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Zoledronic acid
Accession Number
DB00399  (APRD01294, DB06286)
Small Molecule

Zoledronate (zoledronic acid, marketed by Novartis under the trade names Zometa and Reclast) is a bisphosphonate. Zometa is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases.

An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture.

Zoledronate is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.

  • (1-hydroxy-2-(1H-imidazol-1-yl)ethylidene)bisphosphonic acid
  • (1-hydroxy-2-imidazol-1-ylethylidene)diphosphonic acid
  • ácido zoledrónico
  • Anhydrous Zoledronic Acid
  • Zol
  • Zoledronate
  • Zoledronic acid
  • Zoledronic Acid Anhydrous
  • Zoledronic Acid, Anhydrous
External IDs
CGP 42446 / CGP-42446
Product Ingredients
IngredientUNIICASInChI Key
Zoledronate disodium7D7GS1SA24165800-07-7IEJZOPBVBXAOBH-UHFFFAOYSA-L
Zoledronate trisodiumARL915IH66165800-08-8HYMYRPXSMHJPGD-UHFFFAOYSA-A
Zoledronic acid hemipentahydrate1K9U67HDIDNot AvailableAZZILOGHCMYHQY-UHFFFAOYSA-N
Zoledronic acid monohydrate6XC1PAD3KF165800-06-6FUXFIVRTGHOMSO-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AclastaInjection, solution5 mg/100mlIntravenousNovartis Europharm Limited2005-04-15Not applicableEu
AclastaSolution5 mgIntravenousNovartis2005-08-22Not applicableCanada
AclastaInjection, solution5 mg/100mlIntravenousNovartis Europharm Limited2005-04-15Not applicableEu
Act Zoledronic AcidSolution5 mgIntravenousActavis Pharma CompanyNot applicableNot applicableCanada
Act Zoledronic Acid ConcentrateSolution4 mgIntravenousActavis Pharma CompanyNot applicableNot applicableCanada
ReclastInjection, solution5 mg/100mLIntravenousNovartis Pharmaceuticals Corporation2007-04-01Not applicableUs
Zoledronic AcidInjection, solution4 mg/100mLIntravenousHospira, Inc.2017-10-19Not applicableUs
Zoledronic AcidInjection, solution0.04 mg/1mLIntravenousSagent Pharmaceuticals2013-03-02Not applicableUs
Zoledronic Acid - ASolution5 mgIntravenousSandoz Canada IncorporatedNot applicableNot applicableCanada
Zoledronic Acid - ZSolution4 mgIntravenousSandoz Canada Incorporated2014-01-15Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Jamp-zoledronic AcidSolution4 mgIntravenousJamp Pharma CorporationNot applicableNot applicableCanada
PMS-zoledronic AcidSolution4 mgIntravenousPharmascience Inc2014-11-25Not applicableCanada
Taro-zoledronic AcidSolution5 mgIntravenousTaro Pharmaceuticals, Inc.2014-04-02Not applicableCanada
Taro-zoledronic Acid ConcentrateSolution4 mgIntravenousTaro Pharmaceuticals, Inc.2014-02-26Not applicableCanada
Val-zoledronic AcidSolution4 mgIntravenousValeo Pharma Corp.Not applicableNot applicableCanada
Zoledronic acidInjection, solution4 mg/100mLIntravenousDr. Reddy's Laboratories Inc2019-01-15Not applicableUs
Zoledronic AcidInjection, solution, concentrate4 mg/5mLIntravenousGland Pharma Limited2013-09-20Not applicableUs
Zoledronic AcidInjection, solution, concentrate4 mg/5mLIntravenousDr Reddy's Laboratories2013-08-19Not applicableUs
Zoledronic acidInjection, solution, concentrate4 mg/5mLIntravenousHeritage2012-12-20Not applicableUs
Zoledronic AcidInjection, solution5 mg/100mLIntravenousMylan Institutional2018-06-05Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

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CAS number
Average: 272.0896
Monoisotopic: 271.996323708
Chemical Formula
InChI Key
[1-hydroxy-2-(1H-imidazol-1-yl)-1-phosphonoethyl]phosphonic acid



For the treatment of hypercalcemia of malignancy. Also for the treatment of patients with multiple myeloma and patients with documented bone metastases from solid tumors, in conjunction with standard antineoplastic therapy. In May of 2007, the drug was approved for treatment of Paget’s Disease.

Associated Conditions

Zoledronate is a bisphosphonic acid which is an inhibitor of osteoclastic bone resorption. Zoledronate is used to prevent osteoporosis and skeletal fractures, particularly in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia, particularly hypercalcemia of malignancy. It can also be helpful for treating pain from bone metastases.

