC-6 cells with 1,25(OH)(2)D(3) and TGFbeta shifted the dose-response curve to a lower effective concentration (100 pM peptide)."( Regulation of expression of 1,25D3-MARRS/ERp57/PDIA3 in rat IEC-6 cells by TGF beta and 1,25(OH)2D3.
Farach-Carson, MC; Nemere, I; Rohe, B; Safford, SE, 2007
)
0.34
" Fifty-two patients with stage 3 or stage 4 CKD with vitamin D deficiency and elevated PTH concentrations received ergocalciferol dosed per a modified K/DOQI guidelines protocol and adjusted every 3 months."( Impact of ergocalciferol treatment of vitamin D deficiency on serum parathyroid hormone concentrations in chronic kidney disease.
Ho, LT; Hristova, M; Sprague, SM; Zisman, AL, 2007
)
0.34
" The effect of 1,25-dihydroxyvitamin D3 disappears when the dosing solution of phosphate is at 2 M, suggesting that 1,25-dihydroxyvitamin D3 stimulates active transport of phosphate but not diffusion of phosphate."( Characterization of intestinal phosphate absorption using a novel in vivo method.
DeLuca, HF; Williams, KB, 2007
)
0.34
" The present study illustrates an often mentioned beneficial effect of dosing lipid-based formulations; the reduced food effect on bioavailability."( Bioavailability of seocalcitol III. Administration of lipid-based formulations to minipigs in the fasted and fed state.
Grove, M; Müllertz, A; Nielsen, JL; Pedersen, GP, 2007
)
0.34
" There was a monotonic dose-response relation between serum 25(OH)D concentrations at less than 22 wk and risk of preeclampsia."( Maternal vitamin D deficiency increases the risk of preeclampsia.
Bodnar, LM; Catov, JM; Holick, MF; Powers, RW; Roberts, JM; Simhan, HN, 2007
)
0.34
" We examine here, the effect of calcitriol and cisplatin pre-clinically and clinically in canine spontaneous tumors through in vitro studies on tumor cells and through a phase I study of calcitriol and cisplatin to identify the maximum-tolerated dosage (MTD) of this combination in dogs with cancer and to characterize the pharmacokinetic disposition of calcitriol in dogs."( In vitro and in vivo evaluation of combined calcitriol and cisplatin in dogs with spontaneously occurring tumors.
Balkman, CE; Engler, KL; Johnson, CS; Muindi, JR; Page, RL; Ramnath, N; Rassnick, KM; Trump, DL; Yu, WD, 2008
)
0.89
" Cisplatin was given at a fixed dosage of 60 mg/m2."( In vitro and in vivo evaluation of combined calcitriol and cisplatin in dogs with spontaneously occurring tumors.
Balkman, CE; Engler, KL; Johnson, CS; Muindi, JR; Page, RL; Ramnath, N; Rassnick, KM; Trump, DL; Yu, WD, 2008
)
0.61
" The relationship between calcitriol dosage and either Cmax or AUC was linear."( In vitro and in vivo evaluation of combined calcitriol and cisplatin in dogs with spontaneously occurring tumors.
Balkman, CE; Engler, KL; Johnson, CS; Muindi, JR; Page, RL; Ramnath, N; Rassnick, KM; Trump, DL; Yu, WD, 2008
)
0.91
" One patient experienced transient hypercalcemia that normalized after a dosage decrease."( Oral calcitriol for the treatment of persistent proteinuria in immunoglobulin A nephropathy: an uncontrolled trial.
Chow, KM; Chung, KY; Kwan, BC; Leung, CB; Li, PK; Szeto, CC, 2008
)
0.86
" The total dosage of calcitriol during the study was comparable in both groups."( Intravenous calcitriol therapy in an early stage prevents parathyroid gland growth.
Hirakata, H; Iida, M; Taniguchi, M; Tokumoto, M; Tsuruya, K, 2008
)
1.04
" By using the Ussing chamber technique, we found that duodenal epithelia acutely exposed to 10 and 100 nmol/l 1,25-(OH)(2)D(3) rapidly increased the solvent drag-induced calcium transport, but not the transcellular calcium transport, in a dose-response manner."( 1,25-dihydroxyvitamin D(3) rapidly stimulates the solvent drag-induced paracellular calcium transport in the duodenum of female rats.
Charoenphandhu, N; Jantarajit, W; Krishnamra, N; Teerapornpuntakit, J; Tudpor, K, 2008
)
0.35
" Response rate was not affected by transfusion requirement (63%; 58% in untransfused), IPSS and WHO Prognostic Scoring System scores, and weekly rEPO dosage (30-50 000 U vs."( Efficacy of a combination of human recombinant erythropoietin + 13-cis-retinoic acid and dihydroxylated vitamin D3 to improve moderate to severe anaemia in low/intermediate risk myelodysplastic syndromes.
Bertini, M; Boccadoro, M; Darbesio, A; Dellacasa, CM; Ferrero, D; Genuardi, M; Giai, V; Sorasio, R, 2009
)
0.35
" The relationship between FGF23 and PTH is unclear, and the acute effect of pharmacologically dosed PTH on FGF23 secretion is unknown."( Effects of hPTH(1-34) infusion on circulating serum phosphate, 1,25-dihydroxyvitamin D, and FGF23 levels in healthy men.
Burnett-Bowie, SM; Dere, ME; Henao, MP; Leder, BZ; Lee, H, 2009
)
0.35
" From our results, it can offer new opportunities to design and determine individually appropriate therapeutic dosage regimens based on a pharmacokinetic profile and be used for bioequivalence and reevaluation study of generic drug."( Pharmacokinetics of oral calcitriol in healthy human based on the analysis with an enzyme immunoassay.
Jin, SE; Kim, CK; Park, JS, 2009
)
0.66
" Calcitriol inhibited the expression profile of inflammatory cytokine genes in a dose-response manner (P<0."( Calcitriol inhibits TNF-alpha-induced inflammatory cytokines in human trophoblasts.
Avila, E; Barrera, D; Díaz, L; Halhali, A; Hernández, G; Larrea, F; Noyola-Martínez, N, 2009
)
2.71
" Protein and mRNA levels of target genes in the small intestine, colon and liver after intraperitoneal dosing of 1,25(OH)(2)D(3) (0-2."( 1alpha,25-Dihydroxyvitamin D(3) triggered vitamin D receptor and farnesoid X receptor-like effects in rat intestine and liver in vivo.
Chow, EC; Groothuis, GM; Khan, AA; Liu, S; Maeng, HJ; Pang, KS, 2009
)
0.35
" Recent research found that intermittent dosing can reduce hypercalcemia rates."( The efficacy of calcitriol therapy in the management of bone loss and fractures: a qualitative review.
Hebl, S; Huston, AJ; Ling, MN; Morrow, GR; Mustian, KM; Palesh, OG; Peppone, LJ; Purnell, JQ; Reid, ME; Rosier, RN, 2010
)
0.71
" Two series of experiments were carried out to investigate the effects of 1,25-dihydroxyvitammin D(3) (calcitriol) in supraphysiological dosage in combination with varying alimentary Ca supply."( Effects of 1,25-dihydroxyvitamin D3 on calcium and phosphorus homeostasis in sheep fed diets either adequate or restricted in calcium content.
Breves, G; Mrochen, N; Schröder, B; Wilkens, MR, 2010
)
0.58
" Western blots with anti-PKCalpha exhibited redistribution to membranes in a biphasic dose-response curve: slightly stimulated at the lowest dose, maximal at 300pM 1,25(OH)(2)D(3), and equivalent to control levels at the highest dose, paralleling hormone-mediated phosphate uptake."( Protein kinase C isotypes in signal transduction for the 1,25D3-MARRS receptor (ERp57/PDIA3) in steroid hormone-stimulated phosphate uptake.
Nemere, I; Tunsophon, S, 2010
)
0.36
" However no consistent differences between routes of administration, frequencies of dosing or vitamin D preparations have been demonstrated."( Interventions for bone disease in children with chronic kidney disease.
Craig, JC; Geary, DF; Hodson, EM, 2010
)
0.36
" There was a reduction in the dosage and in the number of patients who were treated with paricalcitol and sevelamer."( Cholecalciferol supplementation in hemodialysis patients: effects on mineral metabolism, inflammation, and cardiac dimension parameters.
Aires, I; Amaral, T; Borges, M; Cortez, J; Ferreira, A; Ferreira, C; Gil, C; Jorge, C; Matias, PJ, 2010
)
0.36
" It allows reduction of vitamin D deficiency, better control of mineral metabolism with less use of active vitamin D, attenuation of inflammation, reduced dosing of erythropoiesis-stimulating agents, and possibly improvement of cardiac dysfunction."( Cholecalciferol supplementation in hemodialysis patients: effects on mineral metabolism, inflammation, and cardiac dimension parameters.
Aires, I; Amaral, T; Borges, M; Cortez, J; Ferreira, A; Ferreira, C; Gil, C; Jorge, C; Matias, PJ, 2010
)
0.36
" For IC(50) determination and comparison, dose-response curves with VDR agonists, tacrolimus and mycophenolic acid were performed."( Comparison between VDR analogs and current immunosuppressive drugs in relation to CXCL10 secretion by human renal tubular cells.
Adorini, L; Borgogni, E; Crescioli, C; Mazzinghi, B; Romagnani, P; Sagrinati, C; Serio, M; Sottili, M, 2010
)
0.36
" Dose-response studies of the comedolytic analogs showed that an increase in epidermal thickness was achieved at a lower dose than that needed to induce comedolysis."( Identification of a unique subset of 2-methylene-19-nor analogs of vitamin D with comedolytic activity in the rhino mouse.
Ahrens, JM; Clagett-Dame, M; DeLuca, HF; Nieves, NJ; Plum, LA, 2010
)
0.36
" A dose-response trend existed for increasing concentrations of nicotinamide, but it was not significant."( Pilot, multicenter, double-blind, randomized placebo-controlled bilateral comparative study of a combination of calcipotriene and nicotinamide for the treatment of psoriasis.
Andrashko, Y; Even-Chen, Z; Gottlieb, A; Lebwohl, M; Levine, D; Lipets, I; Pritulo, OA; Svyatenko, TV, 2010
)
0.36
"The relatively small patient numbers, relatively high placebo effect, and maximum in-life portion of only 12 weeks of dosing are weaknesses of the study."( Pilot, multicenter, double-blind, randomized placebo-controlled bilateral comparative study of a combination of calcipotriene and nicotinamide for the treatment of psoriasis.
Andrashko, Y; Even-Chen, Z; Gottlieb, A; Lebwohl, M; Levine, D; Lipets, I; Pritulo, OA; Svyatenko, TV, 2010
)
0.36
" For example, a new formulation of calcipotriene/betamethasone scalp solution has a rapid onset of action with once daily dosing that improves compliance."( Scalp psoriasis.
Kircik, LH; Kumar, S, 2010
)
0.36
" Therefore, we investigated gastrointestinal calcium transport of sheep as influenced by a dietary calcium restriction and/or a supraphysiological dosage of exogenous calcitriol."( Gastrointestinal calcium absorption in sheep is mostly insensitive to an alimentary induced challenge of calcium homeostasis.
Breves, G; Mrochen, N; Schröder, B; Wilkens, MR, 2011
)
0.56
" Our findings on the solvent effects of the skin permeability of OCT are thus useful for designing topical drug formulation, especially in aiming for bioequivalent dosage formulas."( Formulation study of topically applied O/W lotion containing vitamin D3 derivative, focusing on skin permeability of the drug.
Harada, S; Horisawa, E; Kano, S; Sugibayashi, K, 2011
)
0.37
" To the best of our knowledge, this is the first comprehensive report of an in vivo long-term biological response generated by chronic dosing with a nongenomic-selective vitamin D steroid."( 1α,25(OH)₂-vitamin D and a nongenomic vitamin D analogue inhibit ultraviolet radiation-induced skin carcinogenesis.
Dixon, KM; Halliday, GM; Mason, RS; Mohan, R; Norman, AW; Reeve, VE; Rybchyn, MS; Sequeira, VB, 2011
)
0.37
"Etanercept is approved for the treatment of plaque psoriasis at a subcutaneous (SC) dosage of 50 mg twice-weekly for three months, followed by 50 mg SC once-weekly thereafter."( Topical calcipotriene 0.005% and betamethasone dipropionate 0.064% maintains efficacy of etanercept after step-down dose in patients with moderate-to-severe plaque psoriasis: results of an open label trial.
Kircik, LH, 2011
)
0.37
" In this pilot study, we investigated the dose-response to 1α,25-dihdroxyvitamin D(3) (1,α 25(OH)(2) D(3)) and 25-hydroxyvitamin D(3) (25(OH)D(3)) by human OS cell lines, SaOS-2, and 143B."( Effect of 25-hydroxyvitamin D3 and 1 α,25 dihydroxyvitamin D3 on differentiation and apoptosis of human osteosarcoma cell lines.
Anderson, HC; Garimella, R; Keighley, J; Pinson, D; Tancabelic, J; Tawfik, O; Templeton, K; Thompson, L; Wang, S, 2012
)
0.38
" Fourteen animals of each group received a daily dosage of 3mg of 25-OHD(3)."( Influence of the combination of 25-hydroxyvitamin D3 and a diet negative in cation-anion difference on peripartal calcium homeostasis of dairy cows.
Azem, E; Breves, G; Oberheide, I; Schröder, B; Steinberg, W; Wilkens, MR, 2012
)
0.38
"70ng/mL, respectively, following intraperitoneal dosing (20μg/kg 1,25(OH)(2)D(3))."( A local effect of CYP24 inhibition on lung tumor xenograft exposure to 1,25-dihydroxyvitamin D(3) is revealed using a novel LC-MS/MS assay.
Beumer, JH; D'Argenio, DZ; Hershberger, PA; Kanterewicz, B; Parise, RA; Petkovich, M, 2012
)
0.38
" Liposomes can enhance the delivery of drugs into the skin, but a major challenge for the development of dosage forms containing liposomes is to maintain the colloidal stability in the formulation."( Calcipotriol delivery into the skin with PEGylated liposomes.
Basse, LH; Foged, C; Frokjaer, S; Hansen, J; Jorgensen, L; Knudsen, NØ; Rønholt, S; Salte, RD; Thormann, T, 2012
)
0.38
" Inhibitory concentrations were determined by dose-response curves and metabolic activity assays."( Astemizole synergizes calcitriol antiproliferative activity by inhibiting CYP24A1 and upregulating VDR: a novel approach for breast cancer therapy.
Avila, E; Barrera, D; Camacho, J; Díaz, L; Gamboa-Domínguez, A; García-Becerra, R; García-Quiroz, J; Halhali, A; Larrea, F; Medina-Franco, H; Ordaz-Rosado, D; Rivas-Suárez, M; Rodríguez, P; Santos, N, 2012
)
0.69
" Since astemizole improves calcitriol bioavailability and activity, decreased calcitriol dosing is advised for conjoint administration."( Astemizole synergizes calcitriol antiproliferative activity by inhibiting CYP24A1 and upregulating VDR: a novel approach for breast cancer therapy.
Avila, E; Barrera, D; Camacho, J; Díaz, L; Gamboa-Domínguez, A; García-Becerra, R; García-Quiroz, J; Halhali, A; Larrea, F; Medina-Franco, H; Ordaz-Rosado, D; Rivas-Suárez, M; Rodríguez, P; Santos, N, 2012
)
0.99
" These patients provide an experiment by nature enabling us to understand the role of vitamin D, especially in light of the ongoing debate concerning normal vitamin D levels and the supplement dosage that should be recommended."( Vitamin D action: lessons learned from hereditary 1,25-dihydroxyvitamin-D-resistant rickets patients.
Gepstein, V; Tiosano, D, 2012
)
0.38
" Expression of CAMP mRNA and protein increased in a dose-response fashion after exposure of acute myeloid leukemia (AML) cells to the Gemini analog, BXL-01-126, in vitro."( Novel Gemini vitamin D3 analogs: large structure/function analysis and ability to induce antimicrobial peptide.
Akagi, T; Alvarez, R; Borregaard, N; Gery, S; Ho, Q; Koeffler, HP; Kuwayama, Y; Liu, GY; Okamoto, R; Uskokovic, MR, 2014
)
0.4
" Results from a number of clinical trials revealed that sufficient dosing and exposure to calcitriol is critical for achieving antitumor effects during intermittent regimens."( The mechanism of calcitriol in cancer prevention and treatment.
Guo, J; Han, S; Hu, A; Li, R; Li, W; Ma, J; Ma, Q; Ma, Z; Wang, F, 2013
)
0.95
" Dose-response and time-course studies with LPS showed significant increases of plasma Pi and intact parathyroid hormone (iPTH) levels and renal Pi excretion, while renal calcium excretion was significantly decreased."( Downregulation of renal type IIa sodium-dependent phosphate cotransporter during lipopolysaccharide-induced acute inflammation.
Ikeda, S; Iwano, M; Kozai, M; Masuda, M; Miyamoto, K; Nakahashi, O; Nakao, M; Segawa, H; Takeda, E; Takei, Y; Taketani, Y; Tanaka, S; Yamamoto, H, 2014
)
0.4
" Healthy breastfed infants (n = 132) were followed from 1 to 12 months of age as part of a vitamin D dose-response study (NCT00381914)."( Plasma 25-hydroxyvitamin D, more so than its epimer, has a linear relationship to leaner body composition across infancy in healthy term infants.
Berzina, I; Gallo, S; Hazell, TJ; Rodd, C; Vanstone, CA; Weiler, HA, 2014
)
0.4
" Inhibitory concentrations on cell proliferation were calculated by non-linear regression analysis using sigmoidal fitting of dose-response curves."( Calcitriol and its analogues enhance the antiproliferative activity of gefitinib in breast cancer cells.
Díaz, L; Esparza-López, J; García-Becerra, R; García-Quiroz, J; González-González, ME; Ibarra-Sánchez, MJ; Larrea, F; Martínez-Reza, I; Prado-Garcia, H; Segovia-Mendoza, M, 2015
)
1.86
" The low-dose, middle-dose, and high-dose intervention groups were administered with 1,25-(OH)(2)D(3) solution at the dosage of 1, 4 and 10 μg/kg respectively by intraperitoneal injections before asthma challenge."( [Effects of different doses of 1,25-(OH)2D3 on expression of HMGB1 and IL-17 in the lungs of asthmatic mice].
Li, YL; Luan, B; Qiao, JY; Zhang, LM, 2015
)
0.42
" Whether substitution of native vitamin D in these patients is beneficial is a matter of ongoing discussion, as is the optimal dosing schedule."( Efficacy and safety of body weight-adapted oral cholecalciferol substitution in dialysis patients with vitamin D deficiency.
Lhotta, K; Mündle, M; Sprenger-Mähr, H; Zitt, E, 2015
)
0.42
"The dosing regimen of oral cholecalciferol supplementation with 100 IU per kg body weight per week for 26 weeks in dialysis patients with vitamin D deficiency causes a significant increase in 25OHD3 close to the supposed target level of 30 ng/mL and a significant reduction in iPTH, without affecting serum calcium or phosphorous levels."( Efficacy and safety of body weight-adapted oral cholecalciferol substitution in dialysis patients with vitamin D deficiency.
Lhotta, K; Mündle, M; Sprenger-Mähr, H; Zitt, E, 2015
)
0.42
" The pharmacokinetics (PK) and pharmacodynamics (PD) models of KRN23 were assessed following subcutaneous dosing every 28 days over an initial 4-month dose escalation (0."( Population pharmacokinetic and pharmacodynamic analyses from a 4-month intradose escalation and its subsequent 12-month dose titration studies for a human monoclonal anti-FGF23 antibody (KRN23) in adults with X-linked hypophosphatemia.
Carpenter, TO; Gosselin, NH; Imel, EA; Marier, JF; Peyret, T; Zhang, X, 2016
)
0.43
"The best repletion and maintenance dosing regimens with cholecalciferol in vitamin D-deficient HIV-1 patients remain unknown."( An oral high dose of cholecalciferol restores vitamin D status in deficient postmenopausal HIV-1-infected women independently of protease inhibitors therapy: a pilot study.
Biondi, P; Cilli, M; Cipriani, C; Di Traglia, M; Diacinti, D; Falciano, M; Fantauzzi, A; Mezzaroma, I; Minisola, S; Pepe, J; Salotti, A, 2016
)
0.43
"05); the median dosing interval was 6 months (range, 1 to 25."( Short-Term Safety of Zoledronic Acid in Young Patients With Bone Disorders: An Extensive Institutional Experience.
George, S; Hummel, K; Kaplan, P; Levine, MA; Monk, HM; Weber, DR, 2015
)
0.42
" Supplementary dietary cholecalciferol (25-hydroxyvitamin D, 25-OH), the precursor of calcitriol, is commonly employed to combat this problem; however, dosage must be carefully determined as excess dietary vitamin D can cause toxicity resulting in a decrease in bone calcification, hypercalcinemia and renal failure."( Super pharmacological levels of calcitriol (1,25-(OH)2D3) inhibits mineral deposition and decreases cell proliferation in a strain dependent manner in chicken mesenchymal stem cells undergoing osteogenic differentiation in vitro.
Bhanugopan, MS; Chousalkar, KC; Pande, VV; Quinn, JC, 2015
)
0.92
" However, no consistent differences between routes of administration, frequencies of dosing or vitamin D preparations were demonstrated."( Interventions for metabolic bone disease in children with chronic kidney disease.
Craig, JC; Hahn, D; Hodson, EM, 2015
)
0.42
" doses (2, 60, and 120 pmol) and the rebound in 1,25(OH)2D3 tissue concentrations after dosing termination."( Physiologically-Based Pharmacokinetic-Pharmacodynamic Modeling of 1α,25-Dihydroxyvitamin D3 in Mice.
Cao, Y; Chow, EC; Mager, DE; Pang, KS; Quach, HP; Ramakrishnan, V; Yang, QJ, 2016
)
0.43
"Intermittent dosing may improve adherence to vitamin D therapy."( How well are the optimal serum 25OHD concentrations reached in high-dose intermittent vitamin D therapy? a placebo-controlled study on comparison between 100 000 IU and 200 000 IU of oral D3 every 3 months in elderly women.
Löyttyniemi, E; Pekkarinen, T; Välimäki, MJ; Välimäki, VV, 2016
)
0.43
"Hemodialysis patients were enrolled and dosed with 110, 220, 330, 440, or 550 ng of 2MD orally thrice weekly for 4 weeks."( Use of 2MD, a Novel Oral Calcitriol Analog, in Hemodialysis Patients with Secondary Hyperparathyroidism.
Clagett-Dame, M; Coyne, DW; DeLuca, HF; Pandey, R; Plum, LA; Zella, J, 2016
)
0.74
" Due to the availability of new dosages during the 6-year time period of the study, the dose could be and was adjusted for most patients to a daily dosing regimen."( Therapy of Hypoparathyroidism With PTH(1-84): A Prospective Six Year Investigation of Efficacy and Safety.
Bilezikian, JP; Costa, AG; Cremers, S; Cusano, NE; Delgado, Y; Dworakowski, E; Fan, WW; Rubin, MR; Zhang, C, 2016
)
0.43
" However, it is unclear whether supplementation dosage or route of administration should be altered due to this state."( Vitamin D and micro-inflammatory state in hemodialysis patients: a mini review and meta-analysis.
Hu, GC; Huang, L; Zhao, YJ; Zhou, J,
)
0.13
"According to our study, calcitriol in equal dosage is more effective than alfacalcidol in lowering serum PTH level in chronic hemodialysis patients."( Conversion of oral alfacalcidol to oral calcitriol in the treatment of secondary hyperparathyroidism in chronic hemodialysis patients.
Bell, RZ; Bezzaoucha, S; Desforges, K; Lafrance, JP; Lamarche, C; Leblanc, M; Lepage, L; Ouellet, G; Ouimet, D; Pichette, V; Rauscher, S; Vallee, M, 2017
)
1.03
" Serum PTH remained suppressed during the dosing period, but tended to rebound in the paricalcitol groups."( Vitamin D receptor agonist VS-105 directly modulates parathyroid hormone expression in human parathyroid cells and in 5/6 nephrectomized rats.
Chen, YW; Fukagawa, M; Kakuta, T; Kanai, G; Sawada, K; Wessale, JL; Wu-Wong, JR, 2017
)
0.46
" Univariate correlation and multivariable linear regression model showed that oral calcitriol dosage and treatment duration were independently correlated to oxyphil cell ratio."( Comparative proteomic analysis of chief and oxyphil cell nodules in refractory uremic hyperparathyroidism by iTRAQ coupled LC-MS/MS.
Chen, J; Huang, B; Li, S; Mao, J; Ni, L; Tao, Y; Wang, M; Zhang, M, 2018
)
0.71
" FGF23 failed to regulate the expression of any of the studied hydroxylases at the used dosage and treatment length."( Regulation of vitamin D metabolizing enzymes in murine renal and extrarenal tissues by dietary phosphate, FGF23, and 1,25(OH)2D3.
Bettoni, C; Hernando, N; Kägi, L; Pastor-Arroyo, EM; Schnitzbauer, U; Wagner, CA, 2018
)
0.48
"In general, chronotherapy is desirable for a more effective and/or safe dosage regimen."( Chronotherapy of maxacalcitol on skin inflammation induced by topical 12-O-tetradecanoylphorbol-13-acetate in mice.
Ando, H; Fujimura, A; Kumazaki, M; Ushijima, K; Yoshioka, D, 2018
)
0.48
" Furthermore, several studies suggest that lower 25(OH)D serum levels are associated with an increased risk of respiratory infection at all ages in a dose-response manner."( Vitamin D: Immunomodulatory Aspects.
Indolfi, C; Miraglia Del Giudice, M; Strisciuglio, C,
)
0.13
"Two chromatographic methods were developed, optimized and validated for simultaneous determination of calcipotriol monohydrate (CPM) and betamethasone dipropionate (BMD) in the presence of two dosage form additives named; butylated hydroxytoluene (BHT) and alpha-tocopherol (TOCO)."( Validated Chromatographic Methods for Simultaneous Determination of Calcipotriol Monohydrate and Betamethasone Dipropionate in the Presence of Two Dosage Form Additives.
El-Mosallamy, SS; El-Zeany, BA; Hassan, NY; Merey, HA, 2019
)
0.51
" Improvement in PCS was greater in patients whose calcitriol dosage was reduced and duration of disease was shorter."( Quality of Life in Hypoparathyroidism Improves With rhPTH(1-84) Throughout 8 Years of Therapy.
Almonte, MG; Bilezikian, JP; Cusano, NE; Majeed, R; Omeragic, B; Rubin, MR; Tabacco, G; Tay, YD; Williams, J, 2019
)
0.77
"In this systematic review and meta-analysis, neither intermittent nor daily dosing with standard doses of vitamin D alone was associated with reduced risk of fracture, but daily supplementation with both vitamin D and calcium was a more promising strategy."( Vitamin D and Calcium for the Prevention of Fracture: A Systematic Review and Meta-analysis.
Armitage, J; Bennett, D; Chen, Z; Clarke, R; Lin, X; Mafham, M; Yao, P, 2019
)
0.51
" Vitamin D deficiency appears to affect pregnancy outcomes, yet randomized controlled trials of vitamin D supplementation achieve mixed results depending on when supplementation is initiated during pregnancy, the dose and dosing interval, and the degree of deficiency at the onset of pregnancy."( Early-Life Effects of Vitamin D: A Focus on Pregnancy and Lactation.
Hollis, BW; Wagner, CL, 2020
)
0.56
"We conclude that the effects and dose-response of PTH 1-34 treatment differ according to the etiology of hypoparathyroidism."( Therapy with PTH 1-34 or calcitriol and calcium in diverse etiologies of hypoparathyroidism over 27 years at a single tertiary care center.
Cutler, GB; Ferré, EMN; Lionakis, MS; Schmitt, MM; Winer, KK; Ye, S; Zhang, B, 2021
)
0.92
" Calcitriol supplementation to vitamin D-deficient rats at the dosage used augmented endothelium-dependent contraction, possibly due to hypercalcaemia."( Vitamin D deficiency attenuates endothelial function by reducing antioxidant activity and vascular eNOS expression in the rat microcirculation.
Banga Singh, KK; Mokhtar, SS; Rasool, AHG; Wee, CL, 2021
)
1.53
" Improvements in disease severity outcomes were maintained after reducing Cal/BD dosing frequency."( Adjunctive Use of Calcipotriene 0.005%/Betamethasone Dipropionate 0.064% Foam in Patients With Psoriasis Treated With Ixekizumab.
Bagel, J; Nelson, E, 2022
)
0.72
" Twice-weekly maintenance application of topical Cal/BD aerosolized foam has recently been shown to prolong time to remission and is associated with fewer relapses in patients initially treated with standard dosing of the formulation."( The Maintenance Effect of Calcipotriene 0.05% and Betamethasone Dipropionate 0.064% (Cal/BD) Aerosol Foam in Combination With Apremilast.
Kircik, L; Ozyurekoglu, E, 2022
)
0.72
" Further logistic regression analysis and restricted cubic spline model revealed dose-response relationship between cumulative dose of phosphate supplementation and PTH levels."( Hyperparathyroidism in a Large Cohort of Chinese Patients With Tumor-induced Osteomalacia.
Chi, Y; Cui, L; Feng, J; Gong, Y; Huo, L; Jiajue, R; Jiang, Y; Jin, C; Jin, J; Li, M; Li, X; Liu, W; Liu, Y; Lv, W; Ni, X; Pang, Q; Wang, O; Wu, H; Xia, W; Xia, Y; Xing, X; Yu, W; Zhang, D; Zhou, L; Zhou, X, 2023
)
0.91
" A water-free lipid-based formulation system has been developed to improve dosage and cosmetic properties along with patient compliance."( Efficacy and Safety of Water-Free Lipid Formulation System Containing Calcipotriol Against Psoriasis Vulgaris.
Carlsson, A; Holmback, J; Rinwa, P, 2023
)
0.91
" After three days in the hospital, the patient's initial symptoms subsided, resulting in discharge with a prescription of ongoing oral medications including Calcium Carbonate and Vitamin D3 Tablets, Calcitriol Soft Capsules, and Potassium Aspartate and Magnesium Aspartate Tablets, with the same usage and dosage as the above three drugs."( Hypomagnesemia with Secondary Hypocalcemia (HSH): a Case Report.
Jiang, Z; Lin, Y; Zhao, C, 2023
)
1.1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Occurs in Manufacturing (1 Product(s))

Product Categories

Product CategoryProducts
Food & Beverages1

Products

ProductBrandCategoryCompounds Matched from IngredientsDate Retrieved
Orrington Farms Broth Base & Seasoning Chicken -- 12 ozOrrington FarmsFood & Beverages Vit D, maltodextrin, sugar2024-11-29 10:47:42

Roles (11)

RoleDescription
bone density conservation agentAn agent that inhibits bone resorption and/or favor bone mineralization and bone regeneration. Used to heal bone fractures and to treat bone diseases such as osteopenia and osteoporosis.
antipsoriaticA drug used to treat psoriasis.
immunomodulatorBiologically active substance whose activity affects or plays a role in the functioning of the immune system.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
calcium channel modulatorA membrane transport modulator that is able to regulate intracellular calcium levels.
nutraceuticalA product in capsule, tablet or liquid form that provide essential nutrients, such as a vitamin, an essential mineral, a protein, an herb, or similar nutritional substance.
calcium channel agonistAgents that increase calcium influx into calcium channels of excitable tissues.
metaboliteAny intermediate or product resulting from metabolism. The term 'metabolite' subsumes the classes commonly known as primary and secondary metabolites.
hormoneOriginally referring to an endogenous compound that is formed in specialized organ or group of cells and carried to another organ or group of cells, in the same organism, upon which it has a specific regulatory function, the term is now commonly used to include non-endogenous, semi-synthetic and fully synthetic analogues of such compounds.
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
hydroxycalciol
D3 vitaminsA vitamin D that is calciol or its hydroxylated metabolites calcidiol and calcitriol. Calciol (also known as vitamin D3) acts as a hormone precursor, being hydroxylated in the liver to calcidiol (25-hydroxyvitamin D3), which is then further hydroxylated in the kidney to give calcitriol (1,25-dihydroxyvitamin D3), the active hormone.
triolA chemical compound containing three hydroxy groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (20)

PathwayProteinsCompounds
Metabolism14961108
Metabolism of lipids500463
Metabolism of steroids111135
Vitamin D (calciferol) metabolism1210
Biological oxidations150276
Phase I - Functionalization of compounds69175
Cytochrome P450 - arranged by substrate type30110
Vitamins415
Disease1278231
Diseases of metabolism69121
Metabolic disorders of biological oxidation enzymes647
Defective CYP24A1 causes HCAI04
Renin-angiotensin pathway (COVID-19 Disease Map)116
Non-classical role of vitamin D86
Vitamin D metabolism19
Nuclear receptors in lipid metabolism and toxicity03
Biochemical pathways: part I0466
Regulation of Wnt / B-catenin signaling by small molecule compounds010
PI3K/AKT/mTOR - vitamin D3 signaling07
Non-genomic actions of 1,25 dihydroxyvitamin D364

Protein Targets (34)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency19.95260.044717.8581100.0000AID485341
Chain A, Ferritin light chainEquus caballus (horse)Potency10.00005.623417.292931.6228AID485281
USP1 protein, partialHomo sapiens (human)Potency56.23410.031637.5844354.8130AID504865
PPM1D proteinHomo sapiens (human)Potency32.99930.00529.466132.9993AID1347411
Microtubule-associated protein tauHomo sapiens (human)Potency22.38720.180013.557439.8107AID1460
thioredoxin glutathione reductaseSchistosoma mansoniPotency39.81070.100022.9075100.0000AID485364
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency28.18380.035520.977089.1251AID504332
mitogen-activated protein kinase 1Homo sapiens (human)Potency25.11890.039816.784239.8107AID1454
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency13.45740.00798.23321,122.0200AID2546; AID2551
gemininHomo sapiens (human)Potency21.13600.004611.374133.4983AID624296
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.00570.005612.367736.1254AID624032
Interferon betaHomo sapiens (human)Potency32.99930.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)39.70000.11007.190310.0000AID1473738
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)0.00930.00011.753610.0000AID775184
Cytochrome P450 3A4Homo sapiens (human)Ki0.00010.00011.41629.9000AID619442
Androgen receptorHomo sapiens (human)IC50 (µMol)10.00000.00000.875310.0000AID730427
Cytochrome P450 2D6Homo sapiens (human)Ki0.00010.00011.19868.0000AID619442
Vitamin D3 receptorHomo sapiens (human)IC50 (µMol)0.34010.00000.43746.4300AID1140744; AID1254251; AID1266893; AID1267638; AID1267646; AID1375582; AID1408600; AID1408602; AID1417060; AID1455879; AID1465610; AID1505674; AID1506107; AID1852315; AID274535; AID302664; AID488356; AID703638; AID775184
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)0.00930.00002.800510.0000AID775184
Vitamin D3 receptorRattus norvegicus (Norway rat)Ki0.00010.00000.00010.0002AID1235843; AID1267774; AID351849; AID387114; AID392905; AID455160; AID547391; AID547392; AID619442; AID635571; AID672798
Cytochrome P450 2C19Homo sapiens (human)Ki0.00010.00010.830010.0000AID619442
Vitamin D3 receptorBos taurus (cattle)IC50 (µMol)0.00000.00000.00000.0000AID1744118
TransporterRattus norvegicus (Norway rat)Ki0.00010.00010.76295.5000AID635571
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Vitamin D Nuclear ReceptorHomo sapiens (human)Kd0.00050.00050.00050.0005AID977611
Vitamin D3 receptorSus scrofa (pig)Kd0.00010.00010.00010.0001AID472015
Vitamin D-binding proteinHomo sapiens (human)Kd0.02400.02400.02400.0240AID472017
Vitamin D3 receptorHomo sapiens (human)EC50 (µMol)0.03940.00000.14232.1400AID1191646; AID1251250; AID1251254; AID1266894; AID1267641; AID1267643; AID1309798; AID1309799; AID1309800; AID1310892; AID1375589; AID1408601; AID1455877; AID1506105; AID1506106; AID1585399; AID1686027; AID1744114; AID1744119; AID1744120; AID280115; AID321740; AID321741; AID321742; AID326338; AID326340; AID414864; AID414865; AID622098; AID702757; AID702758; AID703640; AID730431; AID760217; AID761797; AID775185
Vitamin D3 receptorHomo sapiens (human)Kd0.00010.00012.46269.5200AID217167
Vitamin D3 receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00020.00000.00020.0003AID303407; AID303411; AID326337; AID387116; AID392907; AID455164; AID635522
Retinoic acid receptor RXR-alphaHomo sapiens (human)EC50 (µMol)0.00160.00010.34279.1000AID1408601
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.00000.00000.20671.4454AID622098
Vitamin D3 receptorMus musculus (house mouse)EC50 (µMol)0.10000.00770.40190.9000AID1585872
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)EC50 (µMol)0.00300.00300.00300.0030AID1852313
Vitamin D3 receptorBos taurus (cattle)EC50 (µMol)0.00010.00000.00010.0001AID280114; AID366868
Vitamin D3 receptor ADanio rerio (zebrafish)EC50 (µMol)0.00550.00550.00550.0055AID1118427
Vitamin D3 receptor ADanio rerio (zebrafish)Kd1.20001.20001.20001.2000AID1661608
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)ED500.00020.00020.00020.0002AID619491
Cytochrome P450 3A4Homo sapiens (human)ED500.00020.00020.00020.0002AID619491
Vitamin D3 receptorHomo sapiens (human)ED500.10070.00050.14280.4100AID274536; AID274537; AID282483; AID302663
Cytochrome P450 2C9 Homo sapiens (human)ED500.00020.00020.00020.0002AID619491
Vitamin D3 receptorRattus norvegicus (Norway rat)ED50500,000.00020.00020.00030.0004AID1267778; AID216837; AID217013; AID228001; AID619491; AID672800
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (205)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
vitamin transmembrane transportVitamin D-binding proteinHomo sapiens (human)
vitamin D metabolic processVitamin D-binding proteinHomo sapiens (human)
vitamin transportVitamin D-binding proteinHomo sapiens (human)
transportVitamin D-binding proteinHomo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
MAPK cascadeAndrogen receptorHomo sapiens (human)
in utero embryonic developmentAndrogen receptorHomo sapiens (human)
regulation of systemic arterial blood pressureAndrogen receptorHomo sapiens (human)
epithelial cell morphogenesisAndrogen receptorHomo sapiens (human)
transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
signal transductionAndrogen receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAndrogen receptorHomo sapiens (human)
cell-cell signalingAndrogen receptorHomo sapiens (human)
spermatogenesisAndrogen receptorHomo sapiens (human)
single fertilizationAndrogen receptorHomo sapiens (human)
positive regulation of cell population proliferationAndrogen receptorHomo sapiens (human)
negative regulation of cell population proliferationAndrogen receptorHomo sapiens (human)
positive regulation of gene expressionAndrogen receptorHomo sapiens (human)
male somatic sex determinationAndrogen receptorHomo sapiens (human)
intracellular estrogen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
androgen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
intracellular receptor signaling pathwayAndrogen receptorHomo sapiens (human)
positive regulation of intracellular estrogen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
Leydig cell differentiationAndrogen receptorHomo sapiens (human)
multicellular organism growthAndrogen receptorHomo sapiens (human)
positive regulation of phosphorylationAndrogen receptorHomo sapiens (human)
positive regulation of MAPK cascadeAndrogen receptorHomo sapiens (human)
positive regulation of insulin-like growth factor receptor signaling pathwayAndrogen receptorHomo sapiens (human)
positive regulation of cell differentiationAndrogen receptorHomo sapiens (human)
negative regulation of integrin biosynthetic processAndrogen receptorHomo sapiens (human)
positive regulation of integrin biosynthetic processAndrogen receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionAndrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIAndrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIIAndrogen receptorHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayAndrogen receptorHomo sapiens (human)
regulation of developmental growthAndrogen receptorHomo sapiens (human)
animal organ formationAndrogen receptorHomo sapiens (human)
male genitalia morphogenesisAndrogen receptorHomo sapiens (human)
epithelial cell proliferationAndrogen receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationAndrogen receptorHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityAndrogen receptorHomo sapiens (human)
activation of prostate induction by androgen receptor signaling pathwayAndrogen receptorHomo sapiens (human)
morphogenesis of an epithelial foldAndrogen receptorHomo sapiens (human)
lateral sprouting involved in mammary gland duct morphogenesisAndrogen receptorHomo sapiens (human)
prostate gland growthAndrogen receptorHomo sapiens (human)
prostate gland epithelium morphogenesisAndrogen receptorHomo sapiens (human)
epithelial cell differentiation involved in prostate gland developmentAndrogen receptorHomo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesisAndrogen receptorHomo sapiens (human)
mammary gland alveolus developmentAndrogen receptorHomo sapiens (human)
positive regulation of epithelial cell proliferation involved in prostate gland developmentAndrogen receptorHomo sapiens (human)
cellular response to steroid hormone stimulusAndrogen receptorHomo sapiens (human)
cellular response to estrogen stimulusAndrogen receptorHomo sapiens (human)
cellular response to testosterone stimulusAndrogen receptorHomo sapiens (human)
seminiferous tubule developmentAndrogen receptorHomo sapiens (human)
non-membrane-bounded organelle assemblyAndrogen receptorHomo sapiens (human)
positive regulation of miRNA transcriptionAndrogen receptorHomo sapiens (human)
regulation of protein localization to plasma membraneAndrogen receptorHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayAndrogen receptorHomo sapiens (human)
male gonad developmentAndrogen receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayAndrogen receptorHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of DNA-templated transcriptionVitamin D3 receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIVitamin D3 receptorHomo sapiens (human)
cell morphogenesisVitamin D3 receptorHomo sapiens (human)
skeletal system developmentVitamin D3 receptorHomo sapiens (human)
calcium ion transportVitamin D3 receptorHomo sapiens (human)
intracellular calcium ion homeostasisVitamin D3 receptorHomo sapiens (human)
lactationVitamin D3 receptorHomo sapiens (human)
negative regulation of cell population proliferationVitamin D3 receptorHomo sapiens (human)
positive regulation of gene expressionVitamin D3 receptorHomo sapiens (human)
negative regulation of keratinocyte proliferationVitamin D3 receptorHomo sapiens (human)
positive regulation of vitamin D 24-hydroxylase activityVitamin D3 receptorHomo sapiens (human)
positive regulation of bone mineralizationVitamin D3 receptorHomo sapiens (human)
phosphate ion transmembrane transportVitamin D3 receptorHomo sapiens (human)
bile acid signaling pathwayVitamin D3 receptorHomo sapiens (human)
mRNA transcription by RNA polymerase IIVitamin D3 receptorHomo sapiens (human)
positive regulation of keratinocyte differentiationVitamin D3 receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIVitamin D3 receptorHomo sapiens (human)
decidualizationVitamin D3 receptorHomo sapiens (human)
intestinal absorptionVitamin D3 receptorHomo sapiens (human)
apoptotic process involved in mammary gland involutionVitamin D3 receptorHomo sapiens (human)
positive regulation of apoptotic process involved in mammary gland involutionVitamin D3 receptorHomo sapiens (human)
regulation of calcidiol 1-monooxygenase activityVitamin D3 receptorHomo sapiens (human)
mammary gland branching involved in pregnancyVitamin D3 receptorHomo sapiens (human)
vitamin D receptor signaling pathwayVitamin D3 receptorHomo sapiens (human)
positive regulation of vitamin D receptor signaling pathwayVitamin D3 receptorHomo sapiens (human)
response to bile acidVitamin D3 receptorHomo sapiens (human)
multicellular organism developmentVitamin D3 receptorHomo sapiens (human)
cell differentiationVitamin D3 receptorHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
positive regulation of cholesterol effluxRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIRetinoic acid receptor RXR-alphaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of thyroid hormone mediated signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
hormone-mediated signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of bone mineralizationRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of transporter activityRetinoic acid receptor RXR-alphaHomo sapiens (human)
response to retinoic acidRetinoic acid receptor RXR-alphaHomo sapiens (human)
peroxisome proliferator activated receptor signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
mRNA transcription by RNA polymerase IIRetinoic acid receptor RXR-alphaHomo sapiens (human)
steroid hormone mediated signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIRetinoic acid receptor RXR-alphaHomo sapiens (human)
retinoic acid receptor signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
positive regulation of vitamin D receptor signaling pathwayRetinoic acid receptor RXR-alphaHomo sapiens (human)
cell differentiationRetinoic acid receptor RXR-alphaHomo sapiens (human)
anatomical structure developmentRetinoic acid receptor RXR-alphaHomo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
osteoblast differentiation1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
vitamin metabolic process1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
response to vitamin D1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
vitamin D metabolic process1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
vitamin D catabolic process1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
vitamin D receptor signaling pathway1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
vitamin D receptor signaling pathwayVitamin D3 receptorBos taurus (cattle)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (108)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
actin bindingVitamin D-binding proteinHomo sapiens (human)
vitamin transmembrane transporter activityVitamin D-binding proteinHomo sapiens (human)
calcidiol bindingVitamin D-binding proteinHomo sapiens (human)
vitamin D bindingVitamin D-binding proteinHomo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
transcription cis-regulatory region bindingAndrogen receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificAndrogen receptorHomo sapiens (human)
RNA polymerase II general transcription initiation factor bindingAndrogen receptorHomo sapiens (human)
transcription coactivator bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificAndrogen receptorHomo sapiens (human)
chromatin bindingAndrogen receptorHomo sapiens (human)
DNA-binding transcription factor activityAndrogen receptorHomo sapiens (human)
nuclear receptor activityAndrogen receptorHomo sapiens (human)
G protein-coupled receptor activityAndrogen receptorHomo sapiens (human)
signaling receptor bindingAndrogen receptorHomo sapiens (human)
steroid bindingAndrogen receptorHomo sapiens (human)
androgen bindingAndrogen receptorHomo sapiens (human)
protein bindingAndrogen receptorHomo sapiens (human)
beta-catenin bindingAndrogen receptorHomo sapiens (human)
zinc ion bindingAndrogen receptorHomo sapiens (human)
enzyme bindingAndrogen receptorHomo sapiens (human)
ATPase bindingAndrogen receptorHomo sapiens (human)
molecular adaptor activityAndrogen receptorHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingAndrogen receptorHomo sapiens (human)
POU domain bindingAndrogen receptorHomo sapiens (human)
molecular condensate scaffold activityAndrogen receptorHomo sapiens (human)
estrogen response element bindingAndrogen receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
DNA-binding transcription factor activityVitamin D3 receptorHomo sapiens (human)
vitamin D response element bindingVitamin D3 receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificVitamin D3 receptorHomo sapiens (human)
DNA bindingVitamin D3 receptorHomo sapiens (human)
nuclear receptor activityVitamin D3 receptorHomo sapiens (human)
protein bindingVitamin D3 receptorHomo sapiens (human)
zinc ion bindingVitamin D3 receptorHomo sapiens (human)
bile acid nuclear receptor activityVitamin D3 receptorHomo sapiens (human)
nuclear retinoid X receptor bindingVitamin D3 receptorHomo sapiens (human)
calcitriol bindingVitamin D3 receptorHomo sapiens (human)
lithocholic acid bindingVitamin D3 receptorHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingVitamin D3 receptorHomo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
vitamin D response element bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
transcription cis-regulatory region bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificRetinoic acid receptor RXR-alphaHomo sapiens (human)
transcription coregulator bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
retinoic acid bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
double-stranded DNA bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
DNA-binding transcription factor activityRetinoic acid receptor RXR-alphaHomo sapiens (human)
nuclear steroid receptor activityRetinoic acid receptor RXR-alphaHomo sapiens (human)
nuclear receptor activityRetinoic acid receptor RXR-alphaHomo sapiens (human)
protein bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
zinc ion bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
enzyme bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
peptide bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
identical protein bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
nuclear vitamin D receptor bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
sequence-specific DNA bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
retinoic acid-responsive element bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
DNA binding domain bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
LBD domain bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
sequence-specific double-stranded DNA bindingRetinoic acid receptor RXR-alphaHomo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
iron ion binding1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
25-hydroxycholecalciferol-24-hydroxylase activity1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
heme binding1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 24-hydroxylase activity1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
25-hydroxycholecalciferol-23-hydroxylase activity1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
vitamin D 25-hydroxylase activity1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
nuclear receptor activityVitamin D3 receptorBos taurus (cattle)
zinc ion bindingVitamin D3 receptorBos taurus (cattle)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (36)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
extracellular regionVitamin D-binding proteinHomo sapiens (human)
extracellular spaceVitamin D-binding proteinHomo sapiens (human)
cytosolVitamin D-binding proteinHomo sapiens (human)
lysosomal lumenVitamin D-binding proteinHomo sapiens (human)
extracellular exosomeVitamin D-binding proteinHomo sapiens (human)
blood microparticleVitamin D-binding proteinHomo sapiens (human)
cytoplasmVitamin D-binding proteinHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membraneAndrogen receptorHomo sapiens (human)
nucleusAndrogen receptorHomo sapiens (human)
nucleoplasmAndrogen receptorHomo sapiens (human)
cytoplasmAndrogen receptorHomo sapiens (human)
cytosolAndrogen receptorHomo sapiens (human)
nuclear speckAndrogen receptorHomo sapiens (human)
chromatinAndrogen receptorHomo sapiens (human)
protein-containing complexAndrogen receptorHomo sapiens (human)
nucleusAndrogen receptorHomo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
nucleusVitamin D3 receptorHomo sapiens (human)
nucleusVitamin D3 receptorHomo sapiens (human)
nucleoplasmVitamin D3 receptorHomo sapiens (human)
cytosolVitamin D3 receptorHomo sapiens (human)
RNA polymerase II transcription regulator complexVitamin D3 receptorHomo sapiens (human)
chromatinVitamin D3 receptorHomo sapiens (human)
receptor complexVitamin D3 receptorHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
nucleusRetinoic acid receptor RXR-alphaHomo sapiens (human)
nucleoplasmRetinoic acid receptor RXR-alphaHomo sapiens (human)
transcription regulator complexRetinoic acid receptor RXR-alphaHomo sapiens (human)
mitochondrionRetinoic acid receptor RXR-alphaHomo sapiens (human)
cytosolRetinoic acid receptor RXR-alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexRetinoic acid receptor RXR-alphaHomo sapiens (human)
chromatinRetinoic acid receptor RXR-alphaHomo sapiens (human)
receptor complexRetinoic acid receptor RXR-alphaHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
mitochondrial inner membrane1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrialHomo sapiens (human)
cytoplasmVitamin D3 receptorBos taurus (cattle)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (771)

