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Histrelin

In Advanced Prostate Cancer

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Abstract

Histrelin is a gonadotropin-releasing hormone agonist available in a diffusion-controlled reservoir drug delivery system for subcutaneous implantation.

The subcutaneous histrelin implant provided sustained suppression of serum testosterone, luteinizing hormone (LH) and prostate-specific antigen levels for up to 1 year in patients with advanced prostate cancer in two phase II or III trials.

In the noncomparative, multicentre, phase III study, serum testosterone was suppressed to castrate levels (i.e. ≤50 ng/dL) within 4 weeks in all patients who received a histrelin acetate 50 mg implant, with 99–100% of histrelin implant recipients maintaining castrate levels for the remainder of the 1-year treatment period. Such efficacy was provided irrespective of patient age or stage of disease.

Although a transient surge in serum testosterone levels occurred after placement of the initial histrelin implant, no acute elevations in testosterone or LH levels were observed in patients whose implant was replaced after 1 year of therapy and suppression of these hormones continued to be maintained.

The histrelin implant was generally well tolerated in patients with advanced prostate cancer in the phase III trial and in a pooled analysis. No patients prematurely discontinued treatment because of adverse events, most of which were the consequence of hormone suppression.

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References

  1. American Cancer Society®. Global cancer facts and figures 2007 [online]. Available from URL: http://www.cancer.org/downloads/STT/Global_Facts_and_Figures_2007_rev2.pdf [Accessed 2009 Dec 16]

  2. Jemal A, Siegel R, Ward E, et al. Cancer statistics, 2009. CA Cancer J Clin 2009 Jul–Aug 31; 59(4): 225–49

    Article  PubMed  Google Scholar 

  3. Thompson I, Thrasher JB, Aus G, et al. Guideline for the management of clinically localized prostate cancer: 2007 update. J Urol 2007 Jun; 177(6): 2106–31

    Article  PubMed  Google Scholar 

  4. Horwich A, Parker C, Kataja V. Prostate cancer: ESMO clinical recommendations for diagnosis, treatment and follow-up. Ann Oncol 2008 May; 19 Suppl. 2: ii45–6

    Article  PubMed  Google Scholar 

  5. Loblaw DA, Virgo KS, Nam R, et al. Initial hormonal management of androgen-sensitive metastatic, recurrent, or progressive prostate cancer: 2007 update of an American Society of Clinical Oncology practice guideline. J Clin Oncol 2007 Apr 20; 25(12): 1596–605

    Article  PubMed  CAS  Google Scholar 

  6. National Institute for Health and Clinical Excellence. Prostate cancer: diagnosis and treatment [online]. Available from URL: http://www.nice.org.uk/nicemedia/pdf/CG58FullGuideline.pdf [Accessed 2009 Dec 9]

  7. National Comprehensive Cancer Network®. NCCN clinical practice guidelines in oncology™ prostate cancer, V.2.2009 [online]. Available from URL: http://www.nccn.org [Accessed 2009 Dec 9]

  8. Heidenreich A, Aus G, Bolla M, et al. EAU guidelines on prostate cancer. Eur Urol 2008 Jan; 53(1): 68–80

    Article  PubMed  Google Scholar 

  9. Kintzel PE, Chase SL, Schultz LM, et al. Increased risk of metabolic syndrome, diabetes mellitus, and cardiovascular disease in men receiving androgen deprivation therapy for prostate cancer. Pharmacotherapy 2008 Dec; 28(12): 1511–22

    Article  PubMed  CAS  Google Scholar 

  10. Freedland SJ, Eastham J, Shore N. Androgen deprivation therapy and estrogen deficiency induced adverse effects in the treatment of prostate cancer. Prostate Cancer Prostatic Dis 2009; 12(4): 333–8

    Article  PubMed  CAS  Google Scholar 

  11. van Poppel H, Nilsson S. Testosterone surge: rationale for gonadotropin-releasing hormone blockers? Urology 2008 Jun; 71(6): 1001–6