Mechanism of action

The action of zoledronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Zoledronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates such as zoledronate appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass.

AFarnesyl pyrophosphate synthase
AGeranylgeranyl pyrophosphate synthase
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Blackbox Warnings

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Poorly absorbed (oral absorption is about 1% of what intravenous absorption is).

Volume of distribution
Not Available
Protein binding

Approximately 22% bound in human plasma, independent of the concentration. However, Canadian product information states binding to human plasma protein is approximately 56%.


Zoledronate does not inhibit human P450 enzymes in vitro and does not undergo biotransformation in vivo.

Route of elimination

In 64 patients with cancer and bone metastases, on average (± s.d.) 39 ± 16% of the administered zoledronic acid dose was recovered in the urine within 24 hours, with only trace amounts of drug found in urine post-Day 2.

Half life

146 hours

  • Renal cl=3.7 +/- 2.0 L/h

There is no experience of acute overdose. Two patients received zoledronate (32 mg) over 5 minutes in clinical trials. Neither patient experienced any clinical or laboratory toxicity. Overdosage may cause clinically significant hypocalcemia, hypophosphatemia, and hypomagnesemia.

Affected organisms
  • Humans and other mammals
Zoledronate Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
AceclofenacThe risk or severity of gastrointestinal bleeding can be increased when Aceclofenac is combined with Zoledronic acid.
AcemetacinThe risk or severity of gastrointestinal bleeding can be increased when Acemetacin is combined with Zoledronic acid.
Acetylsalicylic acidThe risk or severity of gastrointestinal bleeding can be increased when Acetylsalicylic acid is combined with Zoledronic acid.
AcyclovirThe risk or severity of nephrotoxicity and hypocalcemia can be increased when Acyclovir is combined with Zoledronic acid.
AdefovirThe risk or severity of nephrotoxicity and hypocalcemia can be increased when Adefovir is combined with Zoledronic acid.
Adefovir dipivoxilThe risk or severity of nephrotoxicity and hypocalcemia can be increased when Adefovir Dipivoxil is combined with Zoledronic acid.
AlclofenacThe risk or severity of gastrointestinal bleeding can be increased when Alclofenac is combined with Zoledronic acid.
Alendronic acidThe risk or severity of hypocalcemia can be increased when Zoledronic acid is combined with Alendronic acid.
AlmasilateThe serum concentration of Zoledronic acid can be decreased when it is combined with Almasilate.
AlminoprofenThe risk or severity of gastrointestinal bleeding can be increased when Alminoprofen is combined with Zoledronic acid.
Additional Data Available
  • Extended Description
    Extended Description

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  • Severity

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  • Evidence Level
    Evidence Level

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  • Action
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Food Interactions
Not Available


Synthesis Reference

Judith Aronhime, Revital Lifshitz-Liron, "Zoledronic acid crystal forms, zoledronate sodium salt crystal forms, amorphous zoledronate sodium salt, and processes for their preparation." U.S. Patent US20050054616, issued March 10, 2005.

General References
  1. Lyles KW, Colon-Emeric CS, Magaziner JS, Adachi JD, Pieper CF, Mautalen C, Hyldstrup L, Recknor C, Nordsletten L, Moore KA, Lavecchia C, Zhang J, Mesenbrink P, Hodgson PK, Abrams K, Orloff JJ, Horowitz Z, Eriksen EF, Boonen S: Zoledronic acid and clinical fractures and mortality after hip fracture. N Engl J Med. 2007 Nov 1;357(18):1799-809. Epub 2007 Sep 17. [PubMed:17878149]
  2. Reid IR, Brown JP, Burckhardt P, Horowitz Z, Richardson P, Trechsel U, Widmer A, Devogelaer JP, Kaufman JM, Jaeger P, Body JJ, Brandi ML, Broell J, Di Micco R, Genazzani AR, Felsenberg D, Happ J, Hooper MJ, Ittner J, Leb G, Mallmin H, Murray T, Ortolani S, Rubinacci A, Saaf M, Samsioe G, Verbruggen L, Meunier PJ: Intravenous zoledronic acid in postmenopausal women with low bone mineral density. N Engl J Med. 2002 Feb 28;346(9):653-61. [PubMed:11870242]
  3. Durie BG, Katz M, Crowley J: Osteonecrosis of the jaw and bisphosphonates. N Engl J Med. 2005 Jul 7;353(1):99-102; discussion 99-102. [PubMed:16000365]
External Links
Human Metabolome Database
PubChem Compound
PubChem Substance
Therapeutic Targets Database
ATC Codes
M05BB08 — Zoledronic acid, calcium and colecalciferol, sequentialM05BA08 — Zoledronic acid
AHFS Codes
  • 92:24.00 — Bone Resorption Inhibitors
PDB Entries
1zw5 / 2e91 / 2f8c / 2f8z / 2f9k / 2q58 / 3ez3 / 3iba / 3ldw / 3n45
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Clinical Trials