Assay IDTitleYearJournalArticle
AID1661598Binding affinity to H10 region (416 to 426 residues) of zebrafish VDR LBD assessed as stabilization of structural elements at 10 fold excess compound concentration in presence of SRC1 NR2 coactivator peptide measured at 3 and 10 mins by HDX-MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Structural Analysis of VDR Complex with ZK168281 Antagonist.
AID1218496Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as 1alpha,24R,25(OH)3D3 metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID147637Gene transcriptional activity against osteopontin (OPN)1999Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7
Three-dimensional structure-function relationship of vitamin D: side chain location and various activities.
AID352235Effect on intestinal calcium transport in vitamin D-deficient weanling Sprague-Dawley rat assessed as ratio of serosal to mucosal calcium level at 87 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose by everted gut sac2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID1375582Displacement of fluormone from human full length VDR after 2 hrs by fluorescence polarization assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID1375594Agonist activity at VDR in human MCF7 cells assessed as upregulation of p21 expression at 10'-8 M after 48 hrs by Western blot method relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID1375600Agonist activity at VDR in human MCF7 cells assessed as upregulation of p53 expression at 10'-8 M after 48 hrs by Western blot method relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID1235847Induction of transcriptional activity in rat ROS 17/2.8 cells after 16 hrs by 24-hydroxylase luciferase reporter gene assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Novel 9-Alkyl- and 9-Alkylidene-Substituted 1α,25-Dihydroxyvitamin D3 Analogues: Synthesis and Biological Examinations.
AID80964Induced differentiation of human promyelocyte HL-60 cells into monocytes1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
New 1alpha,25-dihydroxy-19-norvitamin D3 compounds of high biological activity: synthesis and biological evaluation of 2-hydroxymethyl, 2-methyl, and 2-methylene analogues.
AID672805Calcium mobilization in vitamin-D deficient weanling Sprague-Dawley rat intestine assessed as increase in serosal/mucosal calcium level at 32 to 7020 pmol, ip administered every 24 hrs for 4 consecutive days measured 24 hrs post last dose by everted gut s2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
A 20S combined with a 22R configuration markedly increases both in vivo and in vitro biological activity of 1α,25-dihydroxy-22-methyl-2-methylene-19-norvitamin D3.
AID1218527Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2D inhibitor quinine2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID303410Ratio of ED50 for drug to 1-alpha,25-dihydroxyvitamin for HL60 cells differentiation by NBT reduction assay2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Design, synthesis, and biological evaluation of a 1alpha,25-dihydroxy-19-norvitamin D3 analogue with a frozen A-ring conformation.
AID216850Percent inhibition of binding to transport protein vitamin D binding protein (DBP)1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Conformationally restricted analogs of 1 alpha, 25-dihydroxyvitamin D3 and its 20-epimer: compounds for study of the three-dimensional structure of vitamin D responsible for binding to the receptor.
AID703624Increase in serum Calcium levels in CD-1 mouse at 0.3 ug/kg, ip administered every other day for 3 weeks measured on day 212012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID619489Induction of human HL60 differentiation assessed as cells reducing nitro blue tetrazolium2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis and biological activity of 2-(3'-hydroxypropylidene)-1α-hydroxy-19-norvitamin D analogues with shortened alkyl side chains.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID387116Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcriptional activation after 16 hrs by luciferase reporter gene assay2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
AID1408639Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as increase in p27 expression at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation by immunohistochemical an2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID224818Bone Calcium-Mobilizing (BCM) activity (260 pmol/day/7 days) in Vitamin D-Deficient Rats on a Low-Calcium Diet2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID352239Effect on intestinal calcium transport in vitamin D-deficient weanling Sprague-Dawley rat assessed as increase in ratio of serosal to mucosal calcium level at 7020 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose by e2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID305710Antiproliferative activity against human HL60 cells assessed NBT positive cells at 0.02 uM after 72 hrs by NBT reduction test2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Rotenoids and flavonoids with anti-invasion of HT1080, anti-proliferation of U937, and differentiation-inducing activity in HL-60 from Erycibe expansa.
AID1585864Inhibition of Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as reduction in oxysterol-induced Gli1 mRNA expression at 1 uM after 24 hrs by q-PCR analysis relative to oxysterol alone2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID1375597Agonist activity at VDR in human MCF7 cells assessed as upregulation of p27 expression at 10'-8 M after 48 hrs by Western blot method relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID775182Induction of human HL60 cell differentiation after 4 days by NBT reduction assay2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Synthesis of VS-105: A novel and potent vitamin D receptor agonist with reduced hypercalcemic effects.
AID1613163Cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 1 uM after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 31.32%)2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID688520Toxicity in mouse assessed as increase in plasma calcium level at 5 ug/kg, ip qd for 4 days measured after 24 to 96 hrs postdose2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of a new vitamin D2 analogue.
AID152813In vitro inhibition of phytohemagglutininin-induced stimulation of human peripheral blood mononuclear cells proliferation2000Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19
Conceptually new 20-epi-22-oxa sulfone analogues of the hormone 1alpha,25-dihydroxyvitamin D(3): synthesis and biological evaluation.
AID1506119Drug uptake in human MG63 cells at 1 uM after 10 mins by HPLC analysis2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
25 S-Adamantyl-23-yne-26,27-dinor-1α,25-dihydroxyvitamin D
AID169314Calcemic activity (in vivo bone calcium mobilization) was measured by the rise in serum calcium in vitamin D and Ca deficient rats by colorimetric assay2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Rational design, synthesis, and biological activity of novel conformationally restricted vitamin D analogues, (22R)- and (22S)-22-ethyl-1,25-dihydroxy-23,24-didehydro-24a,24b-dihomo-20-epivitamin D(3).
AID1267151Effect on bone calcium mobilization in weanling Sprague-Dawley rat assessed as serum calcium level at 780 pmol/day administered as 4 consecutive daily doses measured 24 hrs after last dose relative to control2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis and Biological Activity of 2-Methylene Analogues of Calcitriol and Related Compounds.
AID1465610Displacement of [3H]-1,25-(OH)2D3 from N-terminal GST-tagged human recombinant vitamin D receptor ligand binding domain expressed in Escherichia coli BL21 (DE3) pLys S after 16 hrs2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Vitamin D Analogues with a p-Hydroxyphenyl Group at the C25 Position: Crystal Structure of Vitamin D Receptor Ligand-Binding Domain Complexed with the Ligand Explains the Mechanism Underlying Full Antagonistic Action.
AID702758Transactivation of GAL4-fused VDR ligand binding domain expressed in human HeLa cells after 16 hrs by luciferase reporter gene assay2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Structural basis for the accommodation of bis- and tris-aromatic derivatives in vitamin D nuclear receptor.
AID230235Intestinal Calcium Transport (ICT) activity (260 pmol/day/7 days) in Vitamin D-Deficient Rats on a Low-Calcium Diet2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID321740Effect on VDR transcriptional activity in human osteosarcoma cells2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
(2S,2'R)-analogue of LG190178 is a major active isomer.
AID282483Effect on VDR-mediated transcriptional activity in CV1 cells transfected with human recombinant VDR2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Potent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3).
AID1267646Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with NCoR assessed as decrease in NCoR recruitment by two-hybrid assay2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis, Biological Activities, and X-ray Crystal Structural Analysis of 25-Hydroxy-25(or 26)-adamantyl-17-[20(22),23-diynyl]-21-norvitamin D Compounds.
AID672799Induction of human HL60 cell differentiation after 4 days by NBT reduction assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
A 20S combined with a 22R configuration markedly increases both in vivo and in vitro biological activity of 1α,25-dihydroxy-22-methyl-2-methylene-19-norvitamin D3.
AID337282Induction of terminal cell differentiation in human HL60 cells assessed as inhibition of [3H]thymidine incorporation at 0.001 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID414866Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression at EC50 upto 5 hrs by RT-PCR2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
AID1254251Displacement of [3H]-1alpha,25-dihydroxyvitamin D3 from recombinant human VDR LBD expressed in Escherichia coli BL21 (DE3) pLysS after 16 hrs2015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Fine tuning of agonistic/antagonistic activity for vitamin D receptor by 22-alkyl chain length of ligands: 22S-Hexyl compound unexpectedly restored agonistic activity.
AID688528Cmax in mouse at 5 ug/kg2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of a new vitamin D2 analogue.
AID1267785Induction of intestinal calcium transport in weaning Sprague-Dawley rat assessed as ratio of calcium level in serosal to mucosal at 16 pmol, ip for 4 consecutive dose at an interval of 24 hrs measured 24 hrs after last dose (Rvb = 3.7 to 4.8 No_unit)2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
A Methylene Group on C-2 of 24,24-Difluoro-19-nor-1α,25-dihydroxyvitamin D3 Markedly Increases Bone Calcium Mobilization in Vivo.
AID1118429Antiproliferative activity against ER positive human MCF10AT1 cells after 3 days by [3H]thymidine uptake assay2011MedChemComm, , Volume: 2, Issue:5
Structure-function study of gemini derivatives with two different side chains at C-20, Gemini-0072 and Gemini-0097.
AID760210Toxicity in ovariectomized Sprague-Dawley rat osteoporosis model assessed as increase in serum Ca level at 0.025 mg/kg/day administered 5 times a week for 4 weeks measured 24 hrs post last dose (Rvb = 9.14 +/- 0.24 mg/dL)2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Synthesis of 2α-heteroarylalkyl active vitamin d3 with therapeutic effect on enhancing bone mineral density in vivo.
AID392912Ratio of EC50 of drug to EC50 of [3H]1-alpha,25-(OH)2D3 for induction of cell differentiation of human HL60 cells to monocytes by NBT reduction assay2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID351856Effect on bone calcium mobilization in vitamin D-deficient weanling Sprague-Dawley rat assessed as serum calcium level at 260 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID527089Agonist activity at VDR in human SCC25 cells assessed as induction of TSLP expression at 100 nM2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
An o-aminoanilide analogue of 1α,25-dihydroxyvitamin D(3) functions as a strong vitamin D receptor antagonist.
AID130084Dose required to induce hypercalcemia after administration in mice2001Bioorganic & medicinal chemistry letters, Jan-08, Volume: 11, Issue:1
Synthesis and biological activity of the 1alpha,25-dihydroxyvitamin D3 diastereomer with unnatural configuration at the rings C/D side-chain moiety.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID352234Effect on bone calcium mobilization in vitamin D-deficient weanling Sprague-Dawley rat assessed as serum calcium level at 35100 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID171377Intestinal calcium transport at dose 260 (pmol)2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
2-Ethyl and 2-ethylidene analogues of 1alpha,25-dihydroxy-19-norvitamin D(3): synthesis, conformational analysis, biological activities, and docking to the modeled rVDR ligand binding domain.
AID280115Induction of transactivation of human VDR responsive gene in COS7 cells by rat osteopontin luciferase reporter gene assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
22-Alkyl-20-epi-1alpha,25-dihydroxyvitamin D3 compounds of superagonistic activity: syntheses, biological activities and interaction with the receptor.
AID171376Intestinal calcium transport at dose 130 (pmol)2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
2-Ethyl and 2-ethylidene analogues of 1alpha,25-dihydroxy-19-norvitamin D(3): synthesis, conformational analysis, biological activities, and docking to the modeled rVDR ligand binding domain.
AID303407Displacement of 1-alpha,25-dihydroxyvitamin from rat recombinant VDR2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Design, synthesis, and biological evaluation of a 1alpha,25-dihydroxy-19-norvitamin D3 analogue with a frozen A-ring conformation.
AID337274Induction of terminal cell differentiation in human HL60 cells at 0.1 uM after 4 days by NBT reduction assay1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID196186Serum Calcium Transport mobilization response of Vitamin D-Deficient Rats on a low-calcium diet(amount 500 pmol)1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis and biological activity of 1 alpha, 25-dihydroxy-18-norvitamin D3 and 1 alpha, 25-dihydroxy-18,19-dinorvitamin D3.
AID488261Toxicity in FVB mouse assessed as calcium level in blood at 24 pmol/day administered via osmotic pump for 6 to 7 days measured on day 7 by microchemistry (RVb = 2.0.6 mmol/L)2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID190603Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 500 pmol at 2 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID455166Effect on bone calcium mobilization in weanling Sprague-Dawley rat assessed as serum calcium level at 87 pmol/day, ip administered for 4 consecutive days measured 24 hrs after last dose2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID190749Bone calcium mobilization in rats maintained on a very low calcium diet at a dose 260 (pmol)2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
2-Ethyl and 2-ethylidene analogues of 1alpha,25-dihydroxy-19-norvitamin D(3): synthesis, conformational analysis, biological activities, and docking to the modeled rVDR ligand binding domain.
AID195595Patch clamp determination of calcium current in rat Osteosarcoma cells at 0.5 nM1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
1 alpha,25-dihydroxyvitamin D3 analogs featuring aromatic and heteroaromatic rings: design, synthesis, and preliminary biological testing.
AID171510Support of intestinal calcium transport measured in vitamin D-deficient rats on a low-calcium diet(260)1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
New 1alpha,25-dihydroxy-19-norvitamin D3 compounds of high biological activity: synthesis and biological evaluation of 2-hydroxymethyl, 2-methyl, and 2-methylene analogues.
AID190751Bone calcium mobilization measured in vitamin D-deficient rats on a low-calcium diet(260)1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
New 1alpha,25-dihydroxy-19-norvitamin D3 compounds of high biological activity: synthesis and biological evaluation of 2-hydroxymethyl, 2-methyl, and 2-methylene analogues.
AID191115Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 50 pmol at 48 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID635526Calcium mobilization in vitamin-D deficient weanling rat bone assessed as increase in serum calcium level at 2.1 ug/kg, ip administered daily for 7 consecutive days measured 24 hrs after last dose relative to vehicle treated control2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.
AID1267781Induction of bone mobilization activity in weaning Sprague-Dawley rat assessed as increase in serum calcium level at 87 pmol, ip for 4 consecutive dose at an interval of 24 hrs measured 24 hrs after last dose (Rvb = 4.4 to 4.5 mg/dl)2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
A Methylene Group on C-2 of 24,24-Difluoro-19-nor-1α,25-dihydroxyvitamin D3 Markedly Increases Bone Calcium Mobilization in Vivo.
AID216720Inhibition of 1-alpha,25-(OH)2D3 binding to porcine intestinal vitamin D receptor1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
New 1alpha,25-dihydroxy-19-norvitamin D3 compounds of high biological activity: synthesis and biological evaluation of 2-hydroxymethyl, 2-methyl, and 2-methylene analogues.
AID1455877Agonist activity at VDR in human HL60 cells assessed as induction of cell differentiation after 96 hrs by NBT assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID1235845Induction of differentiation of human HL60 promyelocytes to monocytes after 4 days by nitro blue tetrazolium reduction assay2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Novel 9-Alkyl- and 9-Alkylidene-Substituted 1α,25-Dihydroxyvitamin D3 Analogues: Synthesis and Biological Examinations.
AID1266896Antipoliferative activity against human MCF7 cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.
AID337023Induction of cell differentiation in human HL60 cells assessed as alpha naphthyl esterase activity at 0.01 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID280120Effect on bone calcium mobilization in low-calcium diet fed rat at 100 pmol/day, ip after 7 days2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
22-Alkyl-20-epi-1alpha,25-dihydroxyvitamin D3 compounds of superagonistic activity: syntheses, biological activities and interaction with the receptor.
AID190607Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 500 pmol at 69 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID303411Activity at VDR in rat osteosarcoma cells assessed as 24-hydroxylase transcription by reporter gene assay2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Design, synthesis, and biological evaluation of a 1alpha,25-dihydroxy-19-norvitamin D3 analogue with a frozen A-ring conformation.
AID1585872Activation of VDR in mouse ASZ001 cells assessed as change in Cyp24A1 mRNA expression after 48 hrs by q-PCR analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID1408640Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as increase in Bax expression at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation by immunohistochemical an2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID1585880Inhibition of Hedgehog signaling pathway in VDR-deficient mouse C3H10T1/2 cells assessed as reduction in oxysterol-induced Gli1 mRNA expression at 1 uM after 24 hrs by q-PCR analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID1408609Cell cycle arrest in human MCF7 cells expressing VDR siRNA assessed as accumulation at S phase at 1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 32%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID191095Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5000 pmol at 2 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID3205Relative competitive index values for binding to 25-OH-D3-1-hydroxylase of chick intestine1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Arocalciferols: synthesis and biological evaluation of aromatic side-chain analogues of 1 alpha,25-dihydroxyvitamin D3(1a).
AID1235857Induction of bone calcium mobilization into serum of Sprague-Dawley rat assessed as total serum calcium level at 260 pmol, ip administered 4 doses at 24 hrs interval measured 24 hrs post last dose (Rvb = 4.5 mg/dL)2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Novel 9-Alkyl- and 9-Alkylidene-Substituted 1α,25-Dihydroxyvitamin D3 Analogues: Synthesis and Biological Examinations.
AID1218525Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2C inhibitor sulfaphenazole2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID196189Support of Serum Calcium Transport mobilization response of Vitamin D-Deficient Rats on a low-calcium diet(amount 130 pmol)1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis and biological activity of 1 alpha, 25-dihydroxy-18-norvitamin D3 and 1 alpha, 25-dihydroxy-18,19-dinorvitamin D3.
AID1218465Drug metabolism in CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2B inhibitor orphenadrine2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID82176In vitro activity expressed as effective dose to induce the differentiation of human promyelocytic leukemia (HL-60) cells by NBT reduction assay1999Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7
Three-dimensional structure-function relationship of vitamin D: side chain location and various activities.
AID337316Induction of terminal cell differentiation in human HL60 cells assessed as cell viability at 0.0001 uM by trypan blue exclusion method1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1455899Half life in iv dosed Sprague-Dawley rat2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID216864Percent inhibition of binding to bovine thymus VDR, vitamin D receptor1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Conformationally restricted analogs of 1 alpha, 25-dihydroxyvitamin D3 and its 20-epimer: compounds for study of the three-dimensional structure of vitamin D responsible for binding to the receptor.
AID196190Support of Serum Calcium Transport mobilization response of Vitamin D-Deficient Rats on a low-calcium diet(amount 260 pmol)1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis and biological activity of 1 alpha, 25-dihydroxy-18-norvitamin D3 and 1 alpha, 25-dihydroxy-18,19-dinorvitamin D3.
AID191107Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 500 pmol at 4 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID3209Inhibitory effect (10e-6 M) on the 25-hydroxyvitamin D3-1-hydroxylase activity1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Arocalciferols: synthesis and biological evaluation of aromatic side-chain analogues of 1 alpha,25-dihydroxyvitamin D3(1a).
AID1585884Inhibition of Hedgehog signaling pathway in VDR-deficient mouse C3H10T1/2 cells assessed as change in CYP24A1 mRNA expression at 1 uM after 24 hrs by q-PCR analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID103395In vitro biological evaluation was determined on MCF-7 cell line, results expressed as percentage activity at 50% dose response2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Vitamin D(3): synthesis of seco C-9,11,21-trisnor-17-methyl-1 alpha, 25-dihydroxyvitamin D(3) analogues.
AID741567Toxicity in ovariectomized immatured Sprague-Dawley rat osteoporosis model assessed as effect on serum calcium level at 320 ng/kg, po once daily for 5 times per week for 4 weeks relative to control2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
A series of nonsecosteroidal vitamin D receptor agonists for osteoporosis therapy.
AID1218518Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP1A2 inhibitor furafyline2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1218495Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as 1alpha,23S,25(OH)3D3 metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1423173Hepatoprotective activity against CCL4-induced liver damage in C57BL/6J mouse assessed as reduction in serum TBA levels at 20 ug/kg, po administered 5 times a week via gavage measured at 72 hrs post final CCl4 injection2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Design, Synthesis, and Antifibrosis Activity in Liver of Nonsecosteroidal Vitamin D Receptor Agonists with Phenyl-pyrrolyl Pentane Skeleton.
AID1744113Agonist activity at VDR in human HL-60 cells assessed as induction of cell differentiation of promyelocytes to monocytes at >0.1 nM after 4 days by NBT reduction assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.
AID1585399Agonist activity at human VDR expressed in HOS cells co-expressing human RXR by Dual-Glo luciferase reporter gene assay2018Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24
Structural development of non-secosteroidal vitamin D receptor (VDR) ligands without any asymmetric carbon.
AID472304Toxicity in ip dosed NMRI mouse assessed as maximum tolerable dose inducing minimal increase in serum calcium level administered daily for 7 consecutive days measured after day 7 by colorimetric assay2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Synthesis, conformational analysis, and biological evaluation of 19-nor-vitamin D3 analogues with A-ring modifications.
AID488248Toxicity in FVB mouse assessed as calcium level in blood at 48 pmol/day administered via osmotic pump for 6 to 7 days measured on day 3 by microchemistry (RVb = 2.24 mmol/L)2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID1218462Drug metabolism in CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2A inhibitor 8-methoxypsoralen2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID216859Bind to chick intestinal Vitamin D3 receptor for 1,25-(OH)2-D31990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID190597Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5000 pmol at 4 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID191112Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 50 pmol at 24 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1455882Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 1 uM after 24 hrs by propidium iodide-staining based flow cytometry (Rvb = 31.55%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID81986Cell differentiation activity towards HL-60 cells assessed in terms of 4-nitro-blue tetrazolium (NBT) reactivity1999Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
Synthesis and biological evaluation of 1alpha,24-dihydroxy-25-nitrovitamin D3.
AID321742Effect on VDR transcriptional activity in human Caco-2 cells in presence of 5% fetal calf serum2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
(2S,2'R)-analogue of LG190178 is a major active isomer.
AID1375596Agonist activity at VDR in human MCF7 cells assessed as upregulation of p27 expression at 10'-9 M after 48 hrs by Western blot method relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID190598Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5000 pmol at 69 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID216862Relative affinity for bovine thymus Vitamin D3 receptor (VDR)2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Rational design, synthesis, and biological activity of novel conformationally restricted vitamin D analogues, (22R)- and (22S)-22-ethyl-1,25-dihydroxy-23,24-didehydro-24a,24b-dihomo-20-epivitamin D(3).
AID82342Differentiation inducing effect on HL-60 cells2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID1153075Binding affinity to N-terminal His-tagged human VDR LBD (118 to 427) Q239A mutant at 2-fold molar excess by ESI-MS analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Structural insights into the molecular mechanism of vitamin D receptor activation by lithocholic acid involving a new mode of ligand recognition.
AID1744119Agonist activity at human VDR expressed in African green monkey COS7 cells expressing mouse osteopontin VDRE assessed as induction of receptor transactivation incubated for 16 hrs by luciferase reporter gene assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.
AID81985Cell differentiation activity towards HL-60 cells was assessed in terms of NTB reactivity1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
Synthesis and biological activity of 2-methyl-20-epi analogues of 1 alpha,25-dihydroxyvitamin D3.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID81831Effect on HL-60 cell differentiation1998Bioorganic & medicinal chemistry letters, Jan-20, Volume: 8, Issue:2
A novel and practical route to A-ring enyne synthon for 1 alpha,25-dihydroxyvitamin D3 analogs: synthesis of A-ring diastereomers of 1 alpha,25-dihydroxyvitamin D2 and 3-methyl-1,25-dihydroxyvitamin D3.
AID725926Agonist activity at human VDR expressed in human HCT116 cells co-expressing VDRE assessed as XDR3 transcriptional activity at 20 to 40 uM after 24 hrs by luciferase reporter gene assay relative to control in presence of resveratrol2013Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
Synthesis and biological evaluation of halogenated curcumin analogs as potential nuclear receptor selective agonists.
AID190748Bone calcium mobilization in rats maintained on a very low calcium diet at a dose 130 (pmol)2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
2-Ethyl and 2-ethylidene analogues of 1alpha,25-dihydroxy-19-norvitamin D(3): synthesis, conformational analysis, biological activities, and docking to the modeled rVDR ligand binding domain.
AID664918Antiproliferative activity against NHEK cells incubated for 24 hrs by [3H]thymidine incorporation assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Design, synthesis, and biological action of 20R-hydroxyvitamin D3.
AID81117Compound was evaluated for its relative cell differentiation of human promyelocytic leukemia cells (HL-60)2002Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22
Synthesis and testing of 2alpha-modified 1alpha,25-dihydroxyvitamin D(3) analogues with a double side chain: marked cell differentiation activity.
AID280116Induction of human HL60 cell differentiation to monocytes by NBT reduction assay2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
22-Alkyl-20-epi-1alpha,25-dihydroxyvitamin D3 compounds of superagonistic activity: syntheses, biological activities and interaction with the receptor.
AID1140505Activation of hedgehog signaling pathway in VDR-knockdown mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Structure-activity relationships for vitamin D3-based aromatic a-ring analogues as hedgehog pathway inhibitors.
AID1455873Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID1375589Agonist activity at VDR in human MCF7 cells assessed as increase in transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID343850Displacement of [3H]1-alpha,25-(OH)2D3 from rat recombinant VDR expressed in Escherichia coli BL21 (DE3)2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
2-Substituted-16-ene-22-thia-1alpha,25-dihydroxy-26,27-dimethyl-19-norvitamin D3 analogs: Synthesis, biological evaluation, and crystal structure.
AID652551Antiproliferative activity against human T47D cells assessed as decrease in cell number after 72 hrs by WST assay2011ACS medicinal chemistry letters, Jul-14, Volume: 2, Issue:7
Novel alkynylphosphonate analogue of calcitriol with potent antiproliferative effects in cancer cells and lack of calcemic activity.
AID703638Binding affinity to VDR assessed as inhibition of fluorescent ligand by fluorescence polarization competition assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID1267146Induction of VDR transcriptional activity assessed as activation of 24-hydroxylase gene expression in rat ROS 17/2.8 cells after 16 hrs by luciferase reprter assay2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis and Biological Activity of 2-Methylene Analogues of Calcitriol and Related Compounds.
AID337022Induction of cell differentiation in human HL60 cells assessed as alpha naphthyl esterase activity at 0.001 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID387118Effect on calcium transport in vitamin D-deficient Sprague-Dawley rat intestine assessed as ratio of serosal to mucosal calcium level at 2340 pmol, ip administered 4 consecutive daily doses assessed after 24 hrs of last dose by gut sac assay2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
AID1160919Effect on CYP24A1 in human primary CLL cells assessed as effect on VDR-regulated GADD45alpha mRNA expression at 10 nM incubated for 24 hrs by quantitative RT-PCR method2014Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation.
AID337024Induction of cell differentiation in human HL60 cells assessed as alpha naphthyl esterase activity at 0.1 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID427505Induction of cell differentiation in human NB4 cells assessed as induction of induction of cell surface marker CD14 expression at 1 nM after 48 hrs2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Calcitriol derivatives with two different side chains at C-20. V. Potent inhibitors of mammary carcinogenesis and inducers of leukemia differentiation.
AID191110Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 50 pmol at 12 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID427504Antiproliferative activity against human MCF10CA1a after 3 days by [3H]thymidine uptake assay2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Calcitriol derivatives with two different side chains at C-20. V. Potent inhibitors of mammary carcinogenesis and inducers of leukemia differentiation.
AID216849Binding affinity for rat Vitamin D binding protein1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Synthesis, biological activity, and conformational analysis of four seco-D-15,19-bisnor-1alpha,25-dihydroxyvitamin D analogues, diastereomeric at C17 and C20.
AID652556AUC in mouse at 5 ug/kg2011ACS medicinal chemistry letters, Jul-14, Volume: 2, Issue:7
Novel alkynylphosphonate analogue of calcitriol with potent antiproliferative effects in cancer cells and lack of calcemic activity.
AID1375586Antiproliferative activity against 2D culture of human SKOV3 cells assessed as cell proliferation at 100 nM after 48 hrs by MTT assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID166889Effective dose for transcriptional activation in ROS 17/2.8 osteosarcoma cells2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Characterization of a novel analogue of 1alpha,25(OH)(2)-vitamin D(3) with two side chains: interaction with its nuclear receptor and cellular actions.
AID195597Patch clamp determination of calcium current in rat Osteosarcoma cells at 50.0 nM1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
1 alpha,25-dihydroxyvitamin D3 analogs featuring aromatic and heteroaromatic rings: design, synthesis, and preliminary biological testing.
AID1375584Antiproliferative activity against 2D culture of human MCF7 cells assessed as cell proliferation at 100 nM after 48 hrs by MTT assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID1218519Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP1A2 inhibitor furafyline2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID190605Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 500 pmol at 48 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1140744Displacement of [3H]-1-alpha,25-dihydroxyvitamin D3 from N-terminal GST-tagged human recombinant VDR LBD expressed in Escherichia coli Rosetta2 (DE3) after 16 hrs2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
A mixed population of antagonist and agonist binding conformers in a single crystal explains partial agonism against vitamin D receptor: active vitamin D analogues with 22R-alkyl group.
AID326337Displacement of [3H]1,25-(OH)2D3 from rat recombinant His-tagged VDR ligand-binding domain expressed in Escherichia coli BL212008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
2-Methylene 19-nor-25-dehydro-1alpha-hydroxyvitamin D3 26,23-lactones: synthesis, biological activities and molecular basis of passive antagonism.
AID1164474Ratio of 1alpha,25-(OH)2D3 Ki to compound Ki for full-length recombinant rat vitamin D receptor after 30 mins by liquid scintillation counting2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Synthesis and Biological Activity of 25-Hydroxy-2-methylene-vitamin D3 analogues monohydroxylated in the A-ring.
AID265895Antiproliferative activity against human keratinocyte assessed as inhibition of [3H]TdR uptake relative to calcitriol2006Bioorganic & medicinal chemistry letters, Jun-15, Volume: 16, Issue:12
Design and evaluation of new antipsoriatic antedrug candidates having 16-en-22-oxa-vitamin D3 structures.
AID228114Keq (k1/1-k) for the transformation of vitamin D to previtamin D1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
14-epi stereoisomers of 25-hydroxy- and 1 alpha,25-dihydroxyvitamin D3: synthesis, isomerization to previtamins, and biological studies.
AID741578Prevention of bone mineral density loss in ovariectomized immatured Sprague-Dawley rat osteoporosis model at 20 ng/kg, po once daily for 5 times per week for 4 weeks relative to control2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
A series of nonsecosteroidal vitamin D receptor agonists for osteoporosis therapy.
AID222287In vitro activity expressed as effective dose to inhibit the proliferation of primary cultures of human foreskin keratinocytes by measuring [3H]thymidine incorporation1999Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7
Three-dimensional structure-function relationship of vitamin D: side chain location and various activities.
AID1218522Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP1A1 inhibitor alpha-naphthoflavone2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1613154Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 24 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID216829Affinity for bovine thymus VDR vitamin D receptor1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
Synthesis and biological activity of 2-methyl-20-epi analogues of 1 alpha,25-dihydroxyvitamin D3.
AID1309802Growth inhibition of human SK-MEL-188 cells measured after 48 hrs by MTS/PMS assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Synthesis and Biological Evaluation of Vitamin D3 Metabolite 20S,23S-Dihydroxyvitamin D3 and Its 23R Epimer.
AID1135766Induction of bone calcium mobilization in vitamin-D-deficient chicken assessed per 100 ml of serum at 0.60 nmol, ip using 45Ca2+ and 40Ca2+ after 12 hrs1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Studies on vitamin D (calciferol) and its analogues. 15. 24-Nor-1alpha,25-dihydroxyvitamin D3 and 24-nor-25-hydroxy-5,6-trans-vitamin D3.
AID195596Patch clamp determination of calcium current in rat Osteosarcoma cells at 5.0 nM1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
1 alpha,25-dihydroxyvitamin D3 analogs featuring aromatic and heteroaromatic rings: design, synthesis, and preliminary biological testing.
AID703632Agonist activity at VDR in human SW480-ADH cells assessed as induction of E-cadherin at 10 '-9 M after 24 hrs by Western blot analysis relative to control2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID229240Binding affinity for bovine thymus vitamin D receptor (VDR)2000Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
Syntheses and biological evaluation of novel 2alpha-substituted 1alpha,25-dihydroxyvitamin D3 analogues.
AID1140504Inhibition of hedgehog signaling pathway in non-targeting siRNA treated mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Structure-activity relationships for vitamin D3-based aromatic a-ring analogues as hedgehog pathway inhibitors.
AID351857Effect on bone calcium mobilization in vitamin D-deficient weanling Sprague-Dawley rat assessed as serum calcium level at 780 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID191098Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5000 pmol at 4 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1135765Induction of bone calcium mobilization in vitamin-D-deficient chicken assessed per 100 ml of serum at 3 nmol, ip using 45Ca2+ and 40Ca2+ after 12 hrs1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Studies on vitamin D (calciferol) and its analogues. 15. 24-Nor-1alpha,25-dihydroxyvitamin D3 and 24-nor-25-hydroxy-5,6-trans-vitamin D3.
AID1455875Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID303412Ratio of ED50 for drug to 1-alpha,25-dihydroxyvitamin for VDR in rat osteosarcoma cells assessed as 24-hydroxylase transcription2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Design, synthesis, and biological evaluation of a 1alpha,25-dihydroxy-19-norvitamin D3 analogue with a frozen A-ring conformation.
AID488258Toxicity in FVB mouse assessed as calcium level in blood at 12 pmol/day administered via osmotic pump for 6 to 7 days measured on day 7 by microchemistry (RVb = 2.0.6 mmol/L)2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID664921Inhibition of colony formation of human HaCaT cells2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Design, synthesis, and biological action of 20R-hydroxyvitamin D3.
AID280114Displacement of [3H]1,25-(OH)2D3 from vitamin D receptor in bovine thymus2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
22-Alkyl-20-epi-1alpha,25-dihydroxyvitamin D3 compounds of superagonistic activity: syntheses, biological activities and interaction with the receptor.
AID191124Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5 pmol at 48 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID81823In vitro induction of HL-60 cell differentiation.2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Concise synthesis and biological activities of 2alpha-alkyl- and 2alpha-(omega-hydroxyalkyl)-20-epi-1alpha,25-dihydroxyvitamin D3.
AID1585871Activation of VDR in mouse ASZ001 cells assessed as change in Cyp24A1 mRNA expression at 1 uM after 48 hrs by q-PCR analysis relative to control2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID190606Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 500 pmol at 4 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1744118Displacement of [3H]-1-alpha,25-(OH)2D3 from bovine thymus VDR incubated for 18 hrs by competitive binding assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.
AID1266898Antipoliferative activity against human HepG2 cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID228898Effective dose for Protease sensitivity2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Characterization of a novel analogue of 1alpha,25(OH)(2)-vitamin D(3) with two side chains: interaction with its nuclear receptor and cellular actions.
AID1455871Drug uptake in human MCF7 cells at 1 uM after 10 mins by HPLC analysis2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID652552Antiproliferative activity against mouse LM05e cells assessed as decrease in cell number after 72 hrs by WST assay2011ACS medicinal chemistry letters, Jul-14, Volume: 2, Issue:7
Novel alkynylphosphonate analogue of calcitriol with potent antiproliferative effects in cancer cells and lack of calcemic activity.
AID1218464Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2B inhibitor orphenadrine2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1506106Transactivation of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-SRC-1 and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in SRC-1 recruitment by beta-galactosidase reporter gene based mammalian two-hybrid assa2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
25 S-Adamantyl-23-yne-26,27-dinor-1α,25-dihydroxyvitamin D
AID169297Bone calcium mobilization was tested on normal SD male rats and serum calcium level was reported1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
Synthesis and biological activity of 2-methyl-20-epi analogues of 1 alpha,25-dihydroxyvitamin D3.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID216830Affinity for bovine thymus vitamin D receptor2002Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22
Synthesis and testing of 2alpha-modified 1alpha,25-dihydroxyvitamin D(3) analogues with a double side chain: marked cell differentiation activity.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID260131Antagonistic activity against human VDR in presence of 1,25(OH)2D32006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Vitamin D receptor: ligand recognition and allosteric network.
AID216838Binding affinity for Vitamin D binding protein1998Bioorganic & medicinal chemistry letters, Jan-20, Volume: 8, Issue:2
A novel and practical route to A-ring enyne synthon for 1 alpha,25-dihydroxyvitamin D3 analogs: synthesis of A-ring diastereomers of 1 alpha,25-dihydroxyvitamin D2 and 3-methyl-1,25-dihydroxyvitamin D3.
AID302662Antiproliferative activity against mouse keratinocytes2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
AID196249Compound was evaluated for rat serum Ca concentration1998Bioorganic & medicinal chemistry letters, Jan-20, Volume: 8, Issue:2
A novel and practical route to A-ring enyne synthon for 1 alpha,25-dihydroxyvitamin D3 analogs: synthesis of A-ring diastereomers of 1 alpha,25-dihydroxyvitamin D2 and 3-methyl-1,25-dihydroxyvitamin D3.
AID1135797Induction of bone calcium mobilization in vitamin-D-deficient chicken assessed per 100 ml of serum at 163 nmol, ip using 45Ca2+ and 40Ca2+ after 5 to 36 hrs1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Studies on vitamin D (calciferol) and its analogues. 15. 24-Nor-1alpha,25-dihydroxyvitamin D3 and 24-nor-25-hydroxy-5,6-trans-vitamin D3.
AID1218526Drug metabolism in CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2C inhibitor sulfaphenazole2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1218467Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as 1 uM CYP3A inhibitor-mediated inhibition of metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID337275Induction of terminal cell differentiation in human HL60 cells at 1 uM after 4 days by NBT reduction assay1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID95374In vitro biological evaluation was determined on Keratinocytes, results expressed as percentage activity at 50% dose response2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Vitamin D(3): synthesis of seco C-9,11,21-trisnor-17-methyl-1 alpha, 25-dihydroxyvitamin D(3) analogues.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID190609Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 50 pmol at 12 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID250056Prodifferentiating activity of compound on human leukemia HL-60 cells was determined2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Synthesis and biological activity of 22-oxa CD-ring modified analogues of 1alpha,25-dihydroxyvitamin D3: cis-perhydrindane CE-ring analogues.
AID1235854Induction of intestinal calcium transport in Sprague-Dawley rat assessed as ratio of serosal calcium to mucosal calcium level at 780 pmol, ip administered 4 doses at 24 hrs interval measured 24 hrs post last dose by everted gut sac method (Rvb = 4.1 No_un2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Novel 9-Alkyl- and 9-Alkylidene-Substituted 1α,25-Dihydroxyvitamin D3 Analogues: Synthesis and Biological Examinations.
AID1266899Cytotoxicity against human L02 cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.
AID337314Induction of terminal cell differentiation in human HL60 cells assessed as cell viability at 0.01 uM by trypan blue exclusion method1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1408633Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as reduction in tumor growth at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID1353235Antifibrotic activity against TGFbeta1 stimulated rat LTC-14 cells assessed as inhibition of collagen 1 synthesis at 0.5 uM after 24 hrs by ELISA relative to calcipotriol2018European journal of medicinal chemistry, Feb-25, Volume: 146Design, synthesis and biological evaluation of non-secosteriodal vitamin D receptor ligand bearing double side chain for the treatment of chronic pancreatitis.
AID392915Effect on bone calcium mobilization in vitamin D-deficient weanling rat assessed as increase in serum calcium level at 0.7 ug/kg, ip administered as 7 consecutive daily doses measured 24 hrs after last dose relative to untreated control2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID1408617Induction of apoptosis in human MCF7 cells expressing VDR siRNA assessed as necrotic cells at 1 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.15%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID280117Effect on intestinal calcium transport in low-calcium diet fed rat assessed as serosal:mucosal ratio of calcium at 100 pmol/day, ip after 7 days2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
22-Alkyl-20-epi-1alpha,25-dihydroxyvitamin D3 compounds of superagonistic activity: syntheses, biological activities and interaction with the receptor.
AID1852313Induction of CYP24A1 (unknown orgin) transcriptional activity trasfected in human MCF7 cells incuabted for 48 hrs by luciferase reporter gene assay
AID1824246Inhibition of hedgehog signalling in mouse ASZ001 cells assessed as upregulation of VDR expression in by immunoblot analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma.
AID455168Effect on bone calcium mobilization in weanling Sprague-Dawley rat assessed as serum calcium level at 780 pmol/day, ip administered for 4 consecutive days measured 24 hrs after last dose2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
AID1218490Cmax in healthy human co-treated with 200 mg ketoconazile2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1408616Induction of apoptosis in human MCF7 cells expressing VDR siRNA assessed as late apoptotic cells at 1 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.01%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID635524Calcium mobilization in vitamin-D deficient weanling rat bone assessed as increase in serum calcium level at 0.2 ug/kg, ip administered daily for 7 consecutive days measured 24 hrs after last dose relative to vehicle treated control2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.
AID224820Bone calcium-mobilizing (BCM) activity at 260 pmol/day *7day in vitamin D deficient rats on a low-calcium diet (0.47% Ca)2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID274537Activity on human VDR-mediated transcription of osteocalcin VDRE fused to thymidine kinase promoter/growth hormone reporter gene in CV1 cells2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
AID1218497Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as 1alpha,24S,25(OH)3D3 metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID775185Agonist activity at VDR ligand binding domain (unknown origin) by reporter gene assay2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Synthesis of VS-105: A novel and potent vitamin D receptor agonist with reduced hypercalcemic effects.
AID1473746Ratio of drug concentration at steady state in human at 1 ug/ml, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1506105Transactivation of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-RXRalpha and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in interaction with RXRalpha by beta-galactosidase reporter gene based mammalian two-2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
25 S-Adamantyl-23-yne-26,27-dinor-1α,25-dihydroxyvitamin D
AID455160Displacement of radiolabeled 1-alpha,25-(OH)2D3 from rat recombinant full length VDR2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
AID1585866Activation of VDR in mouse C3H10T1/2 cells assessed as change in Cyp24A1 mRNA expression at 5 uM after 24 hrs by q-PCR analysis relative to control2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID110849In vivo calcemic effects was tested in vitamin D-replete normal NMRI mice by daily intraperitoneal injections of 1-alpha,25(OH)2D32002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Vitamin D(3): synthesis of seco C-9,11,21-trisnor-17-methyl-1 alpha, 25-dihydroxyvitamin D(3) analogues.
AID191122Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5 pmol at 2 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1408606Cell cycle arrest in human MCF7 cells expressing scrambled siRNA assessed as accumulation at S phase at 1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 29.79%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID1408600Displacement of fluormone VDR red from human full-length VDR after 4 hrs by fluorescence polarization assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID387350Effect on calcium transport in vitamin D-deficient Sprague-Dawley rat intestine assessed as ratio of serosal to mucosal calcium level at 32 pmol, ip administered 4 consecutive daily doses assessed after 24 hrs of last dose by gut sac assay2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
AID1218503Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as depletion of parent compound at 1 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1251253Upregulation of LAIR-1 expression in DBA/1 mouse splenocytes at 10'-7 M after overnight incubation by flow cytometric analysis (Rvb = 973 +/- 95 No_unit)2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Chemical Synthesis and Biological Activities of 20S,24S/R-Dihydroxyvitamin D3 Epimers and Their 1α-Hydroxyl Derivatives.
AID1824235Activation of VDR in mouse ASZ001 cells assessed as upregulation of Cyp24A1 mRNA expression at 1 uM measured after 48 hrs by RT-PCR analysis relative to control2022European journal of medicinal chemistry, Jan-15, Volume: 228Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma.
AID775184Binding affinity to VDR (unknown origin)2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Synthesis of VS-105: A novel and potent vitamin D receptor agonist with reduced hypercalcemic effects.
AID352238Effect on intestinal calcium transport in vitamin D-deficient weanling Sprague-Dawley rat assessed as increase in ratio of serosal to mucosal calcium level at 2340 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose by e2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID1218516Drug metabolism in human liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and paclitaxel2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1164478Effect on bone calcium mobilization in weanling Sprague-Dawley rat assessed as serum calcium level at 780 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose (Rvb = 4.2 to 4.9 mg/dL)2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Synthesis and Biological Activity of 25-Hydroxy-2-methylene-vitamin D3 analogues monohydroxylated in the A-ring.
AID191104Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 500 pmol at 2 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID414867Activation of VDR in LPS-stimulated human PBMC assessed as inhibition of TNFalpha mRNA expression at 10 nM at upto 8 hrs by RT-PCR2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
AID764543Displacement of [3H]-1alpha,25 dihydroxyvitamin D3 from bovine thymus VDR after 60 mins relative to 1alpha,25-dihydroxyvitamin D32013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Design and synthesis of novel 1,25-dihydroxyvitamin D3 analogues having a spiro-oxetane fused at the C2 position in the A-ring.
AID1153083Binding affinity to N-terminal His-tagged human VDR LBD (118 to 427) at 2-fold molar excess by ESI-MS analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Structural insights into the molecular mechanism of vitamin D receptor activation by lithocholic acid involving a new mode of ligand recognition.
AID351853Activity at VDR in rat osteosarcoma 17/2.8 cells assessed as transcriptional activation of 24-hydroxylase gene promoter after 16 hrs by luciferase reporter gene assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID169980Compound was evaluated for calcium mobilizing activity in rat serum2000Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
Syntheses and biological evaluation of novel 2alpha-substituted 1alpha,25-dihydroxyvitamin D3 analogues.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID703633Induction of human SW480-ADH cell differentiation assessed as formation of compact epithelioid islands of highly adherent cells at 10 '-8 M after 48 hrs by phase-contrast microscopy2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID1267666Metabolic stability in human MG63 assessed as compound metabolized at 1 uM after 24 hrs by HPLC analysis2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis, Biological Activities, and X-ray Crystal Structural Analysis of 25-Hydroxy-25(or 26)-adamantyl-17-[20(22),23-diynyl]-21-norvitamin D Compounds.
AID672798Displacement of [3H]-1alpha,25(OH)2D3 from recombinant rat VDR after overnight incubation by scintillation counting2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
A 20S combined with a 22R configuration markedly increases both in vivo and in vitro biological activity of 1α,25-dihydroxy-22-methyl-2-methylene-19-norvitamin D3.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID351849Displacement of [3H]1-alpha,25-(OH)2D3 from rat recombinant full length VDR2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID1218520Drug metabolism in CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP1A2 inhibitor furafyline2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1408611Induction of apoptosis in human MCF7 cells expressing scrambled siRNA assessed as early apoptotic cells at 1 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.93%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID635522Agonist activity at rat VDR in ROS 17/2.8 cells transfected with Cyp24a1 reporter plasmid assessed as increase in Cyp24a1 transcription after 16 hrs by luciferase reporter gene assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.
AID527096VDR antagonist activity as NcoR recruitment to CYP24 promoter in ChIP assay at 1uM2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
An o-aminoanilide analogue of 1α,25-dihydroxyvitamin D(3) functions as a strong vitamin D receptor antagonist.
AID302663Activity at human recombinant VDR in ROS 17/2.8 cells transfected with growth hormone fusion gene VDRE assessed as growth hormone level by transcriptional assay2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
AID190611Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 50 pmol at 24 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID366875Induction of cell differentiation in human HL60 cells after 4 days by NBT reduction assay2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
A new class of vitamin D analogues that induce structural rearrangement of the ligand-binding pocket of the receptor.
AID387114Displacement of [3H]1-alpha,25-(OH)2D3 from rat recombinant full length VDR2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
AID24178Compound was tested for rate constant for the transformation of vitamin to previtamin1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
14-epi stereoisomers of 25-hydroxy- and 1 alpha,25-dihydroxyvitamin D3: synthesis, isomerization to previtamins, and biological studies.
AID455167Effect on bone calcium mobilization in weanling Sprague-Dawley rat assessed as serum calcium level at 260 pmol/day, ip administered for 4 consecutive days measured 24 hrs after last dose2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
AID280121Effect on bone calcium mobilization in low-calcium diet fed rat at 325 pmol/day, ip after 7 days2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
22-Alkyl-20-epi-1alpha,25-dihydroxyvitamin D3 compounds of superagonistic activity: syntheses, biological activities and interaction with the receptor.
AID89329Inhibition of growth of human keratinocytes2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
New dermatological agents for the treatment of psoriasis.
AID1613156Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 3.80%)2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID191092Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5000 pmol at 12 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1235849Induction of bone calcium mobilization into serum of Sprague-Dawley rat assessed as serum calcium level at 87 pmol, ip administered 4 doses at 24 hrs interval measured 24 hrs post last dose (Rvb = 4.9 mg/dL)2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Novel 9-Alkyl- and 9-Alkylidene-Substituted 1α,25-Dihydroxyvitamin D3 Analogues: Synthesis and Biological Examinations.
