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

Stem definition	Drug id	CAS RN
calcium metabolism regulator, pharmaceutical aid	2868	118072-93-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: zoledronic acid zoledronate zoledronic acid monohydrate zometa zoledronic acid hydrate	An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS. Molecular weight: 272.09 Formula: C5H10N2O7P2 CLOGP: -1.22 LIPINSKI: 0 HAC: 9 HDO: 5 TPSA: 153.11 ALOGS: -1.92 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

zoledronic acid
zoledronate
zoledronic acid monohydrate
zometa
zoledronic acid hydrate

An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.

Molecular weight: 272.09
Formula: C5H10N2O7P2
CLOGP: -1.22
LIPINSKI: 0
HAC: 9
HDO: 5
TPSA: 153.11
ALOGS: -1.92
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
4	mg	P

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	39 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	2.20 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	11 hours	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.78 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.60 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.01 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Aug. 20, 2001	FDA	NOVARTIS
March 20, 2001	EMA

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
Osteonecrosis of jaw	8061.24	11.50	2848	112762	32275	63341137
Exposed bone in jaw	1437.97	11.50	424	115186	2501	63370911
Bone pain	1053.82	11.50	840	114770	53801	63319611
Osteonecrosis	1017.64	11.50	605	115005	23925	63349487
Metastases to bone	801.03	11.50	491	115119	20528	63352884
Influenza like illness	575.49	11.50	658	114952	66166	63307246
Drug ineffective	568.91	11.50	643	114967	1044122	62329290
Malignant neoplasm progression	551.57	11.50	713	114897	81408	63292004
Pain in jaw	490.22	11.50	494	115116	43002	63330410
Myalgia	483.72	11.50	917	114693	145612	63227800

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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
Osteonecrosis of jaw	6773.45	13.34	1953	43291	15936	34895751
Exposed bone in jaw	1173.51	13.34	295	44949	1291	34910396
Osteonecrosis	806.74	13.34	391	44853	14499	34897188
Bone disorder	425.55	13.34	192	45052	6023	34905664
Pain in jaw	357.08	13.34	218	45026	12822	34898865
Oral cavity fistula	274.72	13.34	59	45185	101	34911586
Bone sequestrum	266.28	13.34	74	45170	508	34911179
Plasma cell myeloma	251.98	13.34	291	44953	41746	34869941
Osteomyelitis	233.20	13.34	182	45062	15954	34895733
Hypocalcaemia	216.81	13.34	208	45036	24081	34887606

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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
Osteonecrosis of jaw	13602.55	11.32	4239	115851	38987	79585311
Exposed bone in jaw	2456.85	11.32	652	119438	3068	79621230
Osteonecrosis	1678.02	11.32	855	119235	30240	79594058
Metastases to bone	808.63	11.32	487	119603	23940	79600358
Bone pain	729.04	11.32	632	119458	55110	79569188
Pain in jaw	629.35	11.32	536	119554	45615	79578683
Bone sequestrum	600.40	11.32	170	119920	1059	79623239
Malignant neoplasm progression	584.96	11.32	863	119227	135127	79489171
Bone disorder	578.72	11.32	360	119730	18753	79605545
Atypical femur fracture	525.63	11.32	221	119869	4968	79619330

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	M05BA08	MUSCULO-SKELETAL SYSTEM DRUGS FOR TREATMENT OF BONE DISEASES DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION Bisphosphonates
ATC	M05BB08	MUSCULO-SKELETAL SYSTEM DRUGS FOR TREATMENT OF BONE DISEASES DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION Bisphosphonates, combinations
CHEBI has role	CHEBI:50646	antiosteoporotic
MeSH PA	D050071	Bone Density Conservation Agents

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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
Osteitis deformans	indication	2089002	DOID:5408
Humoral hypercalcemia of malignancy	indication	47709007
Osteoporosis	indication	64859006	DOID:11476
Postmenopausal osteoporosis	indication	102447009
Bone Metastases of Solid Tumors	indication
Prevention of Glucocorticoid-Induced Osteoporosis	indication
Glucocorticoid Induced Osteoporosis	indication
Osteolytic Lesions of Multiple Myeloma	indication
Hypogonadal Osteoporosis in Males	indication
Drug-induced osteoporosis	off-label use	14651005

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	1.38	acidic
pKa2	5.45	acidic
pKa3	6.59	acidic
pKa4	10.35	acidic
pKa5	11.04	acidic
pKa6	5.92	Basic

