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

Stem definition	Drug id	CAS RN
Vitamin D analogues/derivatives	2066	131918-61-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: zemplar paricalcitol-d6 paricalcitol	suppressed immunoglobulin production & thymic lymphocyte proliferation in vivo Molecular weight: 416.65 Formula: C27H44O3 CLOGP: 5.69 LIPINSKI: 1 HAC: 3 HDO: 3 TPSA: 60.69 ALOGS: -4.79 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

zemplar
paricalcitol-d6
paricalcitol

suppressed immunoglobulin production & thymic lymphocyte proliferation in vivo

Molecular weight: 416.65
Formula: C27H44O3
CLOGP: 5.69
LIPINSKI: 1
HAC: 3
HDO: 3
TPSA: 60.69
ALOGS: -4.79
ROTB: 5

Status: OFP

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

Drug dosage:

Dose	Unit	Route
2	mcg	O
2	mcg	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.00 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	72 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.41 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.89 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	5.30 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
April 17, 1998	FDA	ABBVIE

FDA Adverse Event Reporting System (Female)

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
Death	3210.85	24.54	1261	5713	373120	63108928
Cardiac disorder	460.01	24.54	182	6792	50634	63431414
Infarction	331.21	24.54	73	6901	2568	63479480
Sepsis	234.79	24.54	167	6807	152956	63329092
Myocardial infarction	164.59	24.54	114	6860	99779	63382269
Cardiac failure	159.34	24.54	107	6867	89035	63393013
Cardiovascular disorder	148.84	24.54	54	6920	11758	63470290
Cardio-respiratory arrest	147.19	24.54	88	6886	59871	63422177
Calciphylaxis	146.69	24.54	39	6935	3033	63479015
Adverse event	145.02	24.54	91	6883	67468	63414580
Respiratory arrest	133.03	24.54	67	6907	32578	63449470
Nephrogenic systemic fibrosis	118.52	24.54	36	6938	4520	63477528
Cerebrovascular disorder	85.91	24.54	25	6949	2707	63479341
Blood parathyroid hormone increased	83.29	24.54	25	6949	3013	63479035
Skin induration	77.59	24.54	24	6950	3199	63478849
Acute myocardial infarction	73.21	24.54	45	6929	32079	63449969
Renal transplant	72.97	24.54	19	6955	1361	63480687
Skin hypertrophy	64.08	24.54	21	6953	3370	63478678
Skin tightness	62.93	24.54	22	6952	4294	63477754
Chronic kidney disease	59.10	24.54	45	6929	45353	63436695
Cerebrovascular accident	54.23	24.54	63	6911	107961	63374087
Peritonitis bacterial	52.95	24.54	20	6954	4859	63477189
Drug ineffective	52.25	24.54	25	6949	1044740	62437308
Skin fibrosis	41.18	24.54	11	6963	869	63481179
Hyperphosphataemia	38.79	24.54	13	6961	2235	63479813
Cardiac arrest	38.34	24.54	49	6925	92496	63389552
Blood parathyroid hormone abnormal	38.02	24.54	8	6966	224	63481824
Transplant	37.46	24.54	10	6964	788	63481260
Parathyroidectomy	37.02	24.54	8	6966	255	63481793
Device related infection	34.49	24.54	25	6949	23367	63458681
Shunt occlusion	34.40	24.54	9	6965	656	63481392
Peritoneal dialysis complication	33.27	24.54	10	6964	1210	63480838
Haemorrhagic stroke	33.06	24.54	15	6959	5777	63476271
Arteriovenous fistula thrombosis	32.49	24.54	7	6967	220	63481828
Device related sepsis	31.19	24.54	13	6961	4081	63477967
Acute pulmonary oedema	31.03	24.54	16	6958	8142	63473906
Fibrosis	30.90	24.54	13	6961	4179	63477869
Off label use	30.85	24.54	18	6956	674444	62807604
Azotaemia	30.09	24.54	13	6961	4458	63477590
Joint contracture	29.86	24.54	10	6964	1714	63480334
Pulmonary sepsis	26.74	24.54	9	6965	1567	63480481
Hypercalcaemia	26.15	24.54	23	6951	28299	63453749
Sudden death	24.72	24.54	15	6959	10434	63471614

FDA Adverse Event Reporting System (Male)

