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Description: 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.
Drug Type: Small Molecule; Approved
Pharmacology: 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.
Indication: 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.
Half Life: 146 hours
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Data Correlations | 2 studies

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Genes category icon Genes
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FDPS 100 100
CXCL2 100 100
CCL3 100 100
IL8 99 99
PTGS2 97 97
FCGR3B 95 95
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Biogroups category icon Biogroups
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T-cell Receptor and CD3 Complex 100 100
T-cell Receptor Activation Pathway 100 100
Ribosome 100 100
Cell surface antigen 99 99
I43 - oprin 99 99
Activation of cAMP-dependent Protei… 99 99
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Individual Studies

  • Osteonecrosis of the jaw in Multiple Myeloma patients

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    Transcriptional profiling of peripheral blood mononuclear cells in 11 patients with osteonecrosis of the jaw (ONJ) and multiple myeloma (MM) and compared with the profiles of the 10 myeloma patients on bisphosphonate therapy without osteonecrosis of the jaw and 5 healthy volunteers.

    Authors: Raje Noopur, Vallet Sonia, Chhetri Shweta

    Organization: dana-farber cancer institute medical onc…

  • Drug target sets for approved compounds

    Homo sapiens Homo sapiens | Therapeutic   Therapeutic

    The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information.

    Authors: David S Wishart, Craig Knox, An Chi Guo et al.

    Organization: Department of Computing Science, Univers…
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Associated Researchers

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Thought leaders and organizations working on research involving Zoledronic Acid.

View All Author iconAuthors
  • Fred Saad
  • Peter Mesenbrink
  • Robert E Coleman
  • Jukka Mönkkönen
  • Hannu Mönkkönen
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • Novartis
  • Novartis Pharmaceuticals
  • The Cleveland Clinic
  • Duke University
  • University of Pittsburgh
View All Affiliations icon Organizations
  • University of Sheffield
  • Centre Hospitalier de l'Université de Montréal
  • University of Aberdeen
  • University of Kuopio
  • National and Kapodistrian University of Athens

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