Clinical Trials
1Active Not RecruitingTreatmentNeuroblastomas1
1CompletedBasic ScienceHealthy Postmenopausal Women1
1CompletedOtherHealthy Volunteers1
1CompletedOtherRisk Factors for or a Diagnosis of Osteoporosis1
1CompletedTreatmentBone Metastases / Cancer, Breast / Lung Cancers / Prostate Cancer1
1CompletedTreatmentCLDN18.2-positive Adenocarcinoma of Esophagus / CLDN18.2-positive Adenocarcinoma of the Gastroesophageal Junction / CLDN18.2-positive Gastric Adenocarcinoma1
1CompletedTreatmentCancer, Breast / Multiple Myeloma (MM)1
1CompletedTreatmentMetastatic Hormone Refractory Prostate Cancer1
1CompletedTreatmentMultiple Myeloma Bone Disease1
1CompletedTreatmentProstate Cancer1
1RecruitingTreatmentAcute Lymphoblastic Leukaemias (ALL) / Ewing's Sarcoma (ES) / Leukemia Acute Myeloid Leukemia (AML) / Lymphoma, Hodgkins / Myelodysplastic Syndrome / Myeloproliferative Syndromes / Neuroblastomas / Non-Hodgkin's Lymphoma (NHL) / Primitive Neuroectodermal Tumor / Rhabdomyosarcomas / Sarcoma, Osteogenic1
1RecruitingTreatmentHematopoietic Stem Cell Transplantation (HSCT)1
1TerminatedTreatmentCervical Cancers / Precancerous Conditions1
1TerminatedTreatmentMultiple Myeloma and Plasma Cell Neoplasm1
1, 2Active Not RecruitingTreatmentBone Metastases / Cancer, Breast1
1, 2CompletedSupportive CareCancer, Breast / Hypercalcemia of Malignancy / Metastatic Cancers / Pain NOS1
1, 2CompletedTreatmentMetastatic Cancers / Renal Cancers1
1, 2CompletedTreatmentMultiple Myeloma and Plasma Cell Neoplasm / Pain NOS1
1, 2WithdrawnNot AvailableSickle Cell Disorders1
2Active Not RecruitingPreventionBone Loss / Osteoporosis / Spinal Cord Injuries (SCI) / Spinal Cord Injury, Acute1
2Active Not RecruitingSupportive CareCancer of the Ovary / Hereditary Breast and Ovarian Cancer Syndrome / Hereditary Breast/Ovarian Cancer (brca1, brca2) / Osteoporosis / Ovarian Carcinoma1
2Active Not RecruitingTreatmentOsteogenesis Imperfecta1
2Active Not RecruitingTreatmentOsteoporosis1
2CompletedPreventionBone Loss / Prostate Cancer1
2CompletedSupportive CareCentral Nervous System(CNS)Malignancies / Neoplasms, Brain / Osteoporosis1
2CompletedSupportive CareDuctal Carcinoma In Situ / Estrogen Receptor-Positive Breast Cancer / Progesterone Receptor-positive Breast Cancer / Stage I Breast Carcinoma / Stage II Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2CompletedTreatmentAdenocarcinoma of the Prostate / Prostate Cancer1
2CompletedTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
2CompletedTreatmentAgnogenic Myeloid Metaplasia / Myeloid Metaplasia1
2CompletedTreatmentBack Pain Lower Back1
2CompletedTreatmentBone Loss / Human Immunodeficiency Virus (HIV) Infections / Osteopenia / Osteoporosis1
2CompletedTreatmentBone Metastasis / Gastrointestinal Cancers1
2CompletedTreatmentBone Neoplasms / Cancer, Breast / Prostate Cancer1
2CompletedTreatmentCancer of the Ovary / Leukemias / Malignant Lymphomas / Myelodysplastic Syndromes / Osteoporosis1
2CompletedTreatmentCancer, Breast2
2CompletedTreatmentCancer, Breast / Metastatic Bone Disease1
2CompletedTreatmentCancer, Breast / Multiple Myeloma (MM)1
2CompletedTreatmentDuctal Histologic Type / Locally Advanced Breast Cancer (LABC) / Without Her2 Overexpression1
2CompletedTreatmentHormone-Refractory Prostate Cancer2
2CompletedTreatmentHutchinson-Gilford Syndrome / Progeria1
2CompletedTreatmentLow Bone Mineral Density / Postmenopausal Osteoporosis (PMO)1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentMalignant Neoplasm of Nasopharynx1
2CompletedTreatmentMetastatic Cancers / Prostate Cancer2
2CompletedTreatmentMultiple Myeloma (MM)5
2CompletedTreatmentNeoplasms, Breast1
2CompletedTreatmentOsteogenesis Imperfecta2
2CompletedTreatmentProstate Cancer1
2CompletedTreatmentRenal Cancers / Renal Cell Adenocarcinoma1
