Skip to main content
SpringerLink
Log in

Zoledronic Acid

  • Adis New Drug Profile
  • Published:
Drugs Aims and scope Submit manuscript

Abstract

  • ▴ Zoledronic acid (zoledronate) is a new generation bisphosphonate that inhibits osteoclast bone resorption. It was much more potent than other bisphosphonates at inhibiting 1,25-dihydroxyvitamin D3-induced hypercalcaemia in a rat model and calcium release in vitro.

  • ▴ A single 5-minute intravenous infusion of zoledronic acid (4 or 8mg) was significantly more effective than a 2-hour infusion of pamidronic acid (pamidronic acid disodium, pamidronate disodium) [90mg] in normalising serum calcium levels in patients with hypercalcaemia of malignancy and resulted in a significantly longer median time to relapse (pooled analysis from 2 randomised, double-blind, parallel-group trials).

  • ▴ There were no differences in tolerability between zoledronic acid and pamidronic acid in comparative trials; the most common events in pivotal trials were fever, anaemia, nausea, constipation and dyspnoea. Fever, hypophosphataemia and hypocalcaemia were the most common events in a small phase I trial.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3

Similar content being viewed by others

References

  1. Green MD. Oral bisphosphonates and malignancy. Med J Aust 1997 Aug 18; 167:211–2

    PubMed  CAS  Google Scholar 

  2. Body JJ, Coleman RE, Piccart M. Use of bisphosphonates in cancer patients. Cancer Treat Rev 1996; 22(4): 265–87

    Article  PubMed  CAS  Google Scholar 

  3. Body JJ. Clinical research update: zoledronate. Cancer 1997 Oct 15; 80 Suppl.: 1699–701

    Article  PubMed  CAS  Google Scholar 

  4. Novartis Pharma. Zometa International Monograph. Novartis Pharma (Data on file)

  5. Berenson JR, Vescio R, Henick K, et al. A phase I, open label, dose ranging trial of intravenous bolus zoledronic acid, a novel bisphosphonate, in cancer patients with metastatic bone disease. Cancer 2001 Jan 1; 91(1): 144–54

    Article  PubMed  CAS  Google Scholar 

  6. Green JR, Müller K, Jaeggi KA. Preclinical pharmacology of CGP 42’446, a new, potent, heterocyclic bisphosphonate compound. J Bone Miner Res 1994 May; 9: 745–51

    Article  PubMed  CAS  Google Scholar 

  7. Pataki A, Müller K, Green JR, et al. Effects of short-term treatment with the bisphosphonates zoledronate and pamidronate on rat bone: a comparative histomorphometric study on the cancellous bone formed before, during, and after treatment. Anat Rec 1997 Dec; 249: 458–68

    Article  PubMed  CAS  Google Scholar 

  8. Evans CE, Braidman IP. Effects of two novel bisphosphonates on bone cells in vitro. Bone Miner 1994 Aug; 26: 95–107

    Article  PubMed  CAS  Google Scholar 

  9. Green JR, Seltenmeyer Y, Jaeggi KA, et al. Renal tolerability profile of novel, potent bisphosphonates in two short-term rat models. Pharmacol Toxicol 1997 May; 80: 225–30

    Article  PubMed  CAS  Google Scholar 

  10. Novartis Pharma. Zometa: product information [in German]. Novartis Pharma

  11. Berenson J, Ravera C, Ma P, et al. Population pharmacokinetics (PK) of Zometa [abstract no. 814]. Proceedings of the American Society of Clinical Oncology; 2000 May 20–23; New Orleans, 209a

  12. Major P, Lortholary A, Hon J, et al. Zoledronic acid is superior to pamidronate in the treatment of hypercalcemia of malignancy: a pooled analysis of two randomized, controlled clinical trials. J Clin Oncol 2001 Jan 15; 19(2): 558–67

    PubMed  CAS  Google Scholar 

  13. Body JJ, Lortholary A, Romieu G, et al. A dose-finding study of zoledronate in hypercalcemic cancer patients. J Bone Miner Res 1999; 14(9): 1557–61

    Article  PubMed  CAS  Google Scholar 

  14. Novartis alters zometa study design due to renal function concerns. The Pink Sheet, 2000 Jun 26; 21

Download references

Author information

Authors and Affiliations

  1. Adis International Limited, Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand

    Susan M. Cheer & Stuart Noble

Authors
  1. Susan M. Cheer
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Stuart Noble
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Susan M. Cheer.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Cheer, S.M., Noble, S. Zoledronic Acid. Drugs 61, 799–805 (2001). https://doi.org/10.2165/00003495-200161060-00010

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.2165/00003495-200161060-00010

Keywords

Search

Navigation