Last update 21 Nov 2024

Nicergoline

Last update 21 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(8β)-10-methoxy-1,6-dimethylergoline-8-methanol 5-bromo-3-pyridinecarboxylate (ester), 10-methoxy-1,6-dimethylergoline-8β-methanol 5-bromonicotinate, Nicergo1ine

+ [10]

Target

ADRA1

Mechanism

ADRA1 antagonists(Adrenergic receptor alpha-1 antagonists)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesOther Diseases

Active Indication

DizzinessIntellectual DisabilityMood Disorders+ [5]

Inactive Indication

Affective Disorders, PsychoticAlzheimer Disease

Originator Organization-

Active Organization

Ildong Pharmaceutical Co., Ltd.

Mitsubishi Tanabe Pharma Corp.

Huizhi Pharmaceutical (Dalian) Co., Ltd.

+ [3]

Inactive Organization

Viatris, Inc.

Drug Highest PhaseApproved

First Approval Date

KR (16 Dec 1978),

ArteriosclerosisBrain InfarctionDementia

Regulation-

Structure

Molecular FormulaC24H26BrN3O3

InChIKeyYSEXMKHXIOCEJA-FVFQAYNVSA-N

CAS Registry27848-84-6

Clinical Trials associated with Nicergoline

CTR20241708 / CompletedNot Applicable

健康成年受试者空腹和餐后状态下单次口服尼麦角林片的随机、开放、单剂量、四周期、完全重复交叉设计的生物等效性试验

[Translation] A randomized, open-label, single-dose, four-period, completely repeated crossover bioequivalence study of a single oral dose of nicergoline tablets in healthy adult subjects in the fasting and fed state

主要研究目的：研究空腹和餐后状态下单次口服受试制剂尼麦角林片（规格：30mg，华润双鹤利民药业（济南）有限公司生产）与参比制剂尼麦角林片（Sermion®，规格：30mg，Pfizer Italia S.r.l.生产）在健康成年受试者体内的药代动力学，评价空腹和餐后状态口服两种制剂的生物等效性。次要研究目的：评价健康受试者在空腹和餐后状态下，单次口服尼麦角林片受试制剂和参比制剂后的安全性。

[Translation]

The main purpose of the study is to study the pharmacokinetics of the test preparation Nicergoline Tablets (Specification: 30mg, produced by China Resources Double Crane Limin Pharmaceutical (Jinan) Co., Ltd.) and the reference preparation Nicergoline Tablets (Sermion®, Specification: 30mg, produced by Pfizer Italia S.r.l.) in healthy adult subjects after a single oral administration in the fasting and fed state, and to evaluate the bioequivalence of the two preparations after oral administration in the fasting and fed state. Secondary purpose of the study is to evaluate the safety of the test preparation and reference preparation of Nicergoline Tablets after a single oral administration in healthy subjects in the fasting and fed state.

Start Date22 Jun 2024

Sponsor / Collaborator

China Resources Double-Crane Pharmaceutical (Jinan) Co., Ltd.

CTR20234046 / CompletedNot Applicable

健康受试者餐后状态下单次口服尼麦角林片的生物等效性试验

[Translation] Bioequivalence study of a single oral dose of nicergoline tablets in healthy volunteers in the fed state

主要目的：研究餐后状态下单次口服受试制剂尼麦角林片（规格：30mg，华润双鹤利民药业（济南）有限公司生产）与参比制剂尼麦角林片（商品名Sermion ®，规格：30mg，Pfizer Italia S.r.l. 生产）在健康成年受试者体内的药代动力学，比较受试制剂和参比制剂药代动力学的差异，同时计算主要药动学参数（Cmax、AUC0-t和AUC0-∞），并进行初步比较。次要研究目的：评价健康受试者在餐后状态下，单次口服尼麦角林片受试制剂和参比制剂后的安全性。

[Translation]

Primary objective: To study the pharmacokinetics of the test preparation Nicergoline Tablets (Specification: 30 mg, produced by China Resources Double Crane Limin Pharmaceutical (Jinan) Co., Ltd.) and the reference preparation Nicergoline Tablets (trade name Sermion ®, Specification: 30 mg, produced by Pfizer Italia S.r.l.) in healthy adult subjects after a single oral administration in the fed state, to compare the differences in pharmacokinetics between the test preparation and the reference preparation, and to calculate the main pharmacokinetic parameters (Cmax, AUC0-t and AUC0-∞) and make a preliminary comparison. Secondary objective: To evaluate the safety of the test preparation and the reference preparation of Nicergoline Tablets after a single oral administration in healthy subjects in the fed state.

Start Date12 Dec 2023

Sponsor / Collaborator

China Resources Double-Crane Pharmaceutical (Jinan) Co., Ltd.