2CompletedTreatmentUrologic Neoplasms1
2RecruitingTreatmentAdenocarcinoma of the Pancreas / Recurrent Pancreatic Carcinoma / Stage I Pancreatic Cancer / Stage I Pancreatic Cancer AJCC v6 and v7 / Stage IA Pancreatic Cancer / Stage IA Pancreatic Cancer AJCC v6 and v7 / Stage IB Pancreatic Cancer / Stage IB Pancreatic Cancer AJCC v6 and v7 / Stage II Pancreatic Cancer / Stage II Pancreatic Cancer AJCC v6 and v7 / Stage IIA Pancreatic Cancer / Stage IIA Pancreatic Cancer AJCC v6 and v7 / Stage IIB Pancreatic Cancer / Stage IIB Pancreatic Cancer AJCC v6 and v7 / Stage III Pancreatic Cancer / Stage III Pancreatic Cancer AJCC v6 and v7 / Stage IV Pancreatic Cancer / Stage IV Pancreatic Cancer AJCC v6 and v71
2RecruitingTreatmentBone Metastases / Prostate Cancer1
2RecruitingTreatmentBone Metastasis / Gastrointestinal Cancers1
2RecruitingTreatmentIOP / Osteoporosis1
2RecruitingTreatmentTriple Negative Breast Cancer (TNBC)1
2TerminatedDiagnosticMetastases / Non-Small Cell Lung Carcinoma (NSCLC) / Small Cell Lung Carcinoma1
2TerminatedPreventionBone Loss1
2TerminatedPreventionMultiple Myeloma (MM)1
2TerminatedPreventionProstate Cancer1
2TerminatedTreatmentCancer, Breast1
2TerminatedTreatmentChronic Myeloid Leukemia (CML)1
2TerminatedTreatmentGiant Cell Tumors of Bone / Osteoclastoma1
2TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Malignant Pleural Effusions1
2TerminatedTreatmentRenal Cancers1
2TerminatedTreatmentUterine Cervical Neoplasms1
2Unknown StatusPreventionOsteonecrosis1
2Unknown StatusTreatmentBreast Diseases / Cancer, Breast / Neoplasms / Neoplasms by Site1
2Unknown StatusTreatmentComplex Regional Pain Syndromes (CRPS)1
2Unknown StatusTreatmentHepatocellular,Carcinoma1
2Unknown StatusTreatmentHuman Immunodeficiency Virus (HIV) Infections / Osteopenia / Osteoporosis1
2WithdrawnTreatmentAcute Lymphoblastic Leukaemias (ALL) / Osteonecrosis / Osteoporosis1
2WithdrawnTreatmentPlasma Cell Myeloma1
2, 3CompletedPreventionBone Resorption / Heart Transplantation / Transplantation, Liver1
2, 3CompletedPreventionMetastatic Breast Cancer With Bone Involvement1
2, 3CompletedTreatmentBone Metastases / Metastatic Breast Cancer (MBC)1
2, 3RecruitingTreatmentDiabetes Complications / Neuropathic arthropathy1
2, 3RecruitingTreatmentProstate Cancer2
2, 3TerminatedTreatmentOsteoporosis1
2, 3Unknown StatusTreatmentBeta-Thalassemia / Transplantation, Bone Marrow1
2, 3Unknown StatusTreatmentCancer, Breast1
2, 3Unknown StatusTreatmentSarcoma, Osteogenic1
3Active Not RecruitingSupportive CareBreast Adenocarcinoma / DS Stage I Plasma Cell Myeloma / DS Stage II Plasma Cell Myeloma / Metastatic Malignant Neoplasm to the Bone / Musculoskeletal Complications / Pain NOS / Urinary Complications1
3Active Not RecruitingSupportive CareOsteoporosis / Prostate Cancer1
3Active Not RecruitingTreatmentCancer, Breast2
3Active Not RecruitingTreatmentComplete Traumatic Spinal Cord Injury / Spinal Cord Injuries (SCI)1
3Active Not RecruitingTreatmentComplex Regional Pain Syndrome (CRPS) / Complex Regional Pain Syndrome - Type 1 / Complex Regional Pain Syndrome Type I1
3Active Not RecruitingTreatmentSolitary Osseous Plasmacytoma1
3Active Not RecruitingTreatmentTriple Negative Breast Cancer (TNBC)1
3CompletedPreventionCancer, Breast3
3CompletedPreventionLung Cancer Non-Small Cell Cancer (NSCLC)1
3CompletedPreventionNeoplasms, Breast / Osteoporosis1
3CompletedPreventionNon Small Cell Lung Carcinoma (NSCLC)1
3CompletedSupportive CareBone Metastases3
3CompletedSupportive CareBone Metastases / Malignancies / Malignancies, Hematologic / Multiple Myeloma (MM) / Multiple Myeloma Bone Lesions / Oncology1
3CompletedSupportive CareCancer, Breast / Lung Cancers / Metastatic Cancers / Pain NOS / Prostate Cancer1
3CompletedSupportive CareCancer, Breast / Osteoporosis3