    Article  PubMed  Google Scholar 

  12. Schlegel P. A review of the pharmacokinetic and pharmacological properties of a once-yearly administered histrelin acetate implant in the treatment of prostate cancer. BJU Int 2009 Mar; 103 Suppl. 2: 7–13

    Article  PubMed  CAS  Google Scholar 

  13. Hall MC, Fritzsch RJ, Sagalowsky AI, et al. Prospective determination of the hormonal response after cessation of luteinizing hormone-releasing hormone agonist treatment in patients with prostate cancer. Urology 1999 May; 53(5): 898–903

    Article  PubMed  CAS  Google Scholar 

  14. Oefelein MG. Time to normalization of serum testosterone after 3-month luteinizing hormone-releasing hormone agonist administered in the neoadjuvant setting: implications for dosing schedule and neoadjuvant study consideration. J Urol 1998 Nov; 160(5): 1685–8

    Article  PubMed  CAS  Google Scholar 

  15. Food and Drug Administration. Vantas™ (histrelin implant): US prescribing information [online]. Available from URL: http://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21732lbl.pdf [Accessed 2009 Dec 4]

  16. Orion Pharma (UK) Limited. Vantas 50 mg implant: UK summary of product characteristics [online]. Available from URL: http://emc.medicines.org.uk [Accessed 2009 Dec 4]

  17. Barradell LB, McTavish D. Histrelin: a review of its pharmacological properties and therapeutic role in central precocious puberty. Drugs 1993; 45(4): 570–88

    Article  PubMed  CAS  Google Scholar 

  18. Schlegel PN, Kuzma P, Frick J, et al. Effective long-term androgen suppression in men with prostate cancer using a hydrogel implant with the GnRH agonist histrelin. Urology 2001 Oct; 58(4): 578–82

    Article  PubMed  CAS  Google Scholar 

  19. Schlegel PN. Efficacy and safety of histrelin subdermal implant in patients with advanced prostate cancer. J Urol 2006 Apr; 175(4): 1353–8

    Article  PubMed  CAS  Google Scholar 

  20. Doelle GC, Evans RM, Alexander AN, et al. Single dose responses to the gonadotropin-releasing hormone agonist analogue [(imBz 1)-D-His6,Pro9-NEt]GnRH. Horm Metab Res 1986 Mar; 18(3): 201–2

    Article  PubMed  CAS  Google Scholar 

  21. DeFazio J, Lu JKH, Vale W, et al. Effects of the (imBz1)D-His6, Des-Gly analog of GnRH on gonadotropin and estradiol secretion in normal women. Endocr Res 1984; 10(2): 163–70

    Article  PubMed  CAS  Google Scholar 

  22. Dineen MK, Tierney DS, Kuzma P, et al. An evaluation of the pharmacokinetics and pharmacodynamics of the histrelin implant for the palliative treatment of prostate cancer. J Clin Pharmacol 2005 Nov; 45(11): 1245–9

    Article  PubMed  CAS  Google Scholar 

  23. Chertin B, Spitz IM, Lindenberg T, et al. An implant releasing the gonadotropin hormone-releasing hormone agonist histrelin maintains medical castration for up to 30 months in metastatic prostate cancer. J Urol 2000 Mar; 163(3): 838–44

    Article  PubMed  CAS  Google Scholar 

  24. Fridmans A, Chertin B, Koulikov D, et al. Reversibility of androgen deprivation therapy in patients with prostate cancer. J Urol 2005 Mar; 173(3): 784–9

    Article  PubMed  CAS  Google Scholar 

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Acknowledgements and Disclosures

The manuscript was reviewed by: A. Berruti, Medical Oncology, Department of Clinical and Biological Sciences, University of Torino, Torino, Italy; R.B. Nadler, Northwestern University, Chicago, Illinois, USA.

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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    Emma D. Deeks

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Correspondence to Emma D. Deeks.

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Deeks, E.D. Histrelin. Drugs 70, 623–630 (2010). https://doi.org/10.2165/11204800-000000000-00000

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