ZOLEDRONIC ACID ANHYDROUS

Details

Stereochemistry	ACHIRAL
Molecular Formula	C5H10N2O7P2
Molecular Weight	272.0899
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

c1cn(CC(O)(P(=O)(O)O)P(=O)(O)O)cn1

InChI

InChIKey=XRASPMIURGNCCH-UHFFFAOYSA-N

InChI=1S/C5H10N2O7P2/c8-5(15(9,10)11,16(12,13)14)3-7-2-1-6-4-7/h1-2,4,8H,3H2,(H2,9,10,11)(H2,12,13,14)

HIDE SMILES / InChI

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21386lbl.pdf

bone structure and mass relative to placebo in clinical studies in patients with primary or secondary osteoporosis. While additional benefits were seen when treatment was continued for up to 6 years, as evidenced by a reduced risk of vertebral fractures and higher BMD relative to 3 years’ therapy, there was the minimal advantage of treatment beyond 6 years. Therefore, in patients with low fracture risk, treatment discontinuation should be considered after approximately 5 years’ therapy. Zoledronic acid administered annually or once in 2 years was also effective in preventing bone loss in patients with low bone mass. Zoledronic acid was generally well tolerated, with the most common adverse events (AEs) being transient, mild-to-moderate post-infusion symptoms, which decreased with subsequent infusions.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Farnesyl diphosphate synthase 28 Target ID: CHEMBL1782 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22390415	Inhibitor 7701	Hypercalcemia Disuse osteoporosis Prostate cancer with bone metastasis Renal osteodystrophy Postmenopausal osteoporosis	4.09999999999999964 nM [IC50]
Geranylgeranyl pyrophosphate synthetase 18 Target ID: CHEMBL4769 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17535895	Inhibitor 7701		97 µM [IC50]
Carbonic anhydrase XIV 21 Target ID: CHEMBL3510 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24813742	Inhibitor 7701		92 nM [IC50]
Carbonic anhydrase II 83 Target ID: CHEMBL205 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24650641	Inhibitor 7701		62 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypercalcemia 22 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21386lbl.pdf	Primary	Farnesyl diphosphate synthase	Approved 7997	Zometa Approved Use INDICATIONS AND USAGE Hypercalcemia of Malignancy. Zometa® (zoledronic acid for injection) is indicated for the treatment of hypercalcemia of malignancy. Vigorous saline hydration, an integral part of hypercalcemia therapy, should be initiated promptly and an attempt should be made to restore the urine output to about 2 L/day throughout treatment. Mild or asymptomatic hypercalcemia may be treated with conservative measures (i.e., saline hydration, with or without loop diuretics). Patients should be hydrated dequately throughout the treatment, but overhydration, especially in those patients who have cardiac failure, must be avoided. Diuretic therapy should not be employed prior to correction of hypovolemia. The safety and efficacy of Zometa in the treatment of hypercalcemia associated with hyperparathyroidism or with other non-tumor-related conditions has not been established. Multiple Myeloma and Bone Metastases of Solid Tumors. Zometa is indicated for the treatment of patients with multiple myeloma and patients with documented bone metastases from solid tumors, in conjunction with standard antineoplastic therapy. Prostate cancer should have progressed after treatment with at least one hormonal therapy Launch Date 998179200000
Disuse osteoporosis 9 Sources: https://clinicaltrials.gov/ct2/show/NCT02042872	Primary	Farnesyl diphosphate synthase	Approved 7997	Zometa Approved Use INDICATIONS AND USAGE Hypercalcemia of Malignancy. Zometa® (zoledronic acid for injection) is indicated for the treatment of hypercalcemia of malignancy. Vigorous saline hydration, an integral part of hypercalcemia therapy, should be initiated promptly and an attempt should be made to restore the urine output to about 2 L/day throughout treatment. Mild or asymptomatic hypercalcemia may be treated with conservative measures (i.e., saline hydration, with or without loop diuretics). Patients should be hydrated dequately throughout the treatment, but overhydration, especially in those patients who have cardiac failure, must be avoided. Diuretic therapy should not be employed prior to correction of hypovolemia. The safety and efficacy of Zometa in the treatment of hypercalcemia associated with hyperparathyroidism or with other non-tumor-related conditions has not been established. Multiple Myeloma and Bone Metastases of Solid Tumors. Zometa is indicated for the treatment of patients with multiple myeloma and patients with documented bone metastases from solid tumors, in conjunction with standard antineoplastic therapy. Prostate cancer should have progressed after treatment with at least one hormonal therapy Launch Date 998179200000