AID302667Induction of CYP24 mRNA transcriptional activity in C57BL/6 mouse duodenum at 3 ug/kg, ip after 4 hrs2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
AID1585867Activation of VDR in mouse C3H10T1/2 cells assessed as change in Cyp24A1 mRNA expression at 2.5 uM after 24 hrs by q-PCR analysis relative to control2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID1408607Cell cycle arrest in human MCF7 cells expressing VDR siRNA assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 49.17%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID1164477Effect on bone calcium mobilization in weanling Sprague-Dawley rat assessed as serum calcium level at 87 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose (Rvb = 4.2 to 4.9 mg/dL)2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Synthesis and Biological Activity of 25-Hydroxy-2-methylene-vitamin D3 analogues monohydroxylated in the A-ring.
AID1408603Cell cycle arrest in human MCF7 cells expressing scrambled siRNA assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 49.28%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID252972Percent cell proliferation of human leukemia cell line HL-60 at 1*E-8 M2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Cell differentiation inducers derived from thalidomide.
AID455172Effect on intestinal calcium transport in weanling Sprague-Dawley rat assessed as ratio of serosal to mucosal calcium level at 260 pmol/day, ip administered for 4 consecutive days measured 24 hrs after last dose by everted gut sac method2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
AID601957Antiproliferative activity against human MCF7 cells assessed as DNA level at 1 nM measured after 6 days by calorimetric analysis2011Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D(3) analogues hydroxymethylated at C-26.
AID601958Antiproliferative activity against human MCF7 cells assessed as DNA level at 10 nM measured after 6 days by calorimetric analysis2011Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D(3) analogues hydroxymethylated at C-26.
AID1408614Induction of apoptosis in human MCF7 cells expressing VDR siRNA assessed as live cells at 1 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 98.35%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID216837Vitamin D receptor mediated transcriptional activity in rat osteosarcoma ROS 17/2.8 cells1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Noncalcemic, antiproliferative, transcriptionally active, 24-fluorinated hybrid analogues of the hormone 1alpha, 25-dihydroxyvitamin D3. Synthesis and preliminary biological evaluation.
AID177142In vivo calcemic activity expressed as effective dose for Bone calcium mobilization (BCM) in vitamin D deficient rats1999Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7
Three-dimensional structure-function relationship of vitamin D: side chain location and various activities.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID25537Compound was tested for the backward reaction of conversion of vitamin D to previtaminD1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
14-epi stereoisomers of 25-hydroxy- and 1 alpha,25-dihydroxyvitamin D3: synthesis, isomerization to previtamins, and biological studies.
AID1613155Agonist activity at human VDR expressed in HEK293 cells harboring human RXR and TK-Spp x 3-LUC reporter plasmid at 10'-5 to 10'-9 M after 24 hrs by dual luciferase reporter gene assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID1309799Activation of VDR in human Caco2 cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Synthesis and Biological Evaluation of Vitamin D3 Metabolite 20S,23S-Dihydroxyvitamin D3 and Its 23R Epimer.
AID1135777Induction of intestinal calcium absorption in vitamin-D-deficient chicken assessed per 0.2 ml of plasma at 3 nmol, ip using 45Ca2+ and 40Ca2+ after 12 hrs1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Studies on vitamin D (calciferol) and its analogues. 15. 24-Nor-1alpha,25-dihydroxyvitamin D3 and 24-nor-25-hydroxy-5,6-trans-vitamin D3.
AID1235850Induction of bone calcium mobilization into serum of Sprague-Dawley rat assessed as serum calcium level at 780 pmol, ip administered 4 doses at 24 hrs interval measured 24 hrs post last dose (Rvb = 4.9 mg/dL)2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Novel 9-Alkyl- and 9-Alkylidene-Substituted 1α,25-Dihydroxyvitamin D3 Analogues: Synthesis and Biological Examinations.
AID1135788Induction of intestinal calcium absorption in vitamin-D-deficient chicken assessed per 0.2 ml of plasma at 3 nmol, ip using 45Ca2+ and 40Ca2+ after 12 hrs relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Studies on vitamin D (calciferol) and its analogues. 15. 24-Nor-1alpha,25-dihydroxyvitamin D3 and 24-nor-25-hydroxy-5,6-trans-vitamin D3.
AID190616Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 50 pmol at 69 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID337312Induction of terminal cell differentiation in human HL60 cells assessed as cell viability at 1 uM by trypan blue exclusion method1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID414858Inhibition of IFN-gamma production in human PBMC after 5 days by ELISA-based mixed lymphocyte reaction assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
AID1455895Hypercalcemic effect in ICR mouse assessed as serum calcium levels at 5 ug/kg, ip administered for 7 days measured on day 8 post-dose by MTB-based assay (Rvb = 7.05 mg/dl)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID652548Antiproliferative activity against human HN12 cells assessed as decrease in cell number after 72 hrs by WST assay2011ACS medicinal chemistry letters, Jul-14, Volume: 2, Issue:7
Novel alkynylphosphonate analogue of calcitriol with potent antiproliferative effects in cancer cells and lack of calcemic activity.
AID82979Differentiation activity of human promyelocytic leukemia cells (HL-60) determined by an NBT reduction assay method2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Rational design, synthesis, and biological activity of novel conformationally restricted vitamin D analogues, (22R)- and (22S)-22-ethyl-1,25-dihydroxy-23,24-didehydro-24a,24b-dihomo-20-epivitamin D(3).
AID703634Induction of human SW480-ADH cell differentiation assessed as formation of compact epithelioid islands of highly adherent cells at 10 '-7 M after 48 hrs by phase-contrast microscopy2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID1408615Induction of apoptosis in human MCF7 cells expressing VDR siRNA assessed as early apoptotic cells at 1 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.49%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID1585865Inhibition of Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as reduction in oxysterol-induced Gli1 mRNA expression after 24 hrs by q-PCR analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID414865Activation of VDR in human THP1 cells assessed as increase in cathelicidin antimicrobial peptide mRNA expression by RT-PCR2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
AID703630Agonist activity at VDR in human SW480-ADH cells assessed as induction of E-cadherin at 10 '-8 M after 24 hrs by Western blot analysis relative to control2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID228001In vitro vitamin D receptor-mediated antiproliferative activity in rat osteosarcoma ROS 17/2.8 cells2002Journal of medicinal chemistry, Apr-11, Volume: 45, Issue:8
Conceptually new low-calcemic oxime analogues of the hormone 1 alpha,25-dihydroxyvitamin D(3): synthesis and biological testing.
AID1417060Agonist activity at GAL4 DNA-binding domain fused VDR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-β agonists (SERBAs).
AID1744117Agonist activity at VDR in human HL-60 cells assessed as induction of cell differentiation of promyelocytes to monocytes after 4 days in presence of 1 uM CYP24 inhibitor ketoconazole by NBT reduction assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.
AID387117Effect on calcium transport in vitamin D-deficient Sprague-Dawley rat intestine assessed as ratio of serosal to mucosal calcium level at 260 pmol, ip administered 4 consecutive daily doses assessed after 24 hrs of last dose by gut sac assay2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
AID191119Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5 pmol at 12 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1267787Induction of intestinal calcium transport in weaning Sprague-Dawley rat assessed as ratio of calcium level in serosal to mucosal at 780 pmol, ip for 4 consecutive dose at an interval of 24 hrs measured 24 hrs after last dose (Rvb = 3.7 to 4.8 No_unit)2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
A Methylene Group on C-2 of 24,24-Difluoro-19-nor-1α,25-dihydroxyvitamin D3 Markedly Increases Bone Calcium Mobilization in Vivo.
AID326340Agonist activity at human VDR in HEK293 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
2-Methylene 19-nor-25-dehydro-1alpha-hydroxyvitamin D3 26,23-lactones: synthesis, biological activities and molecular basis of passive antagonism.
AID1408608Cell cycle arrest in human MCF7 cells expressing VDR siRNA assessed as accumulation at G2/M phase at 1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 17.57%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID1423172Hepatoprotective activity against CCL4-induced liver damage in C57BL/6J mouse assessed as reduction in serum ALT levels at 20 ug/kg, po administered 5 times a week via gavage measured at 72 hrs post final CCl4 injection2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Design, Synthesis, and Antifibrosis Activity in Liver of Nonsecosteroidal Vitamin D Receptor Agonists with Phenyl-pyrrolyl Pentane Skeleton.
AID366868Displacement of [3H]1,25-(OH)2D3 from bovine thymus vitamin D receptor2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
A new class of vitamin D analogues that induce structural rearrangement of the ligand-binding pocket of the receptor.
AID303409Induction of differention of human HL60 cells into monocytes by NBT reduction assay2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Design, synthesis, and biological evaluation of a 1alpha,25-dihydroxy-19-norvitamin D3 analogue with a frozen A-ring conformation.
AID635564Calcium transport in vitamin-D deficient weanling rat intestine assessed as intestinal calcium level at 0.2 ug/kg, ip administered daily for 7 consecutive days measured 24 hrs after last dose2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.
AID547395In vivo calcemic activity in vitamin D-deficient Sprague-Dawley rat intestine assessed as effect on calcium transport measured by ratio of serosal to mucosal calcium level at 260 pmol, ip administered 4 consecutive daily doses assessed after 24 hrs of las2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Removal of the 26-methyl group from 19-nor-1α,25-dihydroxyvitamin D₃ markedly reduces in vivo calcemic activity without altering in vitro VDR binding, HL-60 cell differentiation, and transcription.
AID1218529Drug metabolism in CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2D inhibitor quinine2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID619493Induction of bone calcium mobilization in Sprague-Dawley rat assessed as concentration of serum calcium at 87 pmol, ip administered as 4 consecutive doses once in 24 hrs measured 24 hrs post last dose (Rvb = 4.5 mg/dl)2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis and biological activity of 2-(3'-hydroxypropylidene)-1α-hydroxy-19-norvitamin D analogues with shortened alkyl side chains.
AID191106Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 500 pmol at 48 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1455884Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide-staining based flow cytometry (Rvb = 1.74%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID1218502Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as depletion of parent compound at 1 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1118430Antiproliferative activity against ER positive human MCF10CA1a cells after 3 days by [3H]thymidine uptake assay2011MedChemComm, , Volume: 2, Issue:5
Structure-function study of gemini derivatives with two different side chains at C-20, Gemini-0072 and Gemini-0097.
AID216846Binding affinity for rat Vitamin D binding protein1999Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7
Three-dimensional structure-function relationship of vitamin D: side chain location and various activities.
AID392908Effect on calcium transport in vitamin D-deficient weanling rat intestine assessed as increase in ratio of serosal to mucosal calcium level at 0.2 ug/kg, ip administered as 7 consecutive daily doses measured 24 hrs after last dose2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID1218461Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2A inhibitor 8-methoxypsoralen2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID243315Binding affinity for pig nuclear vitamin D receptor2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Synthesis and biological activity of 22-oxa CD-ring modified analogues of 1alpha,25-dihydroxyvitamin D3: cis-perhydrindane CE-ring analogues.
AID1455883Induction of apoptosis in human MCF7 cells assessed as viable cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide-staining based flow cytometry (Rvb = 98.2%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID226139evaluated for increasing effect of serum calcium level in normal rats(Ca)2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID302669Induction of TRPV6 mRNA transcriptional activity in C57BL/6 mouse duodenum at 3 ug/kg, ip after 4 hrs2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
AID171505Support of Intestinal Calcium Transport mobilization response of Vitamin D-Deficient Rats on a low-calcium diet(amount 130 pmol)1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis and biological activity of 1 alpha, 25-dihydroxy-18-norvitamin D3 and 1 alpha, 25-dihydroxy-18,19-dinorvitamin D3.
AID190593Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5000 pmol at 24 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID635571Displacement of [3H]-1alpha,25(OH)2D3 from recombinant rat VDR by scintillation counting2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.
AID1824248Inhibition of hedgehog signalling in mouse Sufu-KO MEF cells assessed as upregulation of VDR expression at 10 uM in by immunoblot analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma.
AID1585877Kinetic solubility of the compound in pH 7.4 phosphate buffered saline2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID703635Agonist activity at VDR in human SW480-ADH cells assessed as repression of c-Myc expression at 10 '-9 M after 24 hrs by Western blot analysis relative to control2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID1473744AUC in human at 1 ug/ml, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID392913Ratio of EC50 of compound to EC50 of [3H]1-alpha,25-(OH)2D3 for VDR in rat ROS 17/2.8 cells by 24-hydroxylase gene transcriptional activation assay2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID1267641Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assay2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis, Biological Activities, and X-ray Crystal Structural Analysis of 25-Hydroxy-25(or 26)-adamantyl-17-[20(22),23-diynyl]-21-norvitamin D Compounds.
AID760209Toxicity in ovariectomized Sprague-Dawley rat osteoporosis model assessed as increase in serum Ca level at 0.1 mg/kg/day administered 5 times a week for 4 weeks measured 24 hrs post last dose (Rvb = 9.14 +/- 0.24 mg/dL)2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Synthesis of 2α-heteroarylalkyl active vitamin d3 with therapeutic effect on enhancing bone mineral density in vivo.
AID619503Effect on intestinal calcium transport activity in Sprague-Dawley rat assessed as ratio of serosal to mucosal calcium concentration at 260 pmol, ip administered as 4 consecutive doses once in 24 hrs measured 24 hrs post last dose (Rvb = 4.1 no unit )2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis and biological activity of 2-(3'-hydroxypropylidene)-1α-hydroxy-19-norvitamin D analogues with shortened alkyl side chains.
AID488251Toxicity in FVB mouse assessed as calcium level in blood at 12 pmol/day administered via osmotic pump for 6 to 7 days measured on day 6 by microchemistry (RVb = 2 mmol/L)2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID459159Antiproliferative activity against human HL60 cells at 0.1 nM after 96 hrs2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Structure-function relationships and crystal structures of the vitamin D receptor bound 2 alpha-methyl-(20S,23S)- and 2 alpha-methyl-(20S,23R)-epoxymethano-1 alpha,25-dihydroxyvitamin D3.
AID351851Induction of human HL60 cell differentiation into monocytes after 4 days by NBT reduction assay2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID414870Induction of hypercalceimia in orally dosed C57BL/6 mouse administered daily for 4 days by colorimetric assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
AID688525Cytotoxicity against mouse LM3 assessed as decrease in cell count after 120 hrs2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of a new vitamin D2 analogue.
AID265894Antiproliferative activity against human keratinocyte assessed as inhibition of [3H]TdR uptake2006Bioorganic & medicinal chemistry letters, Jun-15, Volume: 16, Issue:12
Design and evaluation of new antipsoriatic antedrug candidates having 16-en-22-oxa-vitamin D3 structures.
AID191103Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 500 pmol at 24 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID387125Effect on bone calcium mobilization in vitamin D-deficient Sprague-Dawley rat assessed as serum calcium level at 32 pmol, ip administered 4 consecutive daily doses assessed after 24 hrs of last dose by spectrometry2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
AID1266900Toxicity in rat assessed as serum calcium level at 0.5 ug/kg/day administered for 7 days (Rvb = 7.25 mg/dl)2016European journal of medicinal chemistry, Jan-01, Volume: 107Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.
AID455169Effect on bone calcium mobilization in weanling Sprague-Dawley rat assessed as serum calcium level at 2340 pmol/day, ip administered for 4 consecutive days measured 24 hrs after last dose2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
AID1267780Induction of bone mobilization activity in weaning Sprague-Dawley rat assessed as increase in serum calcium level at 16 pmol, ip for 4 consecutive dose at an interval of 24 hrs measured 24 hrs after last dose (Rvb = 4.4 to 4.5 mg/dl)2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
A Methylene Group on C-2 of 24,24-Difluoro-19-nor-1α,25-dihydroxyvitamin D3 Markedly Increases Bone Calcium Mobilization in Vivo.
AID1375588Antiproliferative activity against 3D culture of human MCF7 cells assessed as cell proliferation at 100 nM after 5 days by DAPI staining-based phase contrast microscopic method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID1408605Cell cycle arrest in human MCF7 cells expressing scrambled siRNA assessed as accumulation at G2/M phase at 1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 19.6%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID619491Induction of VDR-mediated 24-hydroxylase transcription in rat osteosarcoma cells by luciferase reporter gene assay2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis and biological activity of 2-(3'-hydroxypropylidene)-1α-hydroxy-19-norvitamin D analogues with shortened alkyl side chains.
AID230233Intestinal Calcium Transport (ICT) activity (130 pmol/day/7 days) in Vitamin D-Deficient Rats on a Low-Calcium Diet2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID488235Inhibition of HDAC in human SCC4 cells assessed as increase in tubulin acetylation at 1 uM after 24 hrs by Western blot analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1455885Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide-staining based flow cytometry (Rvb = 0.062%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID455173Effect on intestinal calcium transport in weanling Sprague-Dawley rat assessed as ratio of serosal to mucosal calcium level at 780 pmol/day, ip administered for 4 consecutive days measured 24 hrs after last dose by everted gut sac method2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
AID1160917Induction of apoptosis in human primary CLL cells after 48 hrs by Annexin V/propidium iodide staining based flow cytometry2014Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation.
AID455171Effect on intestinal calcium transport in weanling Sprague-Dawley rat assessed as ratio of serosal to mucosal calcium level at 87 pmol/day, ip administered for 4 consecutive days measured 24 hrs after last dose by everted gut sac method2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
AID1408601Transactivation of recombinant human VDR/RXRalpha expressed in HEK293 cells after 24 hrs by Dual-luciferase reporter gene assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID488253Toxicity in FVB mouse assessed as calcium level in blood at 48 pmol/day administered via osmotic pump for 6 to 7 days measured on day 6 by microchemistry (RVb = 2 mmol/L)2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID455162Induction of differentiation of human HL60 promyelocytes into monocytes after 4 days by NBT reduction assay2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
AID488252Toxicity in FVB mouse assessed as calcium level in blood at 24 pmol/day administered via osmotic pump for 6 to 7 days measured on day 6 by microchemistry (RVb = 2 mmol/L)2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID228688Ratio of average ED50 to 1R,25-(OH)2D3 ED501998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
New 1alpha,25-dihydroxy-19-norvitamin D3 compounds of high biological activity: synthesis and biological evaluation of 2-hydroxymethyl, 2-methyl, and 2-methylene analogues.
AID730431Agonist activity at CMX-GAL4 tagged human VDR expressed in HEK293 cells assessed as increase in transcriptional activity by luciferase reporter gene assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange.
AID196185Bone Calcium mobilization response of Vitamin D-Deficient Rats to a single Intravenous Injection of (amount 260 pmol)1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis and biological activity of 1 alpha, 25-dihydroxy-18-norvitamin D3 and 1 alpha, 25-dihydroxy-18,19-dinorvitamin D3.
AID488236Inhibition of HDAC in human SCC4 cells assessed as increase in histone acetylation at 1 uM after 24 hrs by Western blot analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID647366Activation of VDR in human HT-29 cells assessed as up-regulation of CYP24A1 at 0.1 uM by RT-PCR analysis relative to control2012Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
Evaluation of vitamin D3 A-ring analogues as Hedgehog pathway inhibitors.
AID1235853Induction of intestinal calcium transport in Sprague-Dawley rat assessed as ratio of serosal calcium to mucosal calcium level at 87 pmol, ip administered 4 doses at 24 hrs interval measured 24 hrs post last dose by everted gut sac method (Rvb = 4.1 No_uni2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Novel 9-Alkyl- and 9-Alkylidene-Substituted 1α,25-Dihydroxyvitamin D3 Analogues: Synthesis and Biological Examinations.
AID190620Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5 pmol at 24 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID770181Binding affinity to His-6-tagged rat VDR W282R mutant over expressed in Escherichia coli C41 assessed as increase in transition temperature by at 5 mM by CD-based spectropolarimetric analysis2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Crystal structures of hereditary vitamin D-resistant rickets-associated vitamin D receptor mutants R270L and W282R bound to 1,25-dihydroxyvitamin D3 and synthetic ligands.
AID1423176Half life in Sprague-Dawley rat at 20 mg/kg, po by HPLC analysis2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Design, Synthesis, and Antifibrosis Activity in Liver of Nonsecosteroidal Vitamin D Receptor Agonists with Phenyl-pyrrolyl Pentane Skeleton.
AID171373Intestinal Calcium Transport mobilization response of Vitamin D-Deficient Rats on a low-calcium diet(amount 500 pmol)1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis and biological activity of 1 alpha, 25-dihydroxy-18-norvitamin D3 and 1 alpha, 25-dihydroxy-18,19-dinorvitamin D3.
AID224819Bone Calcium-Mobilizing (BCM) activity (260 pmol/day/7 days) in Vitamin D-Deficient Rats on a Low-Calcium Diet (0.02% Ca diet)2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID191116Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 50 pmol at 4 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID619500Effect on intestinal calcium transport activity in Sprague-Dawley rat assessed as ratio of serosal to mucosal calcium concentration at 780 pmol, ip administered as 4 consecutive doses once in 24 hrs measured 24 hrs post last dose (Rvb = 4.5 no unit )2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis and biological activity of 2-(3'-hydroxypropylidene)-1α-hydroxy-19-norvitamin D analogues with shortened alkyl side chains.
AID1423163Transactivation of VDR in human LX2 cells assessed as inhibition of TGFbeta1-induced COL1A1 mRNA expression at 100 nM after 24 hrs by Q-PCR analysis2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Design, Synthesis, and Antifibrosis Activity in Liver of Nonsecosteroidal Vitamin D Receptor Agonists with Phenyl-pyrrolyl Pentane Skeleton.
AID1585887Inhibition of Hedgehog signaling pathway in Sufu-deficient mouse C3H10T1/2 cells assessed as reduction in oxysterol-induced Gli1 mRNA expression after 24 hrs by q-PCR analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID265893Calcemic activity in percutaneously dosed mouse relative to control2006Bioorganic & medicinal chemistry letters, Jun-15, Volume: 16, Issue:12
Design and evaluation of new antipsoriatic antedrug candidates having 16-en-22-oxa-vitamin D3 structures.
AID190602Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 500 pmol at 24 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1164475Ratio of 1alpha,25-(OH)2D3 ED50 to compound ED50 for induction of human HL60 cell differentiation by nitro blue tetrazolium reduction assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Synthesis and Biological Activity of 25-Hydroxy-2-methylene-vitamin D3 analogues monohydroxylated in the A-ring.
AID1455876Antiproliferative activity against human L02 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID1455893Drug uptake in human MCF7 cells at 1 uM after 30 mins by HPLC analysis2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID1140510Effect on CYP24A1 RNA level in non-targeting siRNA treated mouse C3H10T1/2 cells at 0.5 uM after 24 hrs by qPCR analysis2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Structure-activity relationships for vitamin D3-based aromatic a-ring analogues as hedgehog pathway inhibitors.
AID1218523Drug metabolism in CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP1A1 inhibitor alpha-naphthoflavone2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1153074Binding affinity to N-terminal His-tagged human VDR LBD (118 to 427) S235A mutant at 2-fold molar excess by ESI-MS analysis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Structural insights into the molecular mechanism of vitamin D receptor activation by lithocholic acid involving a new mode of ligand recognition.
AID1585873Antiproliferative activity against medulloblastoma cells derived from conditional patched knockout mouse after 48 hrs by [3H]-thymidine incorporation assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID392911Ratio of Ki of the drug to Ki of [3H]1-alpha,25-(OH)2D3 for rat recombinant full length VDR2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID274535Displacement of [3H]1,25-dihydroxyvitamin D3 from human VDR by HAP assay2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
AID647008Induction of vitamin D receptor-mediated differentiation of human HL60 cells at 10'-9 to 10'-5 M by NBT reduction method2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Novel vitamin D receptor ligands bearing a spherical hydrophobic core structure--comparison of bicyclic hydrocarbon derivatives with boron cluster derivatives.
AID741577Prevention of bone mineral density loss in ovariectomized immatured Sprague-Dawley rat osteoporosis model at 80 ng/kg, po once daily for 5 times per week for 4 weeks relative to control2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
A series of nonsecosteroidal vitamin D receptor agonists for osteoporosis therapy.
AID1585876Kinetic solubility of the compound in pH 4 phosphate buffered saline2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID351855Effect on bone calcium mobilization in vitamin D-deficient weanling Sprague-Dawley rat assessed as serum calcium level at 87 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID392909Effect on calcium transport in vitamin D-deficient weanling rat intestine assessed as increase in ratio of serosal to mucosal calcium level at 0.7 ug/kg, ip administered as 7 consecutive daily doses measured 24 hrs after last dose2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID459160Induction of cell differentiation in human HL60 cells assessed as CD11c and CD14 expression at 0.1 nM after 96 hrs relative to untreated control2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Structure-function relationships and crystal structures of the vitamin D receptor bound 2 alpha-methyl-(20S,23S)- and 2 alpha-methyl-(20S,23R)-epoxymethano-1 alpha,25-dihydroxyvitamin D3.
AID260130Inhibition of transactivation of human VDR in COS7 cells2006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Vitamin D receptor: ligand recognition and allosteric network.
AID1267150Effect on bone calcium mobilization in weanling Sprague-Dawley rat assessed as serum calcium level at 87 pmol/day administered as 4 consecutive daily doses measured 24 hrs after last dose relative to control2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis and Biological Activity of 2-Methylene Analogues of Calcitriol and Related Compounds.
AID472017Binding affinity to human vitamin D binding protein2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Synthesis, conformational analysis, and biological evaluation of 19-nor-vitamin D3 analogues with A-ring modifications.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID337307Induction of terminal cell differentiation in human HL60 cells assessed as naphthol AS-D chloroacetate esterase activity at 1 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID55257Evaluated for its binding affinity towards cytosol receptor in human myeloid leukemia cells (HL-60), by using 1-alpha,25-(OH)2D3 as radioligand1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Syntheses and differentiating action of vitamin D endoperoxides. Singlet oxygen adducts of vitamin D derivatives in human myeloid leukemia cells (HL-60).
AID1824238Activation of VDR in mouse C3H 10T1/2 cells assessed as upregulation of Cyp24A1 mRNA expression at 1 uM measured after 48 hrs by RT-PCR analysis relative to control2022European journal of medicinal chemistry, Jan-15, Volume: 228Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma.
AID1277412Agonist activity at VDR-LBD in human DU145 cells assessed as CYP24A1 expression at 7.5 uM after 18 hrs by qRT-PCR method2016European journal of medicinal chemistry, Feb-15, Volume: 109Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites.
AID1218510Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP450 inhibitor SKF525A2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID590448Induction of CYP24 mRNA expression in human A498 cells at 10'-8 M after 4 hrs by RT-PCR analysis2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
1α,25-Dihydroxyvitamin D3-3β-bromoacetate, a potential cancer therapeutic agent: synthesis and molecular mechanism of action.
AID703623Toxicity in CD-1 mouse assessed as body weight loss at 0.3 ug/kg, ip administered every other day for 3 weeks measured on day 212012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID95372In vitro proliferative activity on keratinocyte cells1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Synthesis, biological activity, and conformational analysis of four seco-D-15,19-bisnor-1alpha,25-dihydroxyvitamin D analogues, diastereomeric at C17 and C20.
AID351858Effect on bone calcium mobilization in vitamin D-deficient weanling Sprague-Dawley rat assessed as serum calcium level at 2340 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID82334Evaluated for its ability to induce phagocytosis in human myeloid leukemia cells (HL-60)1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Syntheses and differentiating action of vitamin D endoperoxides. Singlet oxygen adducts of vitamin D derivatives in human myeloid leukemia cells (HL-60).
AID1218512Drug metabolism in human liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and ketoconazole2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID216847Displacement of [3H]25-(OH)-D3 from rat plasma Vitamin D binding protein1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID337311Induction of terminal cell differentiation in human HL60 cells assessed as naphthol AS-D chloroacetate esterase activity at 0.0001 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1267643Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assay2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis, Biological Activities, and X-ray Crystal Structural Analysis of 25-Hydroxy-25(or 26)-adamantyl-17-[20(22),23-diynyl]-21-norvitamin D Compounds.
AID1375592Induction of human HaCaT cell differentiation at 100 nM after 48 hrs2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID635570Induction of human HL60 cell differentiation after 4 days by nitro blue tetrazolium reduction assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.
AID1408613Induction of apoptosis in human MCF7 cells expressing scrambled siRNA assessed as necrotic cells at 1 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.16%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID1408599Displacement of fluormone VDR red from human full-length VDR at 1 uM after 4 hrs by fluorescence polarization assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID1218515Drug metabolism in human liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and tamoxifen2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID343853Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days relative to 1-alpha, 25-(OH)2D32008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
2-Substituted-16-ene-22-thia-1alpha,25-dihydroxy-26,27-dimethyl-19-norvitamin D3 analogs: Synthesis, biological evaluation, and crystal structure.
AID337038Induction of terminal cell differentiation in human HL60 cells at 0.01 uM after 4 days by NBT reduction assay1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID337309Induction of terminal cell differentiation in human HL60 cells assessed as naphthol AS-D chloroacetate esterase activity at 0.01 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1310892Agonist activity at VDR expressed in human HuH7 cells after 24 hrs by pDR3-luciferase reporter gene assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists.
AID1218509Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP450 inhibitor SKF525A2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID337280Induction of terminal cell differentiation in human HL60 cells assessed as inhibition of [3H]thymidine incorporation at 0.1 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1153080Transactivation of human VDR K240A mutant expressed in HEK293 cells coexpressing CYP3A4 at 10 nM by dual luciferase reporter gene assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Structural insights into the molecular mechanism of vitamin D receptor activation by lithocholic acid involving a new mode of ligand recognition.
AID1218494Drug metabolism in human liver microsomes assessed as assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1218498Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as 1alpha,23R,25(OH)3D3 metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1218521Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP1A1 inhibitor alpha-naphthoflavone2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID250033Antiproliferative activity on human breast cancer MCF-7 cells was determined2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Synthesis and biological activity of 22-oxa CD-ring modified analogues of 1alpha,25-dihydroxyvitamin D3: cis-perhydrindane CE-ring analogues.
AID1824232Inhibition of hedgehog signalling in mouse ASZ001 cells assessed as reduction in Gli1 mRNA expression measured after 48 hrs by RT-PCR analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma.
AID1235843Displacement of [3H]-1alpha25-(OH)2D3 from full length recombinant rat vitamin D receptor by scintillation counting analysis2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Novel 9-Alkyl- and 9-Alkylidene-Substituted 1α,25-Dihydroxyvitamin D3 Analogues: Synthesis and Biological Examinations.
AID688523Cytotoxicity against human HCT116 assessed as decrease in cell count after 120 hrs2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of a new vitamin D2 analogue.
AID622098Activity at human VDR expressed in human HOS cells transfected with pGL3-hOc, pCDNA-hVDR and phRL-TK assessed as assessed as transcriptional activation measured 24 hrs post infection by luciferase reporter gene assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Design, synthesis and X-ray crystallographic study of new nonsecosteroidal vitamin D receptor ligands.
AID1408641Hypercalcemic effect in Balb/c nude mouse xenografted with human MCF7 cells assessed as effect on serum calcium level at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation measured on day 17 duri2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID619497Induction of bone calcium mobilization in Sprague-Dawley rat assessed as concentration of serum calcium at 260 pmol, ip administered as 4 consecutive doses once in 24 hrs measured 24 hrs post last dose (Rvb = 4.3 mg/dl)2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis and biological activity of 2-(3'-hydroxypropylidene)-1α-hydroxy-19-norvitamin D analogues with shortened alkyl side chains.
AID1267638Displacement of [3H]-1,25(OH)2D3 from recombinant human VDR ligand binding domain2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis, Biological Activities, and X-ray Crystal Structural Analysis of 25-Hydroxy-25(or 26)-adamantyl-17-[20(22),23-diynyl]-21-norvitamin D Compounds.
AID414864Activation of VDR in human THP1 cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression by RT-PCR2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
AID1218511Drug metabolism in CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP450 inhibitor SKF525A2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID688521Toxicity in mouse assessed as increase in haematocrit at 5 ug/kg, ip qd for 4 days after 72 hrs of last postdose2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of a new vitamin D2 analogue.
AID1140506Inhibition of hedgehog signaling pathway in VDR-knockdown mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Structure-activity relationships for vitamin D3-based aromatic a-ring analogues as hedgehog pathway inhibitors.
AID190594Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5000 pmol at 2 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID326338Agonist activity at human VDR in COS7 cells assessed as induction of transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
2-Methylene 19-nor-25-dehydro-1alpha-hydroxyvitamin D3 26,23-lactones: synthesis, biological activities and molecular basis of passive antagonism.
AID366877Inhibition of 1,25-(OH)2D3-induced cell differentiation in human HL60 cells assessed as morphological changes at 10'-6 M by Wright-Geimsa staining2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
A new class of vitamin D analogues that induce structural rearrangement of the ligand-binding pocket of the receptor.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID190596Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5000 pmol at 48 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID191113Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 50 pmol at 2 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1266897Antipoliferative activity against human Caco2 cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.
AID216841Binding affinity for human vitamin D binding protein (hDBP) relative to 1,25(OH)2D3 (100)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Synthesis, biological activity, and conformational analysis of four seco-D-15,19-bisnor-1alpha,25-dihydroxyvitamin D analogues, diastereomeric at C17 and C20.
AID1455881Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 1 uM after 24 hrs by propidium iodide-staining based flow cytometry (Rvb = 12.41%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID527087Agonist activity at VDR in human SCC25 cells assessed as induction of CYP24 expression at 10 nM2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
An o-aminoanilide analogue of 1α,25-dihydroxyvitamin D(3) functions as a strong vitamin D receptor antagonist.
AID1164476Ratio of 1alpha,25-(OH)2D3 ED50 to compound ED50 for VDR-mediated 24-hydroxylase gene expression in rat ROS 17/2.8 cells after 16 hrs by luciferase reporter assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Synthesis and Biological Activity of 25-Hydroxy-2-methylene-vitamin D3 analogues monohydroxylated in the A-ring.
AID190744Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5 pmol at 4 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID82816In vitro biological evaluation was determined on HL60 cell line, results expressed as percentage activity at 50% dose response2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Vitamin D(3): synthesis of seco C-9,11,21-trisnor-17-methyl-1 alpha, 25-dihydroxyvitamin D(3) analogues.
AID1135787Induction of intestinal calcium absorption in vitamin-D-deficient chicken assessed per 0.2 ml of plasma at 0.60 nmol, ip using 45Ca2+ and 40Ca2+ after 12 hrs relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Studies on vitamin D (calciferol) and its analogues. 15. 24-Nor-1alpha,25-dihydroxyvitamin D3 and 24-nor-25-hydroxy-5,6-trans-vitamin D3.
AID227719Ratio of average ED50 to 1-alpha,25-(OH)2D3 ED50 for binding assay2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
2-Ethyl and 2-ethylidene analogues of 1alpha,25-dihydroxy-19-norvitamin D(3): synthesis, conformational analysis, biological activities, and docking to the modeled rVDR ligand binding domain.
AID1613201Hypercalcemic effect in BALB/C nude mouse xenografted with human MCF7 cells at 0.5 ug/kg, ip administered 3 times per week measured after 15 days2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID1153079Transactivation of human VDR D149A mutant expressed in HEK293 cells coexpressing CYP3A4 at 10 nM by dual luciferase reporter gene assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Structural insights into the molecular mechanism of vitamin D receptor activation by lithocholic acid involving a new mode of ligand recognition.
AID1375599Agonist activity at VDR in human MCF7 cells assessed as upregulation of p53 expression at 10'-9 M after 48 hrs by Western blot method relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID1267786Induction of intestinal calcium transport in weaning Sprague-Dawley rat assessed as ratio of calcium level in serosal to mucosal at 87 pmol, ip for 4 consecutive dose at an interval of 24 hrs measured 24 hrs after last dose (Rvb = 3.7 to 4.8 No_unit)2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
A Methylene Group on C-2 of 24,24-Difluoro-19-nor-1α,25-dihydroxyvitamin D3 Markedly Increases Bone Calcium Mobilization in Vivo.
AID1408612Induction of apoptosis in human MCF7 cells expressing scrambled siRNA assessed as late apoptotic cells at 1 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.98%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID216855Relative binding affinity for chick intestinal Vitamin D3 receptor (VDR)1999Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
Synthesis and biological evaluation of 1alpha,24-dihydroxy-25-nitrovitamin D3.
AID601959Antiproliferative activity against human MCF7 cells assessed as DNA level at 100 nM measured after 6 days by calorimetric analysis2011Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D(3) analogues hydroxymethylated at C-26.
AID216987Binding affinity for bovine thymus vitamin D3 receptor2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID1267664Drug uptake in human MG63 cells at 1 uM after 5 mins by HPLC analysis in presence of 10% FBS2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis, Biological Activities, and X-ray Crystal Structural Analysis of 25-Hydroxy-25(or 26)-adamantyl-17-[20(22),23-diynyl]-21-norvitamin D Compounds.
AID1455880Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide-staining based flow cytometry (Rvb = 56.03%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID82500Inhibition of colony formation assays on HL-60 cells2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Characterization of a novel analogue of 1alpha,25(OH)(2)-vitamin D(3) with two side chains: interaction with its nuclear receptor and cellular actions.
AID1824236Inhibition of hedgehog signalling in mouse C3H 10T1/2 cells assessed as reduction in Gli1 mRNA expression measured after 48 hrs by RT-PCR analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma.
AID171506Support of Intestinal Calcium Transport mobilization response of Vitamin D-Deficient Rats on a low-calcium diet(amount 260 pmol)1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis and biological activity of 1 alpha, 25-dihydroxy-18-norvitamin D3 and 1 alpha, 25-dihydroxy-18,19-dinorvitamin D3.
AID216984Binding affinity at bovine thymus Vitamin D3 receptor relative to 1-alpha,25-Dihydroxyvitamin D3.2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Concise synthesis and biological activities of 2alpha-alkyl- and 2alpha-(omega-hydroxyalkyl)-20-epi-1alpha,25-dihydroxyvitamin D3.
AID216842Percentage binding to Human Vitamin D binding protein, relative competitive index (RCI)2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Characterization of a novel analogue of 1alpha,25(OH)(2)-vitamin D(3) with two side chains: interaction with its nuclear receptor and cellular actions.
AID1191646Inhibition of human VDR-cofactor interaction by EnBio receptor cofactor assay system2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Structural development of stapled short helical peptides as vitamin D receptor (VDR)-coactivator interaction inhibitors.
AID103396Percent inhibition against MCF-7 cell line (50% dose response), relative to 1-alpha,25 (OH)2D3 (100% activity) determined in vitro2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Vitamin D(3): synthesis of seco-C-9,11-bisnor-17-methyl-1 alpha,25-dihydroxyvitamin D(3) analogues.
AID703629Agonist activity at VDR in human SW480-ADH cells assessed as induction of cystatin-D expression at 10 '-8 M after 24 hrs by Western blot analysis relative to control2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID171374Intestinal Calcium Transport mobilization response of Vitamin D-Deficient Rats to a single Intravenous Injection of D3 (amount 260 pmol)1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis and biological activity of 1 alpha, 25-dihydroxy-18-norvitamin D3 and 1 alpha, 25-dihydroxy-18,19-dinorvitamin D3.
AID1613171Antitumor activity against human MCF7 cells xenografted in BALB/C nude mouse assessed as reduction in tumor volume at 0.5 ug/kg, ip administered 3 times per week2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID647006Induction of vitamin D receptor-mediated differentiation of human HL60 cells at 10'-5 M by NBT reduction method2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Novel vitamin D receptor ligands bearing a spherical hydrophobic core structure--comparison of bicyclic hydrocarbon derivatives with boron cluster derivatives.
AID1153082Transactivation of human VDR Q239A mutant expressed in HEK293 cells coexpressing CYP3A4 at 10 nM by dual luciferase reporter gene assay relative to wild-type human VDR2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Structural insights into the molecular mechanism of vitamin D receptor activation by lithocholic acid involving a new mode of ligand recognition.
AID1852315Competitive binding affinity to His-tagged human VDR LBD (156 to 453 residues) expressed in Escherichia coli BL23 (DE3) cells in presence of 1,25D3 by fluorescent polarization assay
AID1408610Induction of apoptosis in human MCF7 cells expressing scrambled siRNA assessed as live cells at 1 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometry (Rvb = 97.93%)2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID337283Induction of terminal cell differentiation in human HL60 cells assessed as inhibition of [3H]thymidine incorporation at 0.0001 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1455886Induction of apoptosis in human MCF7 cells assessed as necrotic cells at 1 uM after 24 hrs by Annexin V-FITC/propidium iodide-staining based flow cytometry (Rvb = 0.031%)2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID1375598Agonist activity at VDR in human MCF7 cells assessed as upregulation of p27 expression at 10'-7 M after 48 hrs by Western blot method relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID1142115Induction of cyp24A1 mRNA expression in HEK293 cells at 100 nM after 24 hrs by real-time PCR2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Combination of triple bond and adamantane ring on the vitamin D side chain produced partial agonists for vitamin D receptor.
AID1613153Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID1235861Induction of intestinal calcium transport in Sprague-Dawley rat assessed as ratio of serosal calcium to mucosal calcium level at 260 pmol, ip administered 4 doses at 24 hrs interval measured 24 hrs post last dose by everted gut sac method (Rvb = 4.3 No_un2015Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
Novel 9-Alkyl- and 9-Alkylidene-Substituted 1α,25-Dihydroxyvitamin D3 Analogues: Synthesis and Biological Examinations.
AID488256Toxicity in FVB mouse assessed as calcium level in blood at 12 pmol/day administered via osmotic pump for 6 to 7 days measured on day 4 by microchemistry (RVb = 2.11 mmol/L)2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID1375595Agonist activity at VDR in human MCF7 cells assessed as upregulation of p21 expression at 10'-7 M after 48 hrs by Western blot method relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID305714Induction of human HL60 cells differentiation assessed as number of cells at 0.02 uM after 72 hrs by NBT reduction test2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Rotenoids and flavonoids with anti-invasion of HT1080, anti-proliferation of U937, and differentiation-inducing activity in HL-60 from Erycibe expansa.
AID216860Affinity for bovine Vitamin D3 receptor1999Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7
Three-dimensional structure-function relationship of vitamin D: side chain location and various activities.
AID190600Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 500 pmol at 12 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID229238Compound was tested for binding affinity against rat serum DBP (vitamin D binding protein)2000Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
Syntheses and biological evaluation of novel 2alpha-substituted 1alpha,25-dihydroxyvitamin D3 analogues.
AID191117Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 50 pmol at 69 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID107136Calcemic effect in vivo in vitamin D-replete normal NMRI mice by daily intraperitoneal injections of compound and 1-alpha,25 (OH)2D3 for 7 consecutive days2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Vitamin D(3): synthesis of seco-C-9,11-bisnor-17-methyl-1 alpha,25-dihydroxyvitamin D(3) analogues.
AID217167Binding affinity to VDR receptor2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
New dermatological agents for the treatment of psoriasis.
AID1353232Inhibition of fluoromone VDR red binding to human VDR LBD expressed in insect cells at 1 uM by fluorescent polarization assay relative to 1,25(OH)2D32018European journal of medicinal chemistry, Feb-25, Volume: 146Design, synthesis and biological evaluation of non-secosteriodal vitamin D receptor ligand bearing double side chain for the treatment of chronic pancreatitis.
AID216985Binding affinity for bovine thymus Vitamin D3 receptor (VDR)1998Bioorganic & medicinal chemistry letters, Jan-20, Volume: 8, Issue:2
A novel and practical route to A-ring enyne synthon for 1 alpha,25-dihydroxyvitamin D3 analogs: synthesis of A-ring diastereomers of 1 alpha,25-dihydroxyvitamin D2 and 3-methyl-1,25-dihydroxyvitamin D3.
AID1613159Induction of apoptosis in human MCF7 cells assessed as viable cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 94.3%)2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID1160921Effect on CYP24A1 in human primary CLL cells assessed as increase in VDR-regulated GADD45alpha mRNA expression at 100 nM incubated for 24 hrs by quantitative RT-PCR method2014Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation.
AID1455872Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID703622Effect on cellular PIP4K2B mRNA level in human SW480-ADH cells at 10 '-9 to 10 '-7 M after 48 hrs by RT-PCR analysis2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID1309801Antiinflammatory activity in DBA/1 mouse splenocytes assessed as upregulation of LAIR1 level by measuring mean fluorescence intensity at 100 nM by flow cytometry (Rvb = 766 +/- 22 au)2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Synthesis and Biological Evaluation of Vitamin D3 Metabolite 20S,23S-Dihydroxyvitamin D3 and Its 23R Epimer.
AID1506120Stability in human MG63 cells assessed as parent compound remaining at 1 uM after 24 hrs by HPLC analysis2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
25 S-Adamantyl-23-yne-26,27-dinor-1α,25-dihydroxyvitamin D
AID352236Effect on intestinal calcium transport in vitamin D-deficient weanling Sprague-Dawley rat assessed as increase in ratio of serosal to mucosal calcium level at 260 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose by ev2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID590449Induction of CYP24 mRNA expression in human A498 cells at 10'-8 M after 16 hrs by RT-PCR analysis2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
1α,25-Dihydroxyvitamin D3-3β-bromoacetate, a potential cancer therapeutic agent: synthesis and molecular mechanism of action.
AID761797Agonist activity at human VDR2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Development of stapled short helical peptides capable of inhibiting vitamin D receptor (VDR)-coactivator interactions.
AID102442In vitro activity expressed as effective dose to inhibit the proliferation of human breast cancer cells (MCF-7) by measuring [3H]thymidine incorporation1999Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7
Three-dimensional structure-function relationship of vitamin D: side chain location and various activities.
AID1218491Cmax in healthy human co-treated with 600 mg ritonavir2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID191121Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5 pmol at 24 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID427506Induction of cell differentiation in human NB4 cells assessed as induction of induction of cell surface marker CD11b expression at 1 nM after 48 hrs2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Calcitriol derivatives with two different side chains at C-20. V. Potent inhibitors of mammary carcinogenesis and inducers of leukemia differentiation.
AID250004Effect of compound on Ca level in mice blood serum was determined2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Synthesis and biological activity of 22-oxa CD-ring modified analogues of 1alpha,25-dihydroxyvitamin D3: cis-perhydrindane CE-ring analogues.
AID1613161Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 56.64%)2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID191247Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5 pmol at 4 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1585882Inhibition of Hedgehog signaling pathway in Sufu-deficient mouse C3H10T1/2 cells assessed as reduction in oxysterol-induced Gli1 mRNA expression at 1 uM after 24 hrs by q-PCR analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID82166Ability to induce differentiation of human promyelocyte HL-60 cells into monocytes.2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
2-Ethyl and 2-ethylidene analogues of 1alpha,25-dihydroxy-19-norvitamin D(3): synthesis, conformational analysis, biological activities, and docking to the modeled rVDR ligand binding domain.
AID455174Effect on intestinal calcium transport in weanling Sprague-Dawley rat assessed as ratio of serosal to mucosal calcium level at 2340 pmol/day, ip administered for 4 consecutive days measured 24 hrs after last dose by everted gut sac method2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
AID1455874Antiproliferative activity against human Caco2 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID619442Displacement of radiolabeled 1alpha, 25-(OH)2D3 from recombinant rat VDR2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis and biological activity of 2-(3'-hydroxypropylidene)-1α-hydroxy-19-norvitamin D analogues with shortened alkyl side chains.
AID1267665Drug uptake in human MG63 cells at 1 uM after 10 mins by HPLC analysis in presence of 10% FBS2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis, Biological Activities, and X-ray Crystal Structural Analysis of 25-Hydroxy-25(or 26)-adamantyl-17-[20(22),23-diynyl]-21-norvitamin D Compounds.
AID703627Agonist activity at VDR in human SW480-ADH cells assessed as induction of E-cadherin at 10 '-7 M after 24 hrs by Western blot analysis relative to control2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID1118427Agonist activity at zebrafish gal4-VDR LBD expressed in human MCF7 cells by luciferase reporter gene based transactivation assay2011MedChemComm, , Volume: 2, Issue:5
Structure-function study of gemini derivatives with two different side chains at C-20, Gemini-0072 and Gemini-0097.
AID1160918Induction of apoptosis in normal human B cells after 48 hrs by Annexin V/propidium iodide staining based flow cytometry2014Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation.
AID1455879Displacement of fluormone VDR red from human full length VDR after 4 hrs by fluorescence polarization assay2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID190591Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5000 pmol at 12 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1218457Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2E inhibitor di-ethyldithiocarbamate2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID688526Cytotoxicity against human T98G assessed as decrease in cell count after 120 hrs2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of a new vitamin D2 analogue.
AID190745Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5 pmol at 69 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1613158Induction of apoptosis in human MCF7 cells assessed as necrotic cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.29%)2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID741576Prevention of bone mineral density loss in ovariectomized immatured Sprague-Dawley rat osteoporosis model at 320 ng/kg, po once daily for 5 times per week for 4 weeks relative to control2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
A series of nonsecosteroidal vitamin D receptor agonists for osteoporosis therapy.
