3-Month Formulation of Goserelin Acetate (‘Zoladex’ 10.8-mg Depot) in Advanced Prostate Cancer: Results from an Italian, Open, Multicenter Trial

Fontana, Dario; M, Mari Ruiz; Martinelli, Antonio; Boccafoschi, C.; Magno, Carlo; Turriziani, M; Maymone, S; Sc, Cunico; Zanollo, A; Montagna, Giacomo; Frongia, Mauro; Jacobellis, U

doi:10.1159/000070142

Cited by 42 publications

(25 citation statements)

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“…With regard to the 20-ng/dl breakpoint, the available data suggest that the classical 3-month depot formulation of leuprolide yields a castration level of testosterone in 87-92% of the patients [23,25] , the novel formulation leuprolide in 88-97.5% [8,9,28,30] , and goserelin in 96% [27] .…”

Section: Testosterone Levels During Androgen Deprivation Therapy Withmentioning

confidence: 99%

Impact of Surgical and Medical Castration on Serum Testosterone Level in Prostate Cancer Patients

et al. 2009

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Introduction: The paper aims at evaluating the role of testosterone levels and their cut-off points in the treatment of prostate cancer with androgen deprivation therapy. Materials and Methods: We performed a non-systematic review of the literature, searching Medline using the following key words: ‘Prostatic neoplasms/therapy’ [MeSH], ‘Buserelin’ [MeSH], ‘Goserelin’ [MeSH], ‘Leuprolide’ [MeSH], ‘Triptorelin’ [MeSH], ‘prostate cancer*’ [tiab], and ‘testoster*’ [tiab]. Results: The most commonly used cut-off point of testosterone to define castration was 50 ng/dl. In this respect, GnRH agonists allowed castration in a very high percentage of patients (87.5–100%). Specifically, triptorelin was reported to yield castration level of testosterone in 98.8%, the classical formulation of leuprolide in 95–98.8% of the cases, and Eligard®, a novel formulation of leuprolide, in 99–100%. With regard to the 20-ng/dl breakpoint, available data suggest that goserelin yields castration level of testosterone in 96%, the classical formulation of leuprolide in 87–92% of the patients, and the novel formulation in 88–97.5%. Conclusions: The clinical significance of different levels of testosterone yielded during androgen deprivation therapy is still unknown. Considering the standard cut-off point of 50 ng/dl, GnRH agonists allowed castration in a very high percentage of patients.

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Section: Testosterone Levels During Androgen Deprivation Therapy Withmentioning

confidence: 99%

Impact of Surgical and Medical Castration on Serum Testosterone Level in Prostate Cancer Patients

et al. 2009

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“…In addition to their use in surgical sutures and prosthetic devices, biodegradable poly(ester) polymers are also used in commercially available injectable products, for example, Risperdal Consta (Risperidone in PLGA) and Lupron Depot (Leuprolide acetate in PLGA) [6,7]. Literature also cites examples of a number of therapeutic agents like small molecules, peptides, and proteins that have been successfully encapsulated into these polymers [8,9]. Depending on the polymer type and the incorporated therapeutic agent, the polymeric dosage form can provide sustained drug levels for varying durations in vivo [10,11].…”

Section: Introductionmentioning

confidence: 99%

Enhanced Degradation of Lactide-co-Glycolide Polymer with Basic Nucleophilic Drugs

D’Souza

Faraj

Dorati

et al. 2015

Advances in Pharmaceutics

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The purpose of this study was to examine the degradative effect of weakly basic nucleophilic drugs on a lactide-co-glycolide (PLGA) polymer in a microsphere formulation. Biodegradable PLGA microspheres of two second-generation atypical antipsychotics, Risperidone and Olanzapine, were manufactured using a solvent extraction/evaporation technique. The effect of drug content, buffer pH and temperature on polymer molecular weight and degradation, were examined via a series of experiments and compared against a control (Placebo PLGA microspheres). In comparison to Placebo microspheres, significant polymer molecular weight reduction was observed upon encapsulation of varying levels of either Risperidone or Olanzapine. There was excellent correlation between the extent of molecular weight reduction during manufacture and the amount of encapsulated drug in the microspheres. Subsequent studies on polymer degradation showed: the following (a) the Placebo and Olanzapine microspheres followed pseudo first order kinetics, (b) Risperidone microspheres exhibited biphasic degradation profiles, and (c) polymer degradation was dependent on temperature, not pH. The findings of these studies show that encapsulation of weakly basic nucleophile type drugs into PLGA can accelerate the biodegradation of the PLGA and have major implications on the design of polymeric microsphere drug delivery systems.