3CompletedSupportive CareHypercalcemia of Malignancy / Lung Cancers / Metastatic Cancers / Pain NOS / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedSupportive CareOsteogenesis Imperfecta1
3CompletedTreatmentAvascular Necrosis of Femoral Head1
3CompletedTreatmentBone Loss / Cancer, Breast1
3CompletedTreatmentBone Marrow Oedema1
3CompletedTreatmentBreast Cancer With Bone Metastasis1
3CompletedTreatmentCancer Prostate1
3CompletedTreatmentCancer, Breast6
3CompletedTreatmentCrohn's Disease (CD) / Osteopenia / Osteoporosis1
3CompletedTreatmentFractures, Bone1
3CompletedTreatmentFunctional Outcomes / Prevention of BMD Loss After THR / Serum Markers of Bone Turnover1
3CompletedTreatmentHip Fractures / Osteoporosis1
3CompletedTreatmentMale Osteoporosis1
3CompletedTreatmentMalignant Lymphomas / Non-Hodgkin's Lymphoma (NHL)1
3CompletedTreatmentMetastatic Cancers / Prostate Cancer2
3CompletedTreatmentMultiple Myeloma and Plasma Cell Neoplasm2
3CompletedTreatmentOne to five years postmenopausal / Osteoporosis1
3CompletedTreatmentPaget's Disease of Bone2
3CompletedTreatmentPain NOS1
3CompletedTreatmentPostmenopausal Osteoporosis (PMO)2
3CompletedTreatmentProstate Cancer3
3CompletedTreatmentTreatment of Bone Metastases1
3Not Yet RecruitingTreatmentOsteoporosis / Thalassemia Majors (Beta-Thalassemia Major)1
3RecruitingPreventionLung Cancer Non-Small Cell Cancer (NSCLC) / Lung Cancers1
3RecruitingSupportive CareMetastatic Renal Cell Carcinoma1
3RecruitingTreatmentEwing's Sarcoma (ES)1
3RecruitingTreatmentGiant Cell Tumors of Bone1
3TerminatedPreventionRheumatoid Arthritis1
3TerminatedTreatmentAIS Grade A to D / Being Diagnosed With a Spinal Cord Injury Less Than 12 Weeks of Etiology Stable / Bone Demineralization Lesions in the Injured Marrow / Female or Male Between 18 and 45 Years / Level of Injury C5 L2 / No Osteoporosis / No Pregnancy1
3TerminatedTreatmentBone Neoplasms / Neoplasms Metastasis / Pain NOS2
3TerminatedTreatmentBreast Cancer With Bone Metastasis1
3TerminatedTreatmentCancer, Breast / Neoplasms Metastasis1
3TerminatedTreatmentDisseminated Sclerosis / Osteoporosis1
3TerminatedTreatmentMultiple Myeloma (MM)2
3TerminatedTreatmentMultiple Myeloma Stage I1
3TerminatedTreatmentProstate Cancer3
3Unknown StatusTreatmentCancer, Breast / Hypercalcemia of Malignancy / Metastatic Cancers1
3Unknown StatusTreatmentCancer, Breast / Metastatic Cancers1
3WithdrawnSupportive CareCancer, Breast / Hypercalcemia of Malignancy / Metastatic Cancers / Pain NOS1
4Active Not RecruitingPreventionMultiple Myeloma (MM)1
4Active Not RecruitingPreventionOsteoporosis1
4Active Not RecruitingTreatmentPostmenopausal Osteoporosis (PMO)1
4CompletedPreventionBone Neoplasms1
4CompletedPreventionFracture Bone / Osteoporosis / Transplantation, Liver1
4CompletedPreventionMultiple Myeloma (MM)1
4CompletedPreventionOsteoarthritis, Hip1
4CompletedPreventionProstate Cancer1
4CompletedPreventionThalassaemic disorders1
4CompletedTreatmentBone Metastases / High NTX Level / Lung Cancer Non-Small Cell Cancer (NSCLC)1
4CompletedTreatmentBone Metastasis / Cancer, Breast / Prostate Cancer1
4CompletedTreatmentBreast Cancer With Metastatic Bone Disease1
4CompletedTreatmentCancer, Breast1
4CompletedTreatmentCancer, Breast / Multiple Myeloma (MM) / Prostate Cancer1
4CompletedTreatmentDisuse Osteoporosis1
4CompletedTreatmentFirst or Second Line HER2-negative Breast Cancer / Metastatic Disease Without Bone Metastasis1
4CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
4CompletedTreatmentHypocalcemia / Paget's Disease of the Bone1
4CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Pleural Effusion, Malignant1
4CompletedTreatmentMalignancies / Neoplasms Metastasis / Pain NOS1
4CompletedTreatmentMultiple Myeloma (MM)1
4CompletedTreatmentNeoplasms Metastasis1