AID110583In Vivo evaluation for the calcemic activity in vitamin D-replete normal in NMRI mice1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Synthesis, biological activity, and conformational analysis of four seco-D-15,19-bisnor-1alpha,25-dihydroxyvitamin D analogues, diastereomeric at C17 and C20.
AID392907Activity at VDR in rat ROS 17/2.8 cells assessed as transcriptional activation of 24-hydroxylase gene promoter after 16 hrs by luciferase reporter gene assay2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID337037Induction of terminal cell differentiation in human HL60 cells at 0.001 uM after 4 days by NBT reduction assay1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1408642Hypercalcemic effect in Balb/c nude mouse xenografted with human MCF7 cells assessed as effect on serum calcium level at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation measured on day 27 (Rvb2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID190743Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5 pmol at 48 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID103409Inhibition of colony formation assays on MCF-7 cells2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Characterization of a novel analogue of 1alpha,25(OH)(2)-vitamin D(3) with two side chains: interaction with its nuclear receptor and cellular actions.
AID725917Agonist activity at RAR (unknown origin) expressed in human HCT116 cells co-expressing RARE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay2013Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
Synthesis and biological evaluation of halogenated curcumin analogs as potential nuclear receptor selective agonists.
AID414863Activation of VDR in LPS-stimulated human PBMC cells assessed as increase in 25-hydroxyvitamin D-24-hydroxylase mRNA expression at 10 nM after upto 8 hrs by RT-PCR2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
AID166890In vitro vitamin D receptor (VDR)-mediated transcriptional potency in rat osteosarcoma ROS 17/2.8 cells2000Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19
Conceptually new 20-epi-22-oxa sulfone analogues of the hormone 1alpha,25-dihydroxyvitamin D(3): synthesis and biological evaluation.
AID1218468Drug metabolism in CD1 mouse liver microsomes assessed as 1 uM CYP3A inhibitor-mediated inhibition of metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID547394Induction of differentiation of human HL60 cells promyelocytes to monocytes after 4 days by NBT reduction assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Removal of the 26-methyl group from 19-nor-1α,25-dihydroxyvitamin D₃ markedly reduces in vivo calcemic activity without altering in vitro VDR binding, HL-60 cell differentiation, and transcription.
AID1661597Binding affinity to H12 region of zebrafish VDR LBD assessed as stabilization of structural elements forming LBP at 10 fold excess compound concentration by HDX-MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Structural Analysis of VDR Complex with ZK168281 Antagonist.
AID635525Calcium mobilization in vitamin-D deficient weanling rat bone assessed as increase in serum calcium level at 0.7 ug/kg, ip administered daily for 7 consecutive days measured 24 hrs after last dose relative to vehicle treated control2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.
AID216833The affinity to the pig intestinal mucosa vitamin D receptor was evaluated in vitro, results expressed as percentage activity at 50% dose response2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Vitamin D(3): synthesis of seco C-9,11,21-trisnor-17-methyl-1 alpha, 25-dihydroxyvitamin D(3) analogues.
AID392906Induction of cell differentiation of human HL60 cells to monocytes by NBT reduction assay2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID230236Intestinal Calcium Transport (ICT) activity (260 pmol/day/7 days) in Vitamin D-Deficient Rats on a Low-Calcium Diet (0.47% Ca diet)2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID305709Antiproliferative activity against human HL60 cells assessed NBT positive cells at 0.01 uM after 72 hrs by NBT reduction test2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Rotenoids and flavonoids with anti-invasion of HT1080, anti-proliferation of U937, and differentiation-inducing activity in HL-60 from Erycibe expansa.
AID619494Induction of bone calcium mobilization in Sprague-Dawley rat assessed as concentration of serum calcium at 780 pmol, ip administered as 4 consecutive doses once in 24 hrs measured 24 hrs post last dose (Rvb = 4.5 mg/dl)2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis and biological activity of 2-(3'-hydroxypropylidene)-1α-hydroxy-19-norvitamin D analogues with shortened alkyl side chains.
AID488356Binding affinity to VDR ligand binding domain by fluorescence polarization competition assay2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID230234Intestinal Calcium Transport (ICT) activity (260 pmol/day/7 days) in Vitamin D-Deficient Rats on a Low-Calcium Diet2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID1613157Induction of apoptosis in human MCF7 cells assessed as late apoptotic cells at 1 uM after 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.61%)2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID1613162Cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 1 uM after 24 hrs by propidium iodide staining based flow cytometric analysis (Rvb = 12.04%)2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of novel nonsteroidal VDR agonists with novel diarylmethane skeleton for the treatment of breast cancer.
AID1585878Half life in rat liver homogenates2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID672800Inhibition of VDR-induced 24-hydroxylase transcription in rat osteosarcoma cells after 16 hrs by luciferase reporter gene assay2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
A 20S combined with a 22R configuration markedly increases both in vivo and in vitro biological activity of 1α,25-dihydroxy-22-methyl-2-methylene-19-norvitamin D3.
AID274536Stabilization of human [35S]VDR against trypsin digestion by protease assay2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
AID472019Antiproliferative activity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Synthesis, conformational analysis, and biological evaluation of 19-nor-vitamin D3 analogues with A-ring modifications.
AID703628Agonist activity at VDR in human SW480-ADH cells assessed as repression of c-Myc expression at 10 '-8 M after 24 hrs by Western blot analysis relative to control2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID281993Metabolic stability in rat kidney perfusate2004Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26
Calcitriol derivatives with two different side chains at C-20. II. Diastereoselective syntheses of the metabolically produced 24(R)-hydroxygemini.
AID488247Toxicity in FVB mouse assessed as calcium level in blood at 24 pmol/day administered via osmotic pump for 6 to 7 days measured on day 3 by microchemistry (RVb = 2.24 mmol/L)2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID244283Percent binding affinity for bovine vitamin D receptor compared to 1a2005Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
New derivatives of 1alpha,25-dihydroxy-19-norvitamin D3 with two substituents at C-2: synthesis and biological activity.
AID392905Displacement of [3H]1-alpha,25-(OH)2D3 from rat recombinant full length VDR2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID1408602Binding affinity to VDR in scrambled siRNA-transfected human MCF7 cells assessed as cell growth inhibition by measuring reduction in BrdU incorporation after 16 hrs by ELISA2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID647368Activation of VDR in mouse C3H10T1/2 cells assessed as up-regulation of CYP24A1 after 24 hrs by RT-PCR analysis relative to control2012Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
Evaluation of vitamin D3 A-ring analogues as Hedgehog pathway inhibitors.
AID414869Inhibition of LPS-induced IL6 production in human PBMC after 24 hrs by ELISA2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
AID337313Induction of terminal cell differentiation in human HL60 cells assessed as cell viability at 0.1 uM by trypan blue exclusion method1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1267157Effect on intestinal calcium transport in weanling Sprague-Dawley rat assessed as increase in ratio of serosal to mucosal calcium level at 780 pmol/day administered as 4 consecutive daily doses measured 24 hrs after last dose relative to control2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis and Biological Activity of 2-Methylene Analogues of Calcitriol and Related Compounds.
AID1187832Antiproliferative activity against human MCF7 cells assessed as inhibition of proliferation after 72 hrs by MTT assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D3 analogues with aromatic side chains attached at C-17.
AID216840Binding affinity for calf serum vitamin D receptor interacting protein2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID635567Calcium transport in vitamin-D deficient weanling rat intestine assessed as intestinal calcium level at 19 ug/kg, ip administered daily for 7 consecutive days measured 24 hrs after last dose2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.
AID103202In vitro cell proliferative activity on MCF-7 cells1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Synthesis, biological activity, and conformational analysis of four seco-D-15,19-bisnor-1alpha,25-dihydroxyvitamin D analogues, diastereomeric at C17 and C20.
AID1218500Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as 1alpha,24S,25(OH)3D3 metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID303413Increase in serum calcium in vitamin D deficient CD1 mouse at 5.4 ug/mg, ip after 24 hrs2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Design, synthesis, and biological evaluation of a 1alpha,25-dihydroxy-19-norvitamin D3 analogue with a frozen A-ring conformation.
AID1506118Drug uptake in human MG63 cells at 1 uM after 5 mins by HPLC analysis2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
25 S-Adamantyl-23-yne-26,27-dinor-1α,25-dihydroxyvitamin D
AID106489In vitro biological evaluation was determined on MG-63 cell line, results expressed as percentage activity at 50% dose response2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Vitamin D(3): synthesis of seco C-9,11,21-trisnor-17-methyl-1 alpha, 25-dihydroxyvitamin D(3) analogues.
AID414868Inhibition of LPS-induced IL12/23p40 production in human PBMC after 24 hrs by ELISA2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
AID217013Vitamin D3 receptor-mediated transcriptional potency in rat osteosarcoma ROS 17/2.8 cells1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Conceptually new sulfone analogues of the hormone 1alpha, 25-dihydroxyvitamin D(3): synthesis and preliminary biological evaluation.
AID81119In vitro induction of cell differentiation in HL-60 cells relative to 1,25(OH)2D3 (100)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Synthesis, biological activity, and conformational analysis of four seco-D-15,19-bisnor-1alpha,25-dihydroxyvitamin D analogues, diastereomeric at C17 and C20.
AID1135776Induction of intestinal calcium absorption in vitamin-D-deficient chicken assessed per 0.2 ml of plasma at 0.60 nmol, ip using 45Ca2+ and 40Ca2+ after 12 hrs1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Studies on vitamin D (calciferol) and its analogues. 15. 24-Nor-1alpha,25-dihydroxyvitamin D3 and 24-nor-25-hydroxy-5,6-trans-vitamin D3.
AID652549Antiproliferative activity against mouse SVEC cells assessed as decrease in cell number after 72 hrs by WST assay2011ACS medicinal chemistry letters, Jul-14, Volume: 2, Issue:7
Novel alkynylphosphonate analogue of calcitriol with potent antiproliferative effects in cancer cells and lack of calcemic activity.
AID1506107Transrepression of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-NCoR and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in NCoR recruitment by beta-galactosidase reporter gene based mammalian two-hybrid assay2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
25 S-Adamantyl-23-yne-26,27-dinor-1α,25-dihydroxyvitamin D
AID635527Calcium mobilization in vitamin-D deficient weanling rat bone assessed as increase in serum calcium level at 19 ug/kg, ip administered daily for 7 consecutive days measured 24 hrs after last dose relative to vehicle treated control2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.
AID1135798Induction of intestinal calcium absorption in vitamin-D-deficient chicken assessed per 0.2 ml of plasma at 163 nmol, ip using 45Ca2+ and 40Ca2+ after 5 to 36 hrs1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Studies on vitamin D (calciferol) and its analogues. 15. 24-Nor-1alpha,25-dihydroxyvitamin D3 and 24-nor-25-hydroxy-5,6-trans-vitamin D3.
AID1505674Displacement of [3H]-1,25D3 from C-terminal GST-tagged human recombinant VDR LBD expressed in Escherichia coli BL21 (DE3) after 16 hrs by radioligand binding assay2018Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14
Identification of the Histidine Residue in Vitamin D Receptor That Covalently Binds to Electrophilic Ligands.
AID229237Inhibition of 1-alpha,25-(OH)2D3 binding to porcine intestinal vitamin D receptor1998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
New 1alpha,25-dihydroxy-19-norvitamin D3 compounds of high biological activity: synthesis and biological evaluation of 2-hydroxymethyl, 2-methyl, and 2-methylene analogues.
AID191099Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5000 pmol at 69 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID337315Induction of terminal cell differentiation in human HL60 cells assessed as cell viability at 0.001 uM by trypan blue exclusion method1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID52879In Vivo evaluation for the calcemic activity in vitamin D-replete normal in ICA chick1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Synthesis, biological activity, and conformational analysis of four seco-D-15,19-bisnor-1alpha,25-dihydroxyvitamin D analogues, diastereomeric at C17 and C20.
AID760217Transactivation of VDR-mediated osteocalcin promoter in human HOS/SF cells after 24 hrs by luciferase reporter gene assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Synthesis of 2α-heteroarylalkyl active vitamin d3 with therapeutic effect on enhancing bone mineral density in vivo.
AID760212Antiosteoporotic activity in ovariectomized Sprague-Dawley rat osteoporosis model assessed as increase in bone mineral density in spine at 0.025 mg/kg/day administered 5 times a week for 4 weeks measured 24 hrs post last dose by dual X-ray absorption mete2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Synthesis of 2α-heteroarylalkyl active vitamin d3 with therapeutic effect on enhancing bone mineral density in vivo.
AID51090Effect on bone calcium mobilization was measured in vivo, in the vitamin D deficient chick1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Arocalciferols: synthesis and biological evaluation of aromatic side-chain analogues of 1 alpha,25-dihydroxyvitamin D3(1a).
AID280118Effect on intestinal calcium transport in low-calcium diet fed rat assessed as serosal:mucosal ratio of calcium at 325 pmol/day, ip after 7 days2007Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
22-Alkyl-20-epi-1alpha,25-dihydroxyvitamin D3 compounds of superagonistic activity: syntheses, biological activities and interaction with the receptor.
AID80955Compound was evaluated for HL-60 cell differentiation which was assessed in terms of expression of antigen CD11b2000Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
Syntheses and biological evaluation of novel 2alpha-substituted 1alpha,25-dihydroxyvitamin D3 analogues.
AID1375587Antiproliferative activity against 2D culture of human HaCaT cells assessed as cell proliferation at 100 nM after 48 hrs by MTT assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID1423169Antifibrotic activity in C57BL/6J mouse model of CCl4-induced liver fibrosis assessed as reduction in hydroxyproline levels in liver at 20 ug/kg, po administered 5 times a week via gavage measured at 72 hrs post final CCl4 injection2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Design, Synthesis, and Antifibrosis Activity in Liver of Nonsecosteroidal Vitamin D Receptor Agonists with Phenyl-pyrrolyl Pentane Skeleton.
AID741569Toxicity in ovariectomized immatured Sprague-Dawley rat osteoporosis model assessed as effect on serum calcium level at 20 ng/kg, po once daily for 5 times per week for 4 weeks relative to control2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
A series of nonsecosteroidal vitamin D receptor agonists for osteoporosis therapy.
AID352237Effect on intestinal calcium transport in vitamin D-deficient weanling Sprague-Dawley rat assessed as increase in ratio of serosal to mucosal calcium level at 780 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose by ev2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID547391Activity at rat recombinant full length VDR expressed in rat ROS 17/2.8 cells transfected with 24-hydroxylase gene promoter assessed as transcriptional activation after 16 hrs by luciferase reporter gene assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Removal of the 26-methyl group from 19-nor-1α,25-dihydroxyvitamin D₃ markedly reduces in vivo calcemic activity without altering in vitro VDR binding, HL-60 cell differentiation, and transcription.
AID1267156Effect on intestinal calcium transport in weanling Sprague-Dawley rat assessed as increase in ratio of serosal to mucosal calcium level at 87 pmol/day administered as 4 consecutive daily doses measured 24 hrs after last dose relative to control2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Synthesis and Biological Activity of 2-Methylene Analogues of Calcitriol and Related Compounds.
AID472015Displacement of [3H]1-alpha,25-(OH)2D3 from VDR in pig intestinal mucosa2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Synthesis, conformational analysis, and biological evaluation of 19-nor-vitamin D3 analogues with A-ring modifications.
AID252629NBT positivity against human leukemia cell line HL-60 at 1*E-8 M2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Cell differentiation inducers derived from thalidomide.
AID337294Induction of terminal cell differentiation in human HL60 cells assessed as inhibition of [3H]thymidine incorporation at 1 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID741568Toxicity in ovariectomized immatured Sprague-Dawley rat osteoporosis model assessed as effect on serum calcium level at 80 ng/kg, po once daily for 5 times per week for 4 weeks relative to control2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
A series of nonsecosteroidal vitamin D receptor agonists for osteoporosis therapy.
AID1160922Effect on CYP24A1 in human primary CLL cells assessed as increase in VDR-regulated CDKN1A mRNA expression at 100 nM incubated for 24 hrs by quantitative RT-PCR method2014Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation.
AID1744120Agonist activity at human VDR expressed in HEK293 cells expressing mouse osteopontin VDRE assessed as induction of receptor transactivation incubated for 16 hrs by luciferase reporter gene assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.
AID1160920Effect on CYP24A1 in human primary CLL cells assessed as effect on VDR-regulated CDKN1A mRNA expression at 10 nM incubated for 24 hrs by quantitative RT-PCR method2014Journal of medicinal chemistry, Sep-25, Volume: 57, Issue:18
Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation.
AID321025-hydroxyvitamin D3-1-hydroxylase activity (10e-6 M) was measured as %control1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Arocalciferols: synthesis and biological evaluation of aromatic side-chain analogues of 1 alpha,25-dihydroxyvitamin D3(1a).
AID725919Agonist activity at glucocorticoid receptor (unknown origin) expressed in human HCT116 cells co-expressing GRE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay2013Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
Synthesis and biological evaluation of halogenated curcumin analogs as potential nuclear receptor selective agonists.
AID647370Inhibition of Hedgehog signaling pathway in mouse C3H10T1/2 cells assessed as down regulation of Gli1 at 0.5 to 5 uM after 24 hrs by RT-PCR analysis2012Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
Evaluation of vitamin D3 A-ring analogues as Hedgehog pathway inhibitors.
AID688529Toxicity in mouse assessed as mortality at 5 ug/kg, ip qd for 4 days2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of a new vitamin D2 analogue.
AID652558Hypercalcemic activity in CF1 mouse assessed as increase in plasma calcium level at 5 to 20 ug/kg, ip qd for 5 days measured after 96 hrs2011ACS medicinal chemistry letters, Jul-14, Volume: 2, Issue:7
Novel alkynylphosphonate analogue of calcitriol with potent antiproliferative effects in cancer cells and lack of calcemic activity.
AID455164Activity at VDR in rat osteosarcoma cells assessed as induction of 24-hydroxylase reporter gene transcription by luciferase reporter gene assay2009Bioorganic & medicinal chemistry, Nov-15, Volume: 17, Issue:22
Removal of the 20-methyl group from 2-methylene-19-nor-(20S)-1alpha,25-dihydroxyvitamin D(3) (2MD) selectively eliminates bone calcium mobilization activity.
AID100406Inhibition of colony formation assays on LNCaP cells; (NR: not reached at <= 10e -6M)2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Characterization of a novel analogue of 1alpha,25(OH)(2)-vitamin D(3) with two side chains: interaction with its nuclear receptor and cellular actions.
AID1251254Transactivation of VDR in human Caco2 cells after 24 hrs by luciferase reporter gene assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Chemical Synthesis and Biological Activities of 20S,24S/R-Dihydroxyvitamin D3 Epimers and Their 1α-Hydroxyl Derivatives.
AID1118431Antiproliferative activity against ER positive human MCF10DCIS.com cells after 3 days by [3H]thymidine uptake assay2011MedChemComm, , Volume: 2, Issue:5
Structure-function study of gemini derivatives with two different side chains at C-20, Gemini-0072 and Gemini-0097.
AID217008Displacement of 50% binding of [3H]alpha,25 (OH)2D3 from pig intestinal mucosa Vitamin D3 receptor2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Vitamin D(3): synthesis of seco-C-9,11-bisnor-17-methyl-1 alpha,25-dihydroxyvitamin D(3) analogues.
AID303414Increase in serum calcium in vitamin D deficient CD1 mouse at 181.5 ug/mg, ip after 24 hrs2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Design, synthesis, and biological evaluation of a 1alpha,25-dihydroxy-19-norvitamin D3 analogue with a frozen A-ring conformation.
AID1744114Agonist activity at VDR in human HL-60 cells assessed as induction of cell differentiation of promyelocytes to monocytes after 4 days by NBT reduction assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.
AID1375585Antiproliferative activity against 2D culture of human PC3 cells assessed as cell proliferation at 100 nM after 48 hrs by MTT assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID103218In vitro activity on human breast adenocarcinoma cell line MCF-7 proliferation2000Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19
Conceptually new 20-epi-22-oxa sulfone analogues of the hormone 1alpha,25-dihydroxyvitamin D(3): synthesis and biological evaluation.
AID1218514Drug metabolism in human liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and ritonavir2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID352240Effect on intestinal calcium transport in vitamin D-deficient weanling Sprague-Dawley rat assessed as increase in ratio of serosal to mucosal calcium level at 35100 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose by 2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID51091Effect on intestinal calcium absorption was measured in vivo, in the vitamin D deficient chick1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Arocalciferols: synthesis and biological evaluation of aromatic side-chain analogues of 1 alpha,25-dihydroxyvitamin D3(1a).
AID387115Induction of differentiation of human HL-60 cells promyelocytes to monocytes after 4 days by NBT reduction assay2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
AID1585869Activation of VDR in mouse ASZ001 cells assessed as change in Cyp24A1 mRNA expression at 5 uM after 48 hrs by q-PCR analysis relative to control2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID217010Binding affinity for porcine intestinal Vitamin D3 receptor (VDR)2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
2-Ethyl and 2-ethylidene analogues of 1alpha,25-dihydroxy-19-norvitamin D(3): synthesis, conformational analysis, biological activities, and docking to the modeled rVDR ligand binding domain.
AID741579Agonist activity at VDR in human MG-63 cells expressing VDRE assessed as induction of osteocalcin production after 4 days relative to 1,25(OH)2D32013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
A series of nonsecosteroidal vitamin D receptor agonists for osteoporosis therapy.
AID191097Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5000 pmol at 48 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID227720Ratio of average ED50 to 1R,25-(OH)2D3 ED501998Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
New 1alpha,25-dihydroxy-19-norvitamin D3 compounds of high biological activity: synthesis and biological evaluation of 2-hydroxymethyl, 2-methyl, and 2-methylene analogues.
AID1266893Binding affinity to vitamin D3 receptor (unknown origin) after 4 hrs using fluormone VDR red by polar screen VDR competitor assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.
AID1309798Activation of VDR in human HaCaT cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Synthesis and Biological Evaluation of Vitamin D3 Metabolite 20S,23S-Dihydroxyvitamin D3 and Its 23R Epimer.
AID601956Antiproliferative activity against human MCF7 cells assessed as DNA level measured after 6 days by calorimetric analysis2011Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D(3) analogues hydroxymethylated at C-26.
AID1661596Binding affinity to zebrafish VDR LBD assessed as stabilization of structural elements forming LBP at 10 fold excess compound concentration by HDX-MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Structural Analysis of VDR Complex with ZK168281 Antagonist.
AID387123Effect on bone calcium mobilization in vitamin D-deficient Sprague-Dawley rat assessed as serum calcium level at 260 pmol, ip administered 4 consecutive daily doses assessed after 24 hrs of last dose by spectrometry2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
AID1408598Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID302666Lipophilicity, log D of the compound2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
AID472303Toxicity in NMRI mouse assessed as increase in serum calcium level at 0.1 ug/kg, ip daily for 7 consecutive days measured after day 7 by colorimetric assay2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Synthesis, conformational analysis, and biological evaluation of 19-nor-vitamin D3 analogues with A-ring modifications.
AID672804Calcium mobilization in vitamin-D deficient weanling Sprague-Dawley rat bone assessed as increase in serum calcium level at 32 to 70200 pmol, ip administered every 24 hrs for 4 consecutive days measured 24 hrs post last dose relative to vehicle treated co2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
A 20S combined with a 22R configuration markedly increases both in vivo and in vitro biological activity of 1α,25-dihydroxy-22-methyl-2-methylene-19-norvitamin D3.
AID216998Affinity for porcine Vitamin D3 receptor1999Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7
Three-dimensional structure-function relationship of vitamin D: side chain location and various activities.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID392914Effect on bone calcium mobilization in vitamin D-deficient weanling rat assessed as increase in serum calcium level at 0.2 ug/kg, ip administered as 7 consecutive daily doses measured 24 hrs after last dose relative to untreated control2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID191108Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 500 pmol at 69 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1218466Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as 1 uM CYP3A inhibitor-mediated inhibition of metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID337025Induction of cell differentiation in human HL60 cells assessed as alpha naphthyl esterase activity at 1 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1585868Inhibition of Hedgehog signaling pathway in mouse ASZ001 cells assessed as reduction in oxysterol-induced Gli1 mRNA expression after 48 hrs by q-PCR analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID321741Effect on VDR transcriptional activity in human osteosarcoma cells in presence of 5% fetal calf serum2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
(2S,2'R)-analogue of LG190178 is a major active isomer.
AID1218459Drug metabolism in CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2E inhibitor di-ethyldithiocarbamate2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID770183Binding affinity to His-6-tagged rat VDR wild type over expressed in Escherichia coli C41 assessed as increase in transition temperature by at 5 mM by CD-based spectropolarimetric analysis2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Crystal structures of hereditary vitamin D-resistant rickets-associated vitamin D receptor mutants R270L and W282R bound to 1,25-dihydroxyvitamin D3 and synthetic ligands.
AID1218460Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2A inhibitor 8-methoxypsoralen2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1162462Displacement of [3H]1alpha,25-(OH)2vitamin D3 from human recombinant VDR expressed in Sf9 cells at 10 uM incubated for 20 hrs by scintillation counting method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and preliminary biological evaluation of new antiproliferative aromatic analogues of 1α,25-dihydroxyvitamin D3.
AID1455896Hypercalcemic effect in ICR mouse at 0.5 ug/kg, ip administered for 7 days measured on day 8 post-dose by MTB-based assay relative to control2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID652559Toxicity in CF1 mouse assessed as mortality at 5 to 20 ug/kg, ip qd for 5 days2011ACS medicinal chemistry letters, Jul-14, Volume: 2, Issue:7
Novel alkynylphosphonate analogue of calcitriol with potent antiproliferative effects in cancer cells and lack of calcemic activity.
AID703631Agonist activity at VDR in human SW480-ADH cells assessed as induction of cystatin-D expression at 10 '-9 M after 24 hrs by Western blot analysis relative to control2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID1473745Drug concentration at steady state in human at 1 ug/ml, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1218513Drug metabolism in human liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and docetaxel2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID670418Agonist activity at VDR expressed in human MG63 cells assessed as stimulation of VDRE-mediated luciferase reporter gene activity after 3 days by luminescence analysis relative to 1,25(OH)2D32012Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
Systematic SAR study of the side chain of nonsecosteroidal vitamin D₃ analogs.
AID1585875Clearance in human liver microsomes assessed per mg protein at 1 uM by LC-MS/MS analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID191094Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5000 pmol at 24 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID343854Effect on osteoclast formation in ddY mouse bone marrow cells co cultured with primary osteoclasts after 3 days2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
2-Substituted-16-ene-22-thia-1alpha,25-dihydroxy-26,27-dimethyl-19-norvitamin D3 analogs: Synthesis, biological evaluation, and crystal structure.
AID688522Cytotoxicity against human HN12 assessed as decrease in cell count after 120 hrs2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of a new vitamin D2 analogue.
AID95375Percent inhibition against Keratinocytes cell line (50% dose response), relative to 1-alpha,25 (OH)2D3 (100% activity) determined in vitro2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Vitamin D(3): synthesis of seco-C-9,11-bisnor-17-methyl-1 alpha,25-dihydroxyvitamin D(3) analogues.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID326343Antagonist activity at human VDR in COS7 cells assessed as inhibition of 1,25-(OH)2D3-induced transcriptional transactivation after 24 hrs by mouse osteopontin luciferase reporter gene assay2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
2-Methylene 19-nor-25-dehydro-1alpha-hydroxyvitamin D3 26,23-lactones: synthesis, biological activities and molecular basis of passive antagonism.
AID1686027Agonist activity at human VDR2016Journal of medicinal chemistry, Oct-13, Volume: 59, Issue:19
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.
AID191248Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 5 pmol at 69 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID81984Relative competitive index values for binding to 25-OH-D3-1-hydroxylase of human HL-60 cells1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Arocalciferols: synthesis and biological evaluation of aromatic side-chain analogues of 1 alpha,25-dihydroxyvitamin D3(1a).
AID302664Displacement of 1-alpha, 25-(OH)[3H]D3 from human VDR expressed in COS1 cells2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
AID477394Inhibition of calciuria in rat at 10 ug/kg, po administered qd for 1 week2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
'Novel alkyl side chain sulfone 1alpha,25-dihydroxyvitamin D3 analogs: a comparison of in vitro antiproliferative activities and in vivo calcemic activities'.
AID1162463Induction of cell differentiation of human HL60 cells incubated for 144 hrs by Wst-1 dye based assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis and preliminary biological evaluation of new antiproliferative aromatic analogues of 1α,25-dihydroxyvitamin D3.
AID760211Antiosteoporotic activity in ovariectomized Sprague-Dawley rat osteoporosis model assessed as increase in bone mineral density in spine at 0.1 mg/kg/day administered 5 times a week for 4 weeks measured 24 hrs post last dose by dual X-ray absorption meter 2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Synthesis of 2α-heteroarylalkyl active vitamin d3 with therapeutic effect on enhancing bone mineral density in vivo.
AID1408596Antiproliferative activity against human BxPC3 cells after 24 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID770182Binding affinity to His-6-tagged rat VDR R270L mutant over expressed in Escherichia coli C41 assessed as increase in transition temperature by at 5 mM by CD-based spectropolarimetric analysis2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Crystal structures of hereditary vitamin D-resistant rickets-associated vitamin D receptor mutants R270L and W282R bound to 1,25-dihydroxyvitamin D3 and synthetic ligands.
AID351983Effect on bone calcium mobilization in vitamin D-deficient weanling Sprague-Dawley rat assessed as serum calcium level at 7020 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
New 1alpha,25-dihydroxy-19-norvitamin D(3) compounds constrained in a single A-ring conformation: synthesis of the analogues by ring-closing metathesis route and their biological evaluation.
AID337021Induction of cell differentiation in human HL60 cells assessed as alpha naphthyl esterase activity at 0.0001 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1267778Transactivation of VDR in rat osteosarcoma cells assessed as 24-hydroxylase transcriptional activity by luciferase reporter gene assay2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
A Methylene Group on C-2 of 24,24-Difluoro-19-nor-1α,25-dihydroxyvitamin D3 Markedly Increases Bone Calcium Mobilization in Vivo.
AID1251250Transactivation of VDR in human HaCaT cells after 24 hrs by luciferase reporter gene assay2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Chemical Synthesis and Biological Activities of 20S,24S/R-Dihydroxyvitamin D3 Epimers and Their 1α-Hydroxyl Derivatives.
AID1140503Activation of hedgehog signaling pathway in non-targeting siRNA treated mouse C3H10T1/2 cells assessed as effect on VDR expression at 0.5 uM after 24 hrs by qPCR analysis2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Structure-activity relationships for vitamin D3-based aromatic a-ring analogues as hedgehog pathway inhibitors.
AID547399In vivo calcemic activity in vitamin D-deficient Sprague-Dawley rat assessed as bone calcium mobilization measured by serum Ca2+ level at 780 pmol, ip administered 4 consecutive daily doses assessed after 24 hrs of last dose by atomic absorption spectrome2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Removal of the 26-methyl group from 19-nor-1α,25-dihydroxyvitamin D₃ markedly reduces in vivo calcemic activity without altering in vitro VDR binding, HL-60 cell differentiation, and transcription.
AID190612Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 50 pmol at 2 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1187833Induction of cell differentiation in human HL60 cells assessed as maturing morphological changes at 30 to 1000 nM after 48 hrs by Wright's-Giemsa staining-based forty microscopic view assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D3 analogues with aromatic side chains attached at C-17.
AID1218504Drug metabolism in CD1 mouse liver microsomes assessed as depletion of parent compound at 1 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID619499Effect on intestinal calcium transport activity in Sprague-Dawley rat assessed as ratio of serosal to mucosal calcium concentration at 87 pmol, ip administered as 4 consecutive doses once in 24 hrs measured 24 hrs post last dose (Rvb = 4.5 no unit )2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis and biological activity of 2-(3'-hydroxypropylidene)-1α-hydroxy-19-norvitamin D analogues with shortened alkyl side chains.
AID488257Toxicity in FVB mouse assessed as calcium level in blood at 24 pmol/day administered via osmotic pump for 6 to 7 days measured on day 4 by microchemistry (RVb = 2.11 mmol/L)2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID619579Effect on intestinal calcium transport activity in Sprague-Dawley rat assessed as ratio of serosal to mucosal calcium concentration at 87 pmol, ip administered as 4 consecutive doses once in 24 hrs measured 24 hrs post last dose (Rvb = 3.9 no unit )2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis and biological activity of 2-(3'-hydroxypropylidene)-1α-hydroxy-19-norvitamin D analogues with shortened alkyl side chains.
AID414857Inhibition of LPS-induced TNFalpha production in human PBMC after 24 hrs by ELISA2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
AID1218524Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2C inhibitor sulfaphenazole2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID392916Effect on bone calcium mobilization in vitamin D-deficient weanling rat assessed as increase in serum calcium level at 2.1 ug/kg, ip administered as 7 consecutive daily doses measured 24 hrs after last dose relative to untreated control2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID703626Agonist activity at VDR in human SW480-ADH cells assessed as induction of cystatin-D expression at 10 '-7 M after 24 hrs by Western blot analysis relative to control2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID387124Effect on bone calcium mobilization in vitamin D-deficient Sprague-Dawley rat assessed as serum calcium level at 2340 pmol, ip administered 4 consecutive daily doses assessed after 24 hrs of last dose by spectrometry2008Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
AID1408638Antitumor activity against human MCF7 cells xenografted in Balb/c nude mouse assessed as increase in p21 expression at 0.5 mg/kg, ip administered three times a week for three weeks starting from day 7 after tumor cell inoculation by immunohistochemical an2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID725918Agonist activity at RXR (unknown origin) expressed in human HCT116 cells co-expressing RXRE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay2013Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
Synthesis and biological evaluation of halogenated curcumin analogs as potential nuclear receptor selective agonists.
AID688527AUC (0 to 24 hrs) in mouse at 5 ug/kg2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of a new vitamin D2 analogue.
AID488355Agonist activity at VDR in human SCC4 cells assessed as induction of CYP24 gene expression at 1 uM after 5 to 10 mins by RT-PCR analysis2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID1251252Antiinflammatory activity in DBA/1 mouse splenocytes assessed as IFNgamma production at 100 nM after 2 hrs by ELISA (Rvb = 731 +/- 15 pg/ml)2015Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
Chemical Synthesis and Biological Activities of 20S,24S/R-Dihydroxyvitamin D3 Epimers and Their 1α-Hydroxyl Derivatives.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID488246Toxicity in FVB mouse assessed as calcium level in blood at 12 pmol/day administered via osmotic pump for 6 to 7 days measured on day 3 by microchemistry (RVb = 2.24 mmol/L)2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
AID1267776Induction of human HL60 cell differentiation assessed as differentiation from promyelocytes to monocytes by NBT assay2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
A Methylene Group on C-2 of 24,24-Difluoro-19-nor-1α,25-dihydroxyvitamin D3 Markedly Increases Bone Calcium Mobilization in Vivo.
AID635566Calcium transport in vitamin-D deficient weanling rat intestine assessed as intestinal calcium level at 2.1 ug/kg, ip administered daily for 7 consecutive days measured 24 hrs after last dose2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.
AID1267774Displacement of [3H]1alpha,25-(OH)2D3 from full-length recombinant rat VDR by scintillation counter2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
A Methylene Group on C-2 of 24,24-Difluoro-19-nor-1α,25-dihydroxyvitamin D3 Markedly Increases Bone Calcium Mobilization in Vivo.
AID1375593Agonist activity at VDR in human MCF7 cells assessed as upregulation of p21 expression at 10'-9 M after 48 hrs by Western blot method relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID217001Percent inhibition of binding to porcine intestinal vitamin D receptor1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Conformationally restricted analogs of 1 alpha, 25-dihydroxyvitamin D3 and its 20-epimer: compounds for study of the three-dimensional structure of vitamin D responsible for binding to the receptor.
AID337281Induction of terminal cell differentiation in human HL60 cells assessed as inhibition of [3H]thymidine incorporation at 0.01 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1266895Antipoliferative activity against human PC3 cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.
AID190614Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 50 pmol at 48 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID217009Binding affinity for porcine intestinal Vitamin D3 receptor (VDR) relative to 1,25(OH)2D3 (100)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
Synthesis, biological activity, and conformational analysis of four seco-D-15,19-bisnor-1alpha,25-dihydroxyvitamin D analogues, diastereomeric at C17 and C20.
AID1423171Hepatoprotective activity against CCL4-induced liver damage in C57BL/6J mouse assessed as reduction in serum AST levels at 20 ug/kg, po administered 5 times a week via gavage measured at 72 hrs post final CCl4 injection2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Design, Synthesis, and Antifibrosis Activity in Liver of Nonsecosteroidal Vitamin D Receptor Agonists with Phenyl-pyrrolyl Pentane Skeleton.
AID1455894Drug metabolism in human MCF7 cells at 1 uM after 24 hrs by HPLC analysis2018Journal of medicinal chemistry, 04-12, Volume: 61, Issue:7
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
AID3084Cells were harvested and were assayed for luciferase and -galactosidase activities (Transcriptional activity)2002Journal of medicinal chemistry, Apr-25, Volume: 45, Issue:9
Rational design, synthesis, and biological activity of novel conformationally restricted vitamin D analogues, (22R)- and (22S)-22-ethyl-1,25-dihydroxy-23,24-didehydro-24a,24b-dihomo-20-epivitamin D(3).
AID305713Induction of human HL60 cells differentiation assessed as number of cells at 0.01 uM after 72 hrs by NBT reduction test2007Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
Rotenoids and flavonoids with anti-invasion of HT1080, anti-proliferation of U937, and differentiation-inducing activity in HL-60 from Erycibe expansa.
AID1423175Oral bioavailability in Sprague-Dawley rat at 20 mg/kg by HPLC analysis2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Design, Synthesis, and Antifibrosis Activity in Liver of Nonsecosteroidal Vitamin D Receptor Agonists with Phenyl-pyrrolyl Pentane Skeleton.
AID244465Percent activation of human vitamin D receptor in COS-7 cell transcription assay2005Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
New derivatives of 1alpha,25-dihydroxy-19-norvitamin D3 with two substituents at C-2: synthesis and biological activity.
AID1585886Inhibition of Hedgehog signaling pathway in Sufu-deficient mouse C3H10T1/2 cells assessed as change in CYP24A1 mRNA expression at 1 uM after 24 hrs by q-PCR analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID216843Relative competitive index for binding to vitamin D binding protein1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Arocalciferols: synthesis and biological evaluation of aromatic side-chain analogues of 1 alpha,25-dihydroxyvitamin D3(1a).
AID191101Ability to mobilize Bone-Calcium transport, following the administration of compound in rats at a concentration of 500 pmol at 12 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1218501Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as 1alpha,23R,25(OH)3D3 metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID177143In vivo calcemic activity expressed as effective dose for Intestinal calcium transport (ICA) in vitamin D deficient rats1999Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7
Three-dimensional structure-function relationship of vitamin D: side chain location and various activities.
AID652555Cmax in mouse at 5 ug/kg2011ACS medicinal chemistry letters, Jul-14, Volume: 2, Issue:7
Novel alkynylphosphonate analogue of calcitriol with potent antiproliferative effects in cancer cells and lack of calcemic activity.
AID1267782Induction of bone mobilization activity in weaning Sprague-Dawley rat assessed as increase in serum calcium level at 780 pmol, ip for 4 consecutive dose at an interval of 24 hrs measured 24 hrs after last dose (Rvb = 4.4 to 4.5 mg/dl)2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
A Methylene Group on C-2 of 24,24-Difluoro-19-nor-1α,25-dihydroxyvitamin D3 Markedly Increases Bone Calcium Mobilization in Vivo.
AID1375601Agonist activity at VDR in human MCF7 cells assessed as upregulation of p53 expression at 10'-7 M after 48 hrs by Western blot method relative to control2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
AID688524Cytotoxicity against human T47D assessed as decrease in cell count after 120 hrs2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Synthesis and biological evaluation of a new vitamin D2 analogue.
AID337036Induction of terminal cell differentiation in human HL60 cells at 0.0001 uM after 4 days by NBT reduction assay1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID741581Agonist activity at VDR in human MG-63 cells expressing VDRE after 3 days by luciferase reporter gene based luminescence assay relative to 1,25(OH)2D32013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
A series of nonsecosteroidal vitamin D receptor agonists for osteoporosis therapy.
AID703636Antiproliferative activity against human MCF7 cells at 10 '-7 M after 48 hrs by MTT assay relative to untreated-control2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID190741Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5 pmol at 2 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1408604Antiproliferative activity against human MCF7 cells expressing VDR siRNA assessed as reduction in BrdU incorporation after 16 hrs by ELISA2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID703625Agonist activity at VDR in human SW480-ADH cells assessed as repression of c-Myc expression at 10 '-7 M after 24 hrs by Western blot analysis relative to control2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1564797Induction of differentiation in human HL60 cells assessed as increase in CD14 positive cells at 100 nM incubated for 48 hrs by 7-AAD staining-based flow cytometric analysis2019European journal of medicinal chemistry, Nov-01, Volume: 181Synthesis and evaluation of 2-carboxy indole derivatives as potent and selective anti-leukemic agents.
AID1218528Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2D inhibitor quinine2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID190615Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 50 pmol at 4 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID1661608Binding affinity to zebrafish VDR LBD assessed as Kd for fluorescein-labeled SRC1 NR2 peptide binding by micro-scale thermophoresis method2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Structural Analysis of VDR Complex with ZK168281 Antagonist.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID265891Binding affinity to chick VDR2006Bioorganic & medicinal chemistry letters, Jun-15, Volume: 16, Issue:12
Design and evaluation of new antipsoriatic antedrug candidates having 16-en-22-oxa-vitamin D3 structures.
AID547392Displacement of [3H]1alpha,25-(OH)2D3 from rat recombinant full length VDR2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Removal of the 26-methyl group from 19-nor-1α,25-dihydroxyvitamin D₃ markedly reduces in vivo calcemic activity without altering in vitro VDR binding, HL-60 cell differentiation, and transcription.
AID227553Ratio of average ED50 to 1-alpha,25-(OH)2D3 ED50 for differentiation assay2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
2-Ethyl and 2-ethylidene analogues of 1alpha,25-dihydroxy-19-norvitamin D(3): synthesis, conformational analysis, biological activities, and docking to the modeled rVDR ligand binding domain.
AID1218458Drug metabolism in dexamethasone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2E inhibitor di-ethyldithiocarbamate2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1266894Agonist activity at vitamin D3 receptor in human HL-60 cells assessed as induction of cell differentiation after 96 hrs by NBT dye-based microscopic analysis2016European journal of medicinal chemistry, Jan-01, Volume: 107Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.
AID392910Effect on calcium transport in vitamin D-deficient weanling rat intestine assessed as increase in ratio of serosal to mucosal calcium level at 2.1 ug/kg, ip administered as 7 consecutive daily doses measured 24 hrs after last dose2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
13-Methyl-substituted des-C,D analogs of (20S)-1alpha,25-dihydroxy-2-methylene-19-norvitamin D3 (2MD): synthesis and biological evaluation.
AID190618Ability to stimulate intestinal-calcium transport by the administration of compound in rats at a concentration of 5 pmol at 12 hr.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Synthesis and biological activity of novel vitamin D analogues: 24,24-difluoro-25-hydroxy-26,27-dimethylvitamin D3 and 24,24-difluoro-1 alpha,25-dihydroxy-26,27-dimethylvitamin D3.
AID303408Ratio of ED50 for drug to 1-alpha,25-dihydroxyvitamin for rat recombinant VDR2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Design, synthesis, and biological evaluation of a 1alpha,25-dihydroxy-19-norvitamin D3 analogue with a frozen A-ring conformation.
AID265892Stability in rat liver microsome relative to maxacalcitol2006Bioorganic & medicinal chemistry letters, Jun-15, Volume: 16, Issue:12
Design and evaluation of new antipsoriatic antedrug candidates having 16-en-22-oxa-vitamin D3 structures.
AID216857Percentage binding to chick intestinal vitamin D3 receptor, relative competitive index (RCI)2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Characterization of a novel analogue of 1alpha,25(OH)(2)-vitamin D(3) with two side chains: interaction with its nuclear receptor and cellular actions.
AID190747Bone calcium mobilization in rats maintained on a very low calcium diet at a dose 130 (pmol)2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
2-Ethyl and 2-ethylidene analogues of 1alpha,25-dihydroxy-19-norvitamin D(3): synthesis, conformational analysis, biological activities, and docking to the modeled rVDR ligand binding domain.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID647367Activation of VDR in mouse C3H10T1/2 cells assessed as up-regulation of CYP24A1 at 0.1 uM by RT-PCR analysis relative to control2012Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
Evaluation of vitamin D3 A-ring analogues as Hedgehog pathway inhibitors.
AID703640Agonist activity at VDR in human MCF7 cells assessed as transcription of CYP24A1 gene after 24 hrs by luciferase reporter gene assay2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Synthesis and biological evaluation of 1α,25-dihydroxyvitamin D₃ analogues with a long side chain at C12 and short C17 side chains.
AID1218463Drug metabolism in prednisone treated CD1 mouse liver microsomes assessed as metabolite formation at 20 uM after 30 mins by LC/MS analysis in presence of NADPH and CYP2B inhibitor orphenadrine2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Cytochrome P450 3A-mediated microsomal biotransformation of 1α,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
AID1585888Inhibition of Hedgehog signaling pathway in VDR-deficient mouse C3H10T1/2 cells assessed as reduction in oxysterol-induced Gli1 mRNA expression after 24 hrs by q-PCR analysis2019European journal of medicinal chemistry, Jan-15, Volume: 162Synthesis and evaluation of third generation vitamin D3 analogues as inhibitors of Hedgehog signaling.
AID1824244Selectivity index, ratio of IC50 for Inhibition of hedgehog signalling in mouse VDR-KO MEF cells to IC50 for inhibition of hedgehog signalling in mouse ASZ001 cells2022European journal of medicinal chemistry, Jan-15, Volume: 228Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma.
AID635565Calcium transport in vitamin-D deficient weanling rat intestine assessed as intestinal calcium level at 0.7 ug/kg, ip administered daily for 7 consecutive days measured 24 hrs after last dose2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
13,13-Dimethyl-des-C,D analogues of (20S)-1α,25-dihydroxy-2-methylene-19-norvitamin D₃ (2MD): total synthesis, docking to the VDR, and biological evaluation.
AID730427Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange.
AID1506121Drug degradation in human MG63 cells at 1 uM after 24 hrs by HPLC analysis2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
25 S-Adamantyl-23-yne-26,27-dinor-1α,25-dihydroxyvitamin D
AID230395Intestinal Calcium Transport (ICT) activity (260 pmol/day/7 days) in Vitamin D-Deficient Rats on a Low-Calcium Diet(0.02% Ca diet)2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis, biological evaluation, and conformational analysis of A-ring diastereomers of 2-methyl-1,25-dihydroxyvitamin D(3) and their 20-epimers: unique activity profiles depending on the stereochemistry of the A-ring and at C-20.
AID337310Induction of terminal cell differentiation in human HL60 cells assessed as naphthol AS-D chloroacetate esterase activity at 0.001 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID1408597Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
AID619580Effect on intestinal calcium transport activity in Sprague-Dawley rat assessed as ratio of serosal to mucosal calcium concentration at 780 pmol, ip administered as 4 consecutive doses once in 24 hrs measured 24 hrs post last dose (Rvb = 3.9 no unit )2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Synthesis and biological activity of 2-(3'-hydroxypropylidene)-1α-hydroxy-19-norvitamin D analogues with shortened alkyl side chains.
AID730426Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity at 10 uM by luciferase and beta-galactosidase reporter gene assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange.
AID1164482Effect on intestinal calcium transport in weanling Sprague-Dawley rat assessed as increase in ratio of serosal to mucosal calcium level at 780 pmol/day, ip administered as 4 consecutive daily doses measured 24 hrs after last dose2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Synthesis and Biological Activity of 25-Hydroxy-2-methylene-vitamin D3 analogues monohydroxylated in the A-ring.
AID760218Binding affinity to human VDR after 2 hrs by fluorescence assay relative to 1alpha,25(OH)2D32013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Synthesis of 2α-heteroarylalkyl active vitamin d3 with therapeutic effect on enhancing bone mineral density in vivo.
AID1661599Binding affinity to H12 region (440 to 445 residues) of zebrafish VDR LBD assessed as stabilization of structural elements by measuring increase in protection at 10 fold excess compound concentration in presence of SRC1 NR2 coactivator peptide measured at2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Structural Analysis of VDR Complex with ZK168281 Antagonist.
AID702757Transactivation of full length human VDR expressed in human HeLa cells assessed as increase in CYP24 transcription after 18 hrs by luciferase reporter gene assay2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Structural basis for the accommodation of bis- and tris-aromatic derivatives in vitamin D nuclear receptor.
AID81122Percent inhibition against HL-60 cell line (50% dose response), relative to 1-alpha,25 (OH)2D3 (100% activity) determined in vitro2002Bioorganic & medicinal chemistry letters, Jun-17, Volume: 12, Issue:12
Vitamin D(3): synthesis of seco-C-9,11-bisnor-17-methyl-1 alpha,25-dihydroxyvitamin D(3) analogues.
AID274538Antiproliferative activity against murine keratinocytes2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
AID1309800Activation of VDR in human Jurkat cells expressing lentiviral VDRE-luciferase vector assessed as VDRE-mediated transcriptional activity measured after 24 hrs by luciferase transcriptional reporter assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
Synthesis and Biological Evaluation of Vitamin D3 Metabolite 20S,23S-Dihydroxyvitamin D3 and Its 23R Epimer.
AID337308Induction of terminal cell differentiation in human HL60 cells assessed as naphthol AS-D chloroacetate esterase activity at 0.1 uM after 4 days1994Journal of natural products, Sep, Volume: 57, Issue:9
Chemical and bioactive constituents from Zanthoxylum simulans.
AID25549Compound was tested for rate constant for the forward reaction of isomerization of previtamin D to vitamin D1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
14-epi stereoisomers of 25-hydroxy- and 1 alpha,25-dihydroxyvitamin D3: synthesis, isomerization to previtamins, and biological studies.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2000Molecular cell, Jan, Volume: 5, Issue:1
The crystal structure of the nuclear receptor for vitamin D bound to its natural ligand.
AID1811Experimentally measured binding affinity data derived from PDB2000Molecular cell, Jan, Volume: 5, Issue:1
The crystal structure of the nuclear receptor for vitamin D bound to its natural ligand.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15,469)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903004 (19.42)18.7374
1990's4738 (30.63)18.2507
2000's3655 (23.63)29.6817
2010's3359 (21.71)24.3611
2020's713 (4.61)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 100.89

