Drug intelligence / Profile preview

antiandrogen + leuprolide acetate

Development stage
Unknown
Lead developer
European Organisation for the Research and Treatment of Cancer
Modality
Peptides, Small Molecules
Administration
Subcutaneous, Oral
01

Overview

This refers to a combination hormonal therapy regimen consisting of a systemic antiandrogen and leuprolide acetate, evaluated by the European Organisation for Research and Treatment of Cancer (EORTC) in the Phase III trial EORTC 22043-30041. The regimen is used as a short-term androgen deprivation therapy (ADT) in conjunction with post-operative external beam radiotherapy for patients with localized or locally advanced prostate cancer (specifically pT3 or pT2R1). Leuprolide acetate is a synthetic peptide and a potent gonadotropin-releasing hormone (GnRH) receptor agonist; chronic administration leads to downregulation of GnRH receptors and suppression of pituitary gonadotropin secretion, ultimately reducing serum testosterone to castrate levels. The concomitant antiandrogen serves to block the androgen receptor, preventing the action of residual adrenal androgens and mitigating the initial testosterone flare associated with GnRH agonist initiation. This combination is typically studied in the adjuvant or salvage setting following radical prostatectomy to improve biochemical-free survival.

Other names
Androgen Deprivation TherapyADTHormone therapyantiandrogen therapy + leuprolide acetate
02

Targets

AR (Adrenergic receptors)GnRHR (Gonadotropin-releasing hormone receptor)

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