帕多芦诺(Pardoprunox Hydrochloride) - 药物靶点：5-HT1A receptor x D2 receptor x D3 receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Pardoprunox、Pardoprunox hydrochloride (USAN)

+ [4]

靶点

5-HT1A receptor x D2 receptor x D3 receptor

作用机制

5-HT1A receptor激动剂(5-羟色胺1A受体激动剂)、D2 receptor激动剂(多巴胺D2受体激动剂)、D3 receptor激动剂(多巴胺D3受体激动剂)

治疗领域

神经系统疾病内分泌与代谢疾病口颌疾病+ [1]

在研适应症-

非在研适应症

侵袭性牙周炎药物性运动障碍运动失调+ [3]

原研机构

Solvay SA

在研机构-

非在研机构

Solvay Pharmaceuticals, Inc.Abbott Products LLC

AbbVie, Inc.

+ [1]

最高研发阶段终止临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C12H16ClN3O2

InChIKeyNQRIKTDKFHAOKC-UHFFFAOYSA-N

CAS号269718-83-4

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关联

15

项与帕多芦诺相关的临床试验

NCT00903838 / Terminated临床2期

A Multicenter, Randomized, Double Blind, Pramipexole Controlled Pilot Study to Assess Efficacy and Safety of Pardoprunox as Adjunct Therapy to L-dopa in the Treatment of Patients With Parkinson's Disease Experiencing Motor Fluctuations and Dyskinesia.

This is a multicenter, randomized, double blind, pramipexole-controlled parallel group study of pardoprunox as adjunctive treatment to levodopa.

开始日期2009-09-01

申办/合作机构

Abbott Products LLC

EUCTR2008-000400-81-IT / Not yet recruitingN/A

A Multicenter, Randomized, Double Blind, Pramipexole Controlled Pilot Study to Assess Efficacy and Safety of Pardoprunox as Adjunct Therapy to L-dopa in the Treatment of Patients with Parkinson?s Disease Experiencing Motor Fluctuations and Dyskinesia - ND

开始日期2009-03-31

申办/合作机构-

EUCTR2008-004943-12-SK / Unknown status临床2期

The Rubens Study:A Multicenter, Randomized, Double-blind, Parallel Group, Placebo and Pramipexole Controlled Study to Explore the Efficacy, Tolerability and Safety of Different Doses and Titration Schedules of Pardoprunox Monotherapy in the Treatment of Patients with Early Stage Parkinson’s Disease - The Rubens Study

开始日期2008-11-24

申办/合作机构-

100 项与帕多芦诺相关的临床结果

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100 项与帕多芦诺相关的转化医学

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100 项与帕多芦诺相关的专利（医药）

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16

项与帕多芦诺相关的文献（医药）

2018-01-01·Neuroepidemiology4区 · 医学

Comprehensive Examination of Therapies for Pain in Parkinson’s Disease: A Systematic Review and Meta-Analysis

4区 · 医学

Review

作者: Vannabouathong, Christopher ; Rizvi, Syed Fayyaz H ; Malik, Suleiman H ; Rana, Abdul Qayyum ; Akhter, Shakib ; Sarfraz, Zainab ; Qureshi, Abdul Rehman ; Rana, Ruqqiyah

Pain in Parkinson’s disease (PD) is a debilitating symptom with a prevalence of 68%, yet is untreated 50% of the time. What is unclear, however, is which treatment is optimal for minimizing pain severity in PD. Thus, the objective of this systematic review and meta-analysis was to investigate the efficacy of a variety of novel, complimentary, and conventional treatments for pain in PD and elucidate which therapy is the most effective. A systematic search was performed using MEDLINE, PsycINFO, Embase, CINAHL, and CENTRAL databases. To identify additional articles, manual searches of reference lists of included trials were also searched. Major neurology conference proceedings occurring between January 2014 and February 2018 were also searched to identify unpublished studies that may be potentially eligible. Twenty-five randomized controlled trials that encompassed medical, surgical, and complementary therapies met our inclusion criteria and exhibited moderate quality evidence. Two reviewers conducted assessments for study eligibility, risk of bias, data extraction, and quality of evidence rating. A conservative random-effects model was used to pool effect estimates of pain severity. The greatest reductions in pain were found with safinamide (Standardized mean difference = –4.83, 95% CI [–5.07 to –4.59], <i>p</i> < 0.0001), followed by cannabinoids and opioids, multidisciplinary team care, catechol-O-methyltransferase inhibitors, and electrical and Chinese therapies. Moderate effects in reducing pain were in pardoprunox and surgery, while the weakest effects were in dopaminergic agonists and miscellaneous therapies. Safinamide is an important adjunct to standard parkinsonian medication for alleviating pain in PD.