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index100.89 (24.57)
Research Supply Index9.76 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index194.71 (26.88)
Search Engine Supply Index2.04 (0.95)

This Compound (100.89)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1,224 (7.60%)5.53%
Reviews1,802 (11.19%)6.00%
Case Studies999 (6.20%)4.05%
Observational40 (0.25%)0.25%
Other12,042 (74.76%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (179)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Additive Renoprotective Effects of Oral Calcitriol in IgA Nephropathy Patients Taking Renin-Angiotensin System Blockers [NCT01237028]168 participants (Actual)Interventional2011-03-31Completed
A Phase I Clinical Trial of Oral Calcitriol With Fixed Dose of Cisplatin and Gemcitabine in Patients With Advanced Solid Tumors [NCT01093092]Phase 114 participants (Actual)Interventional2011-09-30Terminated(stopped due to Study transferring to INOVA Health)
A Psoriasis Plaque Test on LEO 27989 Ointment and Calcipotriol Plus LEO 27989 Ointment in Patients With Psoriasis Vulgaris. [NCT01297166]Phase 125 participants (Actual)Interventional2011-02-28Completed
A Phase I/II Study of High-Dose Calcitriol in Combination With Temozolomide for Patients With Metastatic Melanoma [NCT00301067]Phase 1/Phase 220 participants (Actual)Interventional2005-01-30Completed
Spray® and Vectical Ointment® in the Treatment of Plaque Psoriasis [NCT01205880]Phase 412 participants (Actual)Interventional2009-12-31Completed
Effect of Oral Systemic Administration of Vitamin D on the Rate of Orthodontic Tooth Movement - A Randomized Control Trial [NCT05202496]24 participants (Actual)Interventional2019-11-20Completed
Nutrition and Body Composition in Acute Lymphoblastic Leukemia (Environment and Microenvironment in ALL #2) [NCT01317940]Phase 276 participants (Actual)Interventional2011-03-31Completed
Activated Vitamin D for the Prevention and Treatment of Acute Kidney Injury (ACTIVATE-AKI) [NCT02962102]Phase 2150 participants (Actual)Interventional2017-04-03Completed
A 6-Month, Randomized, Open-Label, Active-Comparator Controlled, Parallel-Group Study With a 6-Month Extension to Evaluate the Safety and Efficacy of Alendronate Sodium 70 mg/Vitamin D3 5600 I.U. Combination Tablets Versus Calcitriol in the Treatment of O [NCT01350934]Phase 4219 participants (Actual)Interventional2011-06-19Completed
Clinical Study to Evaluate the Efficacy of 1,25(OH)2D3 (Calcitriol) Versus Placebo in Recent Onset Type 1 Diabetes(IMDIAB XIII) [NCT01120119]Phase 20 participants InterventionalCompleted
Comparison of Routine Prophylactic Calcium + Calcitriol and Selective Use Based on PTH for the Prevention of Postoperative Hypocalcemia in Patients With Total Thyroidectomy. Randomized Clinical Trial [NCT05252884]180 participants (Anticipated)Interventional2022-03-30Not yet recruiting
Resistance Training and 1,25 (OH)2D3 Administration to Maintain Respiratory Muscle Function and Reduce Pneumonia Risk in Cancer Patients [NCT03469271]Phase 463 participants (Actual)Interventional2018-05-25Completed
Study Role of the Local Treatments on the Microbiome Modulation in the Psoriatic Skin. Study Monocentric, Interventional, Randomized and Single-blind [NCT03584360]Phase 230 participants (Actual)Interventional2018-09-24Completed
Comparison of Efficacy and Safety of Paricalcitol Injection With Maxacalcitol Injection in Adult Japanese Chronic Kidney Disease Subjects Receiving Hemodialysis With Secondary Hyperparathyroidism [NCT01341782]Phase 3255 participants (Actual)Interventional2011-05-31Completed
Topical Vitamin D3, Diclofenac or a Combination of Both to Treat Basal Cell Carcinoma [NCT01358045]Phase 2128 participants (Actual)Interventional2011-11-30Completed
Does Preoperative Calcium and Calcitriol Decrease Rates of Post Thyroidectomy Hypocalcemia? [NCT03869398]82 participants (Actual)Interventional2017-08-01Completed
A Phase II Multicenter Randomized Double-blind Comparator-Controlled Trial of HAT1 Compared to Calcipotriol in Patients With Mild to Moderate Chronic Plaque Psoriasis [NCT03848806]Phase 2174 participants (Actual)Interventional2016-02-29Completed
Phase I Dose-Escalation Study, to Evaluate the Safety, Tolerability and Pharmacokinetics of a Topical Compound 31543 (Calcitriol, USP) in Adult Cancer Patients Receiving Taxane-based Chemotherapy Regimens for the Treatment of Advanced or Recurrent Disease [NCT01588522]Phase 130 participants (Anticipated)Interventional2012-07-31Completed
[NCT01561222]Phase 4300 participants (Anticipated)Interventional2015-07-31Not yet recruiting
A Clinical Trial Phase II of Calcitriol in Combination With 5-fluorouracil, Mitomycin C and Leucovorin in an Open Label-non-randomized Study to Evaluate the Tumor Response in Patients With Advanced Intrahepatic Cholangiocarcinoma [NCT01039181]Phase 228 participants (Anticipated)Interventional2010-01-31Not yet recruiting
Calcipotriol Plus 5-Flourouracil Immunotherapy Before Transplantation for Skin Cancer Prevention in Organ Transplant Recipients [NCT04329221]Phase 262 participants (Anticipated)Interventional2026-01-01Not yet recruiting
Pharmacokinetic and Pharmacodynamic Study of CD 2027 3µg/g Oily Spray Applied Twice Daily for 3 Weeks Under Conditions of Maximized Use in Adults With Plaque-type Psoriasis [NCT00763503]Phase 226 participants (Actual)Interventional2008-09-30Completed
Phase I, Single-center, Randomized, Controlled Trial to Evaluate the Antipsoriatic Efficacy of Calcipotriol in Novel Formulations Compared to Marketed Calcipotriol Products and Evaluation of Their Cutaneous Safety in a Psoriasis Plaque Test [NCT05488990]Phase 1/Phase 224 participants (Actual)Interventional2013-03-25Completed
A Phase III, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group, Multiple-Site Study to Evaluate the Therapeutic Equivalence of a Generic Calcipotriene and Betamethasone Dipropionate Topical Foam, 0.005%/0.064% (Glenmark Pharmaceuticals Ltd) to [NCT03731091]Phase 3494 participants (Actual)Interventional2018-10-31Completed
A Clinical Trial Evaluating the Efficacy and Safety of a Combination Treatment Administered Over 3 Years in Patients at Risk of Experiencing Recurrence of Colorectal Adenomas [NCT00486512]Phase 3350 participants (Actual)Interventional2007-06-30Terminated(stopped due to The overall program was terminated)
Calcitriol Monotherapy for X-Linked Hypophosphatemia: Effects on Mineral Ions, Growth and Skeletal Parameters [NCT03748966]Early Phase 120 participants (Anticipated)Interventional2019-03-28Recruiting
Clinical Study on Treatment of Postmenopausal Osteoporosis (Kidney Deficiency and Blood Stasis Syndrome) With Xulin Jiangu Granules [NCT03563235]Early Phase 160 participants (Anticipated)Interventional2019-09-01Not yet recruiting
Pilot Trial About the Effects of Calcitriol's Treatment in the Neurological Function and Frataxin's Level in Friedreich's Ataxia Patients [NCT04801303]Phase 420 participants (Actual)Interventional2021-08-25Completed
A Randomized Open Label Study to Evaluate Efficacy of Calcitriol Supplementation in COVID-19 Patients With Vitamin D Deficiency [NCT05415254]86 participants (Anticipated)Interventional2022-06-12Not yet recruiting
A Randomized Trial Comparing Pulse Calcitriol and Alfacalcidol for the Treatment of Secondary Hyperparathyroidism in Hemodialysis Patients [NCT01115543]Phase 432 participants (Actual)Interventional2008-08-31Completed
A 28-day, Double-blind, Randomized, Reference-controlled Open Psoriasis Plaque Test for Within Subject Comparison of Efficacy and Safety of Mapracorat 0.1% Ointment and 4 Reference Products in Symptomatic Volunteers With Stable Plaque-type Psoriasis [NCT03399526]Phase 124 participants (Actual)Interventional2013-02-11Completed
A Phase 1b, Randomised, Controlled, Assessor-blinded Proof of Principle Trial to Assess Safety, Tolerability and Pharmacodynamics Effects of Microarray Patches Containing Calcipotriol/Betamethasone Dipropionate in Descaled Skin of Adults With Chronic Plaq [NCT03898583]Phase 115 participants (Actual)Interventional2019-04-15Completed
A Phase II Study of Oral Calcitriol in Combination With Ketoconazole in Castration Resistant Prostate Cancer, Progressing Despite Primary ADT and Abiraterone [NCT03261336]Phase 21 participants (Actual)Interventional2017-01-06Terminated(stopped due to can not meet enrollment)
An Open-Label, Bilaterally-Controlled Single Center Study to Compare the Efficacy of Taclonex Ointment With Hydrogel Patch Occlusion to Taclonex Ointment Without Occlusion in the Treatment of Plaque-Type Psoriasis [NCT00924950]Phase 435 participants (Actual)Interventional2009-06-30Terminated
An Open-label, Multi-center, Randomized, Evaluator-Blinded Study to Evaluate the Safety and Efficacy of Two Treatment Regimens Involving Vectical™ (Calcitriol) Ointment 3 µg/g and Clobex® (Clobetasol Propionate) Spray, 0.05% in the Treatment of Moderate P [NCT00988637]Phase 4138 participants (Actual)Interventional2009-10-31Completed
An Open-Label, Randomized, Parallel Group Study to Assess the Safety and Efficacy of Hectorol® (Doxercalciferol Capsules) in Pediatric Patients With Chronic Kidney Disease Stages 3 and 4 With Secondary Hyperparathyroidism Not Yet on Dialysis [NCT02859896]Phase 384 participants (Anticipated)Interventional2017-01-19Active, not recruiting
[NCT00862693]Phase 440 participants (Anticipated)Interventional2009-03-31Recruiting
Use of Vitamin D in Treatment of Non-Alcoholic Fatty Liver Disease Detected by Transient Elastography [NCT04038853]Phase 4360 participants (Actual)Interventional2015-12-01Completed
Multi-center,Single Blind, Parallel-Controlled Study of the Efficacy and Safety of Calcipotriol Betamethasone Ointment Plus Calcipotriol Ointment in Sequential Therapy to Psoriasis Vulgaris [NCT02191007]230 participants (Actual)Interventional2013-11-30Completed
Vitamin D Replacement in Chronic Kidney Disease and Its Effects on Iron Homeostasis, Serum Hepcidin, and Hemojuvelin Levels. [NCT01988116]Early Phase 140 participants (Actual)Interventional2013-10-31Completed
Effect of Vitamin D Supplementation on Blood Pressure in Elderly People [NCT02047799]Phase 245 participants (Actual)Interventional2013-04-30Completed
Kidney Disease in Type 2 Diabetes Mellitus: Biomarker Discovery and Novel Therapeutics [NCT02410005]Phase 2/Phase 356 participants (Actual)Interventional2014-10-31Terminated(stopped due to Logistic challenges)
Phase II Study of Weekly Intravenous 1,25 Dihydroxycholecelciferol (Calcitriol) + Dexamethasone in Androgen Independent Prostate Cancer [NCT00524589]Phase 218 participants (Actual)Interventional2006-04-30Terminated(stopped due to closed due to futility)
Effects of Vitamin D3 Supplementation on Antioxidant Enzymes Level in Vitamin D3 Deficient COPD Patients [NCT04011930]Phase 240 participants (Anticipated)Interventional2019-03-01Recruiting
Asthma and Vitamin D (a Clinical Pilot Study) [NCT00712205]Phase 420 participants (Anticipated)Interventional2008-08-31Enrolling by invitation
Study of Vitamin D Supplementation to Male HIV Sero-positive Patients [NCT00990678]60 participants (Actual)Interventional2008-04-30Completed
hCAP18 Levels and Vitamin D Deficiency in Chronic Kidney Disease [NCT01026363]0 participants (Actual)Interventional2009-12-31Withdrawn(stopped due to Inadequate enrollment)
A Multicenter Randomized Open-label Clinical Trial of Vitamin D Combined With HD-DXM Versus HD-DXM for the Treatment of ITP [NCT04094805]Phase 460 participants (Anticipated)Interventional2020-10-01Not yet recruiting
A Phase III, Multicentre, Randomized, Observer Blind, Parallel Group, Three Arms, Controlled Clinical Trial to Evaluate the Efficacy and Safety of Topically Applied Calcipotriol/AKVANO 50 μg/g Cutaneous Solution Against Calcipotriol Ointment 50 Micrograms [NCT05174598]Phase 3278 participants (Actual)Interventional2018-10-03Completed
An Open-Label, Study Evaluating Enstilar® (Calcipotriene and Betamethasone Dipropionate) Foam, 0.005%/0.064% QD in Psoriasis Patients Being Treated With Biologic Agents [NCT03080545]Phase 425 participants (Actual)Interventional2017-05-01Completed
Comparing the Quality of Life Associated With Empiric Calcium Repletion and Parathormone (PTH) Based Calcium Repletion for Post Thyroidectomy Hypoparathyroidism [NCT03249012]120 participants (Anticipated)Interventional2017-09-01Recruiting
Influence of Vitamin D on Gene Expression Profile of Breast Cancer Samples From Post-menopausal Patients [NCT00926315]60 participants (Anticipated)Interventional2007-07-31Active, not recruiting
Combination Calcipotriene 0.005% Foam and Fluorouracil 5% Cream for the Treatment of Actinic Keratoses on the Scalp [NCT03996252]Early Phase 115 participants (Actual)Interventional2019-07-01Terminated(stopped due to The study team was not able to start the study and they never completed the IRB submission, so the study was terminated.)
Immunointervention With 1,25-dihydroxy-vitamin D3 in New-onset Type 1 Diabetes [NCT00960635]Phase 20 participants Interventional2001-06-30Completed
Extraction Socket Sealed With Autologous Tooth Root in Ridge Preservation [NCT05601531]60 participants (Anticipated)Interventional2023-01-01Recruiting
Pilot Open-Label Clinical Trial to Test Efficacy and Safety of Combination of Clobex® Spray With Excimer Laser Therapy [Photomedex XTRAC ® Velocity] in the Treatment of Generalized Plaque Psoriasis Followed by Maintenance With Topical Vectical® Ointment [NCT01012713]Phase 430 participants (Actual)Interventional2010-06-30Completed
A Comparative Trial of Calcitriol Versus Placebo for the Preservation of Bone Mass and Strength After Kidney Transplantation [NCT02224144]Phase 267 participants (Actual)Interventional2014-08-18Completed
A Phase 2, Multicenter, Open Label Study of the Safety and Efficacy of High-Dose Pulse Administration DN-101 (Calcitriol) in Patients With Myelodysplastic Syndrome [NCT00057031]Phase 246 participants Interventional2002-11-30Active, not recruiting
A Pilot Study of the Effects of High-Dose Oral Calcitriol in Breast Cancer Patients Prior to Surgery [NCT01293682]Phase 212 participants (Actual)Interventional2010-11-30Completed
Effects of Calcitriol on Podocytes in Diabetic Kidney Disease Patients: Assessment of Urine Podocin, Urine Nephrin, Urine Interleukin-6, Urine KIM-1, Plasma Renin, and Albuminuria [NCT05298163]120 participants (Anticipated)Interventional2022-04-30Not yet recruiting
Effect of 1,25-dihydroxyvitamin D3, Treatment on Insulin Secretion and Muscle Strength in Pre-diabetic Persons [NCT04286529]Phase 117 participants (Actual)Interventional2020-10-01Terminated(stopped due to Difficulty with study logistics due to COVID-19)
A Phase I, Randomized, Open-Label, Three Period Cross-Over Study to Assess the Pharmacokinetics of Oral Calcitriol (ROCALTROL®) in Healthy Volunteers When Administered Alone or When Co-Administered With Lanthanum Carbonate (FOSRENOL®) or Sevelamer Carbona [NCT00925704]Phase 141 participants (Actual)Interventional2009-06-01Completed
A Multicenter, Randomized, Vehicle-controlled, Efficacy and Safety Study of CD2027 3µg/g Oily Spray Applied Twice Daily for 8 Weeks in Subjects With Plaque-type Psoriasis [NCT00763555]Phase 288 participants (Actual)Interventional2008-09-30Completed
A Multi-Center, Open-Label Study to Evaluate the Safety and Efficacy of a Consecutive Treatment Regimen of Clobetasol Propionate 0.05% Spray, Followed by Calcitriol Ointment 3µg/g, in the Management of Moderate to Severe Plaque Psoriasis [NCT00658788]Phase 3305 participants (Actual)Interventional2008-03-31Completed
A Multi Centre, Open Label, Parallel Group, Randomized Controlled Trial to Compare the Safety and Efficacy of Oral Paricalcitol Versus Oral Calcitriol in the Treatment of Secondary Hyperparathyroidism in Dialysis Patients [NCT00800358]69 participants (Actual)Interventional2008-11-30Completed
Effect Of Calcitriol On Neutrophil To Lymphocytes Ratio And High Sensitivity C-Reactive Protein Covid-19 Patients [NCT05765617]Phase 216 participants (Actual)Interventional2021-07-01Completed
Effect of Different Vitamin D Preparations on Circulating FGF23 Levels in Vitamin D Deficient Caucasian and African-American Men and Women [NCT00957879]42 participants (Actual)Interventional2009-05-31Completed
A Phase I Trial of Subcutaneous And/Or Oral Calcitriol [(1,25-COH)2D3] and Carboplatin in Advanced Solid Tumors [NCT00008086]Phase 10 participants Interventional1996-01-31Completed
A Randomized Phase 2 Study of Gemcitabine ± Erlotinib and DN-101 Versus Gemcitabine ± Erlotinib and Placebo in Subjects With Advanced Pancreatic Adenocarcinoma [NCT00536770]Phase 2132 participants (Anticipated)Interventional2007-09-30Suspended(stopped due to DSMB)
Multi-Center Clinical Study on the Relationship Between Vitamin D Receptor Gene Polymorphism and Children's Physical and Intellectual Development [NCT03742310]500 participants (Anticipated)Interventional2019-01-01Not yet recruiting
N-Acetylcysteine and Vitamin D in Infants With Hypoxic Ischemic Encephalopathy Treated With Hypothermia [NCT04643821]Early Phase 130 participants (Actual)Interventional2015-01-01Completed
A Phase 1B, Double-Blind, Placebo-Controlled, Calcitriol Active-Controlled, Daily-Dose, Escalating-Dose, Safety and Tolerance Study of 2MD Soft Gel Capsules in Normal Healthy Postmenopausal Women [NCT01969656]Phase 10 participants InterventionalCompleted
A Prospective, Multicenter Study to Evaluate the Safety of Paricalcitol Capsules as Determined by Hypercalcemia in Pediatric Patients Ages 0 to 16 With Chronic Kidney Disease (CKD) Stage 5 Receiving Peritoneal Dialysis (PD) Within Current Clinical Practic [NCT01134315]61 participants (Actual)Observational2010-06-30Terminated(stopped due to Terminated after FDA agreement.)
A Single Dose, Two-Period, Two-Treatment, Two-Way Crossover Bioequivalency Study of Calcitriol Tablets, 0.25 mg, Under Fasting Conditions [NCT00601328]36 participants (Actual)Interventional2003-07-31Completed
A Phase I/II Study of Oral Calcitriol in Combination With Ketoconazole in Androgen Independent Prostate Cancer [NCT00536991]Phase 1/Phase 251 participants (Actual)Interventional2006-10-31Terminated(stopped due to difficult to recruit)
A Randomized Phase II Trial Of Calcitriol In Patients With Prostatic Intraepithelial Neoplasia [NCT00118066]Phase 212 participants (Actual)Interventional2004-05-31Terminated(stopped due to Slow accruaL, lack of scientific progress)
A Pilot Study of the Effects of High-Dose Oral Calcitriol and Physical Activity on Bone Health in Breast Cancer Survivors [NCT00904033]Phase 241 participants (Actual)Interventional2008-12-01Completed
A Double Blind Randomized Trial, Placebo-controled of 0.0003% Calcitriol Ointment Versus 0.1% Tacrolimus Ointment in the Treatment of Pityriasis Alba [NCT01388517]Phase 439 participants (Actual)Interventional2008-01-31Completed
Nickel Desensitization Using Topical Therapy [NCT01413477]24 participants (Anticipated)Interventional2011-08-31Not yet recruiting
[NCT00006275]20 participants Interventional2000-07-31Completed
Calcitriol or Placebo in Men for Prostate Cancer Active Surveillance [NCT00482157]0 participants (Actual)Interventional2007-02-28Withdrawn
Effects of Calcitriol (1α, 25-[OH]2 Vitamin D3) on Renin Expression in Hypertensive Patients Without Vitamin D Deficiency [NCT00585442]Early Phase 112 participants (Actual)Interventional2007-05-31Terminated(stopped due to Lack of quality data)
Phase II Study of DN-101 (High Dose Pulse Calcitriol), Mitoxantrone, Prednisone in Androgen-Independent Prostate Cancer (AIPC) [NCT00182741]Phase 219 participants (Actual)Interventional2004-09-30Completed
A Plaque Test Comparing 4 Steroids With Daivobet® Ointment and a Vehicle Control for the Treatment of Psoriasis Vulgaris [NCT00845481]Phase 224 participants (Actual)Interventional2009-01-31Completed
The Effect of Calcitriol on Progress and Activity of Lupus Nephritis [NCT01863641]Phase 250 participants (Anticipated)Interventional2013-04-30Recruiting
A Phase 2, Placebo-controlled, Randomized Study to Evaluate the Effect of Pre-operative Vitamin D Supplementation on Hypocalcemia Following Total or Near-total Thyroidectomy [NCT01868750]Phase 267 participants (Anticipated)Interventional2013-05-31Completed
A Phase I/II Clinical Trial of Intravenous (IV) Calcitriol With Fixed Dose of Cisplatin and Docetaxel in Advanced Non-Small Cell Lung Cancer [NCT00794547]Phase 1/Phase 234 participants (Actual)Interventional2008-12-31Terminated
Efficacy and Safety of HAT1, a Novel Topical Therapeutic: An Open Label Pilot Study of HAT1 Compared to Calcipotriol in Patients With Chronic Plaque Psoriasis [NCT03069144]Phase 1/Phase 228 participants (Actual)Interventional2012-01-06Completed
A Randomized Placebo-controlled Double Blinded Trial to Evaluate Cholecalciferol (Vitamin D3) and Calcitriol Treatment on Reducing Blood Pressure in Middle Aged Adults With Stage I Hypertension and Vitamin D Deficiency [NCT00459563]0 participants (Actual)Interventional2007-03-31Withdrawn(stopped due to Inadequate enrollment)
A Phase I Exploratory Study Evaluating 3 Formulations of LEO 29102 Plus Calcipotriol, Ointment, LEO 29102 Ointment, Calcipotriol Ointment, Daivonex® Ointment and Diprosone® Ointment in the Treatment of Psoriasis [NCT01466478]Phase 124 participants (Actual)Interventional2011-11-30Completed
The Efficacy and Safety of Calcitriol for the Treatment of Lupus Nephritis and Persistent Proteinuria [NCT00508898]Phase 40 participants (Actual)Interventional2008-05-31Withdrawn(stopped due to Funding problem; trial abandoned.)
Impact of Vitamin D Therapies on Monocyte Function in Chronic Kidney Disease [NCT01222234]56 participants (Actual)Interventional2010-10-31Completed
A Double Blind, Active-Comparator-, and Vehicle-Controlled, Multiple-Dose Study to Evaluate the Efficacy and Pharmacokinetics of MK-0873 in Patients With Plaque Psoriasis [NCT01235728]Phase 124 participants (Actual)Interventional2010-11-01Completed
To Study the Bone Turnover Markers and Bone Density Changes in Hyperperparathyroid Dialysis Patients Under Calcium Sensing Receptor Agonist Cinacalcet Treatment [NCT04637360]40 participants (Actual)Interventional2018-01-01Completed
Regulation of Bone Formation in Renal Osteodystrophy [NCT00560300]Phase 261 participants (Actual)Interventional2000-11-30Completed
Intervention Using Vitamin D for Elevated Urinary ALbumin in Diabetes (IDEAL-2) [NCT03216564]Phase 3320 participants (Anticipated)Interventional2017-05-10Recruiting
A Phase I Study of Oral Calcitriol in Combination With Ketoconazole in Refractory Advanced Malignancies [NCT00238225]Phase 115 participants (Actual)Interventional2004-11-30Completed
Olux E Foam and Sorilux Foam Combination Therapy for the Maintenance of Treatment Response in Patients With Moderate Plaque Psoriasis [NCT01745133]Phase 463 participants (Actual)Interventional2013-01-31Completed
Pilot, Open-Label, Randomized, Parallel Group Study to Evaluate Clinical/ and Immunological Efficacy/Safety of Locally Delivered 6-MP or Calcitriol vs Purinethol in Non-Steroid Dependent Patients With Active CD [NCT00287170]Phase 1/Phase 215 participants (Actual)Interventional2006-07-31Completed
A Pilot Study of Oral Calcitriol in Patients at High Risk for Lung Cancer [NCT00690924]16 participants (Actual)Interventional2008-07-17Completed
Calcipotriol Plus Hydrocortisone in Psoriasis Vulgaris on the Face and on the Intertriginous Areas [NCT00691002]Phase 31,245 participants (Actual)Interventional2008-05-31Completed
A Phase I Trial Of Oral Calcitriol [1,25-(OH)2D3] And Paclitaxel In Advanced Solid Tumors [NCT00009802]Phase 145 participants (Actual)Interventional1998-06-30Completed
Phase I Study Of Oral, 1,25 Dihydroxycholecalciferol (Calcitriol) + Dexamethasone In Hormone-refractory Prostate Cancer [NCT00010231]Phase 122 participants (Actual)Interventional1999-06-30Completed
Phase 4 Study of Paricalcitol and Calcitriol for Reparative Management of Chronic Allograft Dysfunction and Renocardiac Syndrome in Vitamin D Insufficient Renal Transplant Recipients [NCT01265615]Phase 4109 participants (Actual)Interventional2009-10-31Completed
Additive Renoprotective Effects of Oral Calcitriol in Nondiabetic Chronic Kidney Disease Patients [NCT01512862]Phase 4240 participants (Anticipated)Interventional2012-01-31Recruiting
A Comparative Effectiveness Trial of High-quality Vitamin D3 Nutritional Supplements to Replete Serum Vitamin D [NCT01524874]66 participants (Actual)Interventional2010-08-31Completed
Pharmacokinetics of a Single Oral Dose of Maxmarvil® in Healthy Postmenopausal Women Without a Previous History of Fractures [NCT01526278]Phase 118 participants (Actual)Interventional2011-10-31Completed
Studies With 1,25-Dihydroxycholecalciferol [NCT00001151]Phase 26 participants (Actual)Interventional1976-03-31Terminated(stopped due to Terminated because of lack of drug supply)
Treatment of Hypoparathyroidism With Synthetic Human Parathyroid Hormone 1-34 [NCT00001304]Phase 227 participants (Actual)Interventional1991-10-31Completed
A Phase 2/3 Multicenter, Randomized, Double Blind Study of Docetaxel (Taxotere) Plus DN-101 or Placebo in Androgen Independent Prostate Cancer (AIPC) [NCT00043576]Phase 2/Phase 3250 participants Interventional2002-08-31Active, not recruiting
Phase II Study of Calcitrol Enhanced Carboplatin in Hormone Refractory Prostate Cancer [NCT00017576]Phase 219 participants (Actual)Interventional2000-12-31Completed
Calcitriol and Dexamethasone for Myelodysplastic Syndromes [NCT00030069]Phase 232 participants (Actual)Interventional2001-09-30Completed
Calcitriol + Dexamethasone in Early, Recurrent Prostate Cancer Following Local Therapy, A Phase I/II Trial [NCT00054522]Phase 215 participants (Actual)Interventional2002-04-30Completed
PLA General Hospital [NCT05920512]Phase 1/Phase 210 participants (Anticipated)Interventional2022-04-01Recruiting
A Phase 1/2 Multicenter, Open Label, Dose Ranging Study of DN-101 and Taxotere® in Patients With Advanced (Stage IIIB or IV) Non-Small Cell Lung Cancer (NSCLC) Who Have Failed Previous Therapy With Platinum-Based Chemotherapy [NCT00066885]Phase 1/Phase 280 participants Interventional2003-06-30Completed
A Phase IV, Single-Center, Active-Controlled Cross-Over Pilot Study to Evaluate the Effects of Zemplar Injection and Calcijex on Intestinal Absorption of Calcium [NCT00073710]Phase 430 participants Interventional2004-09-30Completed
A Phase I Study of Intravenous (IV) Calcitriol in Combination With ZD1839 (IRESSA®) in Refractory Solid Tumors [NCT00084708]Phase 153 participants (Actual)Interventional2002-11-30Completed
A Phase IV, Prospective, Randomized, Active-Controlled, Double-Blind, Double-Dummy, Multi-Center Study to Evaluate the Survival Benefits of Zemplar Relative to Calcijex in Subjects With Stage V Chronic Kidney Disease on Hemodialysis [NCT00062699]Phase 42,200 participants Interventional2003-04-30Terminated
[NCT01673204]Phase 4276 participants (Anticipated)Interventional2012-10-31Recruiting
A Phase 4 Randomized Multicenter Open Label Trial of Paricalcitol Versus Calcitriol for Efficacy and Safety in Stage 3 or 4 Ckd Patients With Secondary Hyperparathyroidism [NCT00823303]Phase 4110 participants (Actual)Interventional2009-02-28Completed
PK and PD of Calcitriol Following Twice Daily Application of Calcitriol 3 µg/g Ointment Under Conditions of Maximal Use in Adolescents With Plaque Psoriasis [NCT00419666]Phase 225 participants (Actual)Interventional2006-08-01Completed
A Pilot Trial of 13-cis Retinoic Acid (Isotretinoin) for the Treatment of Men With Oligoasthenoteratozoospermia [NCT02061384]Phase 220 participants (Actual)Interventional2014-08-31Completed
Phase II Study of Calcitriol-Enhanced Docetaxel in Patients With Previously Untreated Metastatic or Locally Advanced Pancreatic Cancer [NCT00238199]Phase 225 participants (Actual)Interventional2002-06-30Completed
A Continuation Study of DN-101 (Calcitriol) and Docetaxel in Subjects Previously Enrolled in Studies DN101-002 or DN101-004 [NCT00285675]Phase 225 participants Interventional2006-04-30Active, not recruiting
Tumor Necrosis Factor-α Induces Vitamin D Resistance in Small Intestinal Calcium Absorption [NCT00427804]9 participants (Actual)Interventional2007-01-31Completed
High vs. Low Calcium Intake in the Presence of High Vitamin D: Effect on Gene Expression in the Colon [NCT00298545]Phase 110 participants (Actual)Interventional2005-11-30Completed
A Phase 3, Randomized, Open-Label Study Evaluating DN-101 in Combination With Docetaxel in Androgen-Independent Prostate Cancer (AIPC) (ASCENT-2) [NCT00273338]Phase 31,200 participants (Anticipated)Interventional2006-01-31Terminated(stopped due to DSMB)
The Safety and Short-Term Efficacy of Calcitriol in the Treatment of Immunoglobulin A Nephropathy [NCT00319761]Phase 410 participants Interventional2006-05-31Completed
[NCT01536938]Phase 2303 participants (Actual)Interventional2012-05-31Completed
Comparison of the Efficacy and Safety With Eldecalcitol and Calcitriol in Postmenopausal Women With Low Bone Mineral Density or Mild Osteoporosis [NCT05902078]Phase 4300 participants (Anticipated)Interventional2023-06-30Not yet recruiting
Effect of Phosphate Binders on FGF-23 During Calcitriol Administration in CKD Stage 3 Patients [NCT01748396]Phase 430 participants (Actual)Interventional2012-07-31Completed
Evaluation of Topical Nicotinamide in Combination With Calcipotriol Compared With Calcipotriol Alone for the Treatment of Mild to Moderate Psoriasis. [NCT01763424]Phase 2/Phase 366 participants (Actual)Interventional2011-07-31Completed
Comparisons of the Effect of Inactive and Active Vitamin D on Serum Sclerostin/dickkopf1 Levels [NCT01765010]Phase 488 participants (Anticipated)Interventional2013-01-31Recruiting
Direct Effect of Paricalcitol on Anemia in Chronic Kidney Disease [NCT01768351]Phase 460 participants (Actual)Interventional2010-10-31Completed
Phase 4 Study of Oral Calcitriol for Reduction of Mild Proteinuria in Patients With CKD [NCT01820832]Phase 460 participants (Anticipated)Interventional2013-03-31Not yet recruiting
Efficacy and Safety of LEO 90105 Ointment (Calcipotriol Hydrate Plus Betamethasone Dipropionate) in Japanese Subjects With Psoriasis Vulgaris [NCT01422434]Phase 3676 participants (Actual)Interventional2011-07-31Completed
Evaluating Hormonal Mechanisms for Vitamin D Receptor Agonist Therapy in Diabetes: The VALIDATE-D Study [NCT01635062]41 participants (Actual)Interventional2012-09-30Completed
Vitamin D as a Therapeutic Adjunct in the Stimulant Treatment of ADHD: a Proof-of-concept Study of Stimulant-induced Dopamine Release Using [11C]-PHNO PET in Healthy Humans [NCT03103750]Phase 124 participants (Actual)Interventional2017-08-15Completed
The Effect of Neutrophil Gelatinase-associated Lipocalin Derived From Osteoblasts and Vascular Smooth Muscle Cells on Vascular Calcification in Chronic Kidney Desease and the Intervention of Paliscalcitol - Clinical Research Section [NCT05720273]Phase 480 participants (Anticipated)Interventional2023-04-01Not yet recruiting
Evaluation of the Efficacy and Safety of Indigo Naturalis Oil Extract and Calcipotriol Solution in Patients With Nail Psoriasis [NCT01445886]Phase 2/Phase 333 participants (Actual)Interventional2011-01-31Completed
Patient Preference of Taclonex Ointment to Taclonex Scalp Suspension in Adult Subjects With Psoriasis Vulgaris [NCT01707043]Phase 420 participants (Actual)Interventional2012-10-31Completed
Vitamin D Plus Celecoxib Therapy to Stimulate Intratumoral Immune Reactivity [NCT00953849]Phase 1/Phase 221 participants (Actual)Interventional2009-11-30Completed
A Multicenter, Randomized, Double Blind, Parallel Group, Vehicle Controlled, Study of the Safety and Efficacy of Calcitriol 3 mcg/g Ointment Applied Twice Daily for 8 Weeks in Pediatric Subjects (2 to 12 Years of Age) With Mild to Moderate Plaque Psoriasi [NCT02186665]Phase 419 participants (Actual)Interventional2014-07-31Completed
An Open-Label Study Evaluating Enstilar® (Calcipotriene and Betamethasone Dipropionate) Foam, 0.005%/0.064% QD in Psoriasis Patients Being Treated With Etanercept or Adalimumab [NCT03827876]Phase 430 participants (Anticipated)Interventional2019-01-16Recruiting
A Randomized Phase III, Three-parallel Arm, Assessor Blind, Multi-centre Study to Evaluate the Efficacy, Safety and Tolerability of AKP02 Cutaneous Spray Versus Enstilar Cutaneous Foam in Subjects With Mild to Moderate Psoriasis. [NCT05249972]Phase 3294 participants (Anticipated)Interventional2022-01-24Recruiting
A Phase II Study of Short-Term Use of Teriparatide (Forteo) in the Treatment of Patients With Postoperative Hypocalcemia [NCT00623974]Phase 27 participants (Actual)Interventional2008-05-31Terminated(stopped due to Terminated due to slow accrual.)
Prevention of Osteoporosis After Cardiac Transplantation [NCT00000412]Phase 3149 participants (Actual)Interventional1997-09-30Completed
[NCT00004402]Phase 330 participants Interventional1999-11-30Completed
A Phase 2B, Double-blind, Randomized, Placebo-controlled, Proof-of-concept Study of an Oral Vitamin D Compound (DP001) in Secondary Hyperparathyroidism in Patients on Hemodialysis [NCT01922843]Phase 262 participants (Actual)Interventional2013-09-30Completed
Vitamin D and Arterial Function in Patients With Chronic Kidney Disease [NCT01384539]Phase 3128 participants (Actual)Interventional2011-07-31Completed
A Phase 1, Single and Multiple Ascending Dose Study to Investigate the Safety, Tolerability, and Pharmacokinetics of VS 105 Following Oral Administration in Healthy and Hemodialysis Subjects [NCT03043482]Phase 169 participants (Actual)Interventional2017-01-24Completed
A Phase IIa Exploratory Study Evaluating the Anti-psoriatic Effect of Daivobet® Gel Applied Then Removed After 10 Minutes, Daivobet® Gel Applied Then Removed After 20 Minutes, Daivobet® Gel Applied for 24 Hours and Daivobet® Gel Vehicle Applied for 24 Hou [NCT01607853]Phase 224 participants (Actual)Interventional2012-06-30Completed
Randomized Controlled Trial of Calcitriol vs. Placebo Among Critically-ill Patients With Sepsis [NCT01689441]Phase 267 participants (Actual)Interventional2013-02-28Completed
Comparison Between Low and High Doses of Prophylactic Vitamin D in Prevention of Osteopenia of Prematurity [NCT04768439]Phase 280 participants (Actual)Interventional2020-08-10Completed
[NCT00004468]0 participants (Actual)Interventional1998-10-31Withdrawn(stopped due to Lack of funds)
Comparing the Effectiveness of High or Low Dose of Active Vitamin D Combined With Neutral Phosphate in Children With X-linked Hypophosphatemia [NCT03820518]Phase 4100 participants (Anticipated)Interventional2017-01-01Recruiting
A Phase I Study of 1,25 Dihydroxy-Vitamin D3 (Calcitriol) in Patients With Prostate Cancer [NCT00004928]Phase 10 participants Interventional1999-10-31Completed
[NCT00004340]Phase 2109 participants Interventional1995-06-30Completed
Testing Restoring Effects of Vitamin D on the Dopamine System: A Human Laboratory Study Among Cocaine Users. [NCT04826133]Early Phase 14 participants (Actual)Interventional2019-03-27Terminated(stopped due to Could not obtain additional funding to continue the research.)
A Phase II Trial of Calcitriol and Naproxen in Patients With Recurrent Prostate Cancer [NCT00383487]Phase 220 participants (Actual)Interventional2005-03-31Terminated(stopped due to Extreme toxicity)
Comparison of Serum Calcium Level Between Preoperative Vitamin D and Non-vitamin D Regimen of Total Parathyroidectomy in End-stage Renal Failure Patients in Rajavithi Hospital [NCT04967469]60 participants (Anticipated)Interventional2020-09-01Recruiting
A Randomized, Prospective, Cross-Over Study of Calcitriol vs. Paricalcitol in the Treatment of Mineral and Bone Disease in Hemodialysis Patients [NCT01725113]Phase 416 participants (Actual)Interventional2012-11-30Terminated(stopped due to Nationwide shortage of study meds in 2013 loss of funding & competing studies)
Study of Combination Therapy With Topical Rapamycin and Calcitriol for Cutaneous Lesions of Tuberous Sclerosis: A Double-blind Randomized Controlled Trial [NCT03140449]Phase 352 participants (Actual)Interventional2013-09-05Completed
Trial to Optimize Mineral Outcomes in End Stage Renal Disease (ESRD) Patients [NCT01100723]Phase 492 participants (Actual)Interventional2010-03-31Completed
Innate Immunity in Acne Vulgaris [NCT01694433]Phase 2/Phase 366 participants (Actual)Interventional2013-02-28Completed
A Phase 3 Study Comparing an Ointment Containing Calcipotriol 25 mcg/g Plus Hydrocortisone 10 mg g With Tacalcitol 4 mcg/g Ointment and the Ointment Vehicle Alone, All Applied Once Daily in the Treatment of Psoriasis Vulgaris on the Face and on the Intert [NCT00640822]Phase 3782 participants (Actual)Interventional2008-02-29Completed
A Pilot Trial of Calcitriol in Localized Prostate Cancer: Investigation of Biologic Effects and Potential Intermediate Endpoints [NCT00084864]Phase 225 participants (Actual)Interventional2002-09-30Terminated(stopped due to sample size is too small to draw a conclusion)
Using 2D/3D Imaging to Analyze the Regeneration Rate of Autologous Bone During Alveolar Bone Preservation Surgery Using Periodontal Valves to Completely Cover Autologous Tooth Roots, Bone Substitutes, and Vitamin D3 Treatment [NCT06141239]48 participants (Anticipated)Interventional2023-12-01Not yet recruiting
Phase II Study of Pulse Calcitriol in Patients With Rising PSA After Definitive Treatment for Prostate Cancer [NCT00004043]Phase 225 participants (Actual)Interventional1999-02-28Completed
Vitamin D as a Therapeutic Adjunct in the Stimulant Treatment of ADHD: a Proof-of-concept Tele-health Study of Stimulant-induced Improvement in Neurocognitive Functioning. [NCT04386811]Phase 124 participants (Anticipated)Interventional2020-08-05Recruiting
Efficacy and Safety of Paricalcitol on the Treatment of Secondary Hyperparathyroidism in Calcitriol Resistant Dialysis Subjects [NCT00664430]Phase 413 participants (Actual)Interventional2009-01-31Terminated(stopped due to Low enrollment rate)
A Phase IV, Randomized, Single-center Study of the Effects of Calcitriol and Paricalcitol on Vascular Calcification in Chronic Kidney Disease Stages 3 and 4 [NCT00752102]Phase 444 participants (Actual)Interventional2008-09-30Completed
A Phase 1, Single- Center, Randomized, Double-blind, Vehicle And Active Comparator-controlled Trial To Evaluate The Antipsoriatic Activity And Safety Of A Topically Applied Pf-06263276 Formulation In A Psoriasis Plaque Test [NCT02193815]Phase 115 participants (Actual)Interventional2014-09-30Completed
Pharmacokinetics and Pharmacodynamics of Calcitriol 3 mcg/g Ointment Applied Twice Daily for 14 Days Under Conditions of Maximal Use in Pediatric Subjects (2 to 12 Years of Age) With Plaque Psoriasis [NCT01766440]Phase 418 participants (Actual)Interventional2013-03-31Completed
A Randomized, Double-Blind Study Comparing TOLMAR Calcipotriene and Betamethasone Suspension to Reference Listed Drug in the Treatment of Scalp Psoriasis [NCT03122353]Phase 1699 participants (Actual)Interventional2017-04-11Completed
Vitamin D Supplementation in Vitamin Deficient Women Undergoing ICSI Cycles: Does it Affect the Fertility Outcome? [NCT03209856]Phase 4200 participants (Actual)Interventional2017-07-06Completed
A Multicenter Open Label Uncontrolled Study of the Long Term Safety and Efficacy of Calcitriol 3 mcg/g Ointment Applied Twice Daily for 26 Weeks in Pediatric Subjects (2 to 16 Years and 11 mo of Age) With Mild to Moderate Plaque Psoriasis [NCT02125279]Phase 454 participants (Actual)Interventional2014-05-31Completed
A Long-term Safety and Efficacy Study of CTAP101 Capsules in Subjects With Stages 3 or 4 Chronic Kidney Disease, Secondary Hyperparathyroidism and Vitamin D Insufficiency (Extension of Study CTAP101-CL-3001 or CTAP101-CL-3002) [NCT02282813]Phase 3298 participants (Actual)Interventional2013-04-30Completed
A Plaque Test Study With LEO 35299 in Psoriasis Vulgaris [NCT01580488]Phase 124 participants (Actual)Interventional2012-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00001151 (1) [back to overview]Number of Participants With Normal Serum Calcium Concentrations
NCT00001304 (7) [back to overview]Serum 25-hydroxyvitamin D Level
NCT00001304 (7) [back to overview]Serum Calcium Level
NCT00001304 (7) [back to overview]Serum Magnesium Level
NCT00001304 (7) [back to overview]Serum Phosphorus Level
NCT00001304 (7) [back to overview]Urinary Creatinine Clearance
NCT00001304 (7) [back to overview]Urine Calcium Excretion Level
NCT00001304 (7) [back to overview]Serum 1,25-hydroxyvitamin D Level
NCT00084864 (1) [back to overview]Number of Participants With Adverse Events, Graded According to NCI CTCAE v2.0
NCT00301067 (6) [back to overview]Number and Frequency of Dose Limiting Toxicities (DLTs) With High-dose Calcitriol in Combination With Temozolomide
NCT00301067 (6) [back to overview]Overall Response Rate
NCT00301067 (6) [back to overview]Overall Survival
NCT00301067 (6) [back to overview]Time to Progression
NCT00301067 (6) [back to overview]Number of Patients With Toxicity
NCT00301067 (6) [back to overview]Overall Survival (OS) Stratified by Vitamin D-Receptor (VDR) Gene Polymorphisms
NCT00419666 (9) [back to overview]Trough Plasma Levels (Ctrough) of Calcitriol
NCT00419666 (9) [back to overview]Time at Which Maximum Concentration (Cmax) Occurred (Tmax)
NCT00419666 (9) [back to overview]The Observed Peak Drug Concentration (Cmax) of Calcitriol
NCT00419666 (9) [back to overview]Change From Baseline in Effect of Calcitriol Ointment on Calcium (Serum Calcium, Urinary (U) Calcium Random) and Phosphorus Homeostasis up to Day 56
NCT00419666 (9) [back to overview]Area Under the Concentration-Time Curve From Pre-Application (T0) Through 9 Hours Post Dosing (AUC [0-9 Hours])
NCT00419666 (9) [back to overview]Area Under the Concentration-Time Curve From Pre-Application (T0) Through 12 Hours Post Dosing (AUC [0-12 Hours])
NCT00419666 (9) [back to overview]Number of Participants With Adverse Events
NCT00419666 (9) [back to overview]Change From Baseline in Effect of Calcitriol Ointment on Calcium (Urinary Calcium/Creatinine Ratio) Homeostasis up to Day 56
NCT00419666 (9) [back to overview]Change From Baseline in Effect of Calcitriol Ointment on Calcium (Serum Calcium Albumin Adjusted) Homeostasis up to Day 56
NCT00427804 (1) [back to overview]Fractional Absorption of Calcium
NCT00524589 (2) [back to overview]Objective Response (Complete or Partial Response)
NCT00524589 (2) [back to overview]Corrected Serum Calcium Expression
NCT00536991 (4) [back to overview]Determine the Maximum Tolerated Dose (MTD)
NCT00536991 (4) [back to overview]Incidence of Toxicity Graded According to the National Cancer Institute CTC Version 3.0
NCT00536991 (4) [back to overview]Objective Tumor Response, Assessed by RECIST
NCT00536991 (4) [back to overview]PSA Response Rate
NCT00640822 (1) [back to overview]Subjects With Controlled Disease According to the Investigator Assessment of the Face at Week 8
NCT00658788 (12) [back to overview]Tolerability Assessment - Stinging/ Burning
NCT00658788 (12) [back to overview]Tolerability Assessment - Telangiectasias
NCT00658788 (12) [back to overview]Overall Disease Severity Success (ODS)
NCT00658788 (12) [back to overview]Percent Change From Baseline in Body Surface Area (% BSA) Affected
NCT00658788 (12) [back to overview]Global Improvement Score
NCT00658788 (12) [back to overview]Overall Disease Severity
NCT00658788 (12) [back to overview]Signs of Psoriasis - Erythema
NCT00658788 (12) [back to overview]Signs of Psoriasis - Plaque Elevation
NCT00658788 (12) [back to overview]Signs of Psoriasis - Scaling
NCT00658788 (12) [back to overview]Tolerability Assessment - Folliculitis
NCT00658788 (12) [back to overview]Tolerability Assessment - Pruritus
NCT00658788 (12) [back to overview]Tolerability Assessment - Skin Atrophy
NCT00664430 (1) [back to overview]Number of Participants With Adverse Events
NCT00690924 (1) [back to overview]Grade III-IV Toxicities or Any Grade II Toxicities Lasting More Than 2 Weeks
NCT00691002 (5) [back to overview]"Participants With Controlled Disease According to the IGA of Disease Severity of the Face at Week 4 (Visit 4) in the Double-blind Phase"
NCT00691002 (5) [back to overview]"Participants With Success According to Total Sign Score (TSS) of the Face at Week 8 (Visit 6) in the Double-blind Phase"
NCT00691002 (5) [back to overview]"Participants With Success According to Total Sign Score of the Intertriginous Areas at Week 8 (Visit 6) in the Double-blind Phase"
NCT00691002 (5) [back to overview]"Participants With Controlled Disease According to the IGA of Disease Severity of the Intertriginous Areas at Week 8 (Visit 6) in the Double-blind Phase"
NCT00691002 (5) [back to overview]"Participants With Controlled Disease According to the Investigator's Global Assessment(IGA) of Disease Severity of the Face at Week 8 (Visit 6) in the Double-blind Phase"
NCT00752102 (1) [back to overview]Coronary Artery (CAC) Score Progression
NCT00763555 (16) [back to overview]Number of Participants With Adverse Events (AEs)
NCT00763555 (16) [back to overview]Percentage of Participants With Success Rate 2 (SR2) at Week 8
NCT00763555 (16) [back to overview]Change From Baseline in Blood Chemistry: Alkaline Phosphatase, Aspartate Aminotransferase (AST) and Alanine Aminotransferase (ALT)
NCT00763555 (16) [back to overview]Change From Baseline in Blood Chemistry: Bilirubin Direct, Bilirubin Total, Blood Urea Nitrogen (BUN) and Creatinine
NCT00763555 (16) [back to overview]Change From Baseline in Vital Sign Parameter: Systolic Blood Pressure and Diastolic Blood Pressure
NCT00763555 (16) [back to overview]Percentage of Participants With a Local Tolerability Score Worse Than Baseline Score
NCT00763555 (16) [back to overview]Change From Baseline in Vital Sign Parameter: Heart Rate
NCT00763555 (16) [back to overview]Percentage of Participants With at Least 1-Grade Improvement From Baseline in Erythema, Scaling and Plaque Elevation
NCT00763555 (16) [back to overview]Percentage of Participants With Success Rate 1 (SR1) at Week 8
NCT00763555 (16) [back to overview]Change From Baseline in Calcitriol Plasma Levels
NCT00763555 (16) [back to overview]Change From Baseline in Dermatologic Sum Score (DSS) at Week 8
NCT00763555 (16) [back to overview]Change From Baseline in Serum Calcium Homeostasis Parameter: Albumin
NCT00763555 (16) [back to overview]Change From Baseline in Serum Calcium Homeostasis Parameter: Albumin-adjusted Calcium
NCT00763555 (16) [back to overview]Change From Baseline in Serum Calcium Homeostasis Parameter: Calcium
NCT00763555 (16) [back to overview]Change From Baseline in Serum Calcium Homeostasis Parameter: Parathyroid Hormone (PTH) Intact
NCT00763555 (16) [back to overview]Change From Baseline in Serum Calcium Homeostasis Parameter: Phosphorus
NCT00794547 (5) [back to overview]Number of Participants That Experience Grade 3 or Greater Neutropenia
NCT00794547 (5) [back to overview]Mean AUC 1,25-D3 Concentration at 12 and 24 Hours
NCT00794547 (5) [back to overview]MTD of Intravenous Calcitriol When Administered Prior to Fixed Dose Cisplatin 75mg/m2 and Docetaxel 75 mg/m2, Every 3 Weeks in Patients With Advanced Non-small Cell Lung Cancer (NSCLC)
NCT00794547 (5) [back to overview]Median Time to Progression
NCT00794547 (5) [back to overview]Median Overall Survival
NCT00823303 (1) [back to overview]Confirmed Hypercalcemia
NCT00845481 (6) [back to overview]The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Diprosalic Ointment
NCT00845481 (6) [back to overview]The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Betnovat® Ointment
NCT00845481 (6) [back to overview]The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Elocon Ointment
NCT00845481 (6) [back to overview]The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Dermovat Ointment
NCT00845481 (6) [back to overview]The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Daivobet® Ointment
NCT00845481 (6) [back to overview]The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Daivobet Ointment Vehicle
NCT00904033 (8) [back to overview]Body Mass Index (Exercise)
NCT00904033 (8) [back to overview]Bone Formation (Calcitriol)
NCT00904033 (8) [back to overview]Bone Formation (Exercise)
NCT00904033 (8) [back to overview]Bone Resorption (Calcitriol)
NCT00904033 (8) [back to overview]Bone Resorption (Exercise)
NCT00904033 (8) [back to overview]Handgrip (kg) Strength - (Exercise)
NCT00904033 (8) [back to overview]Handgrip (kg) Strength - (Calcitriol)
NCT00904033 (8) [back to overview]Body Mass Index (Calcitriol)
NCT00924950 (1) [back to overview]Change in Total Modified PASI Score at Week 4 Compared to Baseline
NCT00925704 (3) [back to overview]Time of Maximum Plasma Concentration (Tmax) for Exogenous Calcitriol
NCT00925704 (3) [back to overview]Maximum Plasma Concentration (Cmax) for Exogenous Calcitriol
NCT00925704 (3) [back to overview]Area Under the Serum Concentration-time Curve (AUC 0-48) for Exogenous Calcitriol
NCT00953849 (4) [back to overview]Change in GM-CSF
NCT00953849 (4) [back to overview]Change in IFN-gamma Levels
NCT00953849 (4) [back to overview]Change in IL-2 Levels
NCT00953849 (4) [back to overview]Change in IL-6 Levels.
NCT00988637 (13) [back to overview]Median Percent (%) Change From Baseline in % Treatable BSA (Body Surface Area) From Baseline to Week 4
NCT00988637 (13) [back to overview]Mean Change From Baseline Scores for the Koo-Menter Psoriasis Index 12-item Quality of Life Questionnaire (PQOL-12) From Baseline to Week 4
NCT00988637 (13) [back to overview]Number of Participants Who Were a Success (Clear/Almost Clear) of Plaque Psoriasis at Week 2 Based on the Overall Disease Severity (ODS), Dichotomized Scale From Baseline to Week 2
NCT00988637 (13) [back to overview]Number of Participants Who Were a Success (Clear/Almost Clear) of Plaque Psoriasis at Week 4 Based on the Overall Disease Severity (ODS), Full Ordinal Scale From Baseline to Week 4
NCT00988637 (13) [back to overview]Number of Participants With Tolerability Assessments Resulting in Adverse Events From Baseline to Week 4
NCT00988637 (13) [back to overview]"Number of Participants Who Responded to the Categories of Possible Answers to the Subject's Satisfaction Survey Question I am Satisfied With my Appearance at Week 4"
NCT00988637 (13) [back to overview]"Number of Participants Who Responded to the Categories of Possible Answers to the Subject's Satisfaction Survey Question I am Satisfied With the Results of This Treatment Program at Week 4"
NCT00988637 (13) [back to overview]"Number of Participants Who Responded to the Categories of Possible Answers to the Subject's Satisfaction Survey Question I Would Use This Treatment Program Again if Recommended by the Dermatologist at Week 4"
NCT00988637 (13) [back to overview]"Number of Participants Who Responded to the Categories of Possible Answers to the Subject's Satisfaction Survey Question The Treatment Program Was Easy to Follow at Week 4"
NCT00988637 (13) [back to overview]Number of Participants in Each Category of the Global Assessment of Improvement (GAI) Scale From Baseline to Week 4
NCT00988637 (13) [back to overview]Number of Participants With a Decrease in Signs of Psoriasis (Erythema) Scores From Baseline to Week 4
NCT00988637 (13) [back to overview]Number of Participants With Decrease in Signs of Psoriasis (Plaque Elevation) Scores From Baseline to Week 4
NCT00988637 (13) [back to overview]Number of Participants With Decrease in Signs of Psoriasis (Scaling) Scores From Baseline to Week 4
NCT01012713 (3) [back to overview]The Secondary Endpoint Will be the Percentage of Patients Achieving a 75% Reduction in Psoriasis Area and Severity Index at Weeks 4 and 8.
NCT01012713 (3) [back to overview]A Tertiary Endpoint Will be the Percentage of Patients Achieving 90% Reduction in Psoriasis Area and Severity Index at Week 12.
NCT01012713 (3) [back to overview]The Primary Endpoint Will be the Percentage of Patients Achieving a 75% Reduction in the Psoriasis Area and Severity Index at Week 12.
NCT01100723 (6) [back to overview]Percent of Patients Achieving Parathyroid Hormone Target ≤ 450
NCT01100723 (6) [back to overview]Percent of Patients Achieving Phosphorous Target ≤ 4.5
NCT01100723 (6) [back to overview]Percent of Patients on Cinacalcet and Vitamin D Analogues
NCT01100723 (6) [back to overview]Percent of Patients Achieving Phosphorous Target ≤ 5.5
NCT01100723 (6) [back to overview]Percent of Patients Achieving Calcium Target ≤ 10.1
NCT01100723 (6) [back to overview]Percent of Patients Achieving Parathyroid Hormone Target ≤ 300
NCT01134315 (8) [back to overview]Mean Baseline and Change From Baseline in Parathyroid Hormone at Final Visit (FV)
NCT01134315 (8) [back to overview]Mean Baseline and Change From Baseline in Albumin at Final Visit (FV)
NCT01134315 (8) [back to overview]Mean Baseline and Change From Baseline in 25-Hydroxy Vitamin D3 at Final Visit (FV)
NCT01134315 (8) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (AEs), Serious AEs (SAEs), Deaths and Discontinuations Due to AEs
NCT01134315 (8) [back to overview]Mean Baseline (BL) and Change From Baseline in Calcium, Inorganic Phosphate (IP), Blood Urea Nitrogen (BUN), Creatinine at Final Visit (FV)
NCT01134315 (8) [back to overview]Mean Baseline (BL) and Change From Baseline in Potassium, Sodium, Chloride, Bicarbonate at Final Visit (FV)
NCT01134315 (8) [back to overview]Mean Baseline and Change From Baseline in 1,25-Dihydroxy Vitamin D3 at Final Visit (FV)
NCT01134315 (8) [back to overview]Percentage of Participants With at Least One Incidence of Hypercalcemia
NCT01222234 (2) [back to overview]Change in 24,25(OH)2D Levels in CKD vs. Non-CKD Subjects Receiving Cholecalciferol
NCT01222234 (2) [back to overview]Monocyte Protein Expression
NCT01235728 (3) [back to overview]Least Squares Mean Percent Change From Baseline (Predose Day 1) of TLS Score for Lesions Treated With MK-0873 and Lesions Treated With Calcitriol
NCT01235728 (3) [back to overview]Least Squares Mean Percent Change From Baseline (Predose Day 1) of Target Lesion Severity (TLS) Score for Lesions Treated With MK-0873 and Lesions Treated With MK-0873 Vehicle
NCT01235728 (3) [back to overview]Mean Maximum Plasma Concentrations at Trough of Day 8, 15, 22, and 29 Following Topical Administration of MK-0873 to Psoriatic Patients
NCT01265615 (10) [back to overview]Serum Creatinine
NCT01265615 (10) [back to overview]GFR (Glomerular Filtration Rate)
NCT01265615 (10) [back to overview]Coronary Calcium Score
NCT01265615 (10) [back to overview]CAD (Chronic Allograft Dysfunction) Degree
NCT01265615 (10) [back to overview]CAD (Chronic Allograft Dysfunction) Degree
NCT01265615 (10) [back to overview]Heart Failure (HF)
NCT01265615 (10) [back to overview]Number of Circulating SP (Side Population) Stem-Progenitor Cells
NCT01265615 (10) [back to overview]Systolic Blood Pressure
NCT01265615 (10) [back to overview]VDR (Vitamin D Receptor) Expression in Kidney
NCT01265615 (10) [back to overview]VDR (Vitamin D Receptor) Expression in Myocardium
NCT01293682 (2) [back to overview]Mean Change in Bone Resorption: NTX (N-terminal Telopeptide)
NCT01293682 (2) [back to overview]Mean Change in Bone Formation: BAP (Bone-specific Alkaline Phosphatase)
NCT01317940 (5) [back to overview]Prevalence of Obesity and Vitamin D Insufficiency in Adolescents With Newly Diagnosed ALL and in Their Siblings
NCT01317940 (5) [back to overview]Bone Mineral Density by QCT in Survivors at Study End (Group B)
NCT01317940 (5) [back to overview]Bone Mineral Density by Quantitative Computed Tomography (QCT) at Study End (Group A)
NCT01317940 (5) [back to overview]Change in Serum Vitamin D Level (Group A)
NCT01317940 (5) [back to overview]Change in Vitamin D Level (Group B)
NCT01341782 (6) [back to overview]Percentage of Participants With Target Intact Parathyroid Hormone (iPTH)
NCT01341782 (6) [back to overview]Percentage of Participants With Target Intact Parathyroid Hormone (iPTH) and Without Hypercalcemia
NCT01341782 (6) [back to overview]Number of Visits at Which Participants Achieved iPTH Control in the Target Range of 60 to 180 pg/mL
NCT01341782 (6) [back to overview]Percentage of Participants With ≥ 50% Reduction in Intact Parathyroid Hormone (iPTH) From Baseline and With No Hypercalcemia
NCT01341782 (6) [back to overview]Percentage of Participants With ≥ 50% Reduction in Intact Parathyroid Hormone (iPTH) From Baseline
NCT01341782 (6) [back to overview]Number of Visits at Which Participants Achieved iPTH Control With ≥ 50% Reduction in Intact Parathyroid Hormone (iPTH) From Baseline
NCT01350934 (7) [back to overview]Base Study: Percentage Change From Baseline in Serum Procollagen Type 1 N-Terminal Propeptide (s-P1NP) at Month 6
NCT01350934 (7) [back to overview]Extension Study: Percentage Change From Baseline in Lumbar Spine BMD at Month 12
NCT01350934 (7) [back to overview]Extension Study: Percentage Change From Baseline in s-CTx at Month 12
NCT01350934 (7) [back to overview]Extension Study: Percentage Change From Baseline in s-P1NP at Month 12
NCT01350934 (7) [back to overview]Extension Study: Percentage of Participants With Serum 25-Hydroxyvitamin (OH) D <20 ng/mL at Month 12
NCT01350934 (7) [back to overview]Base Study: Percentage Change From Baseline in Serum C-Telopeptides of Type 1 Collagen (s-CTx) at Month 6
NCT01350934 (7) [back to overview]Base Study: Percentage Change From Baseline in Lumbar Spine Bone Mineral Density (BMD) at Month 6
NCT01384539 (3) [back to overview]Compare the Efficacy of Calcitriol and Cholecalciferol Supplementation on Plasma Concentrations of C-reactive Protein
NCT01384539 (3) [back to overview]Compare the Effect of Calcitriol and Cholecalciferol Supplementation on Vascular Endothelial Cell Expression of Nf-kB
NCT01384539 (3) [back to overview]Compare the Difference Between the Calcitriol and Cholecalciferol Groups in Conduit Artery Endothelium-dependent Dilation (EDD) in Response to Treatment.
NCT01422434 (4) [back to overview]Change From Baseline in Modified Psoriasis Area and Severity Index (mPASI)
NCT01422434 (4) [back to overview]Change From Baseline in Target Lesion Assessment
NCT01422434 (4) [back to overview]Physician's Global Assessment of Psoriasis
NCT01422434 (4) [back to overview]Change in mPASI From Baseline to Week 1
NCT01445886 (3) [back to overview]Change From Baseline in Modified Target NAPSI for the Single Most Severely Affected Nail
NCT01445886 (3) [back to overview]Physician's and Subject's Global Assessment
NCT01445886 (3) [back to overview]Change From Baseline in Single-handed Nail Psoriasis Severity Index (shNAPSI) at 24 Weeks
NCT01536938 (1) [back to overview]Subjects With 'Controlled Disease' ('Clear'/'Almost Clear' for Subjects w. at Least Moderate Disease at Baseline, 'Clear' for Subjects With Mild Disease at Baseline) According to the Investigator's Global Assessment (IGA) on the Trunk and Limbs at Week 4.
NCT01580488 (6) [back to overview]Change in Erythema From Baseline to Day 22
NCT01580488 (6) [back to overview]Change in Lesion Thickness From Baseline to Day 22
NCT01580488 (6) [back to overview]Change in the Total Clinical Score From Baseline to Day 22
NCT01580488 (6) [back to overview]Change in Infiltration From Baseline to Day 22
NCT01580488 (6) [back to overview]Change in Scaling From Baseline to Day 22
NCT01580488 (6) [back to overview]Change in Skin Thickness From Baseline to Day 22
NCT01607853 (26) [back to overview]Change in Total Clinical Score at Day 15 Compared to Baseline
NCT01607853 (26) [back to overview]Change in Total Clinical Score at Day 18 Compared to Baseline
NCT01607853 (26) [back to overview]Change in Total Clinical Score at Day 4 Compared to Baseline
NCT01607853 (26) [back to overview]Change in Total Clinical Score at Day 8 Compared to Baseline
NCT01607853 (26) [back to overview]Change in Total Clinical Score From Baseline to Day 22
NCT01607853 (26) [back to overview]Change From Baseline in Erythema at Day 11
NCT01607853 (26) [back to overview]Change From Baseline in Erythema at Day 15
NCT01607853 (26) [back to overview]Change From Baseline in Erythema at Day 18
NCT01607853 (26) [back to overview]Change From Baseline in Erythema at Day 22
NCT01607853 (26) [back to overview]Change From Baseline in Erythema at Day 4.
NCT01607853 (26) [back to overview]Change From Baseline in Erythema at Day 8.
NCT01607853 (26) [back to overview]Change From Baseline in Infiltration at Day 11
NCT01607853 (26) [back to overview]Change From Baseline in Infiltration at Day 15
NCT01607853 (26) [back to overview]Change From Baseline in Infiltration at Day 18
NCT01607853 (26) [back to overview]Change From Baseline in Infiltration at Day 22
NCT01607853 (26) [back to overview]Change From Baseline in Infiltration at Day 4
NCT01607853 (26) [back to overview]Change From Baseline in Infiltration at Day 8
NCT01607853 (26) [back to overview]Change From Baseline in Scaling at Day 11
NCT01607853 (26) [back to overview]Change From Baseline in Scaling at Day 15
NCT01607853 (26) [back to overview]Change From Baseline in Scaling at Day 18
NCT01607853 (26) [back to overview]Change From Baseline in Scaling at Day 22
NCT01607853 (26) [back to overview]Change From Baseline in Scaling at Day 4
NCT01607853 (26) [back to overview]Change From Baseline in Scaling at Day 8
NCT01607853 (26) [back to overview]Change in Lesion Thickness Measured by Ultrasound From Baseline to Day 22.
NCT01607853 (26) [back to overview]Change in Skin Thickness - Echo-poor Band - Measured by Ultrasound From Baseline to Day 22
NCT01607853 (26) [back to overview]Change in Total Clinical Score at Day 11 Compared to Baseline
NCT01635062 (3) [back to overview]The Change in Circulating RAS Activity After Calcitriol/Placebo Therapy
NCT01635062 (3) [back to overview]Change in Urine Protein After Calcitriol/Placebo Therapy
NCT01635062 (3) [back to overview]Change in Renal Plasma Flow After Calcitriol/Placebo Therapy
NCT01689441 (3) [back to overview]Plasma Interleukin-6 (IL-6) Levels at 48 Hours
NCT01689441 (3) [back to overview]Plasma Cathelicidin (hCAP18) Protein Levels at 48 Hours
NCT01689441 (3) [back to overview]Urinary Neutrophil Gelatinase-associated Lipocalin (NGAL) / Creatinine Ratio at 48 Hours
NCT01694433 (2) [back to overview]Acne Severity as Assessed With the Investigator's Global Assessment (IGA)
NCT01694433 (2) [back to overview]Lesion Counts (Total, Inflammatory and Non-inflammatory)
NCT01707043 (2) [back to overview]Subjective Subject Preference Survey for the Second Treatment Session
NCT01707043 (2) [back to overview]Subjective Subject Preference Survey for the First Treatment Session
NCT01725113 (8) [back to overview]Amount of Active Vitamin D Analog Used Through Month 3 Post Calcitriol Initiation
NCT01725113 (8) [back to overview]Amount of Active Vitamin D Analog Used Through Month 3 Post Paricalcitol Initiation
NCT01725113 (8) [back to overview]Calcium Levels at Month 3 Post Calcitriol Treatment Initiation
NCT01725113 (8) [back to overview]Calcium Levels at Month 3 Post Paricalcitol Treatment Initiation
NCT01725113 (8) [back to overview]Phosphorus Levels at Month 3 Post Calcitriol Initiation
NCT01725113 (8) [back to overview]Phosphorus Levels at Month 3 Post Paricalcitol Initiation
NCT01725113 (8) [back to overview]PTH Levels at Month 3 Post Calcitriol Treatment Initiation
NCT01725113 (8) [back to overview]PTH Levels at Month 3 Post Paricalcitol Treatment Initiation
NCT01745133 (1) [back to overview]Physician Global Assessement
NCT01766440 (6) [back to overview]Tmax of Calcitriol Plasma Level
NCT01766440 (6) [back to overview]Cmax of Calcitriol Plasma Level
NCT01766440 (6) [back to overview]AUC (0-6h) of Calcitriol Plasma Level
NCT01766440 (6) [back to overview]Cmin of Calcitriol Plasma Level
NCT01766440 (6) [back to overview]AUC (0-9h) of Calcitriol Plasma Level
NCT01766440 (6) [back to overview]AUC (0-12h) of Calcitriol Plasma Level
NCT02061384 (1) [back to overview]Millions of Sperm Per Ejaculate
NCT02125279 (24) [back to overview]Change From Screening in Serum Phosphate Levels at Week 12
NCT02125279 (24) [back to overview]Change From Screening in Serum Phosphate Levels at Week 20
NCT02125279 (24) [back to overview]Change From Screening in Serum Phosphate Levels at Week 26
NCT02125279 (24) [back to overview]Change From Screening in Serum Phosphate Levels at Week 30 (Follow-up)
NCT02125279 (24) [back to overview]Change From Screening in Serum Phosphate Levels at Week 4
NCT02125279 (24) [back to overview]Change From Screening in Urine Calcium/Creatinine Ratio at Week 12
NCT02125279 (24) [back to overview]Change From Screening in Urine Calcium/Creatinine Ratio at Week 26
NCT02125279 (24) [back to overview]Change From Screening in Urine Calcium/Creatinine Ratio at Week 30 (Follow-up)
NCT02125279 (24) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT02125279 (24) [back to overview]Change From Baseline in Percent (%) Body Surface Area (BSA) at Each Visit
NCT02125279 (24) [back to overview]Change From Baseline in Pruritus Score at Each Visit
NCT02125279 (24) [back to overview]Number of Participants With Investigator's Global Assessment of Disease Severity (IGA) Score of 0 (Clear) or 1 (Almost Clear) at Each Visit
NCT02125279 (24) [back to overview]Change From Screening in Serum Albumin Levels at Week 4
NCT02125279 (24) [back to overview]Change From Screening in Serum Albumin Levels at Week 12
NCT02125279 (24) [back to overview]Change From Screening in Serum Albumin Levels at Week 20
NCT02125279 (24) [back to overview]Change From Screening in Serum Albumin Levels at Week 26
NCT02125279 (24) [back to overview]Change From Screening in Serum Albumin Levels at Week 30 (Follow-up)
NCT02125279 (24) [back to overview]Change From Screening in Serum Albumin Levels at Week 8
NCT02125279 (24) [back to overview]Change From Screening in Serum Parathyroid Hormone (PTH) Levels at Week 4
NCT02125279 (24) [back to overview]Change From Screening in Serum Parathyroid Hormone Levels at Week 12
NCT02125279 (24) [back to overview]Change From Screening in Serum Parathyroid Hormone Levels at Week 20
NCT02125279 (24) [back to overview]Change From Screening in Serum Parathyroid Hormone Levels at Week 26
NCT02125279 (24) [back to overview]Change From Screening in Serum Parathyroid Hormone Levels at Week 30 (Follow-up)
NCT02125279 (24) [back to overview]Change From Screening in Serum Parathyroid Hormone Levels at Week 8
NCT02186665 (1) [back to overview]Success of Investigator's Global Assessment (IGA)
NCT02193815 (9) [back to overview]Area Under the Curve (AUC) of Psoriatic Skin Thickness/EPB
NCT02193815 (9) [back to overview]Change From Baseline in Psoriatic Skin Thickness/Echo-Poor Band (EPB) for PF-06263276 4% Solution in Comparison to Corresponding Vehicle at Day 12
NCT02193815 (9) [back to overview]Change From Baseline in Psoriatic Skin Thickness/EPB at Day 8
NCT02193815 (9) [back to overview]Change From Baseline in Psoriatic Skin Thickness/EPB for PF-06263276 4% Solution in Comparison to Daivonex Solution at Day 12
NCT02193815 (9) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs): Specified Skin AEs
NCT02193815 (9) [back to overview]Number of Participants With Potentially Clinically Significant Vital Signs Findings
NCT02193815 (9) [back to overview]Global Clinical Assessment at Day 1, 8 and 12
NCT02193815 (9) [back to overview]Change From Baseline in Psoriatic Skin Thickness/EPB for Tofacitinib 2% Ointment in Comparison to Corresponding Vehicle at Day 12
NCT02193815 (9) [back to overview]Number of Participants With Laboratory Abnormalities Meeting the Criteria for Potential Clinical Concern
NCT02282813 (4) [back to overview]Number of Participants in the Intent to Treat Population With Normal Serum 25-hydroxyvitamin D at End of Treatment (EOT)
NCT02282813 (4) [back to overview]Number of Participants in the Per Protocol Population With Mean Reduction in Plasma Intact Parathyroid Hormone (iPTH) of >/= 30% From Baseline Values at End of Treatment (EOT)
NCT02282813 (4) [back to overview]Number of Participants in the Per Protocol Population With NormalSerum 25-hydroxyvitamin D at End of Treatment (EOT)
NCT02282813 (4) [back to overview]Number of Participants in the Intent to Treat Population With a Mean Reduction in Plasma Intact Parathyroid Hormone (iPTH) of >/= 30% From Baseline Values at End of Treatment (EOT)
NCT02962102 (7) [back to overview]Death Within 7 Days
NCT02962102 (7) [back to overview]Number of Participants Who Received Renal Replacement Therapy Within 7 Days
NCT02962102 (7) [back to overview]Number of Participants With New or Worsening Stage of AKI, Defined by KDIGO Guidelines
NCT02962102 (7) [back to overview]Peak Serum Creatinine (mg/dl)
NCT02962102 (7) [back to overview]28-day Mortality
NCT02962102 (7) [back to overview]ICU- and Hospital-free Days
NCT02962102 (7) [back to overview]Relative Average Change in Serum Creatinine From Day 0 to Days 1-7
NCT03261336 (1) [back to overview]Toxicity and Tolerability of Experimental Arm
NCT03469271 (1) [back to overview]Sniff Nasal Inspiratory Pressure (SNIP)
NCT04286529 (4) [back to overview]Insulin Level
NCT04286529 (4) [back to overview]Glucose Levels
NCT04286529 (4) [back to overview]Glucose Levels
NCT04286529 (4) [back to overview]C-Peptide Level