4CompletedTreatmentNeoplasms Metastasis / Renal Cell Adenocarcinoma1
4CompletedTreatmentOsteoporosis, Osteopenia1
4CompletedTreatmentPaget's Disease of Bone1
4CompletedTreatmentPaget's Disease of the Bone1
4CompletedTreatmentPostmenopausal Osteoporosis (PMO)3
4CompletedTreatmentProstate Cancer6
4CompletedTreatmentProstate Cancer Patients With Bone Metastasis1
4CompletedTreatmentProstate Cancer With Bone Metastasis1
4CompletedTreatmentProstate Cancer With at Least One Bone Lesion in Patients Receiving Hormonal Therapy and Treatment With Bisphosphonates is Indicated1
4CompletedTreatmentRenal Osteodystrophy1
4Enrolling by InvitationPreventionBariatric Surgery Candidate1
4Not Yet RecruitingTreatmentBone Metastasis / Lung Cancer Non-Small Cell Cancer (NSCLC)1
4Not Yet RecruitingTreatmentEarly-Stage Breast Cancer1
4Not Yet RecruitingTreatmentPostmenopausal Osteoporosis (PMO)1
4RecruitingPreventionLung Cancer Metastatic / Tumor necrosis1
4RecruitingTreatmentCancer, Breast / Metastasis / Prostate Cancer1
4RecruitingTreatmentMultiple Myeloma (MM)1
4RecruitingTreatmentOsteogenesis Imperfecta1
4RecruitingTreatmentOsteoporotic Fractures / Postmenopausal Osteoporosis (PMO)1
4RecruitingTreatmentProsthetic Fixation After Cementless Total Hip Arthroplasty1
4RecruitingTreatmentStress Fracture Ankle / Stress Fracture Foot1
4TerminatedTreatmentPrimary Hormone Receptor Negative Breast Cancer in Premenopausal Women1
4Unknown StatusDiagnosticMetastatic Breast Cancer (MBC)1
4Unknown StatusTreatmentBone Mineral Density / Bone Turnover Markers / Image Changes of Lumbar Fusion1
4Unknown StatusTreatmentMultiple Myeloma (MM)1
4WithdrawnTreatmentCystic Fibrosis (CF)1
4WithdrawnTreatmentMultiple Myeloma (MM)1
Not AvailableActive Not RecruitingSupportive CareCancer, Breast / Osteoporosis1
Not AvailableActive Not RecruitingTreatmentEstrogen Receptor-Positive Breast Cancer / Invasive Ductal Breast Carcinoma / Progesterone Receptor-positive Breast Cancer / Stage IA Breast Cancer / Stage IB Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer1
Not AvailableActive Not RecruitingTreatmentOsteonecrosis1
Not AvailableCompletedNot AvailableBone Metastasis / Metastatic Hormone Refractory Prostate Cancer1
Not AvailableCompletedNot AvailableCancer, Breast1
Not AvailableCompletedNot AvailableMultiple Disabilities / Osteoporosis1
Not AvailableCompletedNot AvailableMultiple Myeloma (MM)1
Not AvailableCompletedNot AvailablePostmenopausal Osteoporosis (PMO)1
Not AvailableCompletedPreventionCancer, Breast / Osteoporosis1
Not AvailableCompletedScreeningProstate Cancer1
Not AvailableCompletedTreatmentBone Density / Prostatic Neoplasms1
Not AvailableCompletedTreatmentBone Loss / Fragility Fractures / Osteoporosis1
Not AvailableCompletedTreatmentHypercalcemia / Malignancies / Pain NOS1
Not AvailableCompletedTreatmentImpaired Renal Function1
Not AvailableCompletedTreatmentOsteoporosis2
Not AvailableCompletedTreatmentPostmenopausal Osteoporosis (PMO)1
Not AvailableCompletedTreatmentProstate Cancer1
Not AvailableEnrolling by InvitationNot AvailableAtypical Femoral Fractures / Bisphosphonate Therapy / Osteoporosis1
Not AvailableRecruitingTreatmentBone Loss / Neoplasms, Breast1
Not AvailableTerminatedTreatmentMultiple Myeloma (MM)1
Not AvailableUnknown StatusNot AvailableCancer, Breast1
Not AvailableUnknown StatusPreventionOsteoporosis / Transplantation, Liver1
Not AvailableUnknown StatusSupportive CareCancer, Breast / Hypercalcemia of Malignancy / Metastatic Cancers / Musculoskeletal Complications / Pain NOS1
Not AvailableWithdrawnNot AvailableCancer, Breast1
Not AvailableWithdrawnDiagnosticMusculoskeletal Complications / Neoplasms, Malignant1
Not AvailableWithdrawnSupportive CareBone Marrow Transplant (BMT) / Hematopoietic Stem Cell Transplant (HSCT)1