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 4MG BASE/100ML	ZOMETA	NOVARTIS	N021223	June 17, 2011	RX	INJECTABLE	INTRAVENOUS	8324189	May 29, 2025	BONE METASTASES
EQ 4MG BASE/100ML	ZOMETA	NOVARTIS	N021223	June 17, 2011	RX	INJECTABLE	INTRAVENOUS	8324189	May 29, 2025	HYPERCALCEMIA OF MALIGNANCY
EQ 4MG BASE/100ML	ZOMETA	NOVARTIS	N021223	June 17, 2011	RX	INJECTABLE	INTRAVENOUS	8324189	May 29, 2025	MULTIPLE MYELOMA
EQ 4MG BASE/5ML	ZOMETA	NOVARTIS	N021223	March 7, 2003	RX	INJECTABLE	INTRAVENOUS	8324189	May 29, 2025	BONE METASTASES
EQ 4MG BASE/5ML	ZOMETA	NOVARTIS	N021223	March 7, 2003	RX	INJECTABLE	INTRAVENOUS	8324189	May 29, 2025	HYPERCALCEMIA OF MALIGNANCY
EQ 4MG BASE/5ML	ZOMETA	NOVARTIS	N021223	March 7, 2003	RX	INJECTABLE	INTRAVENOUS	8324189	May 29, 2025	MULTIPLE MYELOMA
EQ 5MG BASE/100ML	RECLAST	SANDOZ	N021817	April 16, 2007	RX	INJECTABLE	INTRAVENOUS	8052987	Oct. 27, 2023	TREATMENT AND PREVENTION OF POSTMENOPAUSAL OR GLUCOCORTICOID-INDUCED OSTEOPOROSIS AND TREATMENT TO INCREASE BONE MASS IN MEN WITH OSTEOPOROSIS

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Farnesyl pyrophosphate synthase	Enzyme	P14324	FPPS_HUMAN	INHIBITOR	Ki	10.15	CHEMBL	CHEMBL
Carbonic anhydrase 9	Enzyme	Q16790	CAH9_HUMAN		IC50	5.27	CHEMBL
Carbonic anhydrase 12	Enzyme	O43570	CAH12_HUMAN		IC50	6.50	CHEMBL
72 kDa type IV collagenase	Enzyme	P08253	MMP2_HUMAN		IC50	5.15	CHEMBL
Carbonic anhydrase 14	Enzyme	Q9ULX7	CAH14_HUMAN		IC50	7.04	CHEMBL
Matrix metalloproteinase-14	Enzyme	P50281	MMP14_HUMAN		IC50	4.90	CHEMBL
Matrix metalloproteinase-9	Enzyme	P14780	MMP9_HUMAN		IC50	4.28	CHEMBL
Neutrophil collagenase	Enzyme	P22894	MMP8_HUMAN		IC50	4.75	CHEMBL
Geranylgeranyl pyrophosphate synthase	Enzyme	O95749	GGPPS_HUMAN		Ki	5.57	CHEMBL
Butyrophilin subfamily 3 member A1	Antibody	O00481	BT3A1_HUMAN		EC50	6.31	CHEMBL

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External reference:

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ID	Source
ZOL	PDB_CHEM_ID
008997	NDDF
134600006	SNOMEDCT_US
15839	MMSL
165800-06-6	SECONDARY_CAS_RN
199263	MMSL
285143	RXNORM
3177	IUPHAR_LIGAND_ID
395926009	SNOMEDCT_US
4021276	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Reclast	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0435	INJECTION, SOLUTION	5 mg	INTRAVENOUS	NDA	32 sections
Reclast	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0435	INJECTION, SOLUTION	5 mg	INTRAVENOUS	NDA	32 sections
zoledronic acid	HUMAN PRESCRIPTION DRUG LABEL	1	50742-416	INJECTION, SOLUTION, CONCENTRATE	4 mg	INTRAVENOUS	ANDA	23 sections
Zoledronic Acid	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9642	INJECTION, SOLUTION, CONCENTRATE	4 mg	INTRAVENOUS	ANDA	26 sections
Zoledronic Acid	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9642	INJECTION, SOLUTION, CONCENTRATE	4 mg	INTRAVENOUS	ANDA	26 sections
ZOLEDRONIC ACID	HUMAN PRESCRIPTION DRUG LABEL	1	0409-4215	INJECTION, SOLUTION, CONCENTRATE	4 mg	INTRAVENOUS	ANDA	28 sections
ZOLEDRONIC ACID	HUMAN PRESCRIPTION DRUG LABEL	1	0409-4215	INJECTION, SOLUTION, CONCENTRATE	4 mg	INTRAVENOUS	ANDA	28 sections
ZOLEDRONIC ACID	HUMAN PRESCRIPTION DRUG LABEL	1	0409-4215	INJECTION, SOLUTION, CONCENTRATE	4 mg	INTRAVENOUS	ANDA	28 sections
Zoledronic acid	HUMAN PRESCRIPTION DRUG LABEL	1	16714-815	INJECTION	4 mg	INTRAVENOUS	ANDA	27 sections
Zoledronic acid	HUMAN PRESCRIPTION DRUG LABEL	1	16729-242	INJECTION	4 mg	INTRAVENOUS	ANDA	27 sections

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