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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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化学的特性
Hygroscopic, white or almost white powder.
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使用
Gonadotropin releasing hormone (gonadorelin) analogue; treatment of prostate cancer.
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定義
ChEBI: An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, D-leucyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. Leuprorelin is a synthetic nonapeptide analogue of gonadotropin-releasi
g hormone, and is used as a subcutaneous hydrogel implant (particularly as the acetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.
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適応症
Leuprolide is a potent LH-RH agonist for the first
several days to a few weeks after initiation of therapy,
and therefore, it initially stimulates testicular and ovarian
steroidogenesis. Because of this initial stimulation of
testosterone production, it is recommended that patients
with prostatic cancer be treated concurrently with
leuprolide and the antiandrogen flutamide (discussed
earlier). Leuprolide is generally well tolerated, with hot
flashes being the most common side effect.
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合成
The synthesis process of Leuprorelin includes the following steps:
(1) Fmoc-Pro-HMPB-AM resin is obtained from Fmoc-Pro-OH and HMPB-AM resin with a substitution degree of 0.2mmol/g～1.2mmol/g as starting materials;
(2) The Fmoc-Pro-HMPB-AM resin was coupled one by one by Fmoc/tBu solid phase method to connect amino acids with protective groups in sequence, and the side chain fully protected leuprolide precursor peptide-HMPB-AM was synthesized Resin;
(3) Cut the side chain fully protected leuprolide precursor peptide-HMPB-AM resin to obtain the side chain fully protected leuprolide precursor peptide;
(4) Fully protected side chain leuprolide precursor peptide undergoes ethylamination to obtain side chain fully protected leuprolide;
(5) Leuprolide is fully protected on the side chain by removing the side chain protecting group to obtain the crude leuprolide peptide;
(6) The crude leuprorelin peptide is separated and purified by a high-pressure liquid phase column and lyophilized to obtain the leuprolide refined peptide.