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
Death	3904.40	27.18	1857	6729	396192	34552153
Cardiac disorder	705.14	27.18	296	8290	42830	34905515
Infarction	487.42	27.18	117	8469	2636	34945709
Myocardial infarction	312.69	27.18	249	8337	120836	34827509
Cardiovascular disorder	236.52	27.18	90	8496	9966	34938379
Adverse event	212.29	27.18	100	8486	18777	34929568
Sepsis	176.10	27.18	210	8376	166351	34781994
Cardiac failure	162.37	27.18	152	8434	91096	34857249
Respiratory arrest	151.18	27.18	91	8495	27952	34920393
Cardio-respiratory arrest	140.61	27.18	113	8473	55160	34893185
Transplant	130.21	27.18	32	8554	794	34947551
Renal transplant	121.95	27.18	36	8550	1813	34946532
Cerebrovascular accident	99.41	27.18	113	8473	84698	34863647
Calciphylaxis	97.83	27.18	27	8559	1065	34947280
Cerebrovascular disorder	92.46	27.18	29	8557	1793	34946552
Infection	77.18	27.18	103	8483	90812	34857533
Shunt thrombosis	71.79	27.18	13	8573	65	34948280
Nephrogenic systemic fibrosis	70.16	27.18	29	8557	3976	34944369
Parathyroidectomy	68.70	27.18	13	8573	86	34948259
Cardiac arrest	68.28	27.18	100	8486	96059	34852286
Skin induration	56.89	27.18	21	8565	2130	34946215
Unevaluable event	53.42	27.18	52	8534	32538	34915807
Shunt occlusion	53.28	27.18	16	8570	854	34947491
Off label use	52.33	27.18	19	8567	419505	34528840
Blood parathyroid hormone increased	52.22	27.18	18	8568	1496	34946849
Drug ineffective	51.63	27.18	24	8562	456727	34491618
Acute myocardial infarction	48.83	27.18	63	8523	53656	34894689
Skin hypertrophy	39.26	27.18	17	8569	2612	34945733
Chronic kidney disease	36.92	27.18	48	8538	41162	34907183
Skin tightness	35.06	27.18	15	8571	2238	34946107
Peritoneal dialysis complication	32.06	27.18	13	8573	1696	34946649

FDA Adverse Event Reporting System (Geriatric)

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
Myocardial infarction	364.78	21.20	231	8114	183898	79552145
Death	354.16	21.20	360	7985	566154	79169889
Cardio-respiratory arrest	281.31	21.20	162	8183	108348	79627695
Cardiac disorder	251.01	21.20	127	8218	65630	79670413
Calciphylaxis	222.09	21.20	56	8289	3714	79732329
Infarction	206.49	21.20	55	8290	4527	79731516
Sepsis	196.52	21.20	187	8158	269241	79466802
Respiratory arrest	162.56	21.20	91	8254	57459	79678584
Cardiac failure	161.89	21.20	132	8213	154710	79581333
Nephrogenic systemic fibrosis	159.67	21.20	48	8297	6112	79729931
Skin induration	124.82	21.20	37	8308	4488	79731555
Acute myocardial infarction	102.86	21.20	76	8269	76960	79659083
Renal transplant	98.00	21.20	27	8318	2520	79733523
Skin hypertrophy	96.55	21.20	31	8314	4897	79731146
Skin tightness	85.18	21.20	29	8316	5493	79730550
Blood parathyroid hormone increased	81.38	21.20	25	8320	3420	79732623
Peritonitis bacterial	79.93	21.20	32	8313	9535	79726508
Parathyroidectomy	75.78	21.20	14	8331	206	79735837
Peritoneal dialysis complication	68.21	21.20	20	8325	2334	79733709
Chronic kidney disease	68.14	21.20	56	8289	66098	79669945
Cardiac arrest	62.08	21.20	83	8262	172013	79564030
Cerebrovascular disorder	59.28	21.20	20	8325	3685	79732358
Skin fibrosis	57.91	21.20	16	8329	1508	79734535
Cardiovascular disorder	54.93	21.20	30	8315	17995	79718048
Shunt thrombosis	53.58	21.20	10	8335	156	79735887
Shunt occlusion	53.53	21.20	15	8330	1489	79734554
Joint contracture	45.87	21.20	15	8330	2509	79733534
Fibrosis	41.73	21.20	17	8328	5292	79730751
Azotaemia	40.56	21.20	19	8326	8257	79727786
Transplant	40.23	21.20	11	8334	997	79735046
Scar	40.07	21.20	23	8322	15173	79720870
Drug ineffective	39.85	21.20	33	8312	1080880	78655163
Peritonitis	38.14	21.20	28	8317	28008	79708035
Cerebrovascular accident	37.39	21.20	62	8283	155230	79580813
Device related infection	37.33	21.20	30	8315	34264	79701779
Arteriovenous fistula thrombosis	36.20	21.20	9	8336	562	79735481
Joint range of motion decreased	35.99	21.20	29	8316	33253	79702790
Device related sepsis	35.85	21.20	16	8329	6224	79729819
Blood parathyroid hormone abnormal	34.58	21.20	8	8337	367	79735676
Hypercalcaemia	32.35	21.20	29	8316	38401	79697642
Cardiopulmonary failure	31.45	21.20	15	8330	6786	79729257
Skin hyperpigmentation	30.43	21.20	15	8330	7288	79728755
Sudden death	29.53	21.20	22	8323	22489	79713554
Off label use	27.30	21.20	33	8312	907182	78828861
Haemorrhagic stroke	27.21	21.20	16	8329	11030	79725013
Hypertensive crisis	26.58	21.20	20	8325	20750	79715293
Nephropathy	26.37	21.20	15	8330	9723	79726320
Shunt malfunction	26.16	21.20	6	8339	265	79735778
Hypocalcaemia	25.96	21.20	29	8316	49895	79686148
Arrhythmia	25.89	21.20	32	8313	61240	79674803
Dialysis	24.12	21.20	18	8327	18444	79717599
General physical health deterioration	23.81	21.20	73	8272	275165	79460878
Hyperphosphataemia	23.35	21.20	12	8333	6364	79729679
Coronary artery disease	22.68	21.20	31	8314	65443	79670600
Toxicity to various agents	22.53	21.20	8	8337	421532	79314511
Hypotonia	22.51	21.20	15	8330	12855	79723188
Extremity contracture	22.48	21.20	8	8337	1724	79734319

