レルゴリクス化学構造式

レルゴリクス

化学名:レルゴリクス

CAS番号.737789-87-6

英語名:Relugolix

CBNumberCB42658205

MFC29H27F2N7O5S

MW623.63

MOL File737789-87-6.mol

别名

レルゴリクス

レルゴリクス (JAN)

1-(4-{1-[(2,6-ジフルオロフェニル)メチル]-5-[(ジメチルアミノ)メチル]-3-(6-メトキシピリダジン-3-イル)-2,4-ジオキソ-1H,2H,3H,4H-チエノ[2,3-d]ピリミジン-6-イル}フェニル)-3-メトキシ尿素

レルゴリクス物理性質

融点	228 °C (decomp)(Solv: ethyl acetate (141-78-6); tetrahydrofuran (109-99-9))
比重(密度)	1.442±0.06 g/cm3(Predicted)
貯蔵温度	Store at -20°C
溶解性	DMSO:20.0(Max Conc. mg/mL);32.1(Max Conc. mM) Ethanol:1.0(Max Conc. mg/mL);1.6(Max Conc. mM)
外見	A crystalline solid
酸解離定数(Pka)	13.17±0.70(Predicted)
色	White to off-white
InChIKey	AOMXMOCNKJTRQP-UHFFFAOYSA-N
SMILES	N(C1=CC=C(C2SC3=C(C=2CN(C)C)C(=O)N(C2=NN=C(OC)C=C2)C(=O)N3CC2=C(F)C=CC=C2F)C=C1)C(NOC)=O

危険有害性情報のコード(GHS)

レルゴリクス化学特性,用途語,生産方法

効能
子宮内膜症治療薬, 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
商品名
レルミナ (武田薬品工業)
説明
Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. It possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.
使用
Relugolix is a highly selective, oral, nonpeptide GnRH antagonist being investigated as a possible prostate cancer treatment
臨床応用
Relugolix was first approved in Japan in 2019, under the brand name Relumina, for the symptomatic treatment of uterine fibroids, and more recently by the United States' FDA in 2020, under the brand name Orgovyx, for the treatment of advanced prostate cancer. Relugolix has also been studied in the symptomatic treatment of endometriosis.
副作用
Common side effects of Relugolix include: hot flashes; flushing of the skin; sweating; weight gain or loss of ability; pain in the muscles, back, joints or bones; fatigue; diarrhoea; constipation; difficulty sleeping; depression; and breast enlargement. More serious side effects include: dizziness; fainting; rapid heartbeat; or chest pain; swelling of the face, lips, mouth or tongue; difficulty breathing or swallowing; rash; measles; redness of the skin; chest pain or tightness in the chest; or pain in the arms, back, neck or jaw; sudden numbness or weakness of the face, arms, or legs (especially on one side of the body); sudden blurred consciousness; difficulty speaking or understanding; sudden difficulty seeing with one or both eyes; or sudden difficulty walking, walking, or seeing with one or both eyes. or sudden difficulty walking, dizziness, loss of balance or coordination, etc.
合成
Relugolix is produced by the reaction of 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione and phenyl N-methoxycarbamate.

レルゴリクス生産企業

737789-87-6, レルゴリクスキーワード

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レルゴリクス

危険有害性情報のコード(GHS)

レルゴリクス 化学特性,用途語,生産方法

レルゴリクス 生産企業

737789-87-6, レルゴリクス キーワード

レルゴリクス化学特性,用途語,生産方法

レルゴリクス生産企業

737789-87-6, レルゴリクスキーワード