Number of Participants With Normal Serum Calcium Concentrations

Normal calcium concentration 8.2-10.6 mg/dL (NCT00001151)
Timeframe: 1 year average

Interventionparticipants (Number)
Group 16

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Serum 25-hydroxyvitamin D Level

Measurements were taken 1 hour before the morning dose of PTH or, calcitriol and calcium; UOM = ng/ml. Measurements were obtained on three successive days (three separate measures) semiannually at the NIH CC for each protocol subject. The average data are the average of these three semi-annual data points for each subject which are then averaged across all the semi-annual means for all subjects within each arm over the three years of study. (NCT00001304)
Timeframe: 3 years

Interventionng/ml (Mean)
Calcitriol and Calcium31
PTH 1-3428

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Serum Calcium Level

Measurements were taken 1 hour before the morning dose of PTH or, calcitriol and calcium; UOM = mmol/liter, normal range 2.05-2.5. Measurements were obtained on three successive days (three separate measures) semiannually at the NIH CC for each protocol subject. The average data are the average of these three semi-annual data points for each subject which are then averaged across all the semi-annual means for all subjects within each arm over the three years of study. (NCT00001304)
Timeframe: 3 years

Interventionmmol/liter (Mean)
Calcitriol and Calcium2
PTH 1-341.92

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Serum Magnesium Level

Measurements were taken 1 hour before the morning dose of PTH or, calcitriol and calcium; UOM = mmol/liter, normal range 0.65-1.05. Measurements were obtained on three successive days (three separate measures) semiannually at the NIH CC for each protocol subject. The average data are the average of these three semi-annual data points for each subject which are then averaged across all the semi-annual means for all subjects within each arm over the three years of study. (NCT00001304)
Timeframe: 3 years

Interventionmmol/liter (Mean)
Calcitriol and Calcium0.75
PTH 1-340.73

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Serum Phosphorus Level

Measurements were taken 1 hour before the morning dose of PTH or, calcitriol and calcium; UOM = mmol/liter, normal range 0.7-1.4. Measurements were obtained on three successive days (three separate measures) semiannually at the NIH CC for each protocol subject. The average data are the average of these three semi-annual data points for each subject which are then averaged across all the semi-annual means for all subjects within each arm over the three years of study. (NCT00001304)
Timeframe: 3 years

Interventionmmol/liter (Mean)
Calcitriol and Calcium4.5
PTH 1-344.6

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Urinary Creatinine Clearance

Measurements were taken 1 hour before the morning dose of PTH or, calcitriol and calcium; UOM = ml/min, normal range 90-125. Measurements were obtained on three successive days (three separate measures) semiannually at the NIH CC for each protocol subject. The average data are the average of these three semi-annual data points for each subject which are then averaged across all the semi-annual means for all subjects within each arm over the three years of study. (NCT00001304)
Timeframe: 3 years

Interventionml/min (Mean)
Calcitriol and Calcium84
PTH 1-3480

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Urine Calcium Excretion Level

Measurements were taken1 hour before the morning dose of PTH or, calcitriol and calcium; UOM = mmol/24 h, normal range 1.25-6.25. Measurements were obtained on three successive days (three separate measures) semiannually at the NIH CC for each protocol subject. The average data are the average of these three semi-annual data points for each subject which are then averaged across all the semi-annual means for all subjects within each arm over the three years of study. (NCT00001304)
Timeframe: 3 years

Interventionmmol/24 h (Mean)
Calcitriol and Calcium8.2
PTH 1-345.8

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Serum 1,25-hydroxyvitamin D Level

Measurements were taken 1 hour before the morning dose of PTH or, calcitriol and calcium; UOM = pg/ml. Measurements were obtained on three successive days (three separate measures) semiannually at the NIH CC for each protocol subject. The average data are the average of these three semi-annual data points for each subject which are then averaged across all the semi-annual means for all subjects within each arm over the three years of study. (NCT00001304)
Timeframe: 3 years

Interventionpg/ml (Mean)
Calcitriol and Calcium40
PTH 1-3443

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Number of Participants With Adverse Events, Graded According to NCI CTCAE v2.0

Number of Participants with Adverse Events, Graded According to NCI CTCAE v2.0 (NCT00084864)
Timeframe: Up to 30 days of the last administration of study procedure

,,,
InterventionParticipants (Count of Participants)
Grade 1Grade 2Grade 3
Arm 1131
Arm 2211
Arm 3210
Arm 4200

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Number and Frequency of Dose Limiting Toxicities (DLTs) With High-dose Calcitriol in Combination With Temozolomide

"Determine number and frequency of dose limiting toxicities (DLT) of high-dose calcitriol when administered with temozolomide in patients with metastatic melanoma for up to 12 cycles of therapy, where 1 cycle equals 28 days.~3 patients per dose cohort will be entered into the trial at doses of 0.2, 0.3, and 0.5 mcg/kg of calcitriol administered orally. If 1 patient experiences dose limiting toxicity (DLT) at any dose, that dose cohort will be expanded to a maximum of 6 patients. If 1 additional patient experiences DLT at that dose stratum, further dose escalation will cease and the dose cohort immediately preceding the dose cohort where the 2 experiences of DLT occurred will be considered the MTD. If no additional patients experience DLT, dose escalation to the next higher dose stratum will take place.~DLT is defined as National Cancer Institute Common Toxicity Criteria, version 3.0 grade 3 toxicity determined to be related to calcitriol." (NCT00301067)
Timeframe: From start of treatment, up to 12 cycles where 1 cycle equals 28 days

InterventionDLT (Number)
Cohort 1 - Temozolomide and Calcitriol0
Cohort 2 - Temozolomide and Calcitriol0
Cohort 3 - Temozolomide and Calcitriol0

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Overall Response Rate

"Overall Response Rate (ORR) is defined as percentage of patients who's best response to treatment is complete response plus those with partial response.~Complete Response (CR): Disappearance of all target lesions.~Partial Response (PR): At least a 30% decrease in the sum of the longest diameter (LD) of target lesions, taking as reference the baseline sum LD." (NCT00301067)
Timeframe: From the start of treatment, every 2 cycles where 1 cycle equals 28 days, for a maximum of 12 cycles

InterventionParticipants (Count of Participants)
Temozolomide and Calcitriol (Cohort 1-3+Expansion)2

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Overall Survival

Overall Survival (OS) will be measured from first day of treatment until death of any cause. Patients still alive at the last data cut off point will be censored. (NCT00301067)
Timeframe: From the first day of treatment until death from any cause, up to a maximum of 6 and half years

InterventionMonths (Median)
Temozolomide and Calcitriol (Cohort 1-3+Expansion)5.5

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Time to Progression

Time to progression (TTP) is measured from the start of treatment until the time of first documentation of disease progression. (NCT00301067)
Timeframe: From the start of treatment, until progressive disease, up to 12 months

InterventionMonths (Median)
Temozolomide and Calcitriol (Cohort 1-3+Expansion)1.81

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Number of Patients With Toxicity

"Toxicity will be assessed for each patient on a seven-day on/seven-day off temozolomide in combination with high-dose calcitriol for every 2 weeks for up to 12 cycles where 1 cycle equals 28 days. Toxicity will be assessed during treatment according to the National Cancer Institute's Common Toxicity Criteria for adverse events version 3.0 (CTCAE v3.0) and defined by any toxicity determined to be at least possibly related to either study drug (temozolomide or calcitriol).~In general adverse events (AEs) will be graded according to the following:~Grade 1 Mild AE Grade 2 Moderate AE Grade 3 Severe AE Grade 4 Life-threatening or disabling AE Grade 5 Death related to AE~Grade 3 and grade 4 toxicities where relatedness to either study drug could not be ruled out were collected and recorded only." (NCT00301067)
Timeframe: From the start of treatment and every 2 weeks for a maximum of 12 cycles, and 30 days post last treatment, where 1 cycle equals 28 days

,,,
Interventionparticipants (Number)
ThrombocytopeniaVascularNauseaVomitingLeukopeniaFatigueAnemiaLymphopeniaHemorrhageRashAnorexia
Cohort 1 - Temozolomide and Calcitriol11000000000
Cohort 2 - Temozolomide and Calcitriol00000000000
Cohort 3 - Temozolomide and Calcitriol00111000000
Expansion - Temozolomide and Calcitriol11001122111

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Overall Survival (OS) Stratified by Vitamin D-Receptor (VDR) Gene Polymorphisms

Investigate the relationship between vitamin D-receptor (VDR) gene polymorphisms in Taq1 and Fok1 (analyzed from baseline blood sample) and Overall Survival (OS). VDR gene analysis was completed using PCR-RFLP based assays. (NCT00301067)
Timeframe: at baseline and until death from any cause up to 6 and half years

InterventionMonths (Median)
VDR genotype (tt+/-ff)non tt+/-ff VDR genotype
Temozolomide and Calcitriol (Cohort 1-3+Expansion)3.87.4

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Trough Plasma Levels (Ctrough) of Calcitriol

Trough plasma levels (Ctrough) of calcitriol was reported. (NCT00419666)
Timeframe: Day 0 (Baseline), Day 14, Day 21, and Day 56

InterventionPicograms Per Millilitre (pg/mL) (Mean)
Day 0 (Baseline)Day 14Day 21Day 56
Calcitriol 3mcg/g65.0462.5361.8761.46

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Time at Which Maximum Concentration (Cmax) Occurred (Tmax)

Tmax is the time to reach maximum concentration and was reported for calcitriol. (NCT00419666)
Timeframe: Day 0 (Baseline), Day 21

Interventionhours (Median)
Day 0 (Baseline)Day 21
Calcitriol 3mcg/g4.003.97

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The Observed Peak Drug Concentration (Cmax) of Calcitriol

Cmax of calcitriol was reported. (NCT00419666)
Timeframe: Day 0 (Baseline), Day 21

Interventionpg/mL (Mean)
Day 0 (Baseline)Day 21
Calcitriol 3mcg/g75.7473.18

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Change From Baseline in Effect of Calcitriol Ointment on Calcium (Serum Calcium, Urinary (U) Calcium Random) and Phosphorus Homeostasis up to Day 56

Calcium homeostasis was analyzed with serum calcium albumin adjusted, serum calcium, urinary calcium/creatinine ratio, urinary (U) calcium random as parameters. Phosphorus homeostasis was analyzed with phosphorus as parameter. Change from baseline in the effect of calcitriol ointment on calcium (serum calcium, U calcium random) and phosphorus homeostasis up to Day 56 was reported. (NCT00419666)
Timeframe: From baseline (Day 0) up to Day 56

Interventionmilligrams per deciliter (Mg/dL) (Mean)
Serum CalciumUrinary (U) Calcium RandomPhosphorus
Calcitriol 3mcg/g0.081.000.20

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Area Under the Concentration-Time Curve From Pre-Application (T0) Through 9 Hours Post Dosing (AUC [0-9 Hours])

The AUC(0-9 hours) that is area under the plasma concentration-time curve from time 0 to 9 hours after dosing was reported. (NCT00419666)
Timeframe: 0 (predose) and 9 hours post dose on Day 0 (Baseline), Day 21

InterventionPicograms. hours per millilitre(pg.h/mL) (Mean)
Day 0 (Baseline)Day 21
Calcitriol 3mcg/g575.12549.29

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Area Under the Concentration-Time Curve From Pre-Application (T0) Through 12 Hours Post Dosing (AUC [0-12 Hours])

The AUC(0-12 hours) that is area under the plasma concentration-time curve from time 0 to 12 hours after dosing was reported. (NCT00419666)
Timeframe: 0 (predose) and 12 hours post dose on Day 0 (Baseline), Day 21

Interventionpg.h/mL (Mean)
Day 0 (Baseline)Day 21
Calcitriol 3mcg/g764.74737.74

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Number of Participants With Adverse Events

An adverse event (AE) was any unfavorable and unintended sign (including an abnormal laboratory finding assessed as clinically significant and different from the baseline visit), symptom, or disease temporally associated with the use of a medicinal (investigational) product, whether or not related to the medicinal (investigational) product. Number of participants with adverse events were reported. (NCT00419666)
Timeframe: From start of the study to Day 56

InterventionParticipants (Count of Participants)
Calcitriol 3mcg/g13

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Change From Baseline in Effect of Calcitriol Ointment on Calcium (Urinary Calcium/Creatinine Ratio) Homeostasis up to Day 56

Calcium homeostasis was analyzed with serum calcium albumin adjusted, serum calcium, urinary calcium/creatinine ratio, urinary (U) calcium random as parameters. Change from baseline in the effect of calcitriol ointment on calcium (urinary calcium/creatinine ratio) homeostasis up to Day 56 was reported. (NCT00419666)
Timeframe: From baseline (Day 0) up to Day 56

InterventionRatio (Mean)
Calcitriol 3mcg/g0.01

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Change From Baseline in Effect of Calcitriol Ointment on Calcium (Serum Calcium Albumin Adjusted) Homeostasis up to Day 56

Calcium homeostasis was analyzed with serum calcium albumin adjusted, serum calcium, urinary calcium/creatinine ratio, urinary (U) calcium random as parameters. Change from baseline in the effect of calcitriol ointment on calcium (serum calcium albumin adjusted) homeostasis up to Day 56 was reported. (NCT00419666)
Timeframe: From baseline (Day 0) up to Day 56

InterventionMillimoles Per Litre (mmol/L) (Mean)
Calcitriol 3mcg/g-0.01

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Fractional Absorption of Calcium

Fractional absorption of calcium (see citation for complete details) (NCT00427804)
Timeframe: 7 week

InterventionPercentage of absorption (Number)
Healthy Control71
Crohn's Disease115

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Objective Response (Complete or Partial Response)

Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR. (NCT00524589)
Timeframe: 1 year

Interventionpercentage of participants (Number)
Dexamethasone and Calcitriol0

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Corrected Serum Calcium Expression

Number of patients with corrected serum calcium levels between 11 mg/dL and 12 mg/dL detected on 1 or more occasions. (NCT00524589)
Timeframe: 1 year

InterventionParticipants (Count of Participants)
Dexamethasone and Calcitriol6

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Determine the Maximum Tolerated Dose (MTD)

Determine the maximum tolerated dose (MTD) of oral calcitriol daily x 3 consecutive days a week in combination with oral ketoconazole (400 mg thrice daily [TID]) + oral hydrocortisone (20 mg AM, 10 mg PM) (NCT00536991)
Timeframe: up to 11 years

Interventionmcg (Number)
Treatment (Calcitriol, Ketoconazole, Hydrocortisone)10

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Incidence of Toxicity Graded According to the National Cancer Institute CTC Version 3.0

Count of participants with serious adverse event. Please refer to the adverse event reporting for more detail. (NCT00536991)
Timeframe: Up to 11 years

InterventionParticipants (Count of Participants)
Phase I/II: Oral Calcitriol, Ketoconazole, Hydrocortisone14

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Objective Tumor Response, Assessed by RECIST

Judged by monthly physical exam and radiographic evaluation. Patients will be considered evaluable for tumor response if they have at least two post-baseline tumor assessments at least 4 weeks apart, received study medication for 8 weeks or if they have evidence of disease progression. Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR. (NCT00536991)
Timeframe: Up to 11 years

Interventionpercentage of participants (Number)
Phase I/II: Oral Calcitriol, Ketoconazole, Hydrocortisone24

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PSA Response Rate

Patients will be considered evaluable for PSA response if they have at least two post-baseline PSA measurements at least 4 weeks apart, or if they have other evidence of disease progression. A PSA response will be considered a PSA decline of at least 50% must be confirmed by a second PSA value four or more weeks later. The reference PSA for these declines should be a PSA measured within 2 weeks prior to the initiation of therapy. (NCT00536991)
Timeframe: Up to 11 years

Interventionpercentage of participants (Number)
Phase I/II: Oral Calcitriol, Ketoconazole, Hydrocortisone35

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Subjects With Controlled Disease According to the Investigator Assessment of the Face at Week 8

(NCT00640822)
Timeframe: Week 8

InterventionParticipants (Number)
Calcipotriol Plus Hydrocortisone Ointment183
Tacalcitol Ointment147
Calcipotriol Plus Hydrocortisone Ointment Vehicle37

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Tolerability Assessment - Stinging/ Burning

(NCT00658788)
Timeframe: Baseline, 2, 4, 8 and 12 weeks

,,,,
Interventionparticipants (Number)
NoneMildModerateSevere
Baseline200443130
Week 122002483
Week 223242131
Week 42453441
Week 823418193

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Tolerability Assessment - Telangiectasias

(NCT00658788)
Timeframe: Baseline, 2, 4, 8 and 12 weeks

,,,,
Interventionparticipants (Number)
NoneMildModerateSevere
Baseline303101
Week 12230500
Week 2284400
Week 4283200
Week 8273100

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Overall Disease Severity Success (ODS)

Success was defined as a one-grade improvement in ODS from baseline. (NCT00658788)
Timeframe: 8 and 12 weeks

Interventionpercentage of participants (Number)
Week 8Week 12
Sequential Treatment Regimen100.084.1

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Percent Change From Baseline in Body Surface Area (% BSA) Affected

(NCT00658788)
Timeframe: 2, 4, 8 and 12 weeks

InterventionPercent Change from Baseline (Mean)
Week 220.1
Week 443.1
Week 846.6
Week 1246.2

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Global Improvement Score

(NCT00658788)
Timeframe: 2, 4, 8 and 12 weeks

,,,
Interventionparticipants (Number)
-1:Symptoms0:No Change1:Minimal Improvement2:Definite Improvement3:Considerable Improvement4:Clearing
Week 1201319495831
Week 2149539311
Week 4024269642
Week 801012437728

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Overall Disease Severity

(NCT00658788)
Timeframe: 2, 4, 8 and 12 weeks

,,,
Interventionparticipants (Number)
ClearAlmost ClearMildModerateSevere/Very Severe
Week 12114570440
Week 205383313
Week 4510053120
Week 896088130

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Signs of Psoriasis - Erythema

(NCT00658788)
Timeframe: 2, 4, 8 and 12 weeks

,,,
Interventionparticipants (Number)
ClearAlmost ClearMildModerateSevere/Very Severe
Week 12124160534
Week 204682357
Week 498157230
Week 8135370322

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Signs of Psoriasis - Plaque Elevation

(NCT00658788)
Timeframe: 2, 4, 8 and 12 weeks

,,,
Interventionparticipants (Number)
ClearAlmost ClearMildModerateSevere/Very Severe
Week 12244561391
Week 2226954241
Week 446783691
Week 8355068170

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Signs of Psoriasis - Scaling

(NCT00658788)
Timeframe: 2, 4, 8 and 12 weeks

,,,
Interventionparticipants (Number)
ClearAlmost ClearMildModerateSevere/Very Severe
Week 12315654263
Week 2256163194
Week 441833790
Week 836537191

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Tolerability Assessment - Folliculitis

(NCT00658788)
Timeframe: Baseline, 2, 4, 8 and 12 weeks

,,,,
Interventionparticipants (Number)
AbsentPresent
Baseline3032
Week 122323
Week 22862
Week 427411
Week 82713

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Tolerability Assessment - Pruritus

(NCT00658788)
Timeframe: Baseline, 2, 4, 8 and 12 weeks

,,,,
Interventionparticipants (Number)
NoneMildModerateSevere
Baseline74848463
Week 12128653210
Week 217991135
Week 42205690
Week 817266315

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Tolerability Assessment - Skin Atrophy

(NCT00658788)
Timeframe: Baseline, 2, 4, 8 and 12 weeks

,,,,
Interventionparticipants (Number)
AbsentPresent
Baseline3032
Week 122332
Week 22862
Week 42787
Week 82704

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Number of Participants With Adverse Events

The occurrence of adverse events was considered a secondary endpoint in this study. For details on adverse events that occurred prior to study termination, refer to the safety section below. (NCT00664430)
Timeframe: Up to 1 year

InterventionParticipants (Number)
Calcitriol Challenge Followed by Paricalcitol3

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Grade III-IV Toxicities or Any Grade II Toxicities Lasting More Than 2 Weeks

"Number of participants with Adverse Events, Grade II lasting more than two weeks or Grade III or higher, graded according to CTEP Version 4 of the NCI Common Terminology Criteria for Adverse Events (CTCAE) will be utilized for AE reporting.~CTEP Version 4 of the CTCAE is identified and located at:~http://ctep.cancer.gov/protocolDevelopment/electronic_applications/ctc.htm." (NCT00690924)
Timeframe: 3 months

Interventionparticipants (Number)
IIIIIIVV
Calcitriol1000

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"Participants With Controlled Disease According to the IGA of Disease Severity of the Face at Week 4 (Visit 4) in the Double-blind Phase"

"The assessment of the disease severity of the face was made using the 6-category scale below.~Clear Almost clear Mild Moderate Severe Very severe~The assessment was made considering the condition of psoriasis vulgaris of the face at the time of the evaluation, not in relation to the condition at a previous visit.~For subjects with a baseline severity of moderate or worse - controlled disease of the face was defined as clear or almost clear according to the IGA of disease severity of the face.~For subjects with a baseline severity of mild - controlled disease of the face was defined as clear according to the IGA of disease severity of the face." (NCT00691002)
Timeframe: At Week 4

InterventionParticipants (Count of Participants)
LEO 80190101
Calcipotriol66
Hydrocortisone61
LEO 80190 Vehicle14

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"Participants With Success According to Total Sign Score (TSS) of the Face at Week 8 (Visit 6) in the Double-blind Phase"

"Success was defined as a TSS score of 0 or 1.~For each clinical sign, a single score, reflecting the average severity of all psoriatic lesions on the face was determined according to the scale below:~Redness 0 = none (no erythema) 1 = mild (faint erythema, pink to very light red) 2 = moderate (definite light red erythema) 3 = severe (dark red erythema) 4 = very severe (very dark red erythema) Thickness 0 = none (no plaque elevation) 1 = mild (slight, barely perceptible elevation) 2 = moderate (definite elevation but not thick) 3 = severe (definite elevation, thick plaque with sharp edge) 4 = very severe (very thick plaque with sharp edge) Scaliness 0 = none (no scaling) 1 = mild (sparse, fine-scale lesions, only partially covered) 2 = moderate (coarser scales, most of lesions covered) 3 = severe (entire lesion covered with coarse scales) 4 = very severe (very thick coarse scales, possibly fissured)~The sum of the three scores constituted a TSS ranging from 0 to 12" (NCT00691002)
Timeframe: At Week 8 (end of treatment for double-blind phase)

InterventionParticipants (Count of Participants)
LEO 80190171
Calcipotriol136
Hydrocortisone131
LEO 80190 Vehicle42

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"Participants With Success According to Total Sign Score of the Intertriginous Areas at Week 8 (Visit 6) in the Double-blind Phase"

"The severity of the subject's psoriasis vulgaris on the intertriginous areas was evaluated in terms of the three clinical signs: redness, thickness and scaliness. All the defined intertriginous areas were rated separately using the same scale as for the investigator's assessment of clinical signs (redness, thickness and scaliness) of the face.~For each clinical sign, a single score, reflecting the average severity of all psoriatic lesions on the face was determined according to the scale below:~Redness 0 = none~= mild~= moderate~= severe~= very severe~Thickness 0 = none~= mild~= moderate~= severe~= very severe~Scaliness 0 = none~= mild~= moderate~= severe~= very severe~A mean score was calculated for each sign (redness, thickness and scaliness) based on scores of all the defined intertriginous areas with psoriasis at baseline and the sum of these mean scores constituted the TSS.~Success was defined as a TSS score of 0 or 1." (NCT00691002)
Timeframe: At Week 8 (end of treatment for double-blind phase)

InterventionParticipants (Count of Participants)
LEO 8019082
Calcipotriol81
Hydrocortisone59
LEO 80190 Vehicle15

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"Participants With Controlled Disease According to the IGA of Disease Severity of the Intertriginous Areas at Week 8 (Visit 6) in the Double-blind Phase"

"The (sub)investigator made an assessment of the disease severity of the intertriginous areas using the 6-category scale below.~Clear, Almost clear, Mild, Moderate, Severe, Very severe The assessment was made considering the condition of psoriasis vulgaris of the intertrigi-nous areas at the time of the evaluation, not in relation to the condition at a previous visit.~For subjects with a baseline severity of moderate or worse - controlled disease of the intertriginous areas was defined as clear or almost clear according to the IGA of disease severity of the intertriginous areas.~For subjects with a baseline severity of mild - controlled disease of the intertriginous areas was defined as clear according to the IGA of disease severity of the intertriginous areas." (NCT00691002)
Timeframe: At Week 8 (end of treatment for double-blind phase)

InterventionParticipants (Count of Participants)
LEO 8019080
Calcipotriol55
Hydrocortisone48
LEO 80190 Vehicle14

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"Participants With Controlled Disease According to the Investigator's Global Assessment(IGA) of Disease Severity of the Face at Week 8 (Visit 6) in the Double-blind Phase"

"The (sub) investigator made an assessment of the disease severity of the face using the 6-category scale below.~Clear, Almost clear, Mild, Moderate, Severe, Very severe~The assessment was made considering the condition of psoriasis vulgaris of the face at the time of the evaluation, not in relation to the condition at a previous visit.~For subjects with a baseline (Visit 1) severity of moderate or worse - controlled disease of the face was defined as clear or almost clear according to the IGA of disease severity of the face.~For subjects with a baseline (Visit 1) severity of mild - controlled disease of the face was defined as clear according to the IGA of disease severity of the face." (NCT00691002)
Timeframe: At Week 8 (end of treatment for double-blind phase)

InterventionParticipants (Count of Participants)
LEO 80190158
Calcipotriol135
Hydrocortisone115
LEO 80190 Vehicle41

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Coronary Artery (CAC) Score Progression

"coronary artery (CAC) score difference between baseline and followup CT scans. It was measured in Agatston units. These are units of amount of calcification in the blood vessels so it's a continuous variable. The amount of calcium was quantified with the Agatston scoring method. Calcium scores were adjusted with a standard calcium phantom that was scanned along with the participant. The phantom contained known calcium density bars and provided a way to calibrate the x-ray attenuation level.~Participants scoring CAC >400 are considered to be at risk for having at least one coronary lesion." (NCT00752102)
Timeframe: 48 weeks

InterventionAgatston units (Mean)
Calcitriol74.38
Paricalcitol106.32

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Number of Participants With Adverse Events (AEs)

AE was any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product and which does not necessarily had a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory value), symptom, or disease temporally associated with the use of a medicinal (investigational) product, whether or not related to the medicinal (investigational) product. (NCT00763555)
Timeframe: up to Week 8

InterventionParticipants (Count of Participants)
Calcitriol 3 mcg/g Spray11
Calcitriol Vehicle9

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Percentage of Participants With Success Rate 2 (SR2) at Week 8

"Success Rate 2 was defined as percentage of participants who achieved clear or almost clear on GSS at Week 8. GSS is a 5-point scale which ranges from 0-4, where 0 = clear, 1 = almost clear, 2 = mild, 3 = moderate, 4 = severe, higher score indicated higher severity. All missing values were imputed by last observation carried forward (LOCF)." (NCT00763555)
Timeframe: Week 8

Interventionpercentage of participants (Number)
Calcitriol 3 mcg/g Spray4.5
Calcitriol Vehicle0.0

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Change From Baseline in Blood Chemistry: Alkaline Phosphatase, Aspartate Aminotransferase (AST) and Alanine Aminotransferase (ALT)

Change from baseline in Blood Chemistry: Alkaline Phosphatase, AST and ALT were reported. (NCT00763555)
Timeframe: Baseline, Week 8

,
Interventioninternational units per liter (IU/L) (Mean)
Alkaline PhosphataseASTALT
Calcitriol 3 mcg/g Spray0.581.420.72
Calcitriol Vehicle-1.03-0.35-1.75

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Change From Baseline in Blood Chemistry: Bilirubin Direct, Bilirubin Total, Blood Urea Nitrogen (BUN) and Creatinine

Change from baseline in Blood Chemistry: Bilirubin Direct, Bilirubin Total, BUN and Creatinine were reported. (NCT00763555)
Timeframe: Baseline, Week 8

,
Interventionmg/dL (Mean)
Bilirubin DirectBilirubin TotalBUNCreatinine
Calcitriol 3 mcg/g Spray-0.020.010.65-0.01
Calcitriol Vehicle-0.030.030.550.03

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Change From Baseline in Vital Sign Parameter: Systolic Blood Pressure and Diastolic Blood Pressure

Change from baseline in vital sign parameter: Systolic Blood Pressure and Diastolic Blood Pressure was reported. (NCT00763555)
Timeframe: Baseline, Week 8

,
Interventionmillimeter of mercury (mmHg) (Mean)
Systolic Blood PressureDiastolic Blood Pressure
Calcitriol 3 mcg/g Spray0.70.2
Calcitriol Vehicle-1.4-1.0

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Percentage of Participants With a Local Tolerability Score Worse Than Baseline Score

Local tolerability skin assessments were performed by the investigator and based on 5-point scale which ranges from 0 to 4. 0 = none (no evidence of local intolerance); 1=mild (minimal erythema and/or edema, slight glazed appearance); 2 = moderate (definite erythema and/or edema with peeling and/or cracking but needs no adaptation of posology); 3 = severe (erythema, edema glazing with fissures, few vesicles or papules) and 4 = very severe (strong reaction spreading beyond the treated area, bullous reaction, erosions). Higher grades indicated worsening of condition. Percentage of participants with increase in score by Week 8 from baseline has been presented here, where the row titles indicate participant's new scores by Week 8. (NCT00763555)
Timeframe: up to Week 8

,
Interventionpercentage of participants (Number)
1 = mild2 = moderate3 = severe4 = very severe
Calcitriol 3 mcg/g Spray4.52.32.32.3
Calcitriol Vehicle7.00.04.72.3

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Change From Baseline in Vital Sign Parameter: Heart Rate

Change from baseline in vital sign parameter: heart rate was reported. (NCT00763555)
Timeframe: Baseline, Week 8

Interventionbeats per minute (Mean)
Calcitriol 3 mcg/g Spray3.1
Calcitriol Vehicle1.4

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Percentage of Participants With at Least 1-Grade Improvement From Baseline in Erythema, Scaling and Plaque Elevation

Erythema (abnormal redness of skin) score is a 5-point scale: 0=None (No detectable erythema. Skin of normal color); 1=Mild (Slight pinkness present); 2=Moderate (Definite redness, easily recognized); 3=Severe (Intense redness) and 4=Severe (Very Intense redness). Scaling (shedding of stratum corneum) score is a 5- point scale: 0=None (No shedding); 1=Mild (Barely perceptible shedding, noticeable only on light scratching or rubbing); 2=Moderate (Obvious but not profuse shedding); 3=Severe (heavy scale production) and 4=Very severe (very thick scales). Plaque elevation (abnormal thickness of psoriasis lesion) score was a 5- point scale: 0=None (Normal skin thickness. No elevation of skin); 1=Mild (Barely perceptible elevation (by touching) of psoriasis plaques); 2=Moderate (Obvious elevation above normal skin level; moderate thickening); 3=Severe (definite thick elevation above normal skin level) and 4=Severe (Very thick elevation). (NCT00763555)
Timeframe: Baseline, Week 8

,
Interventionpercentage of participants (Number)
ErythemaScalingPlaque elevation
Calcitriol 3 mcg/g Spray38.640.934.1
Calcitriol Vehicle25.036.436.4

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Percentage of Participants With Success Rate 1 (SR1) at Week 8

Success Rate 1 was defined as percentage of participants who achieved at least 2-grade improvement from Baseline on Global Severity Score (GSS) at Week 8. GSS is a 5-point scale which ranges from 0-4, where 0 = clear, 1 = almost clear, 2 = mild, 3 = moderate, 4 = severe, higher score indicated higher severity. All missing values were imputed by last observation carried forward (LOCF). (NCT00763555)
Timeframe: Week 8

Interventionpercentage of participants (Number)
Calcitriol 3 mcg/g Spray4.5
Calcitriol Vehicle0.0

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Change From Baseline in Calcitriol Plasma Levels

Change from baseline in calcitriol plasma levels were reported. (NCT00763555)
Timeframe: Baseline, Week 8

Interventionpicograms per milliliter (pg/mL) (Mean)
Calcitriol 3 mcg/g Spray-2.89
Calcitriol Vehicle-8.82

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Change From Baseline in Dermatologic Sum Score (DSS) at Week 8

DSS is the sum of all the individual score of evaluated target lesion that includes plaque elevation (abnormal thickness of the psoriasis lesion), erythema (abnormal redness of the skin), and scaling (shedding of the stratum corneum). Each individual parameters evaluated the affected area by using a 5-point scale ranging from 0 to 4, that is, 0 = None; 1 = Mild; 2 = Moderate; 3 = Severe and 4 =Very severe, where higher score indicated worst condition. All missing values were imputed by last observation carried forward (LOCF). The total score of each parameter ranges from 0-12, where higher score indicated worst condition. (NCT00763555)
Timeframe: Baseline, Week 8

Interventionscore on a scale (Mean)
Calcitriol 3 mcg/g Spray-1.2
Calcitriol Vehicle-1.0

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Change From Baseline in Serum Calcium Homeostasis Parameter: Albumin

Change from baseline in serum calcium homeostasis parameter (Albumin) were reported. (NCT00763555)
Timeframe: Baseline, Week 8

Interventiongrams per deciliter (g/dL) (Mean)
Calcitriol 3 mcg/g Spray-0.16
Calcitriol Vehicle-0.08

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Change From Baseline in Serum Calcium Homeostasis Parameter: Albumin-adjusted Calcium

Change from baseline in serum calcium homeostasis parameter (Albumin-adjusted calcium) were reported. (NCT00763555)
Timeframe: Baseline, Week 8

Interventionmilligrams per deciliter (mg/dL) (Mean)
Calcitriol 3 mcg/g Spray0.07
Calcitriol Vehicle0.03

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Change From Baseline in Serum Calcium Homeostasis Parameter: Calcium

Change from baseline in serum calcium homeostasis parameter (Calcium) were reported. (NCT00763555)
Timeframe: Baseline, Week 8

Interventionmg/dL (Mean)
Calcitriol 3 mcg/g Spray-0.09
Calcitriol Vehicle-0.05

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Change From Baseline in Serum Calcium Homeostasis Parameter: Parathyroid Hormone (PTH) Intact

Change from baseline in serum calcium homeostasis parameter (PTH intact) were reported. (NCT00763555)
Timeframe: Baseline, Week 8

Interventionpg/mL (Mean)
Calcitriol 3 mcg/g Spray7.16
Calcitriol Vehicle5.15

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Change From Baseline in Serum Calcium Homeostasis Parameter: Phosphorus