CTR20233222 / CompletedNot Applicable

健康成年受试者空腹和餐后状态下单次口服尼麦角林片的生物等效性试验

[Translation] Bioequivalence study of a single oral dose of nicergoline tablets in healthy adult volunteers under fasting and fed conditions

主要研究目的：研究空腹和餐后状态下单次口服受试制剂尼麦角林片（规格：10mg，海南通用三洋药业有限公司生产）与参比制剂尼麦角林片（Sermion®，规格：10mg，Pfizer Italia S.r.l.生产，Upjohn EESV持证）在健康成年受试者体内的药代动力学，评价空腹和餐后状态口服两种制剂的生物等效性。次要研究目的：评价健康受试者在空腹和餐后状态下，单次口服尼麦角林片受试制剂和参比制剂后的安全性。

[Translation]

Main study objectives: To study the pharmacokinetics of the test formulation Nicergoline Tablets (Specification: 10 mg, produced by Hainan General Sanyo Pharmaceutical Co., Ltd.) and the reference formulation Nicergoline Tablets (Sermion®, Specification: 10 mg, produced by Pfizer Italia S.r.l., Upjohn EESV certified) in healthy adult subjects after a single oral administration in the fasting and fed state, and to evaluate the bioequivalence of the two formulations in the fasting and fed state. Secondary study objectives: To evaluate the safety of the test formulation and reference formulation of Nicergoline Tablets in healthy subjects after a single oral administration in the fasting and fed state.

Start Date06 Nov 2023

Sponsor / Collaborator

Hainan General Sanyang Pharmaceutical Co. Ltd.

100 Clinical Results associated with Nicergoline

100 Translational Medicine associated with Nicergoline

100 Patents (Medical) associated with Nicergoline

413

Literatures (Medical) associated with Nicergoline

01 Aug 2023·Apoptosis : an international journal on programmed cell death

Apoptosis in Alzheimer's disease: insight into the signaling pathways and therapeutic avenues.

Review

Author: Kumari, Sneha ; Dhapola, Rishika ; Reddy, Dibbanti HariKrishna

Alzheimer's disease (AD) is characterized by the accumulation of hyperphosphorylated tau and amyloid-β (Aβ) protein resulting in synaptic loss and apoptosis. Aβ and tau deposition trigger apoptotic pathways that result in neuronal death. Apoptosis is considered to be responsible for manifestations associated with AD under pathological conditions. It regulates via extrinsic and intrinsic pathways. It activates various proteins including Bcl-2 family proteins like Bax, Bad, Bid, Bcl-XS, Bcl-XL and caspases comprising of initiator, effector and inflammatory caspases carried out through a cascade of events that finally lead to cell disintegration. The apoptotic elements interact with trophic factors, signaling molecules including Ras-ERK, JNK, GSK-3β, BDNF/TrkB/CREB and PI3K/AKT/mTOR. Ras-ERK signaling is involved in the progression of cell cycle and apoptosis. JNK pathway is also upregulated in AD which results in decreased expression of anti-apoptotic proteins. JAK-STAT triggers caspase-3 mediated apoptosis leading to neurodegeneration. The imbalance between autophagy and apoptosis is regulated by PI3K/Akt/mTOR pathway. GSK-3β is involved in the stimulation of pro-apoptotic factors resulting in dysregulation of apoptosis. Drugs like filgrastim, epigallocatechin gallate, curcumin, nicergoline and minocycline are under development which target these pathways and modulate the disease condition. This study sheds light on apoptotic pathways that are cardinal for neuronal survival and perform crucial role in the occurrence of AD along with the trends in therapeutics targeting apoptosis induced AD. To develop prospective treatments for AD, it is desirable to elucidate potential targets including restoration apoptotic balance, regulation of caspases, Bcl-2 and other crucial proteins involved in apoptosis mediated AD.

07 Feb 2023·Eye & Contact Lens: Science & Clinical Practice

Concomitant Bandage Contact Lens, Oral Nicergoline, and Topical Autologous Serum for Severe Neurotrophic Keratitis

Article

Author: Graue-Hernandez, Enrique O ; Polania-Baron, Eduardo J ; Navas, Alejandro ; Ramirez-Miranda, Arturo

Background:To report the outcomes of using the combination of oral nicergoline, autologous serum, and contact lens to enhance corneal epithelization in neurotrophic keratitis and to discuss the clinical potential of this management.Methods:This was a prospective consecutive case series study of eight patients treated for neurotrophic keratitis at the “Conde de Valenciana” Institute of Ophthalmology. Oral nicergoline, autologous serum, and bandage contact lens were initiated at the same time, immediately after stage 3 diagnosis keratitis was confirmed clinically, and until corneal epithelialization was achieved or eminent corneal perforation was seen. In patients where diabetes was a cause, glycosylate hemoglobin was measured to asses metabolic control. Corneal esthesiometry and corrected distance visual acuity were assessed before and after treatment.Results:This study included eight eyes of eight patients (5 men [62.5%], average age 57±17.9 years). All patients completed at least 1 month of follow-up after nicergoline and contact lens suspension. Of the eight eyes, no one had positive culture growth and complete epithelial healing was achieved in all cases. Half of patients had diabetes and had a poor metabolic control. Corneal sensitivity improved in all eyes almost 2 centimeters in Cochet–Bonnet esthesiometry (P=0.01). In addition, final visual acuity gains were obtained (P=0.100).Conclusions:The combination of oral nicergoline, autologous serum, and bandage contact lens simultaneously could be an alternative in the management of stage 3 neurotrophic keratitis when conventional medical treatment has no improvement of corneal epithelization.