Prostate cancer with bone metastasis 9 Sources: https://clinicaltrials.gov/ct2/show/NCT00241111	Primary	Farnesyl diphosphate synthase	Approved 7997	Zometa Approved Use INDICATIONS AND USAGE Hypercalcemia of Malignancy. Zometa® (zoledronic acid for injection) is indicated for the treatment of hypercalcemia of malignancy. Vigorous saline hydration, an integral part of hypercalcemia therapy, should be initiated promptly and an attempt should be made to restore the urine output to about 2 L/day throughout treatment. Mild or asymptomatic hypercalcemia may be treated with conservative measures (i.e., saline hydration, with or without loop diuretics). Patients should be hydrated dequately throughout the treatment, but overhydration, especially in those patients who have cardiac failure, must be avoided. Diuretic therapy should not be employed prior to correction of hypovolemia. The safety and efficacy of Zometa in the treatment of hypercalcemia associated with hyperparathyroidism or with other non-tumor-related conditions has not been established. Multiple Myeloma and Bone Metastases of Solid Tumors. Zometa is indicated for the treatment of patients with multiple myeloma and patients with documented bone metastases from solid tumors, in conjunction with standard antineoplastic therapy. Prostate cancer should have progressed after treatment with at least one hormonal therapy Launch Date 998179200000
Renal osteodystrophy 11 Sources: https://clinicaltrials.gov/ct2/show/NCT01675089	Primary	Farnesyl diphosphate synthase	Approved 7997	Zometa Approved Use INDICATIONS AND USAGE Hypercalcemia of Malignancy. Zometa® (zoledronic acid for injection) is indicated for the treatment of hypercalcemia of malignancy. Vigorous saline hydration, an integral part of hypercalcemia therapy, should be initiated promptly and an attempt should be made to restore the urine output to about 2 L/day throughout treatment. Mild or asymptomatic hypercalcemia may be treated with conservative measures (i.e., saline hydration, with or without loop diuretics). Patients should be hydrated dequately throughout the treatment, but overhydration, especially in those patients who have cardiac failure, must be avoided. Diuretic therapy should not be employed prior to correction of hypovolemia. The safety and efficacy of Zometa in the treatment of hypercalcemia associated with hyperparathyroidism or with other non-tumor-related conditions has not been established. Multiple Myeloma and Bone Metastases of Solid Tumors. Zometa is indicated for the treatment of patients with multiple myeloma and patients with documented bone metastases from solid tumors, in conjunction with standard antineoplastic therapy. Prostate cancer should have progressed after treatment with at least one hormonal therapy Launch Date 998179200000
Postmenopausal osteoporosis 59 Sources: https://clinicaltrials.gov/ct2/show/NCT02499237	Primary	Farnesyl diphosphate synthase	Approved 7997	Zometa Approved Use INDICATIONS AND USAGE Hypercalcemia of Malignancy. Zometa® (zoledronic acid for injection) is indicated for the treatment of hypercalcemia of malignancy. Vigorous saline hydration, an integral part of hypercalcemia therapy, should be initiated promptly and an attempt should be made to restore the urine output to about 2 L/day throughout treatment. Mild or asymptomatic hypercalcemia may be treated with conservative measures (i.e., saline hydration, with or without loop diuretics). Patients should be hydrated dequately throughout the treatment, but overhydration, especially in those patients who have cardiac failure, must be avoided. Diuretic therapy should not be employed prior to correction of hypovolemia. The safety and efficacy of Zometa in the treatment of hypercalcemia associated with hyperparathyroidism or with other non-tumor-related conditions has not been established. Multiple Myeloma and Bone Metastases of Solid Tumors. Zometa is indicated for the treatment of patients with multiple myeloma and patients with documented bone metastases from solid tumors, in conjunction with standard antineoplastic therapy. Prostate cancer should have progressed after treatment with at least one hormonal therapy Launch Date 998179200000