  • Novartis pharmaceuticals corp
  • Novartis AG
Dosage forms
Injection, solutionIntravenous5 mg/100ml
SolutionIntravenous5 mg
InjectionIntravenous4 mg/100mL
InjectionIntravenous4 mg/5mL
InjectionIntravenous5 mg/100mL
Injection, solutionIntravenous0.04 mg/1mL
Injection, solutionIntravenous0.05 mg/1mL
Injection, solution, concentrateIntravenous0.8 mg/1mL
Kit4 mg/5mL
SolutionIntravenous4 mg/100mL
SolutionIntravenous5 mg/100mL
Injection, solutionIntravenous4 mg/100ml
Injection, solution, concentrateIntravenous4 mg/5ml
Injection, solutionIntravenous5 mg
Injection, solution, concentrateIntravenous4 mg/100mL
SolutionIntravenous4 mg
Powder, for solutionIntravenous4 mg
Unit descriptionCostUnit
Zometa 4 mg/5ml Concentrate 5ml Vial1095.69USD vial
Reclast 5 mg/100ml Solution13.39USD ml
Reclast 5 mg/100 ml solution12.88USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent NumberPediatric ExtensionApprovedExpires (estimated)
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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Experimental Properties
water solubilitySparingly solubleNot Available
logP-4.2Not Available
Predicted Properties
Water Solubility3.27 mg/mLALOGPS
pKa (Strongest Acidic)0.66ChemAxon
pKa (Strongest Basic)6.67ChemAxon
Physiological Charge-2ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count5ChemAxon
Polar Surface Area153.11 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity52.16 m3·mol-1ChemAxon
Polarizability20.1 Å3ChemAxon
Number of Rings1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Human Intestinal Absorption-0.9723
Blood Brain Barrier+0.825
Caco-2 permeable-0.6418
P-glycoprotein substrateNon-substrate0.5602
P-glycoprotein inhibitor INon-inhibitor0.943
P-glycoprotein inhibitor IINon-inhibitor0.9961
Renal organic cation transporterNon-inhibitor0.9366
CYP450 2C9 substrateNon-substrate0.8319
CYP450 2D6 substrateNon-substrate0.8201
CYP450 3A4 substrateNon-substrate0.7551
CYP450 1A2 substrateNon-inhibitor0.8531
CYP450 2C9 inhibitorNon-inhibitor0.8576
CYP450 2D6 inhibitorNon-inhibitor0.8935
CYP450 2C19 inhibitorNon-inhibitor0.8319
CYP450 3A4 inhibitorNon-inhibitor0.9334
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9904
Ames testNon AMES toxic0.5596
BiodegradationNot ready biodegradable0.5431
Rat acute toxicity2.3342 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8515
hERG inhibition (predictor II)Non-inhibitor0.8616
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)


