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calcitriol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
Vitamin D analogues/derivatives	466	32222-06-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: rocaltrol calcitriol Dihydroxyvitamin D3 topitriol 1,25-dihydroxyvitamin D3	The physiologically active form of vitamin D. It is formed primarily in the kidney by enzymatic hydroxylation of 25-hydroxycholecalciferol (CALCIFEDIOL). Its production is stimulated by low blood calcium levels and parathyroid hormone. Calcitriol increases intestinal absorption of calcium and phosphorus, and in concert with parathyroid hormone increases bone resorption. Molecular weight: 416.65 Formula: C27H44O3 CLOGP: 6.04 LIPINSKI: 1 HAC: 3 HDO: 3 TPSA: 60.69 ALOGS: -4.80 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

rocaltrol
calcitriol
Dihydroxyvitamin D3
topitriol
1,25-dihydroxyvitamin D3

The physiologically active form of vitamin D. It is formed primarily in the kidney by enzymatic hydroxylation of 25-hydroxycholecalciferol (CALCIFEDIOL). Its production is stimulated by low blood calcium levels and parathyroid hormone. Calcitriol increases intestinal absorption of calcium and phosphorus, and in concert with parathyroid hormone increases bone resorption.

Molecular weight: 416.65
Formula: C27H44O3
CLOGP: 6.04
LIPINSKI: 1
HAC: 3
HDO: 3
TPSA: 60.69
ALOGS: -4.80
ROTB: 6

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
1	mcg	O
1	mcg	P

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	8 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	61 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	11 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.31 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.25 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.00 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Aug. 17, 1978	FDA	VALIDUS PHARMS

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Recalled product	1068.23	11.15	216	25545	1187	63462074
Hypocalcaemia	581.27	11.15	275	25486	31438	63431823
Hypercalcaemia	492.75	11.15	237	25524	28085	63435176
Milk-alkali syndrome	251.51	11.15	60	25701	768	63462493
Calciphylaxis	209.29	11.15	69	25692	3003	63460258
Peritonitis bacterial	188.82	11.15	72	25689	4807	63458454
Blood calcium decreased	156.92	11.15	110	25651	26341	63436920
Tetany	140.55	11.15	46	25715	1955	63461306
Blood parathyroid hormone increased	129.05	11.15	48	25713	2990	63460271
Shunt stenosis	127.72	11.15	32	25729	508	63462753

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Appendicolith	335.00	13.41	148	23868	8453	34924462
Appendicitis	288.76	13.41	159	23857	14648	34918267
Cardiogenic shock	210.11	13.41	162	23854	26456	34906459
Blood phosphorus increased	196.22	13.41	99	23917	7622	34925293
Peritonitis bacterial	193.30	13.41	91	23925	6019	34926896
Stress	183.24	13.41	158	23858	30189	34902726
Ascites	142.99	13.41	168	23848	46403	34886512
Shunt stenosis	141.65	13.41	42	23974	740	34932175
Hypercalcaemia	137.22	13.41	101	23915	15367	34917548
Abdominal distension	133.52	13.41	182	23834	58310	34874605

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hypercalcaemia	469.46	11.35	276	41184	38154	79664774
Recalled product	389.11	11.35	92	41368	862	79702066
Hypocalcaemia	379.66	11.35	266	41194	49658	79653270
Appendicolith	371.97	11.35	147	41313	8404	79694524
Peritonitis bacterial	352.60	11.35	146	41314	9421	79693507
Appendicitis	276.83	11.35	158	41302	20636	79682292
Shunt stenosis	269.27	11.35	74	41386	1317	79701611
Milk-alkali syndrome	231.33	11.35	66	41394	1354	79701574
Arteriovenous fistula site complication	230.90	11.35	61	41399	928	79702000
Blood phosphorus increased	230.50	11.35	111	41349	10236	79692692