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“…Although free of compliance issues and apparently associated with good quality of life (QoL) [54], bilateral orchiectomy has been largely replaced by medical castration with LHRH agonists because of improved patient and physician acceptance. LHRH agonist formulations may differ in testosterone-suppression levels and duration of suppression [55]; however, no data relate these differences to differences in disease progression or survival.…”

Section: Evidence Synthesismentioning

confidence: 99%

Contemporary Role of Androgen Deprivation Therapy for Prostate Cancer

et al. 2012

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Context Androgen deprivation therapy (ADT) for prostate cancer (PCa) represents one of the most effective systemic palliative treatments known for solid tumors. Although clinical trials have assessed the role of ADT in patients with metastatic and advanced locoregional disease, the risk–benefit ratio, especially in earlier stages, remains poorly defined. Given the mounting evidence for potentially life-threatening adverse effects with short- and long-term ADT, it is important to redefine the role of ADT for this disease. Objective Review the published experience with currently available ADT approaches in various contemporary clinical settings of PCa and reported serious treatment-related adverse events. This review addresses the level of evidence associated with the use of ADT in PCa, focusing upon survival outcome measures. Furthermore, this paper discusses evolving approaches targeting androgen receptor signaling pathways and emerging evidence from clinical trials with newer compounds. Evidence acquisition A comprehensive review of the literature was performed, focusing on data from the last 10 yr (January 2000 to July 2011) and using the terms androgen deprivation, hormone treatment, prostate cancer and adverse effects. Abstracts from trials reported at international conferences held in 2010 and 2011 were also evaluated. Evidence synthesis Data from randomized controlled trials and population-based studies were analyzed in different clinical paradigms. Specifically, the role of ADT was evaluated in patients with nonmetastatic disease as the primary and sole treatment, in combination with radiation therapy (RT) or after surgery, and in patients with metastatic disease. The data suggest that in men with nonmetastatic disease, the use of primary ADT as monotherapy has not shown a benefit and is not recommended, while ADT combined with conventional-dose RT (<72 Gy) for patients with high-risk disease may delay progression and prolong survival. The postoperative use of ADT remains poorly evaluated in prospective studies. Likewise, there are no trials evaluating the role of ADT in patients with biochemical relapses after surgery or RT. In patients with metastatic disease, there is a clear benefit in terms of quality of life, reduction of disease-associated morbidity, and possibly survival. Treatment with bilateral orchiectomy, luteinizing hormone–releasing hormone agonist therapy, with and without antiandrogens has been associated with various serious adverse events, including cardiovascular disease, diabetes, and skeletal complications that may also affect mortality. Conclusions Although ADT is an effective treatment of PCa, consistent long-term benefits in terms of quality and quantity of life are predominantly evident in patients with advanced/metastatic disease or when ADT is used in combination with RT (<72 Gy) in patients with high-risk tumors. Implementation of ADT should be evidence based, with special consideration to adverse events and the risk–benefit ratio.

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3-Month Formulation of Goserelin Acetate (‘Zoladex’ 10.8-mg Depot) in Advanced Prostate Cancer: Results from an Italian, Open, Multicenter Trial

Cited by 42 publications

References 10 publications

Impact of Surgical and Medical Castration on Serum Testosterone Level in Prostate Cancer Patients

Impact of Surgical and Medical Castration on Serum Testosterone Level in Prostate Cancer Patients

Enhanced Degradation of Lactide-co-Glycolide Polymer with Basic Nucleophilic Drugs

Contemporary Role of Androgen Deprivation Therapy for Prostate Cancer

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