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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作動薬
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商品名
ゾラデックス (アストラゼネカ); ゾラデックス (アストラゼネカ); ゾラデックス (アストラゼネカ)
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説明
Goserelin acetate, like leuprolide acetate, is a synthetic superagonist nonapeptide analogue of
GnRH that possesses greater potency than the natural hormone. Note that it contains D-Ser(But)
and NH-NHCONH2 in place of Gly6 and Gly10-NH2, respectively. That is, the C terminal modification simply has an NH substituting for the CH2 of Gly, and like the C-terminal
change in leuprolide acetate, this inhibits enzymatic degradation of the peptide by the
postproline carboxyamide peptidase.
Goserelin acetate is available in the form of a small, solid pellet that is administered as an SC
implant for the palliative treatment of advanced, metastatic breast cancer in pre- and
perimenopausal women or, similarly, as a palliative in advanced prostatic cancer. The rationale
for this drug's use is, as described above, its ability as a superagonist to bring the levels of
estradiol or testosterone to near castrate levels, thus slowing the progression of breast or
prostate carcinoma, respectively. Additionally, goserelin acetate is approved for use in treating
endometriosis for up to 6 months.
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化学的特性
White Solid
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使用
Synthetic peptide agonist analog of LH-RH. Antineoplastic (hormonal).
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一般的な説明
Goserelin acetate is a synthetic decapaptide, which is a potent analog of LHRH (luteinizing hormone releasing hormone).
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臨床応用
Goserelin acetate also is used in combination with the antiandrogen flutamide for shrinking
prostate carcinoma before radiation therapy. This maximal androgen blockade combination is
used when the prostate carcinoma has been staged as locally confined to the prostate gland,
with one or both lobes as well as the seminal vesicles involved. The treatment should start 8
weeks before radiation treatment begins and be continued throughout the radiation therapy.
Furthermore, women who are to undergo hysterectomy for menorrhagia can benefit from
previous treatment with goserelin acetate, because it is able to induce endometrial thinning.
This thinning of the endometrium improves the operating environment by causing less
intrauterine bleeding, increased postoperative amenorrhea, and decreased dysmenorrhea
following surgery, which is why goserelin acetate is approved for inducing endometrial thinning
prior to a patient undergoing a hysterectomy for heavy menstrual bleeding.