Mass Spec (NIST)
Not Available
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - DI-ESI-qTof , NegativeLC-MS/MSNot Available


This compound belongs to the class of organic compounds known as bisphosphonates. These are organic compounds containing two phosphonate groups linked together through a carbon atoms.
Organic compounds
Super Class
Organic acids and derivatives
Organic phosphonic acids and derivatives
Sub Class
Direct Parent
Alternative Parents
N-substituted imidazoles / Organic phosphonic acids / Heteroaromatic compounds / Azacyclic compounds / Organopnictogen compounds / Organophosphorus compounds / Organooxygen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives
Bisphosphonate / N-substituted imidazole / Azole / Imidazole / Organophosphonic acid / Heteroaromatic compound / Azacycle / Organoheterocyclic compound / Organic nitrogen compound / Organophosphorus compound
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
imidazoles, 1,1-bis(phosphonic acid) (CHEBI:46557)


Pharmacological action
General Function
Poly(a) rna binding
Specific Function
Key enzyme in isoprenoid biosynthesis which catalyzes the formation of farnesyl diphosphate (FPP), a precursor for several classes of essential metabolites including sterols, dolichols, carotenoids...
Gene Name
Uniprot ID
Uniprot Name
Farnesyl pyrophosphate synthase
Molecular Weight
48275.03 Da
  1. Dunford JE, Thompson K, Coxon FP, Luckman SP, Hahn FM, Poulter CD, Ebetino FH, Rogers MJ: Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J Pharmacol Exp Ther. 2001 Feb;296(2):235-42. [PubMed:11160603]
  2. Glickman JF, Schmid A: Farnesyl pyrophosphate synthase: real-time kinetics and inhibition by nitrogen-containing bisphosphonates in a scintillation assay. Assay Drug Dev Technol. 2007 Apr;5(2):205-14. [PubMed:17477829]
  3. Guo RT, Cao R, Liang PH, Ko TP, Chang TH, Hudock MP, Jeng WY, Chen CK, Zhang Y, Song Y, Kuo CJ, Yin F, Oldfield E, Wang AH: Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases. Proc Natl Acad Sci U S A. 2007 Jun 12;104(24):10022-7. Epub 2007 May 29. [PubMed:17535895]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Pharmacological action
General Function
Metal ion binding
Specific Function
Catalyzes the trans-addition of the three molecules of IPP onto DMAPP to form geranylgeranyl pyrophosphate, an important precursor of carotenoids and geranylated proteins.
Gene Name
Uniprot ID
Uniprot Name
Geranylgeranyl pyrophosphate synthase
Molecular Weight
34870.625 Da
  1. Guo RT, Cao R, Liang PH, Ko TP, Chang TH, Hudock MP, Jeng WY, Chen CK, Zhang Y, Song Y, Kuo CJ, Yin F, Oldfield E, Wang AH: Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases. Proc Natl Acad Sci U S A. 2007 Jun 12;104(24):10022-7. Epub 2007 May 29. [PubMed:17535895]
Small molecule
Pharmacological action
  1. Jahnke W, Henry C: An in vitro assay to measure targeted drug delivery to bone mineral. ChemMedChem. 2010 May 3;5(5):770-6. doi: 10.1002/cmdc.201000016. [PubMed:20209564]
  2. Nancollas GH, Tang R, Phipps RJ, Henneman Z, Gulde S, Wu W, Mangood A, Russell RG, Ebetino FH: Novel insights into actions of bisphosphonates on bone: differences in interactions with hydroxyapatite. Bone. 2006 May;38(5):617-27. Epub 2005 Jul 20. [PubMed:16046206]


Pharmacological action
General Function
Transporter activity
Specific Function
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
Gene Name
Uniprot ID
Uniprot Name
Multidrug resistance-associated protein 1
Molecular Weight
171589.5 Da
  1. Yildiz M, Celik-Ozenci C, Akan S, Akan I, Sati L, Demir R, Savas B, Ozben T, Samur M, Ozdogan M, Artac M, Bozcuk H: Zoledronic acid is synergic with vinblastine to induce apoptosis in a multidrug resistance protein-1 dependent way: an in vitro study. Cell Biol Int. 2006 Mar;30(3):278-82. Epub 2006 Feb 2. [PubMed:16458542]

Drug created on June 13, 2005 07:24 / Updated on May 24, 2019 23:15