Change from baseline in serum calcium homeostasis parameter (Phosphorus) were reported. (NCT00763555)
Timeframe: Baseline, Week 8

Interventionmg/dL (Mean)
Calcitriol 3 mcg/g Spray-0.07
Calcitriol Vehicle0.02

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Number of Participants That Experience Grade 3 or Greater Neutropenia

The second primary objective was to characterize the toxicity and response of patients treated with a combination of calcitriol, cisplatin and docetaxel. Toxicity was assessed, in part, by noting the number of participants that experience grade 3 or greater neutropenia in each phase of the trial. Toxicities were recorded using NCI CTCAE (Common Terminology Criteria for Adverse Events) version 3.0 and were followed for 30 days after the date of withdrawal from study drug. (NCT00794547)
Timeframe: 30 days after last dose

Interventionparticipants (Number)
# of Phase 1 Participants w/ Grade 3+ Neutropenia# of Phase 2 Participants w/ Grade 3+ Neutropenia
Calcitriol + Cisplatin + Docetaxel89

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Mean AUC 1,25-D3 Concentration at 12 and 24 Hours

The mean AUC (area under the curve) concentrations of 1,25-D3 from 0-12 hours and 0-24 hours will be calculated. (NCT00794547)
Timeframe: 12 and 24 hours post dose

Interventionh*ng/mL (Mean)
AUC 0-12 HoursAUC 0-24 Hours
Calcitriol + Cisplatin + Docetaxel15.9531.74

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MTD of Intravenous Calcitriol When Administered Prior to Fixed Dose Cisplatin 75mg/m2 and Docetaxel 75 mg/m2, Every 3 Weeks in Patients With Advanced Non-small Cell Lung Cancer (NSCLC)

The primary objective was to determine the Maximum Tolerated Dose (MTD) of intravenous calcitriol when administered prior to fixed dose cisplatin 75mg/m2 and docetaxel 75 mg/m2, every 3 weeks in patients with advanced non-small cell lung cancer (NSCLC). Accrual duration for the study is 5 years. (NCT00794547)
Timeframe: 5 years

Interventionmcg/m^2 (Number)
Calcitriol + Cisplatin + Docetaxel60

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Median Time to Progression

The second primary objective was to characterize the toxicity and response of patients treated with a combination of calcitriol, cisplatin and docetaxel. To assess the response, median time to progression was determined. Progression was defined as at least a 20% increase in the sum of the longest diameter of target lesions, taking as reference the smallest sum longest diameter recorded since the treatment started or the appearance of one or more new lesions. (NCT00794547)
Timeframe: 5 years

Interventionmonths (Median)
Calcitriol + Cisplatin + Docetaxel5.8

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Median Overall Survival

The second primary objective was to characterize the toxicity and response of patients treated with a combination of calcitriol, cisplatin and docetaxel. To assess the response, overall survival was determined. (NCT00794547)
Timeframe: 5 years

Interventionmonths (Median)
Calcitriol + Cisplatin + Docetaxel8.7

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Confirmed Hypercalcemia

Serum Calcium 10.5 mg/dL or higher, confirmed by repeat measurement. (NCT00823303)
Timeframe: 24 week treatment period

Interventionparticipants (Number)
Paricalcitol3
Calcitriol1

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The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Diprosalic Ointment

The Total Clinical Score is the sum of three psoriasis scores (redness, thickness, and scaliness) and will range from 0 (best) to 9 (worst) (NCT00845481)
Timeframe: Baseline and 3 weeks

InterventionScores on a scale (Mean)
Patients Treated With Diprosalic Ointment-4.50

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The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Betnovat® Ointment

The Total Clinical Score is the sum of three psoriasis scores (redness, thickness, and scaliness) and will range from 0 (best) to 9 (worst) (NCT00845481)
Timeframe: Baseline and 3 weeks

InterventionScores on a scale (Mean)
Patients Treated With Betnovat® Ointment-3.33

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The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Elocon Ointment

The Total Clinical Score is the sum of three psoriasis scores (redness, thickness, and scaliness) and will range from 0 (best) to 9 (worst) (NCT00845481)
Timeframe: Baseline and 3 weeks

InterventionScores on a scale (Mean)
Patients Treated With Elocon Ointment-4.50

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The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Dermovat Ointment

The Total Clinical Score is the sum of three psoriasis scores (redness, thickness, and scaliness) and will range from 0 (best) to 9 (worst) (NCT00845481)
Timeframe: Baseline and 3 weeks

InterventionScores on a scale (Mean)
Patients Treated With Dermovat Ointment-5.71

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The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Daivobet® Ointment

The Total Clinical Score is the sum of three psoriasis scores (redness, thickness, and scaliness) and will range from 0 (best) to 9 (worst) (NCT00845481)
Timeframe: Baseline and 3 weeks

InterventionScores on a scale (Mean)
Patients Treated With Daivobet® Ointment-5.15

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The Absolute Change in Total Clinical Score (TCS) at End of Treatment Compared to Baseline for Daivobet Ointment Vehicle

The Total Clinical Score is the sum of three psoriasis scores (redness, thickness, and scaliness) and will range from 0 (best) to 9 (worst) (NCT00845481)
Timeframe: Baseline and 3 weeks

InterventionScores on a scale (Mean)
Patients Treated With Daivobet® Ointment Vehicle-1.91

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Body Mass Index (Exercise)

"Body Mass Index (BMI) - (Exercise Comparison)~Measure Description: Body Mass Index (BMI) is a person's weight in kilograms divided by the square of height in meters. Values below 18.5 represent Underweight, 18.5 to 24.9 represent Normal or Healthy Weight, 25.0 to 29.9 represent Overweight and 30.0 and above represent Obese." (NCT00904033)
Timeframe: Week 12

Interventionkg/m^2 (Mean)
No Exercise30.0
Exercise30.2

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Bone Formation (Calcitriol)

"Bone Formation using Serum BSAP (Calcitriol comparison)~The Bone-Specific Alkaline Phosphatase (BSAP) assay provides a general index of bone formation and a specific index of total osteoblast activity. BSAP and osteocalcin are the most effective markers of bone formation and are particularly useful for monitoring bone formation therapies and antiresorptive therapies." (NCT00904033)
Timeframe: Week 12

Interventionng/ml (Least Squares Mean)
No Calcitriol12.0
Calcitriol16.3

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Bone Formation (Exercise)

"Bone Formation using Serum BSAP (Exercise comparison)~The Bone-Specific Alkaline Phosphatase (BSAP) assay provides a general index of bone formation and a specific index of total osteoblast activity. BSAP and osteocalcin are the most effective markers of bone formation and are particularly useful for monitoring bone formation therapies and antiresorptive therapies." (NCT00904033)
Timeframe: Week 12

Interventionng/ml (Least Squares Mean)
No Exercise13.8
Exercise14.7

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Bone Resorption (Calcitriol)

"Bone Resorption using Serum NTx (Calcitriol comparison)~Serum NTx level is used to aid in predicting skeletal response (bone mineral density) to antiresorptive therapy and in monitoring bone resorption changes following initiation of antiresorptive therapy. Elevated levels of serum NTx indicate elevated bone resorption. Elevated bone resorption is the primary cause of agerelated bone loss and that low bone mass often results in osteopenia and is the major cause of osteoporosis. The measurement range is in nanoMoles (nm) Bone Collagen Equivalents (BCE)." (NCT00904033)
Timeframe: Week 12

Interventionnm BCE (Least Squares Mean)
No Calcitriol12.5
Calcitriol15.0

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Bone Resorption (Exercise)

"Bone Resorption using Serum NTx (Exercise comparison)~Serum NTx level is used to aid in predicting skeletal response (bone mineral density) to antiresorptive therapy and in monitoring bone resorption changes following initiation of antiresorptive therapy. Elevated levels of serum NTx indicate elevated bone resorption. Elevated bone resorption is the primary cause of agerelated bone loss and that low bone mass often results in osteopenia and is the major cause of osteoporosis. The measurement range is in nanoMoles (NM) Bone Collagen Equivalents (BCE)." (NCT00904033)
Timeframe: Week 12

Interventionnm BCE (Least Squares Mean)
No Exercise13.8
Exercise14.7

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Handgrip (kg) Strength - (Exercise)

"Handgrip (kg) Strength (Exercise comparison)~Hand grip strength can be quantified by measuring the amount of static force that the hand can squeeze around a dynamometer. It is typically measured in kilograms or pounds and varies by sex and age. Normative data for females is AGE 35-39 --> 20.3-34.1kg; AGE 40-44 --> 18.9-32.7kg; AGE 45-49 --> 18.6-32.4kg; AGE 50-54 --> 18.1-31.9kg; AGE 55-59 --> 17.7-31.5kg; AGE 60-64 --> 17.2-31.0kg; AGE 65-69 --> 15.4-27.2kg; AGE 70-99 --> 14.7-24.5kg. Values less than the normal range are considered weak strength. Values greater than the normal range are considered strong strength." (NCT00904033)
Timeframe: Week 12

Interventionkg (Mean)
No Exercise26.6
Exercise27.8

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Handgrip (kg) Strength - (Calcitriol)

"Handgrip (kg) Strength - (Calcitriol comparison)~Hand grip strength can be quantified by measuring the amount of static force that the hand can squeeze around a dynamometer. It is typically measured in kilograms or pounds and varies by sex and age. Normative data for females is AGE 35-39 --> 20.3-34.1kg; AGE 40-44 --> 18.9-32.7kg; AGE 45-49 --> 18.6-32.4kg; AGE 50-54 --> 18.1-31.9kg; AGE 55-59 --> 17.7-31.5kg; AGE 60-64 --> 17.2-31.0kg; AGE 65-69 --> 15.4-27.2kg; AGE 70-99 --> 14.7-24.5kg. Values less than the normal range are considered weak strength. Values greater than the normal range are considered strong strength." (NCT00904033)
Timeframe: Week 12

Interventionkg (Mean)
No Calcitriol27.4
Calcitriol27.1

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Body Mass Index (Calcitriol)

"Body Mass Index(BMI) - (Calcitriol comparison)~Measure Description: Body Mass Index (BMI) is a person's weight in kilograms divided by the square of height in meters. Values below 18.5 represent Underweight, 18.5 to 24.9 represent Normal or Healthy Weight, 25.0 to 29.9 represent Overweight and 30.0 and above represent Obese." (NCT00904033)
Timeframe: Week 12

Interventionkg/m^2 (Mean)
No Calcitriol30.1
Calcitriol30.1

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Change in Total Modified PASI Score at Week 4 Compared to Baseline

Modified psoriasis severity index measures erythema, induration, and scaling each measured from 0-4, with a maximum summed score of 12. A higher score means greater psoriasis severity and a lower score means lower psoriasis severity. (NCT00924950)
Timeframe: 4 weeks

InterventionUnits on a scale (Mean)
Taclonex Ointment Occluded With Hydrogel Patch0.86
Taclonex Alone2.2

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Time of Maximum Plasma Concentration (Tmax) for Exogenous Calcitriol

This shows the effect that lanthanum carbonate or sevelamer carbonate has on the pharmacokinetics of oral calcitriol. Exogenous calcitriol was the difference between total calcitriol value and the baseline exogenous calcitriol value at each sampling timepoint. (NCT00925704)
Timeframe: pre-dose, 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 36, and 48 hours post calcitriol dose

Interventionhours (Median)
Calcitriol (Lanthanum Carbonate)1.27
Calcitriol (Sevelamer Carbonate)0.500

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Maximum Plasma Concentration (Cmax) for Exogenous Calcitriol

This shows the effect that lanthanum carbonate or sevelamer carbonate has on the pharmacokinetics of oral calcitriol. Exogenous calcitriol was the difference between total calcitriol value and the baseline exogenous calcitriol value at each sampling timepoint. (NCT00925704)
Timeframe: pre-dose, 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 36, and 48 hours post calcitriol dose

Interventionpg/ml (Least Squares Mean)
Calcitriol (Lanthanum Carbonate)-2.74
Calcitriol (Sevelamer Carbonate)-9.62

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Area Under the Serum Concentration-time Curve (AUC 0-48) for Exogenous Calcitriol

This shows the effect that lanthanum carbonate or sevelamer carbonate has on the pharmacokinetics of oral calcitriol. Exogenous calcitriol was the difference between total calcitriol value and the baseline exogenous calcitriol value at each sampling timepoint. (NCT00925704)
Timeframe: pre-dose, 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 36, and 48 hours post calcitriol dose

Interventionpg*h/ml (Least Squares Mean)
Calcitriol (Lanthanum Carbonate)111
Calcitriol (Sevelamer Carbonate)-181

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Change in GM-CSF

Change in GM-CSF stimulatory cytokine levels within tumor tissue. (NCT00953849)
Timeframe: baseline and 3 weeks

Interventionpg/100 gm protein (Mean)
Arm 1: Celecoxib3.8
Arm 2: Calcitriol8.1
Arm 3: Celecoxib Plus Calcitriol14.3
Arm 4: No Treatment3.2

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Change in IFN-gamma Levels

Change in IFN-gamma stimulatory cytokine levels within tumor tissue. (NCT00953849)
Timeframe: baseline and 3 weeks

Interventionpg/100 gm protein (Mean)
Arm 1: Celecoxib1.9
Arm 2: Calcitriol2.8
Arm 3: Celecoxib Plus Calcitriol6.3
Arm 4: No Treatment2.0

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Change in IL-2 Levels

Change in IL-2 stimulatory cytokine levels within tumor tissue. (NCT00953849)
Timeframe: baseline and 3 weeks

Interventionpg/100 gm protein (Mean)
Arm 1: Celecoxib1.8
Arm 2: Calcitriol4.0
Arm 3: Celecoxib Plus Calcitriol7.9
Arm 4: No Treatment2.1

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Change in IL-6 Levels.

Change in levels of immune inhibitory/inflammatory mediator IL-6 in tumor tissue. (NCT00953849)
Timeframe: baseline and 3 weeks

Interventionpg/100 gm protein (Mean)
Arm 1: Celecoxib39
Arm 2: Calcitriol46
Arm 3: Celecoxib Plus Calcitriol29
Arm 4: No Treatment132

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Median Percent (%) Change From Baseline in % Treatable BSA (Body Surface Area) From Baseline to Week 4

Median percent (%) change from baseline in % treatable BSA (Body Surface Area) from Baseline to Week 4 (NCT00988637)
Timeframe: Baseline to Week 4

InterventionPercent change (Median)
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)-33.3
Clobex® Spray (Morning) and Vectical® Ointment (Evening)-50.0

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Mean Change From Baseline Scores for the Koo-Menter Psoriasis Index 12-item Quality of Life Questionnaire (PQOL-12) From Baseline to Week 4

Mean change from baseline scores for the Koo-Menter Psoriasis Index 12-item Quality of Life Questionnaire (PQOL-12) from Baseline to Week 4. The Koo-Menter Psoriasis Index is a questionnaire with 12 questions that can be used to assess the effect that psoriasis has on a patient's overall quality of life. The questions are answered on a scale from 0 to 10 with 0 being best and 10 being worst. (NCT00988637)
Timeframe: Baseline to Week 4

InterventionUnits on a scale (Mean)
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)-24.8
Clobex® Spray (Morning) and Vectical® Ointment (Evening)-27.5

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Number of Participants Who Were a Success (Clear/Almost Clear) of Plaque Psoriasis at Week 2 Based on the Overall Disease Severity (ODS), Dichotomized Scale From Baseline to Week 2

Number of participants who were a success (Clear/Almost Clear) of Plaque Psoriasis at Week 2 based on the Overall Disease Severity (ODS), dichotomized scale from Baseline to Week 2. Overall Disease Severity is evaluated on a scale from 0 - 4 (0 = Clear, 1 = Almost Clear, 2 = Mild, 3 = Moderate, 4 = Severe/Very Severe) with 0 being best and 4 being worst. (NCT00988637)
Timeframe: Baseline to week 2

Interventionparticipants (Number)
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)9
Clobex® Spray (Morning) and Vectical® Ointment (Evening)14

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Number of Participants Who Were a Success (Clear/Almost Clear) of Plaque Psoriasis at Week 4 Based on the Overall Disease Severity (ODS), Full Ordinal Scale From Baseline to Week 4

Number of participants who were a success (Clear/Almost Clear) of Plaque Psoriasis at week 4 based on the Overall Disease Severity (ODS), full ordinal scale from baseline to week 4. Overall Disease Severity is evaluated on a scale from 0 - 4 (0 = Clear, 1 = Almost Clear, 2 = Mild, 3 = Moderate, 4 = Severe/Very Severe) with 0 being best and 4 being worst. (NCT00988637)
Timeframe: Baseline to Week 4

Interventionparticipants (Number)
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)14
Clobex® Spray (Morning) and Vectical® Ointment (Evening)28

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Number of Participants With Tolerability Assessments Resulting in Adverse Events From Baseline to Week 4

Number of participants with Tolerability Assessments resulting in Adverse Events from baseline to week 4. Tolerability assessments (Pruritus, telangiectasias, and stinging/burning) are evaluated on a scale from 0 - 3 (0 = None, 1 = Mild, 2 = Moderate, 3 = Severe) with 0 being best and 3 being worst. Skin atrophy and folliculitis are evaluated as absent or present. Changes in tolerability assessments that require a dose modification or concomitant medications/therapy are recorded as adverse events. (NCT00988637)
Timeframe: Baseline to Week 4

Interventionparticipants (Number)
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)4
Clobex® Spray (Morning) and Vectical® Ointment (Evening)2

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"Number of Participants Who Responded to the Categories of Possible Answers to the Subject's Satisfaction Survey Question I am Satisfied With my Appearance at Week 4"

"Number of participants who responded to the categories of possible answers to the Subject's Satisfaction Survey question I am Satisfied with my Appearance at Week 4. Categories of possible answers include Strongly agree, Moderately agree, No opinion, Moderately disagree, and Strongly disagree." (NCT00988637)
Timeframe: Week 4

,
Interventionparticipants (Number)
Strongly agreeModerately agreeNo opinionModerately disagreeStrongly disagreeMissing
Clobex® Spray (Morning) and Vectical® Ointment (Evening)25324511
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)10396933

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"Number of Participants Who Responded to the Categories of Possible Answers to the Subject's Satisfaction Survey Question I am Satisfied With the Results of This Treatment Program at Week 4"

"Number of participants who responded to the categories of possible answers to the Subject's Satisfaction Survey question I am satisfied with the results of this treatment program at Week 4. Categories of possible answers include Strongly agree, Moderately agree, No opinion, Moderately disagree, and Strongly disagree." (NCT00988637)
Timeframe: Week 4

,
Interventionparticipants (Number)
Strongly agreeModerately agreeNo opinionModerately disagreeStrongly disagreeMissing
Clobex® Spray (Morning) and Vectical® Ointment (Evening)42201401
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)23355313

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"Number of Participants Who Responded to the Categories of Possible Answers to the Subject's Satisfaction Survey Question I Would Use This Treatment Program Again if Recommended by the Dermatologist at Week 4"

"Number of participants who responded to the categories of possible answers to the Subject's Satisfaction Survey question I would use this treatment program again if recommended by the dermatologist at Week 4. Categories of possible answers include Strongly agree, Moderately agree, No opinion, Moderately disagree, and Strongly disagree." (NCT00988637)
Timeframe: Week 4

,
Interventionparticipants (Number)
Strongly agreeModerately agreeNo opinionModerately disagreeStrongly disagreeMissing
Clobex® Spray (Morning) and Vectical® Ointment (Evening)50160101
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)37213243

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"Number of Participants Who Responded to the Categories of Possible Answers to the Subject's Satisfaction Survey Question The Treatment Program Was Easy to Follow at Week 4"

"Number of participants who responded to the categories of possible answers to the Subject's Satisfaction Survey question The treatment program was easy to follow at Week 4. Categories of possible answers include Strongly agree, Moderately agree, No opinion, Moderately disagree, and Strongly disagree." (NCT00988637)
Timeframe: Baseline and Week 4

,
Interventionparticipants (Number)
Strongly agreeModerately agreeNo opinionModerately disagreeStrongly disagreeMissing
Clobex® Spray (Morning) and Vectical® Ointment (Evening)5980001
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)6122203

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Number of Participants in Each Category of the Global Assessment of Improvement (GAI) Scale From Baseline to Week 4

Number of participants in each category of the Global Assessment of Improvement (GAI) Scale from Baseline to Week 4. The Global Assessment of Improvement is evaluated on a scale from -1 to 4 (-1 = Symptoms worse, 0 = No change, 1 = Minimal Improvement, 2 = Definite Improvement, 3 = Considerable Improvement and 4 = Clearing) with -1 being worst and 4 being best. (NCT00988637)
Timeframe: Baseline to Week 4

,
Interventionparticipants (Number)
Symptoms worse (-1)No change (0)Minimal Improvement (1)Definite Improvement (2)Considerable Improvement (3)Clearing (4)Missing
Clobex® Spray (Morning) and Vectical® Ointment (Evening)0661018253
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)1292519131

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Number of Participants With a Decrease in Signs of Psoriasis (Erythema) Scores From Baseline to Week 4

Number of participants with a decrease in Signs of Psoriasis (Erythema) scores from Baseline to Week 4. Signs of Psoriasis (Erythema) are evaluated on a scale from 0 - 4 (0 = Clear, 1 = Almost Clear, 2 = Mild, 3 = Moderate, 4 = Severe/Very Severe with 0 being best and 4 being worst. (NCT00988637)
Timeframe: Baseline to Week 4

,
Interventionparticipants (Number)
Clear (0)Almost Clear (1)Mild (2)Moderate (3)Severe/Very Severe (4)
Clobex® Spray (Morning) and Vectical® Ointment (Evening)41532170
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)5631280

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Number of Participants With Decrease in Signs of Psoriasis (Plaque Elevation) Scores From Baseline to Week 4

Number of participants with decrease in Signs of Psoriasis (Plaque Elevation) scores from Baseline to Week 4. Signs of Psoriasis (Plaque Elevation) are evaluated on a scale from 0 - 4 (0 = Clear, 1 = Almost Clear, 2 = Mild, 3 = Moderate, 4 = Severe/Very Severe) with 0 being best and 4 being worst. (NCT00988637)
Timeframe: Baseline to Week 4

,
Interventionparticipants (Number)
Clear (0)Almost Clear (1)Mild (2)Moderate (3)Severe/Very Severe (4)
Clobex® Spray (Morning) and Vectical® Ointment (Evening)11242670
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)61533160

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Number of Participants With Decrease in Signs of Psoriasis (Scaling) Scores From Baseline to Week 4

Number of participants with decrease in Signs of Psoriasis (Scaling) scores from Baseline to Week 4. Signs of Psoriasis (Scaling) are evaluated on a scale from 0 - 4 (0 = Clear, 1 = Almost Clear, 2 = Mild, 3 = Moderate, 4 = Severe/Very Severe) with 0 being best and 4 being worst. (NCT00988637)
Timeframe: Baseline to Week 4

,
Interventionparticipants (Number)
Clear (0)Almost Clear (1)Mild (2)Moderate (3)Severe (4)
Clobex® Spray (Morning) and Vectical® Ointment (Evening)20202350
Vectical® Ointment (Weekdays) and Clobex® Spray (Weekends)12242860

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The Secondary Endpoint Will be the Percentage of Patients Achieving a 75% Reduction in Psoriasis Area and Severity Index at Weeks 4 and 8.

(NCT01012713)
Timeframe: 8 weeks

Interventionpercent (Number)
Week 8Week 4
Open-Label Treatment7245

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A Tertiary Endpoint Will be the Percentage of Patients Achieving 90% Reduction in Psoriasis Area and Severity Index at Week 12.

(NCT01012713)
Timeframe: 12 weeks

Interventionpercent (Number)
Open-Label Treatment45

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The Primary Endpoint Will be the Percentage of Patients Achieving a 75% Reduction in the Psoriasis Area and Severity Index at Week 12.

(NCT01012713)
Timeframe: 12 weeks

Interventionpercent (Number)
Open-Label Treatment83

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Percent of Patients Achieving Parathyroid Hormone Target ≤ 450

Compare the percent of patients achieving an intact PTH target of ≤ 450 pg/ml before and after the application of a computerized dosing protocol for management of CKD-MBD. If multiple values were obtained within a specified evaluation time frame the values were averaged and the average value was then evaluated as to whether it was within or outside the target range. (NCT01100723)
Timeframe: 1 year

Interventionpercent of participants in target (Number)
Post Treatment33

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Percent of Patients Achieving Phosphorous Target ≤ 4.5

Compare the percent of patients achieving a phosphorus of ≤ 4.5 mg/dL before and after the application of a computerized dosing protocol for management of CKD-MBD. If multiple values were obtained within a specified evaluation time frame the values were averaged and the average value was then evaluated as to whether it was within or outside the target range. (NCT01100723)
Timeframe: 1 year

Interventionpercent of participants in target (Number)
Post Treatment29

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Percent of Patients on Cinacalcet and Vitamin D Analogues

Compare the percent of patients on cinacalcet and vitamin D analogues at baseline and at 6 and 12 months after the application of a computerized dosing protocol for management of CKD-MBD. If multiple values were obtained within a specified evaluation time frame the values were averaged and the average value was then evaluated as to whether it was within or outside the target range. (NCT01100723)
Timeframe: 6 months and 1 year

Interventionpercentage of subjects receiving med (Number)
Post Treatment84

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Percent of Patients Achieving Phosphorous Target ≤ 5.5

Compare the percent of patients achieving a phosphorus of ≤ 5.5 mg/dL before and after the application of a computerized dosing protocol for management of CKD-MBD. If multiple values were obtained within a specified evaluation time frame the values were averaged and the average value was then evaluated as to whether it was within or outside the target range. (NCT01100723)
Timeframe: 1 year

Interventionpercent of participants in target (Number)
Results Analyzed at Study Evaluation Time Points.53

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Percent of Patients Achieving Calcium Target ≤ 10.1

Compare the percent of patients achieving a calcium ≤ 10.1 mg/dL before and after the application of a computerized dosing protocol for management of CKD-MBD. If multiple values were obtained within a specified evaluation time frame the values were averaged and the average value was then evaluated as to whether it was within or outside the target range. (NCT01100723)
Timeframe: 1 year

Interventionpercentage of subjects in target (Number)
Post Treatment78

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Percent of Patients Achieving Parathyroid Hormone Target ≤ 300

Compare the percent of patients achieving an intact Parathyroid hormone (PTH) target of ≤ 300 pg/ml before and after the application of a computerized dosing protocol for management of chronic kidney disease-mineral and bone disorder (CKD-MBD). If multiple values were obtained within a specified evaluation time frame the values were averaged and the average value was then evaluated as to whether it was within or outside the target range. (NCT01100723)
Timeframe: 1 year

Interventionpercentage of subjects meeting target (Number)
Post Treatment21

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Mean Baseline and Change From Baseline in Parathyroid Hormone at Final Visit (FV)

Normal ranges for these chemistry measurements varied according to the age of the participant. (NCT01134315)
Timeframe: Baseline, Final Visit (defined as the last post-baseline observation, up to end of study [715 days])

,
Interventionpg/mL (Mean)
BaselineChange from Baseline at FV
Calcitriol592.8-193.4
Paricalcitol571.7-102.5

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Mean Baseline and Change From Baseline in Albumin at Final Visit (FV)

Normal ranges for these chemistry measurements varied according to the age of the participant. (NCT01134315)
Timeframe: Baseline, Final Visit (defined as the last post-baseline observation, up to end of study [715 days])

,
Interventiong/dL (Mean)
BaselineChange from Baseline at FV
Calcitriol3.8-0.1
Paricalcitol3.3-0.0

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Mean Baseline and Change From Baseline in 25-Hydroxy Vitamin D3 at Final Visit (FV)

Normal ranges for these chemistry measurements varied according to the age of the participant. (NCT01134315)
Timeframe: Baseline, Final Visit (defined as the last post-baseline observation, up to end of study [715 days])

Interventionng/mL (Mean)
BaselineChange from Baseline at FV
Calcitriol28.47.5

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Number of Participants With Treatment-Emergent Adverse Events (AEs), Serious AEs (SAEs), Deaths and Discontinuations Due to AEs

AE: any untoward medical occurrence that does not necessarily have a causal relationship with treatment; any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal product, whether or not considered causally related to the use of the product (either paricalcitol or calcitriol); can result from use of the drug as stipulated in the labeling, as well as from accidental or intentional overdose, drug abuse, or drug withdrawal; any worsening of a pre-existing condition or illness. Severity was categorized as mild, moderate, or severe. SAE: AE that results in the death; is life-threatening; results in hospitalization or prolongation of hospitalization; is a congenital anomaly; results in persistent or significant disability/incapacity; is an important medical event requiring medical or surgical intervention to prevent serious outcome; is a spontaneous or elective abortion. For more details, please see the AE section of this record. (NCT01134315)
Timeframe: Monitored from time of informed consent through end of study + 30 days (total of 745 days).

,
Interventionparticipants (Number)
Any AEAny severe AEAny SAEAny AE leading to discontinuation of study drugAny AE leading to discontinuation of studyAny fatal AEDeaths (includes non-treatment-emergent deaths)
Calcitriol3212263122
Paricalcitol17381000

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Mean Baseline (BL) and Change From Baseline in Calcium, Inorganic Phosphate (IP), Blood Urea Nitrogen (BUN), Creatinine at Final Visit (FV)

Normal ranges for these chemistry measurements varied according to the age of the participant. (NCT01134315)
Timeframe: Baseline, Final Visit (defined as the last post-baseline observation, up to end of study [715 days])

,
Interventionmg/dL (Mean)
Calcium, BL (n=15, 30)Calcium, change from BL at FV (n=15, 30)Inorganic Phosphate (IP), BL (n=13, 29)IP, change from BL at FV (n=13, 29)BUN, BL (n=15, 29)BUN, change from BL at FV (n=15, 29)Creatinine, BL (n=15, 29)Creatinine, change from BL at FV (n=15, 29)
Calcitriol9.30.55.90.449.8-1.98.80.3
Paricalcitol9.20.05.8-0.452.7-10.79.40.3

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Mean Baseline (BL) and Change From Baseline in Potassium, Sodium, Chloride, Bicarbonate at Final Visit (FV)

Normal ranges for these chemistry measurements varied according to the age of the participant. (NCT01134315)
Timeframe: Baseline, Final Visit (defined as the last post-baseline observation, up to end of study [715 days])

,
InterventionmEq/L (Mean)
Potassium, BL (n=15, 29)Potassium, change from BL at FV (n=15, 29)Sodium, BL (n=15, 29)Sodium, change from BL at FV (n=15, 29)Chloride, BL (n=15, 29)Chloride, change from BL at FV (n=15, 29)Bicarbonate, BL (n=15, 28)Bicarbonate, change from BL at FV (n=15, 28)
Calcitriol4.4-0.5139.3-0.798.6-1.125.90.1
Paricalcitol4.4-0.1138.00.299.5-0.526.10.2

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Mean Baseline and Change From Baseline in 1,25-Dihydroxy Vitamin D3 at Final Visit (FV)

Normal ranges for these chemistry measurements varied according to the age of the participant. (NCT01134315)
Timeframe: Baseline, Final Visit (defined as the last post-baseline observation, up to end of study [715 days])

Interventionpg/mL (Mean)
BaselineChange from Baseline at FV
Paricalcitol20.0-10.0

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Percentage of Participants With at Least One Incidence of Hypercalcemia

Hypercalcemia was defined as calcium >10.2 mg/dL. Percentage of participants with hypercalcemia is presented for the overall population, the subgroup of participants in the study for less than 3 months, and those in the study for greater than or equal to 3 months. (NCT01134315)
Timeframe: Monitored from time of informed consent through end of study + 30 days (total of 745 days).

,
Interventionpercentage of participants (Number)
Overall population (n=19, 37)Participants <3 months in study (n=2, 5)Participants >=3 months in study (n=17, 32)
Calcitriol54.1062.5
Paricalcitol36.850.035.3

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Change in 24,25(OH)2D Levels in CKD vs. Non-CKD Subjects Receiving Cholecalciferol

(NCT01222234)
Timeframe: 8 weeks of therapy

Interventionng/ml (Mean)
Group 1: CKD Cholecalciferol1.59
Group 3: Non-CKD Cholecalciferol3.59

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Monocyte Protein Expression

Flow cytometry analysis of monocyte CD14, ACE, VDR, and Mac-1 expression (NCT01222234)
Timeframe: 8 weeks of therapy

,
Interventionrelative fluorescence units (Mean)
CD14ACEVDRMac-1
Group 1: Cholecalciferol - CKD341101359279914318
Group 2: Calcitriol - CKD385401360346814278.5

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Least Squares Mean Percent Change From Baseline (Predose Day 1) of TLS Score for Lesions Treated With MK-0873 and Lesions Treated With Calcitriol

Each lesion was evaluated for 3 components: erythema, induration, and scaling. Each component was given a score using the following scale: 0=none, 1=slight, 2=moderate, 3=marked, 4=very marked, with increasing score reflecting increased lesion severity. The TLS score (range 0 to 12) is calculated as the sum of the 3 components. (NCT01235728)
Timeframe: Baseline and Day 29

InterventionPercent Change (Least Squares Mean)
Calcitriol 0.0003%-57.24
MK-0873-47.89

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Least Squares Mean Percent Change From Baseline (Predose Day 1) of Target Lesion Severity (TLS) Score for Lesions Treated With MK-0873 and Lesions Treated With MK-0873 Vehicle

Each lesion was evaluated for 3 components: erythema, induration, and scaling. Each component was given a score using the following scale: 0=none, 1=slight, 2=moderate, 3=marked, 4=very marked, with increasing score reflecting increased lesion severity. The TLS score (range 0 to 12) is calculated as the sum of the 3 components. (NCT01235728)
Timeframe: Baseline and Day 29

InterventionPercent Change (Least Squares Mean)
MK-0873-47.37
MK-0873 Vehicle-42.71

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Mean Maximum Plasma Concentrations at Trough of Day 8, 15, 22, and 29 Following Topical Administration of MK-0873 to Psoriatic Patients

Plasma samples were collected at 12 hours post-dose on Days 8, 15, 22, and 28 to evaluate the mean maximum plasma concentration at trough of MK-0873. (NCT01235728)
Timeframe: Day 8, 15, 22, 29

InterventionnM (Mean)
MK-08733.6

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Serum Creatinine

After an overnight fast, plasma concentrations of hemoglobin, creatinine, cholesterol, glucose, total calcium, and phosphate were measured using an autoanalyzer as described by Adorini L. (2005) (NCT01265615)
Timeframe: on day 180 after Tx

Interventionmg/dL (Mean)
Paricalcitol Treatment2.5
Calcitriol Treatment2.5
Cholecalciferol2.8
Supplemental4.1

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GFR (Glomerular Filtration Rate)

Estimated glomerular filtration rate (eGFR) was calculated using the abbreviated form of the Modification of Diet in Renal Disease (MDRD) study equation: eGFR = exp (5.228 - 1.154 × ln (serum creatinine) - 0.203 × ln (age). Concerning of GFR with Tc99m DTPA renography was used for the complex analysis of renal function. Camera based GFR estimated from Tc99m DTPA renography was named Gates GFR. (NCT01265615)
Timeframe: on day 180

Interventionml/min/1.73 m^2 (Mean)
Paricalcitol Treatment84
Calcitriol Treatment81
Cholecalciferol76
Supplemental54

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Coronary Calcium Score

Bone mineral density assessed by dual-energy X-ray absorptiometry (DXA) of the whole body, lumbar spine and hip was performed using Hologic scanners (QDR 1000W or QDR 2000). The total Agatston coronary calcium score (CCS) was measured as the sum of calcified plaque scores of all the coronary arteries. The amount of calcium present in the coronary arteries is scored according to the Agatson scale, as follows: 0 - no identifiable disease; 1 to 99 - mild disease; 100 to 399 - moderate disease; 400 or higher - severe disease. (NCT01265615)
Timeframe: on day 180

Interventionunits on a scale (Mean)
Paricalcitol Treatment530
Calcitriol Treatment611
Cholecalciferol524
Supplemental990

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CAD (Chronic Allograft Dysfunction) Degree

"CAD degree measured by Banff score after routine renal biopsy (revised 2005/2007 criteria). We assessed antibody-mediated rejection, borderline changes, T-cell-mediated rejection, interstitial fibrosis and tubular atropthy, and other changes. Grades:~Grade I. Mild interstitial fibrosis and tubular atrophy (<25% of cortical area) II. Moderate (26-50%) III. Severe (>50%) (may include non-specific vascular and glomerular sclerosis)" (NCT01265615)
Timeframe: on day 90

InterventionScores on a Banff scale (Mean)
Paricalcitol Treatment1.24
Calcitriol Treatment1.22
Cholecalciferol1.43
Supplemental1.68

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CAD (Chronic Allograft Dysfunction) Degree

"Beyond 180 days, chronic allograft dysfunction (CAD) was characterized by mean Banff degree (revised 2005/2007 criteria) with the data of renal biopsy material. Renal tissue was recovered during routined biopsy. We assessed antibody-mediated rejection, borderline changes, T-cell-mediated rejection, interstitial fibrosis and tubular atropthy, and other changes. Grades:~Grade I. Mild interstitial fibrosis and tubular atrophy (<25% of cortical area) II. Moderate (26-50%) III. Severe (>50%) (may include non-specific vascular and glomerular sclerosis)" (NCT01265615)
Timeframe: day 180 after Tx (transplantation)

InterventionScores on a Banff scale (Mean)
Paricalcitol Treatment1.24
Calcitriol Treatment1.22
Cholecalciferol1.43
Supplemental1.68

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Heart Failure (HF)

"NYHA (New York Heart Association) functional class verified with veloergometry probe and by NYHA clinical classification NYHA Class Symptoms I No symptoms and no limitation in ordinary physical activity, e.g. shortness of breath when walking, climbing stairs etc.~II Mild symptoms and slight limitation during ordinary activity. III Marked limitation in activity due to symptoms, even during less-than-ordinary activity, e.g. walking short distances (20-100 m).~Comfortable only at rest. IV Severe limitations. Experiences symptoms even while at rest. Mostly bedbound patients." (NCT01265615)
Timeframe: on day 180 after Tx (transplantation)

InterventionNYHA functional class of HF (Mean)
Paricalcitol Treatment1.8
Calcitriol Treatment1.9
Cholecalciferol1.9
Supplemental2.5

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Number of Circulating SP (Side Population) Stem-Progenitor Cells

Renal cells and solid tissue were obtained from the normal portion of cortex obtained from surgically removed kidneys or by standart biopsy on day 180. Cytofluorimetric analysis and immunofluorescence were performed as described by Oliver J.A. (2004). Sorting and analysis of different cells was done on a FACS (fluorescent activated cell sorting) and by flow cytometry. Cells were analyzed with EPICS systems (Beckman Coulter). Quantification of mRNA expression was achieved using Assays-on-Demand gene expression kits and the ABI PRISM 7000 Sequence Detection System (Applied Biosystem). (NCT01265615)
Timeframe: on day 180

Interventionper cent of SP cells (Mean)
Paricalcitol Treatment7.6
Calcitriol Treatment6.5
Cholecalciferol5.7
Supplemental4.2

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Systolic Blood Pressure

SBP measured by routine method (NCT01265615)
Timeframe: on day 180

InterventionmmHg (Mean)
Paricalcitol Treatment143
Calcitriol Treatment141
Cholecalciferol147
Supplemental165

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VDR (Vitamin D Receptor) Expression in Kidney

VDR content was determined by using an ELISA developed in this laboratory. The protein concentration of the homogenates was determined by the method of Bradford (1976), using BSA as a standard. (NCT01265615)
Timeframe: on day 180

Interventionfmol VDR/ mg protein (Mean)
Paricalcitol Treatment584
Calcitriol Treatment599
Cholecalciferol478
Supplemental333

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VDR (Vitamin D Receptor) Expression in Myocardium

VDR content was determined by using an ELISA developed in this laboratory. The protein concentration of the homogenates was determined by the method of Bradford (1976), using BSA as a standard. (NCT01265615)
Timeframe: on day 180

Interventionfmol VDR/ mg protein (Mean)
Paricalcitol Treatment801
Calcitriol Treatment715
Cholecalciferol654
Supplemental389

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Mean Change in Bone Resorption: NTX (N-terminal Telopeptide)

Scale score for NTX (N-terminal telopeptide) minimum value = 4.2 nmol BCE; maximum value = 3688 nmol BCE Higher scale score for NTX indicates worse outcome. (NCT01293682)
Timeframe: baseline to 12 weeks

Interventionnmol (Mean)
CalcitriolNA

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Mean Change in Bone Formation: BAP (Bone-specific Alkaline Phosphatase)

Scale score for BAP (Bone-specific alkaline phosphatase) minimum value = 7 mcg/L; maximum value = 329 mcg/L Higher scale score for BAP indicates worse outcome. (NCT01293682)
Timeframe: baseline to 12 weeks

Interventionmcg/L (Mean)
CalcitriolNA

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Prevalence of Obesity and Vitamin D Insufficiency in Adolescents With Newly Diagnosed ALL and in Their Siblings

Insufficiency defined as 25(OH)D < 30 ng/ml (NCT01317940)
Timeframe: 1 timepoint

InterventionParticipants (Count of Participants)
Siblings of Survivors (Group C)0
Newly Diagnosed Patients (Group A)36

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Bone Mineral Density by QCT in Survivors at Study End (Group B)

Bone mineral density (vBMD) at end of study period (Group B: after 6 months) (NCT01317940)
Timeframe: +6 months

,
Interventioncm3 (Mean)
Cortical bone mineral densityCancellous bone mineral density
Survivorship Intervention (Group B)2087.4243.6
Survivorship Standard of Care (Group B)2049.3269.3

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Bone Mineral Density by Quantitative Computed Tomography (QCT) at Study End (Group A)

Bone mineral density (vBMD) at end of study period (Group A: end of Delayed Intensification) (NCT01317940)
Timeframe: +6 months

,,
Interventioncm3 (Mean)
Cortical BMDCancellous BMD
"On-Therapy Natural History (Group A, Tibia)"927.5159.1
On Therapy Standard of Care (Group A)2090.9201.4
On-Therapy Intervention (Group A)2093.1203.8

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Change in Serum Vitamin D Level (Group A)

Change in Vitamin D levels from baseline to study end (Group A: Consolidation through end of Delayed Intensification) (NCT01317940)
Timeframe: +6 months

,,
Interventionng/ml (Mean)
Change in serum Vitamin 25(OH)D levelPost-intervention serum Vitamin 25(OH)D level
"On-Therapy Natural History (Group A)"1.023.3
On Therapy Standard of Care (Group A)-0.3019.0
On-Therapy Intervention (Group A)5.526.5

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Change in Vitamin D Level (Group B)

Change in serum vitamin D level was assessed in survivors at baseline and after 6 months of supplementation (NCT01317940)
Timeframe: +6 months

,
Interventionng/ml (Median)
Change in serum Vitamin 25(OH)D levelPost-intervention serum Vitamin 25(OH)D level
Survivorship Intervention (Group B)1.026.0
Survivorship Standard of Care (Group B)-1.029.0

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Percentage of Participants With Target Intact Parathyroid Hormone (iPTH)

The target iPTH range was 60-180 pg/mL, based on the average of the last 3 weeks of treatment. iPTH was measured before the first dialysis session of each week and analyzed by the central laboratory. (NCT01341782)
Timeframe: The last three weeks of treatment (Weeks 11, 12, and 13)

Interventionpercentage of participants (Number)
Paricalcitol31.5
Maxacalcitol32.8

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Percentage of Participants With Target Intact Parathyroid Hormone (iPTH) and Without Hypercalcemia

The target iPTH range was 60-180 pg/mL, based on the average of the last 3 weeks of treatment, and with no hypercalcemia during the treatment phase. Hypercalcemia was defined as at least 1 corrected calcium value > 11.0 mg/dL or at least 2 corrected calcium values ≥ 10.5 mg/dL. iPTH was measured before the first dialysis session of each week and analyzed by the central laboratory. (NCT01341782)
Timeframe: iPTH measured during the last three weeks of treatment (Weeks 11, 12, and 13). Calcium measured throughout the study (Weeks 1-13).

Interventionpercentage of participants (Number)
Paricalcitol27.7
Maxacalcitol30.5

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Number of Visits at Which Participants Achieved iPTH Control in the Target Range of 60 to 180 pg/mL

iPTH control was defined as being within the target range of 60 to 180 pg/mL. iPTH was measured before the first dialysis session of the week, once a week during the treatment phase and analyzed by the central laboratory. (NCT01341782)
Timeframe: Weeks 2 to 13

Interventionvisits (Mean)
Paricalcitol2.6
Maxacalcitol3.4

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Percentage of Participants With ≥ 50% Reduction in Intact Parathyroid Hormone (iPTH) From Baseline and With No Hypercalcemia

The percentage of participants with greater than or equal to 50% reduction in intact parathyroid hormone (iPTH) from baseline to the average of the last 3 weeks of treatment and with no hypercalcemia during the treatment phase. iPTH was measured before the first dialysis session of each week and analyzed by the central laboratory. Hypercalcemia was defined as at least 1 corrected calcium value > 11.0 mg/dL or at least 2 corrected calcium values ≥ 10.5 mg/dL. (NCT01341782)
Timeframe: Baseline to the last three weeks of treatment (Weeks 11, 12, and 13) for iPTH. Calcium measured throughout the study (Weeks 1-13).

Interventionpercentage of participants (Number)
Paricalcitol34.6
Maxacalcitol39.1

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Percentage of Participants With ≥ 50% Reduction in Intact Parathyroid Hormone (iPTH) From Baseline

The percentage of participants with a greater than or equal to 50% reduction in intact parathyroid hormone (iPTH) from baseline to the average of the last 3 weeks of treatment. iPTH was measured before the first dialysis session of each week and analyzed by the central laboratory. (NCT01341782)
Timeframe: Baseline to the last three weeks of treatment (Weeks 11, 12, and 13)

Interventionpercentage of participants (Number)
Paricalcitol44.9
Maxacalcitol50.8

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Number of Visits at Which Participants Achieved iPTH Control With ≥ 50% Reduction in Intact Parathyroid Hormone (iPTH) From Baseline

iPTH control was defined as a ≥ 50% reduction from baseline. iPTH was measured before the first dialysis session of the week, each week during the treatment phase and analyzed by the central laboratory. (NCT01341782)
Timeframe: Weeks 2 to 13

Interventionvisits (Mean)
Paricalcitol3.9
Maxacalcitol5.3

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Base Study: Percentage Change From Baseline in Serum Procollagen Type 1 N-Terminal Propeptide (s-P1NP) at Month 6

s-P1NP is a biochemical marker of bone turnover that is particularly useful in monitoring bone resorption, a process by which bone is broken down within the body. s-P1NP was measured at baseline and Month 6. (NCT01350934)
Timeframe: Baseline and Month 6

InterventionPercent change (Least Squares Mean)
Fosamax Plus-59.12
Calcitriol-16.75

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Extension Study: Percentage Change From Baseline in Lumbar Spine BMD at Month 12

BMD at the lumbar spine was assessed by DXA at baseline and Month 12. (NCT01350934)
Timeframe: Baseline and Month 12

InterventionPercent change (Least Squares Mean)
Fosamax Plus5.17
Calcitriol2.26

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Extension Study: Percentage Change From Baseline in s-CTx at Month 12

s-CTx is a biochemical marker for bone turnover that has been shown to detect increased bone resorption, a process by which bone is broken down within the body. s-CTx was measured at baseline and Month 12. (NCT01350934)
Timeframe: Baseline and Month 12

InterventionPercent change (Least Squares Mean)
Fosamax Plus-76.15
Calcitriol-24.19

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Extension Study: Percentage Change From Baseline in s-P1NP at Month 12

s-P1NP is a biochemical marker of bone turnover that is particularly useful in monitoring bone resorption, a process by which bone is broken down within the body. s-P1NP was measured at baseline and Month 12. (NCT01350934)
Timeframe: Baseline and Month 12

InterventionPercent change (Least Squares Mean)
Fosamax Plus-68.07
Calcitriol-17.00

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Extension Study: Percentage of Participants With Serum 25-Hydroxyvitamin (OH) D <20 ng/mL at Month 12

"The term vitamin D insufficiency is used to describe vitamin D levels that are low enough to cause secondary hyperparathyroidism, bone loss, and increased risk of skeletal fracture. In this study, a threshold for vitamin D insufficiency was a level of serum 25(OH) D <20 ng/mL." (NCT01350934)
Timeframe: Baseline and Month 12

InterventionPercentage of Participants (Number)
Fosamax Plus4.1
Calcitriol47.1

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Base Study: Percentage Change From Baseline in Serum C-Telopeptides of Type 1 Collagen (s-CTx) at Month 6

s-CTx is a biochemical marker for bone turnover that has been shown to detect increased bone resorption, a process by which bone is broken down within the body. s-CTx was measured at baseline and Month 6. (NCT01350934)
Timeframe: Baseline and Month 6

InterventionPercent change (Least Squares Mean)
Fosamax Plus-79.23
Calcitriol-27.20

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Base Study: Percentage Change From Baseline in Lumbar Spine Bone Mineral Density (BMD) at Month 6

BMD at the lumbar spine was assessed by dual energy X-ray absorptiometry (DXA) at baseline and Month 6. (NCT01350934)
Timeframe: Baseline and Month 6

InterventionPercent change (Least Squares Mean)
Fosamax Plus3.54
Calcitriol1.59

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Compare the Efficacy of Calcitriol and Cholecalciferol Supplementation on Plasma Concentrations of C-reactive Protein

Secondary aims are focused to explore whether vitamin D improves vascular endothelial function through decreases in inflammation (NCT01384539)
Timeframe: 6 months

,
Interventionmg/dL (Median)
BaselineEnd of Study
Calcitriol3.43.9
Cholecalciferol3.03.1

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Compare the Effect of Calcitriol and Cholecalciferol Supplementation on Vascular Endothelial Cell Expression of Nf-kB

The effect of calcitriol and cholecalciferol supplementation will be evaluated calculating the mean change in total vascular endothelial cell NFkB expression. NFkB expression is given as arbitrary units and represent ratios of endothelial cell protein expression to human umbilical vein endothelial cell (HUVEC) expression in order to account for any variation in the staining procedure. (NCT01384539)
Timeframe: 6 months

Interventionratio of NFkB to HUVEC expression (Mean)
Cholecalciferol0.03
Calcitriol-0.01

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Compare the Difference Between the Calcitriol and Cholecalciferol Groups in Conduit Artery Endothelium-dependent Dilation (EDD) in Response to Treatment.

