Triptorelin 6-Month Formulation in the Management of Patients with Locally Advanced and Metastatic Prostate Cancer

Lundström, Eija; Rencken, R. K.; Wyk, Johann H. van; Coetzee, L.; Bahlmann, Johann C.M.; Reif, Simon; Strasheim, Erdam A.; Bigalke, Martin C.; Pontin, A. R.; Goedhals, L.; Steyn, D. G.; Heyns, Chris F.; Aldera, Luigi A.; Mackenzie, Thomas M.; Purcea, Daniela; Grosgurin, Pierre; Porchet, Hervé

doi:10.2165/11319690-000000000-00000

Cited by 48 publications

(70 citation statements)

References 12 publications

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“…Triptorelin has been formulated as the pamoate salt to improve the manufacturing process and to aid in the development of slow-release formulations (a 6-month formulation of triptorelin pamoate exists and is used in the treatment of prostate cancer [31,32]). Pamoic acid, also called embonic acid, is a naphthoic acid derivative.…”

Section: Discussionmentioning

confidence: 99%

A 6-Month Trial of the Efficacy and Safety of Triptorelin Pamoate (11.25 mg) Every 3 Months in Children with Precocious Puberty: A Retrospective Comparison with Triptorelin Acetate

Zénaty

Blumberg²,

Liyanage³

et al. 2016

Horm Res Paediatr

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Background/Aims: To evaluate the efficacy and safety of a triptorelin pamoate (11.25 mg) 3-month formulation in the management of central precocious puberty (CPP) (TP Study) and to retrospectively compare it with a triptorelin acetate (11.25 mg) 3-month formulation (TA Study). Methods: We conducted two phase III, multicentre, single-stage, non-comparative, open-label studies. In the TP Study, patients with CPP received an intramuscular injection of triptorelin pamoate 11.25 mg at baseline and 3 months after baseline. Hormonal changes as well as safety and efficacy endpoints were measured at baseline, 3 months, and 6 months. Results: The baseline characteristics of the 37 patients in the TP Study were similar to those of the TA Study population. A suppressed luteinising hormone (LH) response (LH peak ≤3 IU/l) to the gonadotrophin-releasing hormone test at 3 months (primary endpoint) occurred in 83.8 and 82.8% of the cases in the TP and the TA Study, respectively. At 6 months, a suppressed LH response occurred in 86.5 and 96.8% of the cases in the TP and the TA Study, respectively. Pubertal development was slowed in both studies. Adverse events were mild to moderate and resolved without sequelae in the TP Study. Conclusion: Triptorelin pamoate 11.25 mg administered at 3-month intervals is an effective and well-tolerated treatment in patients with CPP. The efficacy and safety profiles appear similar to those reported in the literature for triptorelin acetate 11.25 mg.

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Section: Discussionmentioning

confidence: 99%

A 6-Month Trial of the Efficacy and Safety of Triptorelin Pamoate (11.25 mg) Every 3 Months in Children with Precocious Puberty: A Retrospective Comparison with Triptorelin Acetate

Zénaty

Blumberg²,

Liyanage³

et al. 2016

Horm Res Paediatr

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“…The LHRH agonist [D-Trp6]LHRH is clinically approved for the treatment of hormone-dependent cancers, predominantly prostate cancer. Over the course of treatment, [D-Trp6]LHRH causes a surge of testosterone release at the beginning and then a reduction to levels similar to postcastration levels approximately 4 wk after injection (20,21). Retinoic acid is involved in the regulation of steroidogenesis, and its use significantly reduces cortisol secretion (19).…”

Section: Impact Of Lhrh Agonist [D-trp6]lhrh and Retinoic Acid On Enbmentioning

confidence: 99%

Transplantation of bovine adrenocortical cells encapsulated in alginate

Balyura

Gelfgat

Ehrhart‐Bornstein

et al. 2015

Proc. Natl. Acad. Sci. U.S.A.

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Current treatment options for adrenal insufficiency are limited to corticosteroid replacement therapies. However, hormone therapy does not replicate circadian rhythms and has unpleasant side effects especially due to the failure to restore normal function of the hypothalamic-pituitary-adrenal (HPA) axis. Adrenal cell transplantation and the restoration of HPA axis function would be a feasible and useful therapeutic strategy for patients with adrenal insufficiency. We created a bioartificial adrenal with 3D cell culture conditions by encapsulation of bovine adrenocortical cells (BACs) in alginate (enBACs). We found that, compared with BACs in monolayer culture, encapsulation in alginate significantly increased the life span of BACs. Encapsulation also improved significantly both the capacity of adrenal cells for stable, long-term basal hormone release as well as the response to pituitary adrenocorticotropic hormone (ACTH) and hypothalamic luteinizing hormone-releasing hormone (LHRH) agonist, [D-Trp6]LHRH. The enBACs were transplanted into adrenalectomized, immunodeficient, and immunocompetent rats. Animals received enBACs intraperitoneally, under the kidney capsule (free cells or cells encapsulated in alginate slabs) or s.c. enclosed in oxygenating and immunoisolating βAir devices. Graft function was confirmed by the presence of cortisol in the plasma of rats. Both types of grafted encapsulated cells, explanted after 21-25 d, preserved their morphology and functional response to ACTH stimulation. In conclusion, transplantation of a bioartificial adrenal with xenogeneic cells may be a treatment option for patients with adrenocortical insufficiency and other stress-related disorders. Furthermore, this model provides a microenvironment that ensures 3D cell-cell interactions as a unique tool to investigate new insights into cell biology, differentiation, tissue organization, and homeostasis.adrenal | alginate encapsulation | cell transplantation | LHRH A drenal insufficiency is the failure of adrenocortical cells to produce adequate amounts of glucocorticoids and/or mineralocorticoids. These steroid hormones play a central role in the body's homeostasis of energy, salt, and fluid; thus, adrenal insufficiency is a potentially life-threatening condition. The most relevant causes of adrenal insufficiency are autoimmune disorders (up to 80%); infectious diseases; hereditary factors; traumatic, metabolic, or neoplastic conditions; or surgical bilateral adrenalectomy, sometimes due to a compulsory therapeutic strategy in the treatment of adrenal tumors or congenital adrenal hyperplasia

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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.…”

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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Triptorelin 6-Month Formulation in the Management of Patients with Locally Advanced and Metastatic Prostate Cancer

Cited by 48 publications

References 12 publications

A 6-Month Trial of the Efficacy and Safety of Triptorelin Pamoate (11.25 mg) Every 3 Months in Children with Precocious Puberty: A Retrospective Comparison with Triptorelin Acetate

A 6-Month Trial of the Efficacy and Safety of Triptorelin Pamoate (11.25 mg) Every 3 Months in Children with Precocious Puberty: A Retrospective Comparison with Triptorelin Acetate

Transplantation of bovine adrenocortical cells encapsulated in alginate

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

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