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	H05BX02	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS CALCIUM HOMEOSTASIS ANTI-PARATHYROID AGENTS Other anti-parathyroid agents
FDA CS	M0007651	Ergocalciferols
CHEBI has role	CHEBI:50827	antiparathyroid drugs
FDA EPC	N0000175849	Vitamin D Analog
FDA EPC	N0000175907	Vitamin D2 Analog

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

Disease	Relation	SNOMED_ID	DOID
Hyperparathyroidism Secondary to Chronic Renal Failure	indication
Poisoning by digitalis glycoside	contraindication	12876009
Hyperphosphatemia	contraindication	20165001	DOID:0050459
Hypervitaminosis D	contraindication	27712000	DOID:9971
Hypercalcemia	contraindication	66931009	DOID:12678

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
0.002MG/ML (0.002MG/ML)	ZEMPLAR	ABBVIE	N020819	Feb. 1, 2000	RX	SOLUTION	INTRAVENOUS	Oct. 18, 2023	FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
0.005MG/ML (0.005MG/ML)	ZEMPLAR	ABBVIE	N020819	April 17, 1998	RX	SOLUTION	INTRAVENOUS	Oct. 18, 2023	FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
0.01MG/2ML (0.005MG/ML)	ZEMPLAR	ABBVIE	N020819	Feb. 1, 2000	RX	SOLUTION	INTRAVENOUS	Oct. 18, 2023	FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
1MCG	ZEMPLAR	ABBVIE	N021606	May 26, 2005	RX	CAPSULE	ORAL	Oct. 18, 2023	INDICATED IN PEDIATRIC PATIENTS 10 YEARS AND OLDER FOR THE PREVENTION AND TREATMENT OF SECONDARY HYPERPARATHYROIDISM ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD) STAGES 3 AND 4 AND CKD STAGE 5 IN PATIENTS ON HEMODIALYSIS OR PERITONEAL DIALYSIS
2MCG	ZEMPLAR	ABBVIE	N021606	May 26, 2005	RX	CAPSULE	ORAL	Oct. 18, 2023	INDICATED IN PEDIATRIC PATIENTS 10 YEARS AND OLDER FOR THE PREVENTION AND TREATMENT OF SECONDARY HYPERPARATHYROIDISM ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD) STAGES 3 AND 4 AND CKD STAGE 5 IN PATIENTS ON HEMODIALYSIS OR PERITONEAL DIALYSIS
4MCG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	ZEMPLAR	ABBVIE	N021606	May 26, 2005	DISCN	CAPSULE	ORAL	Oct. 18, 2023	INDICATED IN PEDIATRIC PATIENTS 10 YEARS AND OLDER FOR THE PREVENTION AND TREATMENT OF SECONDARY HYPERPARATHYROIDISM ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD) STAGES 3 AND 4 AND CKD STAGE 5 IN PATIENTS ON HEMODIALYSIS OR PERITONEAL DIALYSIS

