Calcifediol Anhydrous

Summary

Calcifediol Anhydrous (CHEMBL1040) is an approved small-molecule bone density conservation agent.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Clinical trials: 16
• Chemistry: 400.6 Da · C27H44O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1040
Name	Calcifediol Anhydrous
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5283731
ChEBI	CHEBI:17933
Molecular formula	C27H44O2
Molecular weight	400.6
InChIKey	JWUBBDSIWDLEOM-DTOXIADCSA-N

SMILES: C[C@H](CCCC(C)(C)O)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](CCC3=C)O)C

IUPAC name: (1S,3Z)-3-[(2E)-2-[(1R,3aS,7aR)-1-[(2R)-6-hydroxy-6-methylheptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexan-1-ol

ChEBI definition: A hydroxycalciol that is calciol in which the hydrogen at position 25 has been replaced by a hydroxy group. A prehormone resulting from the oxidation of calciol in the liver, it is further hydroxylated in the kidney to give calcitriol, the active form of vitamin D3.

Pharmacological roles (ChEBI): bone density conservation agent, nutraceutical.

Other ChEBI roles (chemical / environmental): metabolite, human metabolite, mouse metabolite.

Also known as: Calcifediol anhydrous, Calcifediol, anhydrous, SID26754888, SID50110817, SID144205540, CALCIFEDIOL, calcifediol, Calcidiol

Parent form; salt/anhydrous children: CHEMBL3544909, CHEMBL4594399

Patent coverage: 2,670 distinct patent families (8,496 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Nuclear receptor ROR-gamma, Sterol regulatory element-binding protein 1, Vitamin D3 receptor.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 5 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P48281	6.22	EC50	600	nM	CHEMBL_ACT_19167917
SREBF1	5.93	IC50	1176	nM	CHEMBL_ACT_23217972
P51450	5.4	Potency	3981	nM	CHEMBL_ACT_4770137
P51450	5.15	Potency	7080	nM	CHEMBL_ACT_4774379

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

0 indication records carry no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 16.

Phase distribution

Phase	Trials
PHASE4	4
PHASE2	4
Not specified	4
PHASE2/PHASE3	2
PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06258850	PHASE4	NOT_YET_RECRUITING	REstoration of VItamin D in Pulmonary Arterial Hypertension
NCT01939977	PHASE4	COMPLETED	Efficacy and Safety of Paricalcitol in the Reduction of Secondary Hyperparathyroidism After Kidney Transplantation.
NCT02805907	PHASE4	COMPLETED	Efficacy of Calcifediol Supplementation in Asthma Control in Asthmatic Patients With Vitamin D Deficiency (ACViD)
NCT03588884	PHASE4	COMPLETED	Repeated-dose Safety, Efficacy, Pharmacokinetic and Pharmacodynamic of CTAP101, Immediate-release Calcifediol, High-dose Cholecalciferol, and Paricalcitol Plus Low-dose Cholecalciferol in Patients With Secondary Hyperparathyroidism, Chronic Kidney Disease 3-4 and Vitamin D Insufficiency
NCT02548364	PHASE3	COMPLETED	Effect of Vitamin D on Ventricular Remodeling in Patients With Acute Myocardial Infarction (VITDAMI)
NCT04386850	PHASE2/PHASE3	UNKNOWN	Oral 25-hydroxyvitamin D3 and COVID-19
NCT04735926	PHASE2/PHASE3	COMPLETED	Efficacy and Safety of Calcifediol vs Placebo in Subjects With Vitamin D Deficiency
NCT02527668	PHASE2	COMPLETED	To Test the Effect of Calcifediol Hy.D Supplementation on Muscle Function and Bone Quality in Younger Postmenopausal Women With Osteopenia
NCT02962102	PHASE2	COMPLETED	Activated Vitamin D for the Prevention and Treatment of Acute Kidney Injury
NCT03602261	PHASE2	TERMINATED	Safety, Efficacy, PK and PD of CTAP101 (Calcifediol) ER Capsules for SHPT in HD Patients VDI
NCT04366908	PHASE2	COMPLETED	Prevention and Treatment With Calcifediol of COVID-19 Induced Acute Respiratory Syndrome
NCT03401541	EARLY_PHASE1	COMPLETED	25-Hydroxyvitamin D Pharmacokinetic Study
NCT01398202	Not specified	COMPLETED	Dietary Supplementation With 25-hydroxyvitamin D3 in Older Adults
NCT02349282	Not specified	COMPLETED	The Effect of Calcifediol (Hy.D 25 SD/S) and Vitamin D3 on Muscle Strength in a Frail Elderly Population
NCT05819918	Not specified	COMPLETED	Calcifediol in the Treatment of COVID 19
NCT06279910	Not specified	COMPLETED	Calcifediol in the Treatment of SARS-CoV-2 Disease (COVID-19).

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).