Therapeutic effects of leuprorelin microspheres in prostate cancer

Sharifi, Roohollah; Ratanawong, Chirasakdi; Jung, Ashley; Wu, Zhi Gang; Browneller, Robert; Lee, Mary

doi:10.1016/s0169-409x(97)00054-9

Cited by 28 publications

(18 citation statements)

References 53 publications

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“…In the first phase the product is released within a relatively short time from the surface of the spheres, and this functions as the initiation dose and establishes an effective plasma concentration 16. In the second phase, the microspheres are “digested” over 6 months and release the API as a maintenance dose to achieve the same constant plasma concentrations over time.…”

Section: Formulationsmentioning

confidence: 99%

Six-month leuprorelin acetate depot formulations in advanced prostate cancer: a clinical evaluation

Tunn¹,

Gruca²,

Bacher³

2013

CIA

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For nearly three decades, gonadotropin-releasing hormone (GnRH) agonists, particularly leuprorelin acetate (LA), have served as an important part of the treatment armamentarium for prostate cancer. The introduction of LA depot formulations provided a significant improvement in the acceptance of this therapy; however, their indicated treatment duration of 1 to 4 months was still not long enough to satisfy all medical needs. For this reason some manufacturers developed new injectable formulations that provide testosterone suppression for 6 months. This review article assesses key publications in order to compare these long-acting, commercially available, LA depot formulations and their clinical performance. The literature search identified 14 publications; by excluding reviews, duplications, and non-English articles, only three original papers describing clinical trial remained for review: two focused on microsphere-based LA formulations with either a 30 mg or 45 mg dose and one focused on a gel-based leuprorelin acetate with a 45 mg dose. All products were tested in individual clinical trials and have demonstrated their efficacy and safety.

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Section: Formulationsmentioning

confidence: 99%

Six-month leuprorelin acetate depot formulations in advanced prostate cancer: a clinical evaluation

Tunn¹,

Gruca²,

Bacher³

2013

CIA

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“…However, incorporating triptorelin into a biocompatible, biodegradable copolymer (poly-D,L-lactide-co-glycolide) as microgranules has enabled the creation of 1-, 3-, and 6-month depot formulations of the drug 6. Similar advances have facilitated development of long-term leuprolide acetate depot formulations 23,24. The first such product, a monthly 7.5 mg leuprolide acetate depot formulation, earned US Food and Drug Administration (FDA) approval for treatment of advanced prostate cancer in 1989 25.…”

Section: Evolution Of Anti-androgenic Therapiesmentioning

confidence: 99%

Six-month gonadotropin releasing hormone (GnRH) agonist depots provide efficacy, safety, convenience, and comfort

Crawford

Phillips²

2011

CMR

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Two different 6-month GnRH agonist depot formulations approved for palliative treatment of advanced and metastatic prostate cancer in the United States – leuprolide acetate 45 mg and triptorelin pamoate 22.5 mg – provide patients with efficacy and safety comparable to those of existing 1-, 3-, and 4-month GnRH agonist depots. However, the 6-month formulations can increase patient convenience, comfort, and compliance by reducing the number of physician visits and injections required. At the conclusion of their pivotal trials, the 6-month formulations demonstrated efficacy rates in achieving chemical castration (serum testosterone ≤50 ng/dL) that ranged between 93% and 99%. As with existing GnRH agonist depot formulations, hot flashes represented the most common adverse event reported in trials of 6-month leuprolide acetate or triptorelin. As such, these products may prove useful not only for their labeled indication, but also as adjuncts to other treatments such as radical prostatectomy, radiotherapy, and chemotherapy. We recommend further research, including head-to-head trials between the 6-month GnRH depots, to refine our understanding of these products.

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“…The earlier depot formulations of leuprolide use lyophilized microsphere (10–30 mm) drug delivery systems 26. Leuprolide microspheres contain the active compound in biodegradable, highly lipophilic synthetic polymer microspheres 27,28. However, the single relatively large sphere formed by Atrigel presents a smaller surface area protecting the leuprolide acetate from degradation on the surface.…”

Section: Introductionmentioning

confidence: 99%

Leuprolide acetate 1-, 3- and 6-monthly depot formulations in androgen deprivation therapy for prostate cancer in nine European countries: evidence review and economic evaluation

Wex¹,

Sidhu²,

Odeyemi³

et al. 2013

CEOR

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ObjectiveLeuprolide is an established luteinizing hormone–releasing hormone (LHRH) agonist used as first-line treatment in advanced prostate cancer. As different formulations and dosing schedules are likely to have economic implications, we aimed to evaluate their efficacy, safety, and costs in nine European countries: Austria, Belgium, Czech Republic, Hungary, Italy, Latvia, Netherlands, Poland, and Portugal.MethodsDatabase searches identified 13 clinical trials of leuprolide 1- (1 M), 3- (3 M) and 6-monthly (6 M). Only data on leuprolide with Atrigel were compared for all three formulations, which had the same efficacy, safety, and adherence. Cost-minimization analysis accounting for cost of Eligard®, specialist consultations, and diagnostics during up to 12 months follow-up was conducted. The perspective was that of public payers.ResultsNo significant differences were observed in the percentages of intention-to-treat patients achieving testosterone levels ≤ 50 ng/dL following treatment with Eligard® 1 M (93.3%), 3 M (98.3%), and 6 M (97.3%) (P > 0.05), and adverse event profiles of the three formulations were comparable. Overall, 6 M was the least expensive, with average total annual costs from €788 (Belgium) to €1839 (Portugal). The 3 M option was between 2.5% (Hungary) and 37.6% (Belgium) more expensive than 6 M; 1 M formulation was the most expensive, with costs 15.5% and 151.6% more expensive than 6 M for those countries, respectively. The 3 M option was 11.2%–45.3% less expensive than 1 M. Total costs were associated with frequency of visits for injection and monitoring. The 1 M required twelve visits, 3 M 4.4–4.8 visits, and 6 M 2.1–2.3 visits. Up to 50% additional visits could be funded with the savings resulting from switching eligible patients from 1 M and 3 M to 6 M. Results were stable in univariate and probabilistic sensitivity analyses.ConclusionEligard® formulations offer comparable efficacy and safety, but different dosing schedules require different number of visits. The 6 M formulation offers the greatest cost savings and should be considered the treatment of choice in eligible patients in Europe.

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Therapeutic effects of leuprorelin microspheres in prostate cancer

Cited by 28 publications

References 53 publications

Six-month leuprorelin acetate depot formulations in advanced prostate cancer: a clinical evaluation

Six-month leuprorelin acetate depot formulations in advanced prostate cancer: a clinical evaluation

Six-month gonadotropin releasing hormone (GnRH) agonist depots provide efficacy, safety, convenience, and comfort

Leuprolide acetate 1-, 3- and 6-monthly depot formulations in androgen deprivation therapy for prostate cancer in nine European countries: evidence review and economic evaluation

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