Alfacalcidol

Summary

Alfacalcidol (CHEMBL1601669) is an approved small-molecule bone density conservation agent (ATC A11CC03); indicated across 8 conditions including osteoporosis and muscle tissue disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A11CC03
• Indications: 8 conditions
• Clinical trials: 31
• Chemistry: 400.6 Da · C27H44O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1601669
Name	Alfacalcidol
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	5282181
ChEBI	CHEBI:31186
ATC	A11CC03
Molecular formula	C27H44O2
Molecular weight	400.6
InChIKey	OFHCOWSQAMBJIW-AVJTYSNKSA-N

SMILES: C[C@H](CCCC(C)C)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C/3\C[C@H](C[C@@H](C3=C)O)O)C

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

ChEBI definition: A member of the class of D3 vitamins that is calciol in which the hydrogen at the 1α position is replaced by a hydroxy group. It is an active metabolite of cholecalciferol, which performs important functions in regulation of the calcium balance and the bone metabolism.

Pharmacological roles (ChEBI): bone density conservation agent.

Also known as: .alpha.-calcidol, 1.alpha-hydroxycholecalciferol, 1.alpha.(oh)d3, 1.alpha.-hydroxycholecalciferol, 1.alpha.-hydroxyvitamin d3, Alfa d, Alfacalcidol, Alfarol, Alpha d3, Alphacalcidol, Alpharol, Alsiodol

Patent coverage: 2,002 distinct patent families (5,908 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: Sodium-dependent noradrenaline transporter, Type-1 angiotensin II receptor, Adenosine receptor A3.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 5 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SLC6A2	6	IC50	1009	nM	CHEMBL_ACT_7642968
SLC6A2	6	Ki	1000	nM	CHEMBL_ACT_7642969
AGTR1	5.08	AC50	8400	nM	CHEMBL_ACT_25177241

Target pathways

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

Indications & clinical

Indications

8 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
osteoporosis	3	MONDO:0005298	EFO:0003882
muscle tissue disorder	3	MONDO:0003939	EFO:0002970
postmenopausal osteoporosis	3	MONDO:0008159	EFO:0003854
pelvic organ prolapse	3	MONDO:0000082	EFO:0004710
calcinosis	2	MONDO:0002123	EFO:0003837
scoliosis	2	MONDO:0005392	EFO:0004273
kidney failure	2	MONDO:0001106	EFO:1002048

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 31.

Phase distribution

Phase	Trials
PHASE4	13
Not specified	7
PHASE3	5
PHASE2	5
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00168909	PHASE4	COMPLETED	Influence of Alfacalcidol on Falls in Osteopenic/Osteoporotic Postmenopausal Women (ALFA Study)
NCT00483275	PHASE4	WITHDRAWN	Fall Prevention by Alfacalcidol and Training
NCT00668330	PHASE4	COMPLETED	Steroid Induced Osteoporosis in Patients With Systemic Lupus Erythematosus
NCT01115543	PHASE4	COMPLETED	Efficacy and Safety of Alfacalcidol Compared to Calcitriol for Treatment of Secondary Hyperparathyroidism
NCT01430104	PHASE4	COMPLETED	A Study of Teriparatide in Japanese Osteoporosis Patients
NCT01765010	PHASE4	UNKNOWN	The Effect of Inactive and Active Vitamin D on Serum Sclerostin/dickkopf1 Levels
NCT02747381	PHASE4	COMPLETED	The Effect of Vitamin D Supplementation on the Pulmonary Functions of Adult Asthmatic Egyptian Patients
NCT03147677	PHASE4	COMPLETED	Clinical Study of Treating Type 2 Diabetic Nephropathy With Alfacalcidol and Irbesartan
NCT03210688	PHASE4	COMPLETED	Active Vitamin D And Reduced Dose Prednisolone for Treatment in Minimal Change Nephropathy
NCT03292744	PHASE4	UNKNOWN	Effect of Alfacalcidol to Respiratory Infection and Immune Response of Indonesian Elderly
NCT04085770	PHASE4	COMPLETED	Short Term Effect of Vitamin D Supplementation on the Clinical Outcomes in Patients Undergoing Valve Replacement Surgery
NCT06272227	PHASE4	UNKNOWN	Effect of Alfacalcidol on Muscle Function in Osteoporosis Patients
NCT06385093	PHASE4	UNKNOWN	A Study on the Prevention and Treatment of GIOP With Eldecalcitol
NCT00144456	PHASE3	COMPLETED	A New Active Vitamin D, ED-71 for Osteoporosis
NCT00165698	PHASE3	COMPLETED	Efficacy and Safety Study on Menatetrenone in the Treatment of Postmenopausal Osteoporosis Women
NCT02327091	PHASE3	COMPLETED	The Effect of Alfacalcidol on Muscle Strength in Elderly Indonesian Women : A Randomized Controlled Trial
NCT04405960	PHASE3	COMPLETED	Role of Alphacalcidol Supplement to Reduce Pain and COMP in Geriatric Knee Osteoarthritis Patients
NCT05505253	PHASE3	COMPLETED	Alfacalcidol Supplementation on Levator Ani Muscle Strength of Menopausal Pelvic Organ Prolapse Patients
NCT06016400	PHASE2/PHASE3	UNKNOWN	Using Vitamin D to Reduce Oral Mucosal Inflammation in Chemotherapy Patients With Oral Squamous Cell Carcinoma
NCT03582917	PHASE2	RECRUITING	The Role of VitD in Rehabilitation of Idiopathic Adolescent Scoliosis
NCT01231438	PHASE2	COMPLETED	Treatment of Early Stage Renal Failure With Active Vitamin D or a Phosphate Binder.
NCT01364688	PHASE2	UNKNOWN	Oral Alfacalcidol and Coronary Artery Calcification in Predialysis Chronic Kidney Disease
NCT01774812	PHASE2	COMPLETED	Vitamin D and Cardiac Autonomic Tone in Hemodialysis
NCT02824718	PHASE2	COMPLETED	Recombinant Human rhPTH(1-34) VS Association Alfacalcidol/Hydrochlorothiazide in Severe Primary Hypoparathyroidism
NCT00469599	Not specified	TERMINATED	Treatment of Secondary Hyperparathyroidism in the Uremic Patient
NCT01020253	Not specified	UNKNOWN	The Effectiveness of Two Osteoporosis Drugs on Prosthetic Bone Mineral Density (BMD) Loss After Total Hip Arthroplasty(THA)
NCT01752244	Not specified	UNKNOWN	Assessing the Effects of Alfacalcidol Intake on Expression of Involed Gene in Metabolism in Obese Subjects
NCT01974167	Not specified	UNKNOWN	Eldecalcitol for GLucocorticoid Induced OsteopoRosIs Versus Alfacalcidol
NCT02895061	Not specified	COMPLETED	Effectiveness of Oral Alfacalcidol for Secondary Hyperparathyroidism in Chronic Hemodialysis Patients.
NCT04146259	Not specified	COMPLETED	Changes in Circulating Sclerostin Levels During Acute Postsurgical Hypoparathyroidism
NCT04967469	Not specified	COMPLETED	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

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

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