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A11CC04	ALIMENTARY TRACT AND METABOLISM VITAMINS VITAMIN A AND D, INCL. COMBINATIONS OF THE TWO Vitamin D and analogues
ATC	D05AX03	DERMATOLOGICALS ANTIPSORIATICS ANTIPSORIATICS FOR TOPICAL USE Other antipsoriatics for topical use
CHEBI has role	CHEBI:24621	hormones
CHEBI has role	CHEBI:25212	metabolites
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:38807	calcium channel agonists
CHEBI has role	CHEBI:38808	calcium channel modulators
CHEBI has role	CHEBI:50646	antiosteoporotic
CHEBI has role	CHEBI:50733	Dietary Supplement
CHEBI has role	CHEBI:50748	antipsoriatic drug

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Hypophosphatemia	indication	4996001
Hypocalcemia	indication	5291005
Renal osteodystrophy	indication	16726004	DOID:13068
Hypoparathyroidism	indication	36976004	DOID:11199
Plaque psoriasis	indication	200965009
Hyperparathyroidism Secondary to Chronic Renal Failure	indication
Hypocalcemia from End-Stage Renal Disease with Dialysis	indication
Neonatal hypocalcemic tetany	off-label use	18442000
Vitamin D deficiency	off-label use	34713006
Rickets	off-label use	41345002	DOID:10609

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.7	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
3MCG/GM	VECTICAL	GALDERMA LABS LP	N022087	Jan. 23, 2009	RX	OINTMENT	TOPICAL	July 17, 2023	NEW PATIENT POPULATION

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Vitamin D3 receptor	Nuclear hormone receptor	P11473	VDR_HUMAN	AGONIST	EC50	8.40	WOMBAT-PK	CHEMBL
Vitamin D 25-hydroxylase	Enzyme	Q6VVX0	CP2R1_HUMAN				WOMBAT-PK
Vitamin D-binding protein	Secreted	P02774	VTDB_HUMAN		Kd	7.62	CHEMBL
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial	Enzyme	O15528	CP27B_HUMAN				WOMBAT-PK
Vitamin D3 receptor	Transcription factor		VDR_RAT		Ki	10.30	CHEMBL
Vitamin D3 receptor	Transcription factor		VDR_CHICK		Ki	10.60	CHEMBL
Vitamin D3 receptor	Transcription factor		VDR_BOVIN		EC50	10.30	CHEMBL
Vitamin D3 receptor	Nuclear hormone receptor		VDR_PIG		Kd	10.15	CHEMBL
Vitamin D3 receptor A	Nuclear hormone receptor		VDRA_DANRE		EC50	8.26	CHEMBL
Vitamin D3 receptor	Nuclear hormone receptor		VDR_MOUSE		EC50	7	CHEMBL

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External reference:

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ID	Source
VDX	PDB_CHEM_ID
001017	NDDF
1311	MMSL
152323	RXNORM
259333003	SNOMEDCT_US
2779	IUPHAR_LIGAND_ID
4017800	VUID
4017800	VANDF
4021906	VANDF
42410	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Calcitriol	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0007	CAPSULE	0.25 ug	ORAL	ANDA	22 sections
Calcitriol	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0007	CAPSULE	0.25 ug	ORAL	ANDA	22 sections
Calcitriol	HUMAN PRESCRIPTION DRUG LABEL	1	0054-3120	SOLUTION	1 ug	ORAL	ANDA	23 sections
Calcitriol	HUMAN PRESCRIPTION DRUG LABEL	1	0054-3120	SOLUTION	1 ug	ORAL	ANDA	23 sections
Calcitriol	HUMAN PRESCRIPTION DRUG LABEL	1	0054-3120	SOLUTION	1 ug	ORAL	ANDA	23 sections
Calcitriol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7352	CAPSULE, LIQUID FILLED	0.25 ug	ORAL	ANDA	26 sections
Calcitriol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7352	CAPSULE, LIQUID FILLED	0.25 ug	ORAL	ANDA	26 sections
Calcitriol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7353	CAPSULE, LIQUID FILLED	0.50 ug	ORAL	ANDA	26 sections
Calcitriol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7353	CAPSULE, LIQUID FILLED	0.50 ug	ORAL	ANDA	26 sections
Calcitriol	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9728	INJECTION	1 ug	INTRAVENOUS	ANDA	24 sections

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