C_max

Value	Dose	Co-administered	Analyte	Population
264 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21563999	4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered:		ZOLEDRONIC ACID plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
420 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21563999	4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered:		ZOLEDRONIC ACID plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
39 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/21563999	4 mg single, intravenous dose: 4 mg route of administration: Intravenous experiment type: SINGLE co-administered:		ZOLEDRONIC ACID plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
16 mg 1 times / 4 weeks multiple, intravenous Highest studied dose Dose: 16 mg, 1 times / 4 weeks Route: intravenous Route: multiple Dose: 16 mg, 1 times / 4 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/12412821	unhealthy, 40-79 years Health Status: unhealthy Age Group: 40-79 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/12412821	Sources: https://pubmed.ncbi.nlm.nih.gov/12412821
16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	Other AEs: Skeletal pain, Fever... Other AEs: Skeletal pain (30%) Fever (20%) Anorexia (20%) Diarrhea (20%) Constipation (10%) Nausea (20%) Myalgia (20%) Arthralgia (10%) Anemia (30%) Rigors (20%) Coughing (20%) Leg edema (10%) Urinary tract infection (10%) Fatigue (40%) Sources: https://pubmed.ncbi.nlm.nih.gov/11148571

AEs

AE	Significance	Dose	Population
Arthralgia	10%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Constipation	10%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Leg edema	10%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Urinary tract infection	10%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Anorexia	20%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Coughing	20%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Diarrhea	20%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Fever	20%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Myalgia	20%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Nausea	20%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Rigors	20%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Anemia	30%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Skeletal pain	30%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571
Fatigue	40%	16 mg single, intravenous Highest studied dose Dose: 16 mg Route: intravenous Route: single Dose: 16 mg Sources: https://pubmed.ncbi.nlm.nih.gov/11148571	unhealthy, 54 years (range: 34–73 years) Health Status: unhealthy Age Group: 54 years (range: 34–73 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/11148571

Overview

CYP3A4	CYP2C9	CYP2D6	hERG

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP450 21	CYP 231

Drug as perpetrator

Target	Modality	Activity	Metabolite	Clinical evidence
CYP450 36	inhibitor 2614 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021817s000_PharmR_P1.pdf#page=50 Page: 50	no

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
CYP 231	substrate 2752 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5682380/	no

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY10182
001 Chemical	DY114281
1PlusChem LLC	1P001WU2
1PlusChem LLC	1P001WU3
1PlusChem LLC	1P00HETU
A2B Chem	AA88411
A2B Chem	AI11570
AA Blocks	AA001WAN
ACT Chemical	ACT11723
AK Scientific	2821AH
AK Scientific	8418AA
AK Scientific	H683
AK Scientific	J90125
AK Scientific	Y1607
APExBIO	A1352
AbovChem LLC	HY-13777
AbovChem LLC	HY-13777A
Ambeed	A211103
Ambeed	A364741
Angene	AGN-PC-0JLNL0
Angene	AGN-PC-0Q8TBJ
AstaTech	H11422
AstaTech	T71894
BLDpharm	BD233916
BLDpharm	BD41357
BLDpharm	BD9477
BOC Sciences	118072-93-8
BOC Sciences	165800-06-6
BOC Sciences	165800-07-7
BOC Sciences	904894-54-8
Bide Pharmatech	BD41357
Bide Pharmatech	BD9477
BioSynth	Q-201946
BlocksMatrix Scientific	93212
BlocksMatrix Scientific	95289
Bosche Scientific	Z0157
Bosche Scientific	Z2411
Capot Chemical	14894
Cayman Chemical	14984
Chem Scene	CS-2975
ChemShuttle	109840
ChemShuttle	169426
Compound Cloud	121586
Compound Cloud	23649597
Compound Cloud	23725076
Compound Cloud	68740
Compound Cloud	72734361
Coresyn	CM14379
Enamine	BBV-57275855
Enamine	EN300-117269
Enamine	EN300-209119
Fluorochem	219821
Fragmenta	PHO012
Hairui	HR117434
Hairui	HR138453
Hangzhou APIChem Technology	AC-1092
Hangzhou APIChem Technology	AC-22574
Hangzhou APIChem Technology	AC-5897
Hangzhou Yuhao Chemical Technology	LT6069
Hangzhou Yuhao Chemical Technology	YH65702
HongKong Chemhere	SCE37103
IBScreen	BB_SC-12492
IBScreen	Bio-0112
KeyOrganics	KS-1132
Lab Network	LN00192430
Lab Network	LN00225983
Lab Seeker	SC-14082
Lan Pharmatech	LQT-B48943
MedChem Express	HY-13777A
MolPort	MolPort-023-332-212
Molcore	MC10182
Molcore	MC114281
Molnova	M10613
MuseChem	I002170
MuseChem	R002158
MuseChem	R044095
Nanjing Pope Bio-tech	NSTH-D16119
Norris Pharm	NSTH-D16119
PI Chemicals	PI-28079
PI Chemicals	PI-34022
Princeton BioMolecular Research	OSSL_857224
ShangHai Biochempartner	BCP10611
ShangHai Biochempartner	BCP22750
Sigma Aldrich	1724827
Sigma Aldrich	1724827\|USP
Sigma Aldrich	PHR1893
Sigma Aldrich	SML0223
Sigma Aldrich	SML0223\|SIGMA
StruChem	SC-14082
Synthonix	SL098902
TargetMol	T6739
Tetrahedron	TS35263
Tetrahedron	TS59546
Tetrahedron	TS94483
Toronto Research Chemicals	O701023
Toronto Research Chemicals	Z623500
Toronto Research Chemicals	Z623501
Vitas-M Laboratory	STL452893
W&J PharmaChem	100737
W&J PharmaChem	50C243359
W&J PharmaChem	RT-
Wonderchem	WD02TRW
Wonderchem	WD04U6U
Wonderchem	WD05CG3
Wonderchem	WD05CG4
ZINC	ZINC000003803652	http://zinc15.docking.org/substances/ZINC000003803652
eMolecules	27676223
eMolecules	44457481
eMolecules	45916703
eMolecules	56967816
eMolecules	6719817
eMolecules	72979108
eMolecules	902698
eNovation Chemicals	D459028
mcule	MCULE-1604726355

