GnRH Antagonist: a New and an Effective Way of Treatment of Advanced Prostate Cancer

Tomabal, Bertrand; Raghunath, SK; Srivatsa, N; Nagaraj, V.H

doi:10.1007/s13193-016-0611-4

Cited by 1 publication

(2 citation statements)

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“…Prostate cancer is the second most common cause of cancer-related deaths in men, representing a major source of morbidity and mortality. Androgen deprivation therapy (ADT) is the primary treatment for patients with advanced prostate cancer at disease presentation, which can be achieved either with surgical or chemical castration [23]. Both GnRH agonists and GnRH antagonists act as ADT, but they have different mechanisms of action.…”

Section: Discussionmentioning

confidence: 99%

“…GnRH agonists work by initially increasing the production of testosterone, which is followed by a decrease in testosterone levels. GnRH antagonists, on the other hand, directly block the production of testosterone [3,23]. Data from clinical trials [24] and meta-analyses of clinical trials [25] suggest GnRH antagonists achieved improved PSA progression-free survival, overall survival, joint-related symptoms, urinary tract infection events and musculoskeletal events compared with GnRH agonists.…”

Section: Discussionmentioning

confidence: 99%

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Safety, Pharmacokinetic and Pharmacodynamic Evaluation of Teverelix for the Treatment of Hormone-Sensitive Advanced Prostate Cancer: Phase 2 Loading-Dose-Finding Studies

MacLean¹,

Ulys

Jankevičius

et al. 2023

Medicina

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Background and objectives: Teverelix drug product (DP) is a gonadotropin-releasing hormone antagonist in development for the treatment of patients with prostate cancer in whom androgen deprivation therapy is indicated. The aim of this paper is to present the results of five Phase 2 studies that assessed the pharmacokinetics, pharmacodynamics, efficacy and safety of different loading dose regimens of teverelix DP. Methods: Five single-arm, uncontrolled clinical trials were conducted in patients with advanced prostate cancer. The five different loading dose regimens of teverelix DP tested were (a) a single 90 mg subcutaneous (SC) injection of teverelix DP given on 3 consecutive days (Days 0, 1 and 2); (b) a single 90 mg intramuscular (IM) injection of teverelix DP given 7 days apart (Days 0 and 7); (c) a single 120 mg SC injection of teverelix DP given on 2 consecutive days (Days 0 and 1); (d) 2 × 60 mg SC injections of teverelix DP given on 3 consecutive days (Days 0, 1 and 2), and (e) 2 × 90 mg SC injections of teverelix DP given on 3 consecutive days (Days 0, 1 and 2). The primary efficacy parameter was the duration of action of an initial loading dose regimen in terms of suppression of testosterone to below the castration level (0.5 ng/mL). Results: Eighty-two patients were treated with teverelix DP. Two regimens (90 mg and 180 mg SC on 3 consecutive days) had a mean duration of castration of 55.32 days and 68.95 days with >90% of patients having testosterone levels < 0.5 ng/mL at Day 28. The mean onset of castration for the SC regimens ranged from 1.10 to 1.77 days, while it was slower (2.4 days) with IM administration. The most common adverse event (AE) was injection site reaction. No AEs of severe intensity were reported. Conclusions: Teverelix DP is safe and well tolerated. Castrate levels of testosterone can be rapidly achieved following the subcutaneous injection of teverelix DP on 3 consecutive days. Streamlining of the administration of the loading dose and identifying a suitable maintenance dose will be investigated in future trials.

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Section: Discussionmentioning

confidence: 99%