デガレリクス 化学特性,用途語,生産方法
効能
抗悪性腫瘍薬, 性腺刺激ホルモン放出ホルモン受容体拮抗薬
説明
Antagonists of GnRH have proven to be an effective therapy for
hormonally regulated cancers, such as prostate and some types of
breast. As analogs of GnRH, they bind competitively and reversibly
to GnRH receptors in the pituitary gland, thereby blocking the release
of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). In
men, the reduction of LH triggers the ablation of testosterone secretion
from the testes, and these castration-like levels have been essential in
the effective management of advanced prostate cancer. In comparison
to GnRH agonists, antagonists do not suffer from a potential flare of
the disease as a result of an initial stimulation of the hypothalamic-pituitary-gonadal axis prior to down-regulation of the GnRH
receptor. Moreover, GnRH antagonists provide beneficial effects more
rapidly postdosing and result in a more efficient suppression of gonadotropin levels.
With this in mind, degarelix acetate has been launched
as a third-generation GnRH antagonist for the treatment of prostate
cancer, and it joins other third-generation agents, ganirelix and cetronelix, on the market.
使用
Degarelix, is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
臨床応用
Ferring launched degarelix acetate, a gonadotrophin-releasing
hormone (GnRH) antagonist, in 2009 in the U.S. for the treatment
of prostate cancer. The compound has been approved by the
E.U. for the same indication, and in the same year it was launched
in the UK and Germany. Degarelix has been developed as a
one-month or three-month sustained-release injectable formulation.
Compared to other GnRH antagonists, degarelix displays
improved aqueous solubility, longer acting effects and weaker
histamine-releasing properties.
副作用
The most common adverse events included injection site reactions (pain, erythema, swelling, or induration), hot flashes, increased weight, and increases in serum levels of transaminases and gamma-glutamyltransferase. In addition to being contraindicated in patients with a previous hypersensitivity to degarelix, it should not be administered to women who are or may become pregnant as fetal harm can occur. Since long-term androgen deprivation therapy prolongs the QT interval, physicians should consider whether the benefits of degarelix outweigh the potential risks in patients with congenital long QT syndrome, electrolyte abnormalities, or congestive heart failure or in patients taking antiarrhythmic medications.
デガレリクス 上流と下流の製品情報
原材料
準備製品