Delving into the Latest Updates on Quinagolide Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(+-)-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]

Target

D2 receptor

Mechanism

D2 receptor agonists(Dopamine D2 receptor agonists)

Therapeutic Areas

Nervous System DiseasesEndocrinology and Metabolic Disease

Active Indication

Hyperprolactinemia

Inactive Indication

AdenomyosisEndometriosisOvarian Hyperstimulation Syndrome+ [1]

Originator Organization

Novartis AG

Active Organization

Novartis AG

Inactive Organization

Ferring Pharmaceuticals A/SFerring BVFerring, Inc.

Drug Highest PhaseApproved

First Approval Date

ZA (24 Sep 1997),

Hyperprolactinemia

Regulation-

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Structure

Molecular FormulaC20H33N3O3S

InChIKeyGDFGTRDCCWFXTG-NZYAKQSMSA-N

CAS Registry87056-78-8

View All Structures (2)

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.

Start Date19 Aug 2019

Sponsor / Collaborator

Ferring Pharmaceuticals A/S

EUCTR2018-000915-26-IT / Not yet recruitingPhase 2

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

Start Date15 Jul 2019

Sponsor / Collaborator

Ferring Pharmaceuticals A/S

NCT03692403 / CompletedPhase 2

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

Start Date26 Dec 2018

Sponsor / Collaborator

Ferring Pharmaceuticals A/S

100 Clinical Results associated with Quinagolide Hydrochloride

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100 Translational Medicine associated with Quinagolide Hydrochloride

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100 Patents (Medical) associated with Quinagolide Hydrochloride

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206

Literatures (Medical) associated with Quinagolide Hydrochloride

01 Sep 2024·Journal of Dairy Science

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

Article

Author: 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.

16 Feb 2024·The Journal of Organic Chemistry

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

Article

Author: 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.

01 Jan 2023·Frontiers in pharmacology

Research advances in drug therapy of endometriosis.

Review

Author: 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 Deals associated with Quinagolide Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Quinagolide Hydrochloride	G02CB04	DB09097

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Hyperprolactinemia	ZA	Novartis AG	24 Sep 1997

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Adenomyosis	Phase 1	DE	Ferring Pharmaceuticals A/S	19 Aug 2019
Adenomyosis	Phase 1	IT	Ferring Pharmaceuticals A/S	19 Aug 2019
Adenomyosis	Phase 1	DK	Ferring Pharmaceuticals A/S	19 Aug 2019
Endometriosis	Phase 1	IT	Ferring BV	21 Jun 2019
Endometriosis	Phase 1	PL	Ferring BV	21 Jun 2019
Endometriosis	Phase 1	DK	Ferring BV	21 Jun 2019
Endometriosis	Phase 1	DE	Ferring BV	21 Jun 2019
Pain	Phase 1	US	Ferring Pharmaceuticals A/S	26 Dec 2018
Ovarian Hyperstimulation Syndrome	Phase 1	ES	Ferring Pharmaceuticals A/S	01 Jun 2006

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03749109 (QLARITY, CTgov)	Phase 2	Endometriosis \| Adenomyosis	67	Quinagolide 1080 µg (Quinagolide 1080 µg)	jvzzldkjxz(iridlinarz) = evpiodmpkm aukqihvyuh (kpbrkvwjbw, sbzsywblvq - efeusibqba) View more	-	07 Sep 2022
NCT03749109 (QLARITY, CTgov)	Phase 2	Endometriosis \| Adenomyosis	67	Placebo (Placebo)	jvzzldkjxz(iridlinarz) = bgobetztbv aukqihvyuh (kpbrkvwjbw, eddxlcwhsf - doavftxszb) View more	-	07 Sep 2022
Pubmed \| Fertil Steril	Not Applicable	Hyperprolactinemia	9	Quinagolide	szcrbjqlzw(twbvnlhhgw) = swwwncaavg rnaqfeodnf (yjqqfkllie )	-	01 Mar 2011