EDD will be measured by brachial artery flow-mediated dilation (FMD). The mean change in percent FMD from baseline will be documented. (NCT01384539)
Timeframe: 6 months

Interventionpercent change in FMD (Mean)
Cholecalciferol-0.5
Calcitriol0.3

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Change From Baseline in Modified Psoriasis Area and Severity Index (mPASI)

"The primary response criterion was the percentage change in m-PASI from baseline to Week 4.~The extent of and severity of redness, thickness and scaliness of psoriasis were recorded for each of three regions (arms, trunk and legs) and these were used to calculate mPASI using the following formula:~Arms: 0.2(R+T+S)E = X Trunk: 0.2(R+T+S)E = Y Legs: 0.2(R+T+S)E = Z where R = score for redness (using a scale from 0 to 4, where o is non signs and 4 is the most severe signs) T = score for thickness (using a scale from 0 to 4, where o is non signs and 4 is the most severe signs) S = score for scaliness (using a scale from 0 to 4, where o is non signs and 4 is the most severe signs) E = score for extent (using a scale from 0 to 6, where 0 is no involvement and 6 is 90-100% involvemnet) The sum of X + Y + Z gave the total m-PASI, which could range from 0 to 64.8." (NCT01422434)
Timeframe: Baseline to Week 4

Interventionpercentage of change (Mean)
Dovonex® Ointment-50.5
LEO 90105 Ointment-64.3
Rinderon® - DP Ointment-53.6

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Change From Baseline in Target Lesion Assessment

"Percentage change in composite severity score of the target lesion from baseline to Week 4.~At Visit 1, the investigator selected a target lesion. Location was recorded as trunk, limb excluding elbow and/or knee.~At Visits 1-4, the investigator assessed the severity of the target lesion for each sign (redness, thickness and scaliness) on a scale from 0 to 8 where 0 is no signs of redness, thickness or scaliness and 8 is the most severe signs of redness, thickeness or scaliniess.~The individual scores for redness, thickness and scaliness were added together to give a single composite score for severity of the target lesion which could range from 0 to 24. The percentage change in the composite severity score from baseline to each visit was also calcutated." (NCT01422434)
Timeframe: Baseline to Week 4

Interventionpercentage of change (Mean)
Dovonex® Ointment-57.1
LEO 90105 Ointment-70.5
Rinderon® - DP Ointment-58.6

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Physician's Global Assessment of Psoriasis

"Subjects with 'clear' or 'almost clear' disease by physician's global assessment on the following 6 point scale: clear, almost clear, mild, moderate, severe, very severe.~The assessment represents the average lesion severity on the trunk and limbs. The assessment was based on the condition of the disease at the time of evaluation, and not in relation to the condition at a previous visit." (NCT01422434)
Timeframe: Week 4

Interventionparticipants (Number)
Dovonex® Ointment52
LEO 90105 Ointment89
Rinderon® - DP Ointment43

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Change in mPASI From Baseline to Week 1

The extent of and severity of redness, thickness and scaliness of psoriasis were recorded for each of three regions (arms, trunk and legs) and these were used to calculate mPASI. The m-PASI could range from 0 to 64.8. The least severe outcome is 0 and the most severe outcome is 64.8 (NCT01422434)
Timeframe: Baseline to Week 1

Interventionpercentage of change (Mean)
Dovonex® Ointment-23.7
LEO 90105 Ointment-39.1
Rinderon® - DP Ointment-29.5

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Change From Baseline in Modified Target NAPSI for the Single Most Severely Affected Nail

"The target nail will be assessed by two dermatologists before treatment and at week 4, 8, 12, 16, 20, 24 using modified target NAPSI score (mtNAPSI, 0-96).~mtNAPSI evaluation: a target nail is divided into 4 quadrants and for each quadrant the nail parameters (oil drop, onycholysis, hyperkeratosis, hemorrhages, pitting, leukonychia, red spots on the lunula, and crumbling) are assessed separately: 0 = no sign, 1 = mild, 2 = moderate, and 3 = severe; the range of mtNAPSI is between 0 and 96, with higher score indicating more severe symptoms." (NCT01445886)
Timeframe: Baseline and 24 weeks

,
Interventionunits on a scale (Mean)
baselineweek 24
Calcipotriol Solution16.99.5
Indigo Naturalis Oil Extract17.75.9

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Physician's and Subject's Global Assessment

"The Physician's and Subject's Global Assessment (PGA and SGA) will be assessed by two dermatologists and participant himself/herself respectively after treatment 24 weeks.~A 6-point scale was used for both SGA and PGA: 0 = worse, 1 = 0-24% clearing with little or no change, 2 = 25-49% clearing with slight improvement, 3 = 50-74% clearing with moderate improvement, 4 = 75-99% clearing with striking improvement, 5 = cleared. A score between 3 and 5 was considered to be a positive response and a score between 0 and 2 a poor response." (NCT01445886)
Timeframe: Week 24

,
Interventionunits on a scale (Mean)
PGA 1PGA 2SGA
Calcipotriol Solution2.52.32.6
Indigo Naturalis Oil Extract3.73.43.9

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Change From Baseline in Single-handed Nail Psoriasis Severity Index (shNAPSI) at 24 Weeks

"The nails will be assessed by two dermatologists at baseline and after treatment 4, 8, 12, 16, 20, 24 weeks using single-handed Nail Psoriasis Severity Index (shNAPSI) score. shNAPSI evaluation: Each nail is given a score for nail bed psoriasis (0-4) and nail matrix psoriasis (0-4) , the total of which is the score for that nail (0-8); the range of shNAPSI of one hand is between 0 and 40, with higher score indicating more severe symptoms. Nail bed psoriasis: presence of any of the nail bed features (onycholysis, hemorrhages, hyperkeratosis, oil drop (salmon patch dyschroma): 0 for none, 1 for 1 quadrant only, 2 for 2 quadrants, 3 for 3 quadrants, and 4 for 4 quadrants. Nail matrix psoriasis: presence of any of the nail matrix features (pitting, leukonychia red spots in the lunula, crumbling): 0 for none, 1 if present in 1 quadrant of the nail, 2 if present in 2 quadrants of the nail, 3 if present in 3 quadrants of the nail, and 4 if present in 4 quadrants of the nail." (NCT01445886)
Timeframe: Baseline and 24 weeks

,
Interventionunits on a scale (Mean)
baselineweek 24
Calcipotriol Solution27.420.4
Indigo Naturalis Oil Extract27.214.4

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Subjects With 'Controlled Disease' ('Clear'/'Almost Clear' for Subjects w. at Least Moderate Disease at Baseline, 'Clear' for Subjects With Mild Disease at Baseline) According to the Investigator's Global Assessment (IGA) on the Trunk and Limbs at Week 4.

Assessment of disease severity (Plaque thickening, Scaling and Erythema) using a 5-point scale (Clear, Almost clear, Mild, Moderate, Severe), based on the condition of the disease at the time of evaluation. (NCT01536938)
Timeframe: 4 weeks

Interventionparticipants (Number)
LEO 9010045
Betamethasone Dipropionate31
Calcipotriol Aerosol Foam15

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Change in Erythema From Baseline to Day 22

Investigator's rating of the clinical appearance of erythema. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01580488)
Timeframe: Baseline to Day 22

Interventionunits on a scale (Mean)
B LEO 35299 20 mg/g-0.91
C LEO 35299 20 mg/g-0.67
E LEO 35299 10 mg/g-0.54
F LEO 35299 10 mg/g-0.70
Daivonex® Ointment: Calcipotriol 50 Mcg/g Ointment-1.09
Daivonex® Ointment-1.07

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Change in Lesion Thickness From Baseline to Day 22

Change in total skin thickness measured by ultrasound from baseline to end of treatment (NCT01580488)
Timeframe: Baseline to Day 22

Interventionmillimeters (Mean)
B LEO 35299 20 mg/g-0.31
C LEO 35299 20 mg/g-0.18
E LEO 35299 10 mg/g-0.22
F LEO 35299 10 mg/g-0.24
Daivonex® Ointment: Calcipotriol 50 Mcg/g Ointment-0.36
Daivonex® Ointment-0.38

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Change in the Total Clinical Score From Baseline to Day 22

Investigator's rating of the clinical appearance of a psoriatic lesion. Maximum score is 9 (most severe); minimum score is 0 (least severe). The single items erythema, scaling, and infiltration (maximum score 3 each) are summed to obtain the Total Clinical Score. Total Clinical Score range from 0 (all symptoms absent) to 9 (all symptoms severe) (NCT01580488)
Timeframe: Baseline to Day 22

Interventionunits on a scale (Mean)
B LEO 35299 20 mg/g-2.8
C LEO 35299 20 mg/g-1.9
E LEO 35299 10 mg/g-1.5
F LEO 35299 10 mg/g-1.8
Daivonex® Ointment: Calcipotriol 50 Mcg/g Ointment-4.0
Daivonex® Ointment-3.3

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Change in Infiltration From Baseline to Day 22

Investigator's rating of the clinical appearance of infiltration. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01580488)
Timeframe: Baseline to Day 22

Interventionunits on a scale (Mean)
B LEO 35299 20 mg/g-0.87
C LEO 35299 20 mg/g-0.59
E LEO 35299 10 mg/g-0.46
F LEO 35299 10 mg/g-0.46
Daivonex® Ointment: Calcipotriol 50 Mcg/g Ointment-1.48
Daivonex® Ointment-1.11

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Change in Scaling From Baseline to Day 22

Investigator's rating of the clinical appearance of scaling . Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01580488)
Timeframe: Baseline to Day 22

Interventionunits on a scale (Mean)
B LEO 35299 20 mg/g-1.09
C LEO 35299 20 mg/g-0.74
E LEO 35299 10 mg/g-0.61
F LEO 35299 10 mg/g-0.67
Daivonex® Ointment: Calcipotriol 50 Mcg/g Ointment-1.52
Daivonex® Ointment-1.30

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Change in Skin Thickness From Baseline to Day 22

Change in skin thickness - echo-poor band measured by ultrasound from baseline to end of treatment (NCT01580488)
Timeframe: Baseline to Day 22

Interventionmillimeters (Mean)
B LEO 35299 20 mg/g-0.40
C LEO 35299 20 mg/g-0.29
E LEO 35299 10 mg/g-0.24
F LEO 35299 10 mg/g-0.40
Daivonex® Ointment: Calcipotriol 50 Mcg/g Ointment-0.57
Daivonex® Ointment-0.49

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Change in Total Clinical Score at Day 15 Compared to Baseline

Investigator's rating of the clinical appearance of a psoriatic lesion. Maximum score is 9 (most severe); minimum score is 0 (least severe). The single items erythema, scaling, and infiltration (maximum score 3 each) are summed to obtain the Total Clinial Score. (NCT01607853)
Timeframe: Baseline to day 15

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-3.0
Daivobet® Gel Applied Then Removed After 20 Minutes-2.8
Daivobet® Gel Applied for 24 Hours-3.9
Daivobet® Gel Vehicle Applied for 24 Hours-0.9

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Change in Total Clinical Score at Day 18 Compared to Baseline

Investigator's rating of the clinical appearance of a psoriatic lesion. Maximum score is 9 (most severe); minimum score is 0 (least severe). The single items erythema, scaling, and infiltration (maximum score 3 each) are summed to obtain the Total Clinical Score. (NCT01607853)
Timeframe: Baseline to day 18

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-3.4
Daivobet® Gel Applied Then Removed After 20 Minutes-3.4
Daivobet® Gel Applied for 24 Hours-4.3
Daivobet® Gel Vehicle Applied for 24 Hours-1.1

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Change in Total Clinical Score at Day 4 Compared to Baseline

Investigator's rating of the clinical appearance of a psoriatic lesion. Maximum score is 9 (most severe); minimum score is 0 (least severe). The single items erythema, scaling, and infiltration (maximum score 3 each) are summed to obtain the Total Clinical Score. (NCT01607853)
Timeframe: Baseline to day 4

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.5
Daivobet® Gel Applied Then Removed After 20 Minutes-0.5
Daivobet® Gel Applied for 24 Hours-0.4
Daivobet® Gel Vehicle Applied for 24 Hours-0.1

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Change in Total Clinical Score at Day 8 Compared to Baseline

Investigator's rating of the clinical appearance of a psoriatic lesion. Maximum score is 9 (most severe); minimum score is 0 (least severe). The single items erythema, scaling, and infiltration (maximum score 3 each) are summed to obtain the Total Clinical Score. (NCT01607853)
Timeframe: Baseline to day 8

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-1.5
Daivobet® Gel Applied Then Removed After 20 Minutes-1.4
Daivobet® Gel Applied for 24 Hours-1.6
Daivobet® Gel Vehicle Applied for 24 Hours-0.2

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Change in Total Clinical Score From Baseline to Day 22

Investigator's rating of the clinical appearance of a psoriatic lesion. Maximum score is 9 (most severe); minimum score is 0 (least severe). The single items erythema, scaling, and infiltration (maximum score 3 each) are summed to obtain the Total Clincal Score (NCT01607853)
Timeframe: baseline to day 22

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-3.6
Daivobet® Gel Applied Then Removed After 20 Minutes-3.7
Daivobet® Gel Applied for 24 Hours-4.9
Daivobet® Gel Vehicle Applied for 24 Hours-1.3

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Change From Baseline in Erythema at Day 11

Investigator's rating of the clinical appearance of erythema. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 11

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.79
Daivobet® Gel Applied Then Removed After 20 Minutes-0.85
Daivobet® Gel Applied for 24 Hours-1.06
Daivobet® Gel Vehicle Applied for 24 Hours-0.27

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Change From Baseline in Erythema at Day 15

Investigator's rating of the clinical appearance of erythema. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 15

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-1.00
Daivobet® Gel Applied Then Removed After 20 Minutes-1.04
Daivobet® Gel Applied for 24 Hours-1.29
Daivobet® Gel Vehicle Applied for 24 Hours-0.31

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Change From Baseline in Erythema at Day 18

Investigator's rating of the clinical appearance of erythema. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 18

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-1.04
Daivobet® Gel Applied Then Removed After 20 Minutes-1.19
Daivobet® Gel Applied for 24 Hours-1.42
Daivobet® Gel Vehicle Applied for 24 Hours-0.46

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Change From Baseline in Erythema at Day 22

Investigator's rating of the clinical appearance of erythema. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 22

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-1.17
Daivobet® Gel Applied Then Removed After 20 Minutes-1.31
Daivobet® Gel Applied for 24 Hours-1.56
Daivobet® Gel Vehicle Applied for 24 Hours-0.42

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Change From Baseline in Erythema at Day 4.

Investigator's rating of the clinical appearance of erythema. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 4

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.17
Daivobet® Gel Applied Then Removed After 20 Minutes-0.23
Daivobet® Gel Applied for 24 Hours-0.23
Daivobet® Gel Vehicle Applied for 24 Hours-0.06

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Change From Baseline in Erythema at Day 8.

Investigator's rating of the clinical appearance of erythema. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 8

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.54
Daivobet® Gel Applied Then Removed After 20 Minutes-0.56
Daivobet® Gel Applied for 24 Hours-0.67
Daivobet® Gel Vehicle Applied for 24 Hours-0.15

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Change From Baseline in Infiltration at Day 11

Investigator's rating of the clinical appearance of infiltration. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 11

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.63
Daivobet® Gel Applied Then Removed After 20 Minutes-0.60
Daivobet® Gel Applied for 24 Hours-0.81
Daivobet® Gel Vehicle Applied for 24 Hours-0.08

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Change From Baseline in Infiltration at Day 15

Investigator's rating of the clinical appearance of infiltration. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 15

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.81
Daivobet® Gel Applied Then Removed After 20 Minutes-0.73
Daivobet® Gel Applied for 24 Hours-1.19
Daivobet® Gel Vehicle Applied for 24 Hours-0.15

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Change From Baseline in Infiltration at Day 18

Investigator's rating of the clinical appearance of infiltration. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 18

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-1.00
Daivobet® Gel Applied Then Removed After 20 Minutes-0.98
Daivobet® Gel Applied for 24 Hours-1.42
Daivobet® Gel Vehicle Applied for 24 Hours-0.17

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Change From Baseline in Infiltration at Day 22

Investigator's rating of the clinical appearance of infiltration. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 22

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-1.08
Daivobet® Gel Applied Then Removed After 20 Minutes-1.06
Daivobet® Gel Applied for 24 Hours-1.60
Daivobet® Gel Vehicle Applied for 24 Hours-0.31

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Change From Baseline in Infiltration at Day 4

Investigator's rating of the clinical appearance of infiltration. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 4

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.10
Daivobet® Gel Applied Then Removed After 20 Minutes-0.08
Daivobet® Gel Applied for 24 Hours-0.10
Daivobet® Gel Vehicle Applied for 24 Hours0.02

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Change From Baseline in Infiltration at Day 8

Investigator's rating of the clinical appearance of infiltration. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 8

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.33
Daivobet® Gel Applied Then Removed After 20 Minutes-0.33
Daivobet® Gel Applied for 24 Hours-0.38
Daivobet® Gel Vehicle Applied for 24 Hours0.00

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Change From Baseline in Scaling at Day 11

Investigator's rating of the clinical appearance of scaling. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 11

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.90
Daivobet® Gel Applied Then Removed After 20 Minutes-0.88
Daivobet® Gel Applied for 24 Hours-1.08
Daivobet® Gel Vehicle Applied for 24 Hours-0.35

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Change From Baseline in Scaling at Day 15

Investigator's rating of the clinical appearance of scaling. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 15

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-1.15
Daivobet® Gel Applied Then Removed After 20 Minutes-1.04
Daivobet® Gel Applied for 24 Hours-1.40
Daivobet® Gel Vehicle Applied for 24 Hours-0.42

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Change From Baseline in Scaling at Day 18

Investigator's rating of the clinical appearance of scaling. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 18

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-1.35
Daivobet® Gel Applied Then Removed After 20 Minutes-1.27
Daivobet® Gel Applied for 24 Hours-1.50
Daivobet® Gel Vehicle Applied for 24 Hours-0.48

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Change From Baseline in Scaling at Day 22

Investigator's rating of the clinical appearance of scaling. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 22

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-1.31
Daivobet® Gel Applied Then Removed After 20 Minutes-1.31
Daivobet® Gel Applied for 24 Hours-1.71
Daivobet® Gel Vehicle Applied for 24 Hours-0.54

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Change From Baseline in Scaling at Day 4

Investigator's rating of the clinical appearance of scaling. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 4

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.19
Daivobet® Gel Applied Then Removed After 20 Minutes-0.19
Daivobet® Gel Applied for 24 Hours-0.10
Daivobet® Gel Vehicle Applied for 24 Hours-0.08

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Change From Baseline in Scaling at Day 8

Investigator's rating of the clinical appearance of scaling. Maximum score is 3 (most severe); minimum score is 0 (absent). (NCT01607853)
Timeframe: Baseline to day 8

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.60
Daivobet® Gel Applied Then Removed After 20 Minutes-0.46
Daivobet® Gel Applied for 24 Hours-0.56
Daivobet® Gel Vehicle Applied for 24 Hours-0.06

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Change in Lesion Thickness Measured by Ultrasound From Baseline to Day 22.

(NCT01607853)
Timeframe: Baseline to day 22

Interventionmillimeters (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.61
Daivobet® Gel Applied Then Removed After 20 Minutes-0.80
Daivobet® Gel Applied for 24 Hours-0.90
Daivobet® Gel Vehicle Applied for 24 Hours-0.11

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Change in Skin Thickness - Echo-poor Band - Measured by Ultrasound From Baseline to Day 22

(NCT01607853)
Timeframe: Baseline to day 22

Interventionmillimeters (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-0.57
Daivobet® Gel Applied Then Removed After 20 Minutes-0.54
Daivobet® Gel Applied for 24 Hours-0.62
Daivobet® Gel Vehicle Applied for 24 Hours-0.06

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Change in Total Clinical Score at Day 11 Compared to Baseline

Investigator's rating of the clinical appearance of a psoriatic lesion. Maximum score is 9 (most severe); minimum score is 0 (least severe). The single items erythema, scaling, and infiltration (maximum score 3 each) are summed to obtain the Total Clinical Score. (NCT01607853)
Timeframe: Baseline to day 11

Interventionunits on a scale (Mean)
Daivobet® Gel Applied Then Removed After 10 Minutes-2.3
Daivobet® Gel Applied Then Removed After 20 Minutes-2.3
Daivobet® Gel Applied for 24 Hours-3.0
Daivobet® Gel Vehicle Applied for 24 Hours-0.7

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The Change in Circulating RAS Activity After Calcitriol/Placebo Therapy

The below results represent the change in Plasma Renin Activity. (NCT01635062)
Timeframe: baseline and 2 weeks following calcitriol/placebo therapy

Interventionng/mL/h (Median)
Calcitriol0
Placebo-1.3

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Change in Urine Protein After Calcitriol/Placebo Therapy

Subjects have their urine protein assessed at baseline while sodium loaded and again 3 weeks after randomized therapy with calcitriol or placebo. (NCT01635062)
Timeframe: baseline and 3 weeks following calcitriol/placebo therapy

Interventionmg/24h (Mean)
Calcitriol21.1
Placebo8.1

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Change in Renal Plasma Flow After Calcitriol/Placebo Therapy

Subjects had their renal plasma flow assessed at baseline while sodium loaded, and again after 3 weeks of randomized therapy with either calcitriol (up to 0.75 mcg daily) or placebo. (NCT01635062)
Timeframe: baseline and 3 weeks following calcitriol/placebo therapy

InterventionmL/min/1.73m2 (Mean)
Calcitriol-16.4
Placebo-0.6

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Plasma Interleukin-6 (IL-6) Levels at 48 Hours

(NCT01689441)
Timeframe: 48 hours

Interventionpg/ml (Median)
Calcitriol41
Placebo32

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Plasma Cathelicidin (hCAP18) Protein Levels at 48 Hours

(NCT01689441)
Timeframe: 48 hours

Interventionng/ml (Median)
Calcitriol76
Placebo82

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Urinary Neutrophil Gelatinase-associated Lipocalin (NGAL) / Creatinine Ratio at 48 Hours

NGAL is a urinary marker of renal tubular injury. NGAL levels were normalized to the urinary creatinine concentration to account for the influence of dilution on biomarker concentrations. (NCT01689441)
Timeframe: 48 hours

Interventionmg/mg (Median)
Calcitriol0.6
Placebo0.7

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Acne Severity as Assessed With the Investigator's Global Assessment (IGA)

Investigator's Global Assessment (IGA) is a 5-point scale of acne severity, ranging from 0 (Clear) to 4 (Severe) (NCT01694433)
Timeframe: Weeks 2, 4, 8 & 12

,
Interventionscore on a scale (Mean)
IGA at Week 2IGA at Week 4IGA at Week 8IGA at Week 12
Calcipotriene Cream2.772.832.212.23
Placebo2.92.592.482.31

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Lesion Counts (Total, Inflammatory and Non-inflammatory)

Lesion counts will be assessed by one of the investigator physicians or nurse practitioner. (NCT01694433)
Timeframe: Weeks 2, 4, 8 & 12

,
InterventionLesions (Mean)
Inflammatory lesions at Week 2Inflammatory lesions at Week 4Inflammatory lesions at Week 8Inflammatory lesions at Week 12Non-inflammatory lesions at Week 2Non-inflammatory lesions at Week 4Non-inflammatory lesions at Week 8Non-inflammatory lesions at Week 12Total lesions at Week 2Total lesions at Week 4Total lesions at Week 8Total lesions at Week 12
Calcipotriene Cream18.415.812.110.530.935.522.119.651.051.434.230.1
Placebo13.49.910.27.033.134.424.320.246.544.334.5527.24

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Subjective Subject Preference Survey for the Second Treatment Session

Subjective Subject Preference Survey The Subjective Subject Preference Survey consist of 15 questions relating to patients preference of study drug. The survey includes questions such as how the medication feels to touch, how greasy it is, and time it takes to apply. The final question asks patients to rate the overall appeal of the vehicle. Questions are scored on a 7-point scale, where a score of 1 is extremely unpleasant, 4 is neutral, and a score of 7 is extremely appealing. Total preference score based on the Subjective Subject Preference Survey could range from 15-105. (NCT01707043)
Timeframe: 3 days

Interventionunits on a scale (Mean)
Taclonex Scalp Suspension First Then Taclonex Ointment78.9
Taclonex Ointment First, Then Taclonex Scalp Suspension69.4

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Subjective Subject Preference Survey for the First Treatment Session

Subjective Subject Preference Survey The Subjective Subject Preference Survey consist of 15 questions relating to patients preference of study drug. The survey includes questions such as how the medication feels to touch, how greasy it is, and time it takes to apply. The final question asks patients to rate the overall appeal of the vehicle. Questions are scored on a 7-point scale, where a score of 1 is extremely unpleasant, 4 is neutral, and a score of 7 is extremely appealing. Total preference score based on the Subjective Subject Preference Survey could range from 15-105. (NCT01707043)
Timeframe: 3 days

Interventionunits on a scale (Mean)
Taclonex Scalp Suspension First Then Taclonex Ointment81.1
Taclonex Ointment First, Then Taclonex Scalp Suspension77.6

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Amount of Active Vitamin D Analog Used Through Month 3 Post Calcitriol Initiation

(NCT01725113)
Timeframe: Up to Month 6

Interventionmcg (Mean)
Calcitriol36.9

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Amount of Active Vitamin D Analog Used Through Month 3 Post Paricalcitol Initiation

(NCT01725113)
Timeframe: Up to Month 6

Interventionmcg (Mean)
Paricalcitol134.6

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Calcium Levels at Month 3 Post Calcitriol Treatment Initiation

(NCT01725113)
Timeframe: Up to Month 6

Interventionmg/dl (Mean)
Calcitriol8.78

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Calcium Levels at Month 3 Post Paricalcitol Treatment Initiation

(NCT01725113)
Timeframe: Up to Month 6

Interventionmg/dl (Mean)
Paricalcitol8.6

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Phosphorus Levels at Month 3 Post Calcitriol Initiation

(NCT01725113)
Timeframe: Up to Month 6

Interventionmg/dl (Mean)
Calcitriol4.09

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Phosphorus Levels at Month 3 Post Paricalcitol Initiation

(NCT01725113)
Timeframe: Up to Month 6

Interventionmg/dl (Mean)
Paricalcitol4.45

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PTH Levels at Month 3 Post Calcitriol Treatment Initiation

(NCT01725113)
Timeframe: Up to Month 6

Interventionpg/dl (Mean)
Calcitriol309.58

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PTH Levels at Month 3 Post Paricalcitol Treatment Initiation

(NCT01725113)
Timeframe: Up to Month 6

Interventionpg/dl (Mean)
Paricalcitol332.83

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Physician Global Assessement

"Percentage of participants with clear or almost clear skin on the PGA scale. 0 = clear~= almost clear~= mild~= moderate~= severe" (NCT01745133)
Timeframe: 10 weeks

Interventionpercentage of patients (Number)
Vehicle 68%68
Calcipotriene 80%80
Calcipotriene + Clobetasol Propionate 79%79

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Tmax of Calcitriol Plasma Level

Tmax of calcitriol plasma level at Day 14 (NCT01766440)
Timeframe: Day 14

Interventionhour (Mean)
Calcitriol 3 mcg/g Ointment1.46

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Cmax of Calcitriol Plasma Level

Cmax of calcitriol plasma level at Day 14 (Peak plasma concentration of calcitriol from Day 1 to Day 14) (NCT01766440)
Timeframe: Day 14

Interventionpg/mL (Mean)
Calcitriol 3 mcg/g Ointment120.7

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AUC (0-6h) of Calcitriol Plasma Level

AUC (0-6h) of calcitriol plasma level at Day 14 (Pre-dose to 6 hours post-dose) (NCT01766440)
Timeframe: Day 14

Interventionpg*h/mL (Mean)
Calcitriol 3 mcg/g Ointment650.3

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Cmin of Calcitriol Plasma Level

Cmin of calcitriol plasma level at Day 14 (NCT01766440)
Timeframe: Day 14

Interventionpg/mL (Mean)
Calcitriol 3 mcg/g Ointment92.6

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AUC (0-9h) of Calcitriol Plasma Level

AUC (0-9h) of calcitriol plasma level at Day 14 (Pre-dose to 9 hours post-dose. For subjects with a body weight of <15 kg, AUC (0-9h) was extrapolated based on the pre-dose to 6 hours post-dose PK samples.) (NCT01766440)
Timeframe: Day 14

Interventionpg*h/mL (Mean)
Calcitriol 3 mcg/g Ointment952.6

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AUC (0-12h) of Calcitriol Plasma Level

AUC (0-12h) of calcitriol plasma level at Day 14 (For subjects with a body weight of < 15 kg, AUC (0-9h) was extrapolated based on the pre-dose to 6 hours post dose PK samples. For subjects with a body weight of ≥ 15 kg, AUC (0-12h) was extrapolated based on the pre-dose to 9 hours post-dose PK samples.) (NCT01766440)
Timeframe: Day 14

Interventionpg*h/mL (Mean)
Calcitriol 3 mcg/g Ointment1268.9

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Millions of Sperm Per Ejaculate

Millions of sperm per ejaculate in men treated with 13-cis retinoic acid (NCT02061384)
Timeframe: Up to 20-weeks

InterventionMillions of sperm per ejaculate (Median)
13-cis Retinoic Acid2.5
Calcitriol 0.25 mcg3.8

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Change From Screening in Serum Phosphate Levels at Week 12

Change from screening (the last test prior to the first study medication application) in serum phosphate levels at week 12 were reported. (NCT02125279)
Timeframe: Screening, Week 12

Interventionmmol/L (Mean)
Calcitriol 3 mcg/g0.0237

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Change From Screening in Serum Phosphate Levels at Week 20

Change from screening (the last test prior to the first study medication application) in serum phosphate levels at week 20 were reported. (NCT02125279)
Timeframe: Screening, Week 20

Interventionmmol/L (Mean)
Calcitriol 3 mcg/g0.0079

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Change From Screening in Serum Phosphate Levels at Week 26

Change from screening (the last test prior to the first study medication application) in serum phosphate levels at week 26 were reported. (NCT02125279)
Timeframe: Screening, Week 26

Interventionmmol/L (Mean)
Calcitriol 3 mcg/g0.0091

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Change From Screening in Serum Phosphate Levels at Week 30 (Follow-up)

Change from screening (the last test prior to the first study medication application) in serum phosphate levels at week 30 were reported. (NCT02125279)
Timeframe: Screening, Week 30 (Follow-up)

Interventionmmol/L (Mean)
Calcitriol 3 mcg/g0.0145

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Change From Screening in Serum Phosphate Levels at Week 4

Change from screening (the last test prior to the first study medication application) in serum phosphate levels at week 4 were reported. (NCT02125279)
Timeframe: Screening, Week 4

Interventionmmol/L (Mean)
Calcitriol 3 mcg/g0.0334

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Change From Screening in Urine Calcium/Creatinine Ratio at Week 12

Change from screening (the last test prior to the first study medication application) in urine calcium/creatinine ratio at week 12 were reported. (NCT02125279)
Timeframe: Screening, Week 12

InterventionRatio (Mean)
Calcitriol 3 mcg/g-0.0164

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Change From Screening in Urine Calcium/Creatinine Ratio at Week 26

Change from screening (the last test prior to the first study medication application) in urine calcium/creatinine ratio at week 26 were reported. (NCT02125279)
Timeframe: Screening, Week 26

InterventionRatio (Mean)
Calcitriol 3 mcg/g0.0456

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Change From Screening in Urine Calcium/Creatinine Ratio at Week 30 (Follow-up)

Change from screening (the last test prior to the first study medication application) in urine calcium/creatinine ratio at week 30 were reported. (NCT02125279)
Timeframe: Screening, Week 30 (Follow-up)

InterventionRatio (Mean)
Calcitriol 3 mcg/g0.0715

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Number of Participants With Treatment Emergent Adverse Events (TEAEs)

An adverse event (AE) is any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product and which does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory value), symptom, or disease temporally associated with the use of a medicinal (investigational) product, whether or not related to the medicinal (investigational) product. A TEAE is defined as an AE with an onset date on or after the first application of the study drug. (NCT02125279)
Timeframe: Up to Week 30

InterventionParticipants (Count of Participants)
Calcitriol 3 mcg/g20

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Change From Baseline in Percent (%) Body Surface Area (BSA) at Each Visit

Percent BSA was calculated by modified rules of nines (pediatric participants). Estimate were made from the following for a child up to the age of one year: head and neck total for front and back - 18%; thorax and abdomen-front -18%; thorax and abdomen-back - 18%; each upper limb total for front and back - 9%; each lower limb total for front and back - 14%. For over the age of one year, the relative percentage of BSA changes as follows: the head decreases by 1% per year and the lower limbs increase by 0.5% per year. By the age of ten years, the relative proportions assume the values for adult BSA as follows: perineum becomes 1%; each lower limb becomes a total of 18% front and back; head and neck become 9% total for front and back. (NCT02125279)
Timeframe: Baseline, Weeks 4, 8, 12, 20, 26 and 30 (Follow-up)

InterventionPercent BSA (Mean)
Week 4Week 8Week 12Week 20Week 26Week 30
Calcitriol 3 mcg/g-1.3-2.5-3.4-4.4-3.9-4.7

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Change From Baseline in Pruritus Score at Each Visit

Pruritus was scored on a 0 to 4 point scale. Where, 0 = none (no-itching); 1 = mild (slight itching, not really bothersome); 2 = moderate (definite itching that is somewhat bothersome without loss of sleep); 3 = severe (intense itching that has caused pronounced discomfort, night rest interrupted); 4 = very severe (very severe itching that has caused pronounced discomfort during the night and daily activities). Positive change from baseline indicate worsening of indication. (NCT02125279)
Timeframe: Baseline, Weeks 4, 8, 12, 20, 26 and 30 (Follow-up)

InterventionUnits on a scale (Mean)
Week 4Week 8Week 12Week 20Week 26Week 30
Calcitriol 3 mcg/g-0.6-0.7-0.7-0.7-0.9-0.8

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Number of Participants With Investigator's Global Assessment of Disease Severity (IGA) Score of 0 (Clear) or 1 (Almost Clear) at Each Visit

The IGA is a 0 to 4 point scale. Where, 0 = clear (no signs of psoriasis except for residual hypopigmentation/hyperpigmentation); 1 = almost clear (just perceptible erythema, no induration, and no scaling); 2 = mild (mild erythema, no induration, and mild or no scaling); 3 = moderate (moderate erythema, mild induration, and mild or no scaling); 4 = severe (severe erythema, moderate to severe induration, and scaling of any degree). (NCT02125279)
Timeframe: Weeks 4, 8, 12, 20, 26 and 30 (Follow-up)

InterventionParticipants (Count of Participants)
Week 4Week 8Week 12Week 20Week 26Week 30
Calcitriol 3 mcg/g3515141917

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Change From Screening in Serum Albumin Levels at Week 4

Change from screening (the last test prior to the first study medication application) in serum albumin levels at week 4 were reported. (NCT02125279)
Timeframe: Screening, Week 4

Interventiongram per liter (g/L) (Mean)
Calcitriol 3 mcg/g-1.0

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Change From Screening in Serum Albumin Levels at Week 12

Change from screening (the last test prior to the first study medication application) in serum albumin levels at week 12 were reported. (NCT02125279)
Timeframe: Screening, Week 12

Interventiong/L (Mean)
Calcitriol 3 mcg/g-0.8

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Change From Screening in Serum Albumin Levels at Week 20

Change from screening (the last test prior to the first study medication application) in serum albumin levels at week 20 were reported. (NCT02125279)
Timeframe: Screening, Week 20

Interventiong/L (Mean)
Calcitriol 3 mcg/g-1.1

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Change From Screening in Serum Albumin Levels at Week 26

Change from screening (the last test prior to the first study medication application) in serum albumin levels at week 26 were reported. (NCT02125279)
Timeframe: Screening, Week 26

Interventiong/L (Mean)
Calcitriol 3 mcg/g-0.8

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Change From Screening in Serum Albumin Levels at Week 30 (Follow-up)

Change from screening (the last test prior to the first study medication application) in serum albumin levels at week 30 were reported. (NCT02125279)
Timeframe: Screening, Week 30 (Follow-up)

Interventiong/L (Mean)
Calcitriol 3 mcg/g-0.2

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Change From Screening in Serum Albumin Levels at Week 8

Change from screening (the last test prior to the first study medication application) in serum albumin levels at week 8 were reported. (NCT02125279)
Timeframe: Screening, Week 8

Interventiong/L (Mean)
Calcitriol 3 mcg/g-1.0

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Change From Screening in Serum Parathyroid Hormone (PTH) Levels at Week 4

Change from screening (the last test prior to the first study medication application) in serum PTH levels at week 4 were reported. (NCT02125279)
Timeframe: Screening, Week 4

InterventionPicomole per liter (pmol/L) (Mean)
Calcitriol 3 mcg/g0.14

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Change From Screening in Serum Parathyroid Hormone Levels at Week 12

Change from screening (the last test prior to the first study medication application) in serum PTH levels at week 12 were reported. (NCT02125279)
Timeframe: Screening, Week 12

Interventionpmol/L (Mean)
Calcitriol 3 mcg/g0.04

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Change From Screening in Serum Parathyroid Hormone Levels at Week 20

Change from screening (the last test prior to the first study medication application) in serum PTH levels at week 20 were reported. (NCT02125279)
Timeframe: Screening, Week 20

Interventionpmol/L (Mean)
Calcitriol 3 mcg/g0.17

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Change From Screening in Serum Parathyroid Hormone Levels at Week 26

Change from screening (the last test prior to the first study medication application) in serum PTH levels at week 26 were reported. (NCT02125279)
Timeframe: Screening, Week 26

Interventionpmol/L (Mean)
Calcitriol 3 mcg/g-0.07

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Change From Screening in Serum Parathyroid Hormone Levels at Week 30 (Follow-up)

Change from screening (the last test prior to the first study medication application) in serum PTH levels at week 30 were reported. (NCT02125279)
Timeframe: Screening, Week 30 (Follow-up)

Interventionpmol/L (Mean)
Calcitriol 3 mcg/g0.37

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Change From Screening in Serum Parathyroid Hormone Levels at Week 8

Change from screening (the last test prior to the first study medication application) in serum PTH levels at week 8 were reported. (NCT02125279)
Timeframe: Screening, Week 8

Interventionpmol/L (Mean)
Calcitriol 3 mcg/g0.09

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Success of Investigator's Global Assessment (IGA)

"The number of subjects with a minimum improvement of 2 grades from baseline in the IGA score and a severity rating of 0 (clear) of 1 (almost clear) at Week 8 (LOCF).~The IGA was evaluated at each visit on the following 0 to 4 point scale:~0 - Clear: No signs of psoriasis except for residual hypopigmentation / hyperpigmentation~- Almost Clear: Just perceptible erythema, no induration, and no scaling~- Mild: Mild erythema, no induration, and mild or no scaling~- Moderate: Moderate erythema, mild induration, and mild or no scaling~- Severe: Severe erythema, moderate to severe induration, and scaling of any degree" (NCT02186665)
Timeframe: Baseline to Week 8

InterventionParticipants (Count of Participants)
Calcitriol Ointment3
Placebo7

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Area Under the Curve (AUC) of Psoriatic Skin Thickness/EPB

The AUC of psoriatic skin thickness/EPB from Day 1 to Day 12 was determined using the linear trapezoidal rule. The mean raw values are reported. (NCT02193815)
Timeframe: Day 1 (baseline) up to Day 12

Interventionmicrometers*day (Mean)
PF-06263276 4% Solution4082.60
PF-06263276 Vehicle4161.40
Tofacitinib 2% Ointment3271.93
Tofacitinib Vehicle4013.07
Daivonex Solution3322.40
Daivonex Ointment3165.47

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Change From Baseline in Psoriatic Skin Thickness/Echo-Poor Band (EPB) for PF-06263276 4% Solution in Comparison to Corresponding Vehicle at Day 12

Psoriatic skin thickness was measured using a 20 megahertz (MHz) high frequency sonograph. Serial A-scans were composed and presented on a monitor as a section of the skin. (NCT02193815)
Timeframe: Day 1 (Baseline), Day 12

,
Interventionmicrometers (Mean)
BaselineChange at Day 12
PF-06263276 4% Solution358.917.7
PF-06263276 Vehicle353.132.9

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Change From Baseline in Psoriatic Skin Thickness/EPB at Day 8

(NCT02193815)
Timeframe: Day 1 (Baseline), Day 8

,,,,,
Interventionmicrometers (Mean)
BaselineChange at Day 8
Daivonex Ointment364.1-104.7
Daivonex Solution376.1-98.8
PF-06263276 4% Solution358.918.0
PF-06263276 Vehicle353.138.5
Tofacitinib 2% Ointment364.1-90.5
Tofacitinib Vehicle357.315.1

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Change From Baseline in Psoriatic Skin Thickness/EPB for PF-06263276 4% Solution in Comparison to Daivonex Solution at Day 12

(NCT02193815)
Timeframe: Day 1 (Baseline), Day 12

Interventionmicrometers (Mean)
PF-06263276 4% Solution17.7
Daivonex Solution-135.5

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Number of Participants With Treatment-Emergent Adverse Events (AEs) or Serious Adverse Events (SAEs): Specified Skin AEs

An AE was any untoward medical occurrence in a participant who received study drug. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. Treatment-emergent are events between first dose of study drug and up to 28 days after last dose that were absent before treatment or that worsened relative to pre-treatment state. AEs included both SAEs and non-SAEs. The number of participants with specified skin AEs was reported. (NCT02193815)
Timeframe: Baseline up to 28 days after last study drug administration (Day 21)

,,,,,
Interventionparticipants (Number)
Specified Skin AEsSpecified Skin SAEs
Daivonex Ointment20
Daivonex Solution00
PF-06263276 4% Solution00
PF-06263276 Vehicle00
Tofacitinib 2% Ointment00
Tofacitinib Vehicle00

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Number of Participants With Potentially Clinically Significant Vital Signs Findings

Vital signs assessment included pulse rate and blood pressure. Criteria for vital sign values meeting potential clinical concern included: supine/sitting pulse rate <40 or >120 beats per minute (bpm), standing pulse rate <40 or >140 bpm; systolic blood pressure (SBP) >=30 millimeters of mercury (mmHg) change from baseline in same posture or SBP <90 mmHg, diastolic blood pressure (DBP) >=20 mmHg change from baseline in same posture or DBP <50 mmHg. (NCT02193815)
Timeframe: Baseline up to Day 12

Interventionparticipants (Number)
SBP <90 mmHgDBP <50 mmHgPulse Rate <40 or >120 bpmMaximum Increase from Baseline in SBP >=30 mmHgMaximum Increase from Baseline in DBP >=20 mmHg
All Participants00000

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Global Clinical Assessment at Day 1, 8 and 12

"Global Clinical Assessment of the test fields was performed by visual examination using a 5-point score (-1=worsened; 0=unchanged [no effect]; 1=slight improvement; 2=clear improvement but not completely healed; 3=completely healed). Clinically apparent differences in erythema and infiltration will contribute to this global assessment. At baseline (Day 1), the score was documented as 0 (unchanged)." (NCT02193815)
Timeframe: Day 1, Day 8, Day 12

,,,,,
Interventionparticipants (Number)
Day 1: Score -1Day 1: Score 0Day 1: Score 1Day 1: Score 2Day 1: Score 3Day 8: Score -1Day 8: Score 0Day 8: Score 1Day 8: Score 2Day 8: Score 3Day 12: Score -1Day 12: Score 0Day 12: Score 1Day 12: Score 2Day 12: Score 3
Daivonex Ointment0150000168012480
Daivonex Solution0150001194011670
PF-06263276 4% Solution015000013200013200
PF-06263276 Vehicle015000015000015000
Tofacitinib 2% Ointment0150000483004830
Tofacitinib Vehicle015000014010011310

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Change From Baseline in Psoriatic Skin Thickness/EPB for Tofacitinib 2% Ointment in Comparison to Corresponding Vehicle at Day 12

(NCT02193815)
Timeframe: Day 1 (Baseline), Day 12

,
Interventionmicrometers (Mean)
BaselineChange at Day 12
Tofacitinib 2% Ointment364.1-117.8
Tofacitinib Vehicle357.30.1

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Number of Participants With Laboratory Abnormalities Meeting the Criteria for Potential Clinical Concern

The following laboratory parameters were analyzed: hematology (hemoglobin, hematocrit, red blood cell [RBC] count, RBC morphology, platelet count, white blood cell [WBC] count, total neutrophils, eosinophils, monocytes, basophils, lymphocytes); blood chemistry (blood urea nitrogen [BUN], creatinine, glucose, calcium, sodium, potassium, chloride, total bicarbonate, aspartate aminotransferase [AST], alanine aminotransferase [ALT], total bilirubin, alkaline phosphatase, uric acid, albumin, and total protein; urinalysis (pH, glucose, protein, blood, ketones, nitrites, leukocyte esterase, urobilinogen, urine bilirubin, microscopy [if urine dipstick was positive for blood, protein, nitrites or leukocyte esterase]); others (e.g., urine human chorionic gonadotropin [hCG] for females of childbearing potential). (NCT02193815)
Timeframe: Baseline up to Day 12

Interventionparticipants (Number)
All Participants6

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Number of Participants in the Intent to Treat Population With Normal Serum 25-hydroxyvitamin D at End of Treatment (EOT)

Number of Participants in the Intent to Treat Population with serum 25-hydroxyvitamin D >/= 30 ng/mL at End of Treatment (EOT) (NCT02282813)
Timeframe: up to 6 months

Interventionparticipants (Number)
CTAP101 Capsules (Not Randomized; 6 Mos Treatment)87
CTAP101 Capsules (Not Randomized; 12 Mos Treatment)124
CTAP101 Caps 2 x 30 mcg Daily for 12 wk+Adjunctive38

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Number of Participants in the Per Protocol Population With Mean Reduction in Plasma Intact Parathyroid Hormone (iPTH) of >/= 30% From Baseline Values at End of Treatment (EOT)

Number of subjects in the per protocol population with a mean reduction in plasma intact parathyroid hormone (iPTH) of >/= 30% from pretreatment baseline values at end of treatment (EOT), classified as responders (NCT02282813)
Timeframe: up to 6 months

Interventionparticipants (Number)
CTAP101 Capsules (Not Randomized; 6 Mos Treatment)34
CTAP101 Capsules (Not Randomized; 12 Mos Treatment)64
CTAP101 Caps 2 x 30 mcg Daily for 12 wk+Adjunctive29

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Number of Participants in the Per Protocol Population With NormalSerum 25-hydroxyvitamin D at End of Treatment (EOT)

Number of Participants in the per protocol population with serum 25-hydroxyvitamin D >/= 30 ng/mL at End of Treatment (EOT) (NCT02282813)
Timeframe: up to 6 months

Interventionparticipants (Number)
CTAP101 Capsules (Not Randomized; 6 Mos Treatment)86
CTAP101 Capsules (Not Randomized; 12 Mos Treatment)120
CTAP101 Caps 2 x 30 mcg Daily for 12 wk+Adjunctive37

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Number of Participants in the Intent to Treat Population With a Mean Reduction in Plasma Intact Parathyroid Hormone (iPTH) of >/= 30% From Baseline Values at End of Treatment (EOT)

Number of subjects in the intent to treat population with a mean reduction in plasma intact parathyroid hormone (iPTH) of >/= 30% from pretreatment baseline values at end of treatment (EOT), classified as responders (NCT02282813)
Timeframe: up to 6 months

Interventionparticipants (Number)
CTAP101 Capsules (Not Randomized; 6 Mos Treatment)34
CTAP101 Capsules (Not Randomized; 12 Mos Treatment)66
CTAP101 Caps 2 x 30 mcg Daily for 12 wk+Adjunctive30

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Death Within 7 Days

All-cause mortality within 7 days following randomization (NCT02962102)
Timeframe: 7 days

InterventionParticipants (Count of Participants)
Calcifediol4
Calcitriol9
Placebo6

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Number of Participants Who Received Renal Replacement Therapy Within 7 Days

Number of participants who received renal replacement therapy within 7 days following randomization (NCT02962102)
Timeframe: 7 days

InterventionParticipants (Count of Participants)
Calcifediol1
Calcitriol1
Placebo4

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Number of Participants With New or Worsening Stage of AKI, Defined by KDIGO Guidelines

Any of the following: 1) an increase in serum creatinine ≥50% compared to the immediate pre-randomization value; 2) new or progressive stage of oliguria; or 3) receipt of renal replacement therapy. Oliguria stages 1, 2, and 3 are defined as urine output (UOP) <0.5 ml/kg/h for 6-12h, <0.5 ml/kg/h for >12h, and <0.3 ml/kg/h for ≥24h or anuria for ≥12h, respectively. (NCT02962102)
Timeframe: 7 days

InterventionParticipants (Count of Participants)
Calcifediol20
Calcitriol23
Placebo19

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Peak Serum Creatinine (mg/dl)

Highest serum creatinine value on days 1 to 7 (NCT02962102)
Timeframe: 7 days

Interventionmg/dl (Median)
Calcifediol1.2
Calcitriol1.3
Placebo1.2

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28-day Mortality

All-cause mortality assessed during the 28 days following randomization (NCT02962102)
Timeframe: 28 days

InterventionParticipants (Count of Participants)
Calcifediol10
Calcitriol16
Placebo10

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ICU- and Hospital-free Days

28 minus the number of days in the ICU or hospital, with 0 assigned to patients who die before 28 days (NCT02962102)
Timeframe: 28 days

,,
InterventionDays (Median)
ICU-free daysHospital-free days
Calcifediol205
Calcitriol164
Placebo110

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Relative Average Change in Serum Creatinine From Day 0 to Days 1-7

Average percentage change in serum creatinine assessed on days 1-7 as compared to day 0 (NCT02962102)
Timeframe: 7 days

InterventionRelative average percent increase (Median)
Calcifediol-2.3
Calcitriol-7.1
Placebo-7.4

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Toxicity and Tolerability of Experimental Arm

Descriptive analysis of observed toxicity and patient reports of tolerating experimental treatment (NCT03261336)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
Calcitriol, Ketoconazole, Hydrocortisone1

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Sniff Nasal Inspiratory Pressure (SNIP)

SNIP is a test of maximal inspiratory muscle force exerting from the diaphram. Patients sniff forcefully through one nostril while the other is obstructed. The best of 10 measurements is recorded. (NCT03469271)
Timeframe: 8 weeks

InterventioncmH20 (Mean)
Training and Placebo90
Sham Training and Vitamin D3 Metabolite87
Training and Vitamin D3 Metabolite89
Sham Training and Placebo109

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Insulin Level

Blood will be obtained to measure insulin level after a glucose tolerance test. The glucose tolerance test involves an overnight fast and then participants will ingest a drink containing 75 grams of glucose with blood obtained over a 120 minute period. (NCT04286529)
Timeframe: Baseline and 8 weeks

,,,
InterventionuIU/mL (Mean)
Baseline8 Weeks
Men-Calcitriol4.75
Men-Placebo33
Premenopausal Women-Calcitriol4.64
Premenopausal Women-Placebo2.44

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Glucose Levels

Blood will be obtained to measure glucose after a glucose tolerance test. The glucose tolerance test involves an overnight fast and then participants will ingest a drink containing 75 grams of glucose with blood obtained over a 120 minute period. (NCT04286529)
Timeframe: Baseline and 8 weeks

,,
Interventionmg/dL (Mean)
Baseline8 weeks
Men-Calcitriol9098
Men-Placebo8985
Premenopausal Women-Calcitriol7685

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Glucose Levels

Blood will be obtained to measure glucose after a glucose tolerance test. The glucose tolerance test involves an overnight fast and then participants will ingest a drink containing 75 grams of glucose with blood obtained over a 120 minute period. (NCT04286529)
Timeframe: Baseline and 8 weeks

Interventionmg/dL (Mean)
Baseline
Premenopausal Women-Placebo82

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C-Peptide Level

Blood will be obtained to measure c-peptide level after a glucose tolerance test. The glucose tolerance test involves an overnight fast and then participants will ingest a drink containing 75 grams of glucose with blood obtained over a 120 minute period. (NCT04286529)
Timeframe: Baseline and 8 weeks

,,,
Interventionnmol/L (Mean)
Baseline8 Weeks
Men-Calcitriol0.60.74
Men-Placebo0.70.49
Premenopausal Women-Calcitriol0.50.55
Premenopausal Women-Placebo0.50.52

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