01 Jan 2023·Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova

[Study of the effect of Unifuzol on cognitive impairment and damage to the hippocampus and cerebral cortex during course administration to rats with bilateral stenosis of the common carotid arteries, causing chronic circulatory failure].

Article

Author: Kovalenko, A L ; Lycheva, N A ; Kuznetsova, E V ; Myagkova, I A ; Morkovin, E I ; Kurkin, D V ; Shmidt, M V ; Bakulin, D A ; Robertus, A I ; Tarasov, A S

OBJECTIVETo study the effect of Unifuzol (L-arginine sodium succinate) on cognitive impairment, cerebral blood flow, and damage to the tissues of the hippocampus and cerebral cortex during a 10-day course of administration to rats with chronic cerebral ischemia (CCI) caused by bilateral stenosis of the common carotid arteries (CCA).MATERIAL AND METHODSThe study was conducted on male rats with CCI caused by bilateral stenosis of the CCA by 60%. 40 days after surgery, rats received Unifusol (21, 42 and 84 ml/kg), nicergoline (10 mg/kg), citicoline (500 mg/kg) or placebo (0.9% NaCl) for 10 days. Next, cognitive impairments were assessed in the Morris Water Maze and the New Object Recognition (NOR) test, as well as the level of motor and exploratory activity in the Open Field test. The level of cerebral blood flow was determined immediately after the CCA stenosis and at the end of the experiment. Animals were euthanized in a CO₂ incubator, after which the brain was removed and subjected to morphometric analysis.RESULTSIn animals that were modeled with CCA stenosis, pronounced behavioral and cognitive impairments occurred as a result of a decrease in blood flow in the vessels of the brain and subsequent changes in the tissues of the hippocampus and the cerebral cortex. Intravenous course administration of Unifuzol at doses of 42 and 84 ml/kg to animals with CCI was comparable in efficiency to nicergoline and citicoline, which was expressed in greater preservation of the cognitive abilities of animals in the Morris Water Maze and NOR tests. In the Open Field test, animals injected with Unifusol at doses of 42 and 84 ml/kg performed more acts of motor and exploratory activity than animals from the placebo group, and had a higher level of cerebral blood flow (compared to animals that were injected with citicoline). Based on the results of a morphological study, it was found that the most significant neuroprotective effect was provided by nicergoline and Unifuzol (at doses of 42 and 84 ml/kg).CONCLUSIONUnifuzol at a course of administration at doses of 42 and 84 ml/kg, comparable to the reference drugs nicergoline and citicoline, reduces the severity of psychoneurological deficit in animals with CCI, comparable to them improves the microcirculation of brain tissues, preventing damage to brain tissues.

100 Deals associated with Nicergoline

External Link

KEGG	Wiki	ATC	Drug Bank
D01290	Nicergoline	C04AE02	DB00699

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Dizziness	CN	Ethypharm SAS	15 Dec 2000
Intellectual Disability	CN	Ethypharm SAS	15 Dec 2000
Mood Disorders	CN	Pfizer Inc.	17 Sep 1999
Peripheral Vascular Diseases	CN	Pfizer Inc.	17 Sep 1999
Arteriosclerosis	KR	Ildong Pharmaceutical Co., Ltd.	16 Dec 1978
Brain Infarction	KR	Ildong Pharmaceutical Co., Ltd.	16 Dec 1978
Dementia	KR	Ildong Pharmaceutical Co., Ltd.	16 Dec 1978

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Brain Infarction	Phase 1	CN	Kunshan Rotam Reddy Pharmaceutical Co. Ltd.	30 Apr 2020
Dementia, Vascular	Phase 1	CN	Kunshan Rotam Reddy Pharmaceutical Co. Ltd.	30 Apr 2020

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ARVO2023	Not Applicable	Neurotrophic keratitis	8	Oral Nicergoline	(pzljgqwytf) = cfwkqymjsk brgqnjsdwb (rtceclofvw )	-	23 Apr 2023
ARVO2023	Not Applicable	Neurotrophic keratitis	8	Systemic niicergoline	(pzljgqwytf) = azwcoykcah brgqnjsdwb (rtceclofvw )	-	23 Apr 2023
ARVO2017	Not Applicable	Persistent corneal epithelial defect	9	Nicergoline 10mg	lqgbbunxju(jrhecjfpcb) = nqbfzcmlso zcfsungtxe (foctczadjv )	-	07 May 2017

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