GM-1485(GM-1485) - 药物靶点：FKBP_专利_临床

概要

基本信息

药物类型

小分子化药

别名

NIL-A

靶点

FKBP

作用机制

FKBP调节剂(FK506结合蛋白调节剂)

治疗领域

肿瘤神经系统疾病内分泌与代谢疾病+ [6]

在研适应症-

非在研适应症

前列腺腺癌艾滋病相关性肾病骨病+ [6]

原研机构

Eisai Co., Ltd.

在研机构-

非在研机构

GliaMed, Inc.Arisyn Therapeutics Inc

Eisai Co., Ltd.

+ [2]

最高研发阶段终止临床2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C12H19NO4

InChIKeyFOPALECPEUVCTL-QMMMGPOBSA-N

CAS号186268-78-0

关联

7

项与 GM-1485 相关的临床试验

CTRI/2023/07/055388 / Not yet recruitingN/A

A study to assess the anxiety and stress among the parents of children undergoing electivesurgery at selected departments of SGPGIMS, Lucknow, Uttar pradesh, India - NIL

开始日期2023-07-31

申办/合作机构-

CTRI/2023/07/055612 / Not yet recruiting临床2/3期IIT

An Anatomical Study Of Krikatika Marma And Its Clinical Application On Manyasthambha (cervical spondylosis) - NIL

开始日期2023-07-26

申办/合作机构-

CTRI/2023/07/054944 / Not yet recruiting临床2/3期

A clinical study to evaluate the efficacy of Eladi choorna in the management of garbhini chardi w.s.r Emesis Gravidarum. - Nil

开始日期2023-07-20

申办/合作机构-

100 项与 GM-1485 相关的临床结果

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100 项与 GM-1485 相关的转化医学

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100 项与 GM-1485 相关的专利（医药）

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8

项与 GM-1485 相关的文献（医药）

2014-06-01·JAMA Neurology1区 · 医学

Measuring Disease Progression in Early Parkinson Disease

1区 · 医学

Article

作者: Bodis-Wollner, Ivan ; Shulman, Lisa M. ; Parashos, Sotirios A. ; Biglan, Kevin M. ; Liang, Grace S. ; Ross, G. Webster ; Tilley, Barbara C. ; Luo, Sheng ; He, Bo

IMPORTANCEOptimizing assessments of rate of progression in Parkinson disease (PD) is important in designing clinical trials, especially of potential disease-modifying agents.OBJECTIVETo examine the value of measures of impairment, disability, and quality of life in assessing progression in early PD.DESIGN, SETTING, AND PARTICIPANTSInception cohort analysis of data from 413 patients with early, untreated PD who were enrolled in 2 multicenter, randomized, double-blind clinical trials.INTERVENTIONSParticipants were randomly assigned to 1 of 5 treatments (67 received creatine, 66 received minocycline, 71 received coenzyme Q10, 71 received GPI-1485, and 138 received placebo). We assessed the association between the rates of change in measures of impairment, disability, and quality of life and time to initiation of symptomatic treatment.MAIN OUTCOMES AND MEASURESTime between baseline assessment and need for the initiation of symptomatic pharmaceutical treatment for PD was the primary indicator of disease progression.RESULTSAfter adjusting for baseline confounding variables with regard to the Unified Parkinson's Disease Rating Scale (UPDRS) Part II score, the UPDRS Part III score, the modified Rankin Scale score, level of education, and treatment group, we assessed the rate of change for the following measurements: the UPDRS Part II score; the UPDRS Part III score; the Schwab and England Independence Scale score (which measures activities of daily living); the Total Functional Capacity scale; the 39-item Parkinson's Disease Questionnaire, summary index, and activities of daily living subscale; and version 2 of the 12-item Short Form Health Survey Physical Summary and Mental Summary. Variables reaching the statistical threshold in univariate analysis were entered into a multivariable Cox proportional hazards model using time to symptomatic treatment as the dependent variable. More rapid change (ie, worsening) in the UPDRS Part II score (hazard ratio, 1.15 [95% CI, 1.08-1.22] for 1 scale unit change per 6 months), the UPDRS Part III score (hazard ratio, 1.09 [95% CI, 1.06-1.13] for 1 scale unit change per 6 months), and the Schwab and England Independence Scale score (hazard ratio, 1.29 [95% CI, 1.12-1.48] for 5 percentage point change per 6 months) was associated with earlier need for symptomatic therapy.CONCLUSIONSAND RELEVANCE In early PD, the UPDRS Part II score and Part III score and the Schwab and England Independence Scale score can be used to measure disease progression, whereas the 39-item Parkinson's Disease Questionnaire and summary index, Total Functional Capacity scale, and the 12-item Short Form Health Survey Physical Summary and Mental Summary are not sensitive to change.TRIAL REGISTRATIONclinicaltrials.gov Identifiers: NCT00063193 and NCT00076492.

