盐酸喹高利特(Quinagolide Hydrochloride) - 药物靶点：D2 receptor_在研适应症：高催乳素血症_专利_临床

概要

基本信息

药物类型

小分子化药

别名

(+-)-N,N-Diethyl-N'-((3R*,4aR*,10aS*)-1,2,3,4,4a,5,10,10a-octahydro-6-hydroxy-1-propylbenzo(g)quinolin-3-yl)sulfamide、Norprolac、Quinagolide

+ [5]

靶点

D2 receptor

作用机制

D2 receptor激动剂(多巴胺D2受体激动剂)

治疗领域

神经系统疾病内分泌与代谢疾病

在研适应症

高催乳素血症

非在研适应症

子宫腺肌病子宫内膜异位症卵巢过度刺激综合征+ [1]

原研机构

Novartis AG

在研机构

Novartis AG

非在研机构

Ferring Pharmaceuticals A/SFerring BVFerring, Inc.

最高研发阶段批准上市

首次获批日期

南非 (1997-09-24),

高催乳素血症

最高研发阶段(中国)-

特殊审评-

登录后查看时间轴

结构

分子式C20H33N3O3S

InChIKeyGDFGTRDCCWFXTG-NZYAKQSMSA-N

CAS号87056-78-8

查看全部结构式(2)

关联

7

项与盐酸喹高利特相关的临床试验

NCT03749109 / Completed临床2期

A Randomised, Double-blind, Placebo-controlled, Proof-of-mechanism Phase 2 Trial Investigating the Effect of Quinagolide Extended-release Vaginal Ring on Reduction of Lesions Assessed by High-resolution Magnetic Resonance Imaging in Women With Endometrioma, Deep Infiltrating Endometriosis, and/or Adenomyosis

This will be a randomized, double-blind, placebo-controlled, proof-of-mechanism phase 2 trial investigating the effect of quinagolide extended-release vaginal ring on reduction of lesions assessed by high-resolution magnetic resonance imaging in women with endometrioma, deep infiltrating endometriosis, and/or adenomyosis.

开始日期2019-08-19

申办/合作机构

Ferring Pharmaceuticals A/S

EUCTR2018-000915-26-IT / Not yet recruiting临床2期

A randomised, double-blind, placebo-controlled, proof-of-mechanism phase 2 trial investigating the effect of quinagolide extended-release vaginal ring on reduction of lesions assessed by high-resolution magnetic resonance imaging in women with endometrioma, deep infiltrating endometriosis, and/or adenomyosis - QLARITY

开始日期2019-07-15

申办/合作机构

Ferring Pharmaceuticals A/S

NCT03692403 / Completed临床2期

A Randomized, Double-blind, Placebo-controlled, Phase 2 Trial Assessing the Efficacy, Safety and Dose-response of Quinagolide Extended-release Vaginal Rings Administered Sequentially for 4 Menstrual Cycles in Women With Moderate to Severe Endometriosis-related Pain

To evaluate the efficacy of three doses of quinagolide administered as an extended-release vaginal ring compared to placebo on reduction of moderate to severe endometriosis-related pain

开始日期2018-12-26

申办/合作机构

Ferring Pharmaceuticals A/S

100 项与盐酸喹高利特相关的临床结果

登录后查看更多信息

100 项与盐酸喹高利特相关的转化医学

登录后查看更多信息

100 项与盐酸喹高利特相关的专利（医药）

登录后查看更多信息

206

项与盐酸喹高利特相关的文献（医药）

2024-09-01·Journal of Dairy Science

Effect of prolactin concentration during the dry period on the subsequent milk production of dairy cows

Article

作者: Lanctôt, S ; Deacon, A-M ; Deacon, A.-M. ; Lanctôt, S. ; Thibault, C ; Thibault, C. ; Blouin, R. ; Lacasse, P. ; Blouin, R ; Lacasse, P

Shortening the dry period has a negative impact on milk production of the following lactation. One possible explanation is that a period of low prolactin (PRL) concentration is necessary to restore mammary gland milk production capacity. Therefore, the objective of this study was to determine the effect of lowering blood PRL level on subsequent lactation milk production. In this experiment, quinagolide was used to inhibit PRL secretion during the dry period. Thirty Holstein cows were randomly assigned one of 3 dry period managements: a conventional (60 d) dry period (CD) and 2 short (35 d) dry period treatments (SD). Short dry period cows received either water (SDwater) or quinagolide (2 mg, SDquin) injections twice daily from dry-off until 14 d before calving. Cows were followed during the first 20 wks of the subsequent lactation. When CD cows were dry but SD cows were lactating, concentration of PRL was lower in the CD cows than in the SD cows. During the injection period, PRL of SDquin cows was lower than that of the other treatments and was greater in the blood of SDwater than in that of CD cows. After the injection period until calving, no difference in PRL concentration was observed between treatments. After calving, PRL concentration of the SDquin cows was greater than those of CD and SDwater cows. During the first 20 wks of lactation, energy corrected milk (ECM) was lower in SDwater cows than in CD and SDquin cows. The ECM of the latter groups were not different. During the same period, mammary expression of genes related to milk synthesis, pro-apoptotic genes, as well as the expression of the short and long isoforms of the PRLR genes were not affected; however, the expression of SOCS3 gene tended to be lower for the SDquin than the SDwater cows. Lowering the PRL level during short dry period restored milk production to the level normally observed after a conventional dry period, which suggests that higher PRL levels during short dry period are the cause of the lower milk production after a short dry period. Ultimately, strategies to lower blood PRL level may help the adoption of short dry period.

