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Details

Stereochemistry ABSOLUTE
Molecular Formula C30H50O5
Molecular Weight 490.715
Optical Activity UNSPECIFIED
Defined Stereocenters 7 / 7
E/Z Centers 2
Charge 0

SHOW SMILES / InChI
Structure of ELDECALCITOL

SMILES

[H][C@@]1(CC[C@@]2([H])\C(CCC[C@]12C)=C\C=C3\C[C@@H](O)[C@@H](OCCCO)[C@H](O)C3=C)[C@H](C)CCCC(C)(C)O

InChI

InChIKey=FZEXGDDBXLBRTD-AYIMTCTASA-N
InChI=1S/C30H50O5/c1-20(9-6-15-29(3,4)34)24-13-14-25-22(10-7-16-30(24,25)5)11-12-23-19-26(32)28(27(33)21(23)2)35-18-8-17-31/h11-12,20,24-28,31-34H,2,6-10,13-19H2,1,3-5H3/b22-11+,23-12-/t20-,24-,25+,26-,27-,28-,30-/m1/s1

HIDE SMILES / InChI

Molecular Formula C30H50O5
Molecular Weight 490.715
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 7 / 7
E/Z Centers 2
Optical Activity UNSPECIFIED

Description

Eldecalcitol (1α, 25-dihydroxy-2β-[3-hydroxypropyloxy] vitamin D3; ED-71) is an analog of the active form of vitamin D. Eldecalcitol has a hydroxypropyloxy group at the 2β-position of 1,25(OH)2D3. Compared with 1,25(OH)2D3, eldecalcitol has a higher affinity for serum vitamin D-binding protein (DBP), binds more weakly to vitamin D receptor, and shows lower potency in suppression of serum parathyroid hormone. The plasma half-life of eldecalcitol is longer than that of 1,25(OH)2D3, probably due to the higher affinity for DBP. In addition to regulation of calcium metabolism carried out by conventional vitamin D analogs, eldecalcitol possesses a strong inhibitory effect on bone resorption and causes a significant increase in bone mineral density. EDIROL (Eldecalcitol) has been approved for the treatment of osteoporosis in Japan.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
EDIROL

Cmax

ValueDoseCo-administeredAnalytePopulation
95.37 pg/mL
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
100.42 pg/mL
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
61.3 pg/mL
0.5 μg single, oral
ELDECALCITOL serum
Homo sapiens
104.3 pg/mL
1 μg single, oral
ELDECALCITOL serum
Homo sapiens
30.6 pg/mL
0.25 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
30.6 pg/mL
0.1 μg 1 times / day steady-state, oral
ELDECALCITOL serum
Homo sapiens
61 pg/mL
0.5 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
115.5 pg/mL
1 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
37.9 pg/mL
0.1 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
107.9 pg/mL
0.25 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
195.4 pg/mL
0.5 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
407.9 pg/mL
1 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
99.66 pg/mL
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
73.85 pg/mL
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
80.9 pg/mL
0.75 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
243.5 pg/mL
0.75 μg 1 times / day steady-state, oral
ELDECALCITOL serum
Homo sapiens
99.83 pg/mL
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
6977.4 pg × h/mL
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
6956.2 pg × h/mL
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
2086.6 pg × h/mL
0.5 μg single, oral
ELDECALCITOL serum
Homo sapiens
4545.1 pg × h/mL
1 μg single, oral
ELDECALCITOL serum
Homo sapiens
778 pg × h/mL
0.1 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
2180 pg × h/mL
0.25 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
3988 pg × h/mL
0.5 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
8496 pg × h/mL
1 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
5996.1 pg × h/mL
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
5076.8 pg × h/mL
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
1368 pg × h/mL
0.75 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
4964 pg × h/mL
0.75 μg 1 times / day steady-state, oral
ELDECALCITOL serum
Homo sapiens
6560.7 pg × h/mL
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
56.89 h
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
55.84 h
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
52.5 h
1 μg single, oral
ELDECALCITOL serum
Homo sapiens
55.1 h
0.25 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
51.9 h
0.5 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
54.3 h
1 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
48.03 h
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
45.88 h
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens
48.4 h
0.75 μg 1 times / day multiple, oral
ELDECALCITOL serum
Homo sapiens
48.7 h
0.75 μg 1 times / day steady-state, oral
ELDECALCITOL serum
Homo sapiens
52.99 h
0.75 μg single, oral
ELDECALCITOL serum
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
3.8%
ELDECALCITOL serum
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
In general, for adults, take 0.75mcg of EDIROL (Eldecalcitol) once a day. It should be decreased according to your symptoms. 1 capsule contains 0.5mcg of the active ingredient.
Route of Administration: Oral
In Vitro Use Guide
Gene expression was analyzed in chondrocytes that were isolated from wildtype neonatal mice, cultured, and treated with ED-71 (Eldecalcitol) (10 nM). In primary chondrocytes cultured with ED-71, the gene expression of Erg and lubricin/proteoglycan 4 significantly increased, as compared to that of cells cultured without ED-71.
Substance Class Chemical
Record UNII
I2JP8UE90H
Record Status Validated (UNII)
Record Version