2014-08-01·Current Opinion in Neurology2区 · 医学

Treatment of early Parkinson's disease

2区 · 医学

Review

作者: Lyons, Kelly E. ; Pahwa, Rajesh

PURPOSE OF REVIEWThis review summarizes currently available treatment options and treatment strategies, investigational treatments, and the importance of exercise for early Parkinson's disease.RECENT FINDINGSThe available treatment options for early Parkinson's disease have changed little in the past decade and include carbidopa/levodopa, dopamine agonists, and monoamine oxidase type B (MAO-B) inhibitors. However, we discuss changes in treatment strategies, including dosing and the use of combination therapy used in an attempt to reduce or delay the appearance of motor complications and other adverse events. We will also review several investigational treatments that have shown promise for the treatment of early Parkinson's disease, including a new extended release formulation of carbidopa/levodopa (IPX066), safinamide which inhibits MAO-B, dopamine uptake and glutamate and pardoprunox which is a 5HT-1A agonist and a partial dopamine agonist. Finally, we discuss recent studies focusing on exercise as an important component in the management of early Parkinson's disease.SUMMARYAdvances in the management of early Parkinson's disease include evolving treatment strategies, new investigational treatments, and earlier implementation of various forms of exercise.

2013-12-31·Current Medicinal Chemistry

Dual Ligands Targeting Dopamine D2 and Serotonin 5-HT<sub>1A</sub> Receptors as New Antipsychotical or Anti-Parkinsonian Agents

Review

作者: Na Ye ; Ao Zhang ; Zilan Song

Psychiatric disorders like schizophrenia and neurodegenerative diseases like Parkinson's disease are associated with poly-factorial pathogenic mechanisms, with several neurotransmitter systems closely involved. In addition to the cerebral dopaminergic (DA) system, the serotoninergic (5-HT) system also plays a crucial role in regulating psychoemotional, cognitive and motor functions in the central nervous system (CNS). Among the large 5-HT receptor family, accumulating data have revealed new insights into the therapeutic benefit of the 5-HT1A receptor in treating various CNS disorders, especially schizophrenia and Parkinson's disease. The present review discusses the advance of dual agents with mixed actions at the dopamine D2 and serotonin 5-HT1A receptors in the treatment of these diseases. Aripiprazole was the only marketed drug with dual D2 and 5-HT1A profile. It is a partial D2 and 5-HT1A receptor agonist and has been prescribed as an atypical antipsychotical drug. Two other drugs Cariprazine and Pardoprunox are being investigated in clinic. Most of the other candidate compounds, including Bifeprunox, Sarizotan, Mazapertine succinate, PF-217830, and Adoprazine were discontinued due to either non-optimal pharmacokinetic properties or insufficient therapeutical efficacy. Although much effort has been done to highlight the advantages of the 5-HT1A and D2 dual approach, it has to be pointed out that many of these drugs showed poly-pharmacological profile by targeting many other receptors and/or transporters besides the D2 and 5-HT1A receptors. In this regard, 'pure' compounds exclusively acting on the D2 and 5-HT1A receptors are highly needed to further validate this approach. Meanwhile, safety concerns and in vivo pharmacokinetic alerts should also be implanted to the drug design art early.

100 项与帕多芦诺相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D09366	帕多芦诺	-	DB12061

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
帕金森病	临床3期	亚洲	Solvay SA	-
帕金森病	临床3期	北美洲	Solvay SA	-
帕金森病	临床3期	欧洲	Solvay SA	-
帕金森病	临床3期	-	AbbVie, Inc.	-
帕金森病	临床3期	亚洲	Solvay SA	-
帕金森病	临床3期	南非	Solvay SA	-
帕金森病	临床3期	-	AbbVie, Inc.	-
帕金森病	临床3期	南非	Solvay SA	-
帕金森病	临床3期	北美洲	Solvay SA	-
帕金森病	药物发现	欧洲	Solvay SA	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00406588 (Pubmed \| Parkinsonism Relat Disord)	临床3期	帕金森病	295	Pardoprunox	(壓壓餘鏇衊鹹構選願餘) = 鏇憲構鹽鑰簾鏇鹹鏇選顧積壓齋選壓壓願壓觸 (顧淵齋淵簾觸獵簾衊膚 )	-	2012-05-01
				Placebo	(壓壓餘鏇衊鹹構選願餘) = 齋壓築簾窪築夢醖衊願顧積壓齋選壓壓願壓觸 (顧淵齋淵簾觸獵簾衊膚 )