ELDECALCITOL

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 Search

SMILES

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

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

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	7 / 7
E/Z Centers	2
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24101867 | https://www.chugai-pharm.co.jp/english/news/detail/20110121150000.html

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 Target	Pharmacology	Condition	Potency
Vitamin D receptor 25 Target ID: CHEMBL1977 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24101867	Agonist 2752
Vitamin D-binding protein 2 Target ID: CHEMBL2259 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24101867	Binding Agent 1076

Conditions

Condition	Modality	Targets	Highest Phase	Product
Osteoporosis 101 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21902297 https://www.ncbi.nlm.nih.gov/pubmed/24101867	Primary		Approved 8583	EDIROL Approved Use EDIROL (Eldecalcitol) is indicated for the treatment of osteoporosis. Launch Date 2011

C_max

Value	Dose	Analyte	Population
95.37 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=34 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=351	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
100.42 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=34 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=351	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
61.3 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=380	0.5 μg single, oral dose: 0.5 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
104.3 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=380	1 μg single, oral dose: 1 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
30.6 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	0.25 μg 1 times / day multiple, oral dose: 0.25 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
30.6 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	0.1 μg 1 times / day steady-state, oral dose: 0.1 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
61 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	0.5 μg 1 times / day multiple, oral dose: 0.5 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
115.5 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	1 μg 1 times / day multiple, oral dose: 1 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
37.9 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	0.1 μg 1 times / day multiple, oral dose: 0.1 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
107.9 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	0.25 μg 1 times / day multiple, oral dose: 0.25 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
195.4 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	0.5 μg 1 times / day multiple, oral dose: 0.5 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
407.9 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	1 μg 1 times / day multiple, oral dose: 1 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
99.66 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=404	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
73.85 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=404	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
80.9 pg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/450045_3112006M1022_1_010_1F.pdf#page=25 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=418	0.75 μg 1 times / day multiple, oral dose: 0.75 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
243.5 pg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/450045_3112006M1022_1_010_1F.pdf#page=25 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=418	0.75 μg 1 times / day steady-state, oral dose: 0.75 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
99.83 pg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/450045_3112006M1022_1_010_1F.pdf#page=25 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=349	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
6977.4 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=34 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=351	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
6956.2 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=34 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=351	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2086.6 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=380	0.5 μg single, oral dose: 0.5 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4545.1 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=380	1 μg single, oral dose: 1 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
778 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	0.1 μg 1 times / day multiple, oral dose: 0.1 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
2180 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	0.25 μg 1 times / day multiple, oral dose: 0.25 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
3988 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	0.5 μg 1 times / day multiple, oral dose: 0.5 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
8496 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	1 μg 1 times / day multiple, oral dose: 1 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
5996.1 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=404	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5076.8 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=404	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1368 pg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/450045_3112006M1022_1_010_1F.pdf#page=25 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=418	0.75 μg 1 times / day multiple, oral dose: 0.75 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
4964 pg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/450045_3112006M1022_1_010_1F.pdf#page=25 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=418	0.75 μg 1 times / day steady-state, oral dose: 0.75 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
6560.7 pg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/450045_3112006M1022_1_010_1F.pdf#page=25 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=349	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
56.89 h OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=34 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=351	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
55.84 h OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=34 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=351	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
52.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=380	1 μg single, oral dose: 1 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
55.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	0.25 μg 1 times / day multiple, oral dose: 0.25 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
51.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \|https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	0.5 μg 1 times / day multiple, oral dose: 0.5 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
54.3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=37 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=38 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=390	1 μg 1 times / day multiple, oral dose: 1 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
48.03 h OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=404	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
45.88 h OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=40 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=404	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
48.4 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/450045_3112006M1022_1_010_1F.pdf#page=25 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=418	0.75 μg 1 times / day multiple, oral dose: 0.75 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
48.7 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/450045_3112006M1022_1_010_1F.pdf#page=25 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=418	0.75 μg 1 times / day steady-state, oral dose: 0.75 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
52.99 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/450045_3112006M1022_1_010_1F.pdf#page=25 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_K100_1.pdf#page=349	0.75 μg single, oral dose: 0.75 μg route of administration: Oral experiment type: SINGLE co-administered:	ELDECALCITOL serum	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
3.8% OTHER GOV'T https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_A100_1.pdf#page=36 \| https://www.pmda.go.jp/drugs/2011/P201100025/450045000_22300AMX00416_I100_1.pdf#page=49			ELDECALCITOL serum	Homo sapiens