2012-07-01·Journal of Neuroscience Research3区 · 医学

GM1485, a nonimmunosuppressive immunophilin ligand, promotes neurofunctional improvement and neural regeneration following stroke

3区 · 医学

Article

作者: Peter A. DeRosa ; E. Sander Connolly ; David E. Weinstein ; Sergey A. Sosunov ; Andrew F. Ducruet ; Brad E. Zacharia

AbstractStroke is the leading cause of disability in the industrialized world, and the development of pharmacologic strategies to promote poststroke recovery is of paramount importance. GM1485, a nonimmunosuppressive immunophilin ligand, promotes regeneration of multiple cell types following injury. In the present study, we evaluated the effect of GM1485 treatment on functional recovery and neurogenesis following rat stroke. Transient cerebral ischemia was induced in rats receiving daily GM1485 (5 mg/kg) beginning 24 hr postischemia and continuing for a total of 6 weeks. Neurological function was evaluated over this period using a battery of neurobehavioral tests, and immunostaining for stem‐cell markers was performed following animal sacrifice. An in vitro model of oxidative stress was also employed to evaluate the ability of GM1485 to mediate stem‐cell‐like induction and plasticity. GM1485‐treated rats demonstrated improved neurological function as well as increased Sox2+ cells in the ipsilateral SVZ and striatum relative to vehicle‐treated rats. Additionally, GM1485‐treated fibroblasts subjected to oxidative stress were reprogrammed to a stem‐cell‐like phenotype and were able to differentiate down a neuronal lineage. These data demonstrate that GM1485 administration improves neurological function and is consistent with an upregulation of endogenous neurogenesis following stroke in rats. Further experiments are necessary to characterize the molecular pathways involved in these processes. © 2012 Wiley Periodicals, Inc.

2004-01-01·Neuroscience3区 · 医学

Neuroimmunophilins: A novel drug therapy for the reversal of neurodegenerative disease?

3区 · 医学

Review

作者: M.O. Poulter ; J.P. Steiner ; K.B. Payne

Neuroimmunophilin ligands (NILs) are drugs derived from the immunosuppressant FK506 (tacrolimus) that have been shown to have variable efficacy in reversing neuronal degeneration and preventing cell death. In a wide range of animal models mimicking Parkinson's disease, dementia and even surgical nerve damage they induce re-sprouting, are neurotrophic or prevent nerve damage. The neurotrophic mechanism of action of these compounds is not known and may be dependent on the type of damage and genetic variability at the species or cellular level. Some evidence suggests that NILs may act through a family of proteins called FK506 binding proteins, some of which may regulate steroid hormone receptors. Other evidence suggests that NILs may protect neurons by upregulating the antioxidant glutathione and stimulating nerve regrowth by inducing the production of neurotrophic factors. Initial clinical trials have had mixed success. In one, patients with moderately severe Parkinson's disease showed no overall improvement in fine motor skills following 6 months of treatment by the neuroimmunophilin GPI 1485. But these patients did exhibit decreased loss of dopaminergic nerve terminals with a low dose of GPI 1485 and in fact some increase in dopaminergic terminals within 6 months of the higher dose of GPI 1485 drug treatment. As a result, a second phase II clinical trial using a patient population with less severe degeneration has been initiated concurrent with an investigation of GPI 1485 and other neuroprotective therapies funded by the National Institute of Neurological Disorders and Stroke. Another clinical trial ongoing at this time is exploring the use of a neuroimmunophilin ligand to prevent nerve degeneration and erectile dysfunction resulting from prostatectomy. In summary, neuroimmunophilins show promise to reverse some forms of neurodegeneration but exact factors that predict outcome have not been identified.

100 项与 GM-1485 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB05814

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
前列腺腺癌	临床2期	美国	Symphony Neuro Development Co.	2003-12-01
前列腺腺癌	临床2期	美国	Eisai, Inc.	2003-12-01
软骨疾病	临床2期	-	Arisyn Therapeutics Inc	-
软骨疾病	临床2期	-	Arisyn Therapeutics Inc	-
软骨疾病	临床2期	-	Eisai Co., Ltd.	-
勃起功能障碍	临床2期	-	Arisyn Therapeutics Inc	-
勃起功能障碍	临床2期	-	Arisyn Therapeutics Inc	-
帕金森病	临床2期	-	Arisyn Therapeutics Inc	-
帕金森病	临床2期	-	Arisyn Therapeutics Inc	-
软骨疾病	药物发现	-	Eisai Co., Ltd.	-