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Vitamin D3 receptor	Nuclear hormone receptor	P11473	VDR_HUMAN	AGONIST	EC50	8.70		WOMBAT-PK	CHEMBL

External reference:

ID	Source
4021107	VUID
N0000148562	NUI
D00930	KEGG_DRUG
4021107	VANDF
C0249582	UMLSCUI
CHEBI:7931	CHEBI
CHEMBL1200622	ChEMBL_ID
DB00910	DRUGBANK_ID
C084656	MESH_SUPPLEMENTAL_RECORD_UI
5281104	PUBCHEM_CID
2791	IUPHAR_LIGAND_ID
7688	INN_ID
6702D36OG5	UNII
221005	RXNORM
11702	MMSL
206206	MMSL
5234	MMSL
d04312	MMSL
007498	NDDF
108946001	SNOMEDCT_US
126233000	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-1658	INJECTION, SOLUTION	5 ug	INTRAVENOUS	NDA	27 sections
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-1658	INJECTION, SOLUTION	5 ug	INTRAVENOUS	NDA	27 sections
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4314	CAPSULE, LIQUID FILLED	2 ug	ORAL	NDA	28 sections
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4314	CAPSULE, LIQUID FILLED	2 ug	ORAL	NDA	28 sections
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4317	CAPSULE, LIQUID FILLED	1 ug	ORAL	NDA	28 sections
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4317	CAPSULE, LIQUID FILLED	1 ug	ORAL	NDA	28 sections
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4637	INJECTION, SOLUTION	2 ug	INTRAVENOUS	NDA	27 sections
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-4637	INJECTION, SOLUTION	2 ug	INTRAVENOUS	NDA	27 sections
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-9036	CAPSULE, LIQUID FILLED	1 ug	ORAL	NDA	28 sections
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-9036	CAPSULE, LIQUID FILLED	1 ug	ORAL	NDA	28 sections
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-9037	CAPSULE, LIQUID FILLED	2 ug	ORAL	NDA	28 sections
Zemplar	HUMAN PRESCRIPTION DRUG LABEL	1	0074-9037	CAPSULE, LIQUID FILLED	2 ug	ORAL	NDA	28 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9596	INJECTION	5 ug	INTRAVENOUS	NDA	24 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9624	INJECTION	5 ug	INTRAVENOUS	NDA	24 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9625	INJECTION	2 ug	INTRAVENOUS	NDA	24 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1007	INJECTION, SOLUTION	2 ug	INTRAVENOUS	NDA	29 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1008	INJECTION, SOLUTION	5 ug	INTRAVENOUS	NDA	29 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	10888-5001	CAPSULE, LIQUID FILLED	1 ug	ORAL	ANDA	26 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	10888-5002	CAPSULE, LIQUID FILLED	2 ug	ORAL	ANDA	26 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	10888-5003	CAPSULE, LIQUID FILLED	4 ug	ORAL	ANDA	26 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	16729-310	INJECTION, SOLUTION	2 ug	INTRAVENOUS	NDA	24 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	16729-310	INJECTION, SOLUTION	2 ug	INTRAVENOUS	NDA	24 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	16729-311	INJECTION, SOLUTION	5 ug	INTRAVENOUS	NDA	24 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	16729-311	INJECTION, SOLUTION	5 ug	INTRAVENOUS	NDA	24 sections
Paricalcitol	HUMAN PRESCRIPTION DRUG LABEL	1	17478-033	INJECTION, SOLUTION	5 ug	INTRAVENOUS	ANDA	26 sections
Paricalcitol	Human Prescription Drug Label	1	25000-012	CAPSULE, LIQUID FILLED	1 ug	ORAL	ANDA	24 sections
Paricalcitol	Human Prescription Drug Label	1	25000-014	CAPSULE, LIQUID FILLED	2 ug	ORAL	ANDA	24 sections
Paricalcitol	Human Prescription Drug Label	1	25000-017	CAPSULE, LIQUID FILLED	4 ug	ORAL	ANDA	24 sections
PARICALCITOL	HUMAN PRESCRIPTION DRUG LABEL	1	40051-612	CAPSULE	1 ug	ORAL	ANDA	18 sections
PARICALCITOL	HUMAN PRESCRIPTION DRUG LABEL	1	40051-613	CAPSULE	2 ug	ORAL	ANDA	18 sections