Doses

Dose	Population	Adverse events
0.75 ug single, oral Highest studied dose Dose: 0.75 ug Route: oral Route: single Dose: 0.75 ug Sources: https://pubmed.ncbi.nlm.nih.gov/30117129/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/30117129/	Other AEs: Alanine aminotransferase increased, Aspartate aminotransferase increased... Other AEs: Alanine aminotransferase increased (2 patients) Aspartate aminotransferase increased (1 pt) Lactate dehydrogenase increased (1 pt) Leucocyte count increased (1 pt) Neutrophil count increased (1 pt) Triglyceride increased (1 pt) Leukocyturia (1 pt) Urobilinogenuria (1 pt) Dry pharynx (1 pt) Rash (1 pt) Diarrhea (1 pt) Sources: https://pubmed.ncbi.nlm.nih.gov/30117129/
0.75 ug 1 times / day steady-state, oral Studied dose Dose: 0.75 ug, 1 times / day Route: oral Route: steady-state Dose: 0.75 ug, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24101867/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/24101867/	Other AEs: Nasopharyngitis, Contusion... Other AEs: Nasopharyngitis (62.9%) Contusion (22.5%) Urine calcium increased (25.6%) Blood calcium increased (21%) Back pain (13.6%) Osteoarthritis (15.5%) Arthralgia (10.2%) Eczema (10.2%) Constipation (7.4%) Headache (9.7%) Diarrhea (9.5%) Gastroenteritis (8.7%) Periarthritis (8.5%) Spinal fracture (7.2%) Cystitis (6.8%) Hypertension (7.8%) Gastritis (6.4%) Pain in extremity (5.9%) Stomatitis (7%) Dermatitis contact (7.2%) Insomnia (6.4%) Dizziness (5.5%) Cataract (6.1%) Joint sprain (5.5%) Spinal osteoarthritis (4.4%) Stomach discomfort (5.1%) Exanthem (2.8%) Death (grade 5, 0.8%) Cancer (2.1%) Urolithiasis (1.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/24101867/

AEs

PubMed

Title	Date	PubMed
Effect of eldecalcitol on articular cartilage through the regulation of transcription factor Erg in a murine model of knee osteoarthritis.	2018-01-01	29097208
Treatment of osteoporosis with eldecalcitol, a new vitamin D analog: a comprehensive review and meta-analysis of randomized clinical trials.	2016	26869769
Eldecalcitol, a vitamin D analog, reduces bone turnover and increases trabecular and cortical bone mass, density, and strength in ovariectomized cynomolgus monkeys.	2013-11	23774444
Eldecalcitol for the treatment of osteoporosis.	2013	24101867
Spotlight on eldecalcitol in osteoporosis.	2012-01-01	22191725
Eldecalcitol: a review of its use in the treatment of osteoporosis.	2011-09-10	21902297
Hydrogen/deuterium exchange reveals distinct agonist/partial agonist receptor dynamics within vitamin D receptor/retinoid X receptor heterodimer.	2010-10-13	20947021
A new active vitamin D, ED-71, increases bone mass in osteoporotic patients under vitamin D supplementation: a randomized, double-blind, placebo-controlled clinical trial.	2005-09	15972580
Synthetic studies of vitamin D analogues. XIV. Synthesis and calcium regulating activity of vitamin D3 analogues bearing a hydroxyalkoxy group at the 2 beta-position.	1993-06	8396500

Patents

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 Created by `admin` on `Mon Mar 31 18:34:18 GMT 2025` Edited by `admin` on `Mon Mar 31 18:34:18 GMT 2025`
Record UNII	I2JP8UE90H
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ELDECALCITOL

Official Name

English

ED-71

Preferred Name

English

Eldecalcitol [WHO-DD]

Common Name

English

(5Z,7E)-2.BETA.-(3-HYDROXYPROPOXY)-9,10-SECOCHOLESTA-5,7,10(19)-TRIENE-1.ALPHA.,3.BETA.,25-TRIOL

Common Name

English

eldecalcitol [INN]

Common Name

English

ELDECALCITOL [MI]

Common Name

English

ELDECALCITOL [JAN]

Common Name

English

ELDECALCITOL [MART.]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C39713