PubMed

Title	Date	PubMed
Metastatic bone disease and tumour-induced hypercalcaemia: the role of bisphosphonates.	2001 Jun	12066026
FDA grants priority review for ZOMETA.	2001 Oct	12113096
Bisphosphonates in the treatment of metastatic breast cancer.	2001 Oct	12013536
The use of zoledronic acid, a novel, highly potent bisphosphonate, for the treatment of hypercalcemia of malignancy.	2002	12490736
The new bisphosphonate, Zometa (zoledronic acid), decreases skeletal complications in both osteolytic and osteoblastic lesions: a comparison to pamidronate.	2002	12442349
U.S. Food and Drug Administration drug approval summaries: imatinib mesylate, mesna tablets, and zoledronic acid.	2002	12401901
The role of bisphosphonates in breast cancer management: review article.	2002	12240791
FDA approves ZOMETA for treatment of cancer-related bone complications.	2002 Apr	12113230
Bisphosphonates: biological response modifiers in breast cancer.	2002 Aug	12196279
Highly potent geminal bisphosphonates. From pamidronate disodium (Aredia) to zoledronic acid (Zometa).	2002 Aug 15	12166945
Advances in the biology and treatment of myeloma bone disease.	2002 Dec	12520479
The anti-tumour activity of bisphosphonates.	2002 Dec	12470981
Disease modifying and anti-nociceptive effects of the bisphosphonate, zoledronic acid in a model of bone cancer pain.	2002 Dec	12467993
Monosodium [1-hydroxy-2-(1H-imidazol-3-ium-4-yl)ethane-1,1-diyl]bis(phosphonate) tetrahydrate (monosodium isozoledronate).	2002 Dec	12466610
Pharmacological treatments for prostate cancer.	2002 Dec	12457434
The role of osteoclastic activity in prostate cancer skeletal metastases.	2002 Feb	12532187
Distinct mechanisms of bisphosphonate action between osteoblasts and breast cancer cells: identity of a potent new bisphosphonate analogue.	2002 Feb	12002344
The effects of local administration of Zoledronate solution on the tooth movement and periodontal ligament.	2002 Jul	12411180
New drugs 2002, part III.	2002 Jul	12352871
Osteoporosis: challenges and new opportunities for therapy.	2002 Jul	12197306
Bisphosphonates for cancer patients: why, how, and when?	2002 Jul	12136223
Zoledronate once-yearly increases bone mineral density--implications for osteoporosis.	2002 Jul	12083999
Adaptive dose finding for phase I clinical trials of drugs used for chemotherapy of cancer.	2002 Jul 15	12111891
An investigation of bone resorption and Dictyostelium discoideum growth inhibition by bisphosphonate drugs.	2002 Jul 4	12086477
Electrolyte abnormalities with zoledronic acid therapy.	2002 Jul-Aug	12184414
Zoledronic acid. A bisphosphonate for hypercalcemia of malignancy and osteolytic metastases.	2002 Jul-Aug	12100107
Novel approaches to the management of bone metastases in patients with breast cancer.	2002 Jun	12138408
Bisphosphonates influence the proliferation and the maturation of normal human osteoblasts.	2002 Jun	12109626
Bisphosphonates and osteoporosis.	2002 Jun 27	12087149
Bisphosphonates inhibit stromelysin-1 (MMP-3), matrix metalloelastase (MMP-12), collagenase-3 (MMP-13) and enamelysin (MMP-20), but not urokinase-type plasminogen activator, and diminish invasion and migration of human malignant and endothelial cell lines.	2002 Mar	11984068
Treatment of malignant hypercalcaemia.	2002 May	11996631
The bisphosphonate zoledronic acid impairs Ras membrane [correction of impairs membrane] localisation and induces cytochrome c release in breast cancer cells.	2002 May 6	11986784
Pharmacokinetics and pharmacodynamics of zoledronic acid in cancer patients with bone metastases.	2002 Nov	12412821
Severe increase in creatinine with hypocalcaemia in thalidomide-treated myeloma patients receiving zoledronic acid infusions.	2002 Nov	12406106
Pamidronate causes apoptosis of plasma cells in vivo in patients with multiple myeloma.	2002 Nov	12406088
Bisphosphonates inhibit angiogenesis in vitro and testosterone-stimulated vascular regrowth in the ventral prostate in castrated rats.	2002 Nov 15	12438248
Development and validation of a highly sensitive RIA for zoledronic acid, a new potent heterocyclic bisphosphonate, in human serum, plasma and urine.	2002 Nov 7	12408879
The use of bisphosphonates in patients with breast cancer.	2002 Nov-Dec	12514566
Bisphosphonate therapy in multiple myeloma: past, present, future.	2002 Nov-Dec	12460229
Zoledronic acid improves the mechanical properties of normal and healing bone.	2002 Nov-Dec	12446169
Zoledronic acid.	2002 Nov-Dec	12434471
Gateways to clinical trials.	2002 Oct	12500432
Zoledronic acid: new preparation. Just a me-too: no advance in hypercalcemia of malignancy.	2002 Oct	12378744
Intravenous zoledronic acid in postmenopausal women with low bone mineral density.	2002 Oct	12356057
The IL-6 receptor super-antagonist Sant7 enhances antiproliferative and apoptotic effects induced by dexamethasone and zoledronic acid on multiple myeloma cells.	2002 Oct	12239628
Use of zoledronate to treat osteoblastic versus osteolytic lesions in a severe-combined-immunodeficient mouse model.	2002 Oct 1	12359769
A randomized, placebo-controlled trial of zoledronic acid in patients with hormone-refractory metastatic prostate carcinoma.	2002 Oct 2	12359855
Novel antiangiogenic effects of the bisphosphonate compound zoledronic acid.	2002 Sep	12183663
American Society of Clinical Oncology clinical practice guidelines: the role of bisphosphonates in multiple myeloma.	2002 Sep 1	12202673
[Bisphosphonates in bone metastases. Fewer fractures, less pain].	2002 Sep 26	12422697

