Degarelix

Degarelix 구조식 이미지
카스 번호:
214766-78-6
상품명:
Degarelix
동의어(영문):
Degarelix acetate;FirMagon;Dikarek;DEGARELIX;Degarelix-d7;Degarelix impurity;DEGARELIX USP/EP/BP;Degarelix acetate salt;Degarelix, Degarelix acetate;Degarelix acetate(FE-200486,Degarelix)
CBNumber:
CB52448443
분자식:
C82H103ClN18O16
포뮬러 무게:
1632.26
MOL 파일:
214766-78-6.mol

Degarelix 속성

밀도
1.325±0.06 g/cm3(Predicted)
저장 조건
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
용해도
DMSO:10.0(Max Conc. mg/mL);6.13(Max Conc. mM)
H2O:25.0(Max Conc. mg/mL);15.32(Max Conc. mM)
산도 계수 (pKa)
10.38±0.40(Predicted)
시퀀스
Ac-D-2-Nal-D-4-Cl-Phe-D-3-Pal-Ser-4-Aph(Hor)-4-D-Aph(Cbm)-Leu-Lys(ipr)-Pro-D-Ala-NH2
InChIKey
MEUCPCLKGZSHTA-XYAYPHGZSA-N
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
유해 물질 데이터 214766-78-6(Hazardous Substances Data)
그림문자(GHS): GHS hazard pictograms
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H360 태아 또는 생식능력에 손상을 일으킬 수 있음 생식독성 물질 구분 1A, 1B 위험 GHS hazard pictograms
예방조치문구:

Degarelix C화학적 특성, 용도, 생산

개요

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.

용도

Degarelix, is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.

Clinical Use

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.

부작용

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.

Degarelix 준비 용품 및 원자재

원자재

준비 용품


Degarelix 공급 업체

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sales@coreychem.com China 29914 58

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