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

Abstract

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.

Nano-encapsulation of a novel anti-Ran-GTPase peptide for blockade of regulator of chromosome condensation 1 (RCC1) function in MDA-MB-231 breast cancer cells

“…Similarly, FDA approval is in place for other peptide drugs incorporated within polymeric carriers, such as leuprolide acetate indicated for the treatment of advanced prostate and breast cancers (Sethi and Sanfilippo, 2009), and a controlled release formulation based on octreotide acetate-loaded PLGA for tumour treatment in neuroendocrine disorders and carcinoid syndrome (Anthony and Freda, 2009). A PLGAbased microparticle formulation of triptorelin pamoate used for advanced prostate cancer and other indications, was given regulatory approval in 2000 (Crawford and Phillips, 2011).…”

Are all gonadotrophin‐releasing hormone agonists equivalent for the treatment of prostate cancer? A systematic review

“…As testosterone stimulates the growth of cancerous prostate cells, reducing the circulating level of testosterone to that achieved by surgical castration is the goal of androgendeprivation therapy (ADT) for prostate cancer [1,2]. ADT is indicated for high-risk localised, locally advanced or metastatic prostate cancer [3].…”

“…ADT is indicated for high-risk localised, locally advanced or metastatic prostate cancer [3]. Castration can be achieved with bilateral orchidectomy or treatment with a GnRH agonist or antagonist [1,3]. GnRH agonists are the most widely used form of ADT, and are often used in combination with radiotherapy or radical prostatectomy [3].…”

“…GnRH agonists typically have short half-lives (4.9 h for goserelin and 2.8 h for triptorelin, for example [9,10]), which renders them incompatible with chronic parenteral administration [10,11]. Sustained-release formulations of each of these products have been developed to reduce the number of injections, improve convenience, and increase adherence [1,12]. Modern formulations of GnRH agonists consist of biocompatible biodegradable polymeric matrices, delivered by either subcutaneous (s.c.) or intramuscular (i.m.)…”

Leuprorelin and Triptorelin in the treatment of Prostate Cancer: Medication adherence, Persistence and Economic Evaluation in Five Years of Analysis

“…For this two drugs have been demonstrated to have comparable tolerability as monthly such as quarterly administration [18,19]. The development of depot formulations, 1-3 and six months was made to improve the patient's compliance with same drug safety and tolerability [20]. The loss of medication adherence is a global problem that affects the clinical outcome and economic health [21,22].…”