2024-02-16·The Journal of Organic Chemistry

Streamlined Stereoselective Entry to (−)-Quinagolide and to 3-Substituted Octahydrobenzo[g]-Quinolines

Article

作者: Pineschi, Mauro ; Ryberg, Per ; Comparini, Lucrezia Margherita ; Favero, Lucilla ; Di Pietro, Sebastiano ; Sardelli, Francesca

A very short stereoselective synthesis of enantiomerically pure (3S, 4aS, 10aR)-quinagolide has been developed. The key steps involved are a copper-catalyzed regioselective arylation of (S)-epichlorohydrin with 1,6-dimethoxynaphthalene and a diastereoselective trans-reduction of a cyclic enamine intermediate. The possibility to use both enantiomers of epichlorohydrin and the diastereodivergency found in the reduction process paves the way for a general preparation also in the nonracemic form of chiral trans-fused 3-substituted octahydrobenzo[g]quinolines that are privileged structures in medicinal chemistry.

2023-01-01·Frontiers in pharmacology

Research advances in drug therapy of endometriosis.

Review

作者: Shi, Jianyou ; Guo, Chun ; Zhuo, Yuan ; Wang, Lin ; Tan, Xin ; Zheng, Wei ; Chen, Lu ; Jiang, Zhongliang ; Yu, Dongke ; Banda, Srikanth ; Feng, Guimei

Endometriosis is one of the most common benign gynecological disorders in reproductive-aged women. The major symptoms are chronic pelvic pain and infertility. Despite its profound impact on women's health and quality of life, its pathogenesis has not been fully elucidated, it cannot be cured and the long-term use of drugs yields severe side effects and hinders fertility. This review aims to present the advances in pathogenesis and the newly reported lead compounds and drugs managing endometriosis. This paper investigated Genetic changes, estrogen-dependent inflammation induction, progesterone resistance, imbalance in proliferation and apoptosis, angiogenesis, lymphangiogenesis and neurogenesis, and tissue remodeling in its pathogenesis; and explored the pharmacological mechanisms, constitutive relationships, and application prospects of each compound in the text. To date, Resveratrol, Bay1316957, and bardoxifene were effective against lesions and pain in controlled animal studies. In clinical trials, Quinagolide showed no statistical difference with the placebo group; the results of phase II clinical trial of the IL-33 antibody have not been announced yet; clinical trial stage III of vilaprisan was suspended due to drug toxicity. Elagolix was approved for the treatment of endometriosis-related pain, but clinical studies of Elagolix for the pretreatment of patients with endometriosis to before In vitro fertilization treatment have not been fulfilled. The results of a clinical study of Linzagolix in patients with moderate to severe endometriosis-related pain have not been disclosed yet. Letrozole improved the fertility of patients with mild endometriosis. For endometriosis patients with infertility, oral GnRH antagonists and aromatase inhibitors are promising drugs, especially Elagolix and Letrozole.

100 项与盐酸喹高利特相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
-	盐酸喹高利特	G02CB04	DB09097

研发状态

批准上市

10 条最早获批的记录,

登录

后查看更多信息

适应症	国家/地区	公司	日期
高催乳素血症	南非	Novartis AG	1997-09-24

未上市

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
子宫腺肌病	临床1期	德国	Ferring Pharmaceuticals A/S	2019-08-19
子宫腺肌病	临床1期	意大利	Ferring Pharmaceuticals A/S	2019-08-19
子宫腺肌病	临床1期	丹麦	Ferring Pharmaceuticals A/S	2019-08-19
子宫内膜异位症	临床1期	意大利	Ferring BV	2019-06-21
子宫内膜异位症	临床1期	波兰	Ferring BV	2019-06-21
子宫内膜异位症	临床1期	丹麦	Ferring BV	2019-06-21
子宫内膜异位症	临床1期	德国	Ferring BV	2019-06-21
疼痛	临床1期	美国	Ferring Pharmaceuticals A/S	2018-12-26
卵巢过度刺激综合征	临床1期	西班牙	Ferring Pharmaceuticals A/S	2006-06-01

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03749109 (QLARITY, CTgov)	临床2期	子宫内膜异位症 \| 子宫腺肌病	67	Quinagolide 1080 µg (Quinagolide 1080 µg)	憲齋壓網築選遞鏇蓋製(艱蓋鹹構艱窪齋襯糧簾) = 獵淵蓋簾襯醖淵鏇窪齋簾鬱衊範夢蓋艱衊餘網 (餘艱鬱鑰衊醖襯齋艱淵, 淵獵襯顧憲衊遞網糧願 ~ 鹽糧願顧憲繭範選蓋獵) 更多	-	2022-09-07
NCT03749109 (QLARITY, CTgov)	临床2期	子宫内膜异位症 \| 子宫腺肌病	67	Placebo (Placebo)	憲齋壓網築選遞鏇蓋製(艱蓋鹹構艱窪齋襯糧簾) = 顧壓鬱廠鹹鬱築艱艱蓋簾鬱衊範夢蓋艱衊餘網 (餘艱鬱鑰衊醖襯齋艱淵, 獵顧襯淵願遞壓鑰夢鬱 ~ 膚廠廠獵構蓋襯築淵鬱) 更多	-	2022-09-07
Pubmed \| Fertil Steril	N/A	高催乳素血症	9	Quinagolide	鑰鏇齋範簾鹽築鏇襯淵(壓窪膚淵醖製遞鹽獵憲) = 廠餘膚窪製觸廠觸鹹鬱憲鬱獵憲壓蓋鏇壓廠衊 (範壓鹽醖醖廠壓窪顧餘 )	-	2011-03-01