Patents

Sample Use Guides

In Vivo Use Guide

The maximum recommended dose of Zometa in hypercalcemia of malignancy is 4 mg. The 4 mg dose must be given as a single-dose intravenous infusion over no less than 15 minutes.

Route of Administration: Intravenous

In Vitro Use Guide

For the transfection of the T24 human bladder cancer cells, pCMV6 empty vector (OriGene, Rockville, MD, USA) and pCMV6 TAp73 vector were transfected into cells using Lipofectamine™ 2000 (Invitrogen Life Technologies). After 6 h, the medium was refreshed and cultured for 48 h. Then the cells were treated with ZA (200 μM).

Name

Type

Language

ZOLEDRONIC ACID ANHYDROUS

Common Name

English

PHOSPHONIC ACID, (1-HYDROXY-2-(1H-IMIDAZOL-1-YL)ETHYLIDENE)BIS-

Common Name

English

ANHYDROUS ZOLEDRONIC ACID

Common Name

English

(1-HYDROXY-2-IMIDAZOL-1-YLETHYLIDENE)DIPHOSPHONIC ACID

Systematic Name

English

ZOLEDRONIC ACID [INN]

Common Name

English

ZOLEDRONIC ACID [WHO-DD]

Common Name

English

NSC-721517

Code

English

ZOLEDRONIC ACID [MI]

Common Name

English

ZOLEDRONATE

Common Name

English

Classification Tree Code System Code

NDF-RT

N0000175579