Delving into the Latest Updates on Nicergoline with Synapse

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-

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Structure/Sequence

Molecular FormulaC24H26BrN3O3

InChIKeyYSEXMKHXIOCEJA-FVFQAYNVSA-N

CAS Registry27848-84-6

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

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100 Translational Medicine associated with Nicergoline

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100 Patents (Medical) associated with Nicergoline

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419

Literatures (Medical) associated with Nicergoline

01 Dec 2024·Seminars in Respiratory and Critical Care Medicine

Medications to Modify Aspiration Risk: Those That Add to Risk and Those That May Reduce Risk

Review

Author: Mergulhão, Paulo ; Froes, Filipe ; Gonçalves-Pereira, João

AbstractAspiration pneumonia results from the abnormal entry of fluids into the respiratory tract. We present a review of drugs known to affect the risk of aspiration. Drugs that increase the risk of aspiration pneumonia can be broadly divided into those that affect protective reflexes (like cough and swallowing) due to direct or indirect mechanisms, and drugs that facilitate gastric dysbiosis or affect esophageal and intestinal motility. Chief among the first group are benzodiazepines and antipsychotics, while proton pump inhibitors are the most well-studied in the latter group. Pill esophagitis may also exacerbate swallowing dysfunction. On the other hand, some research has also focused on pharmaceutical modulation of the risk of aspiration pneumonia. Angiotensin-converting enzyme inhibitors have been demonstrated to be associated with a decrease in the hazard of aspiration pneumonia in high-risk patients of Chinese or Japanese origin. Drugs like amantadine, nicergoline, or folic acid have shown some promising results in stroke patients, although the available evidence is thus far not enough to allow for any meaningful conclusions. Importantly, antimicrobial prophylaxis has been proven to be ineffective. Focusing on modifiable risk factors for aspiration pneumonia is relevant since this may help to reduce the incidence of this often severe problem. Among these, several commonly used drug classes have been shown to increase the risk of aspiration pneumonia. These drugs should be withheld in the high-risk population whenever possible, alongside general measures, such as the semirecumbent position during sleep and feeding.

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.

100 Deals associated with Nicergoline

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External Link

KEGG	Wiki	ATC	Drug Bank
D01290	Nicergoline	C04AE02	DB00699

R&D Status

Approved

10 top approved records.

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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.

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Indication	Highest Phase	Country/Location	Organization	Date
Affective Disorders, Psychotic	Phase 3	CN	Kunshan Rotam Reddy Pharmaceutical Co. Ltd.	30 Apr 2020
Alzheimer Disease	Phase 3	US	Pfizer Inc.	-
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

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ARVO2023	Not Applicable	Neurotrophic keratitis	8	Oral Nicergoline	(arrluzxfhe) = rspclwuwqg ohbgzijmly (euefzuezgd )	-	23 Apr 2023
ARVO2023	Not Applicable	Neurotrophic keratitis	8	Systemic niicergoline (Autologous Serum)	(arrluzxfhe) = rnjhaxdtyf ohbgzijmly (euefzuezgd )	-	23 Apr 2023
ARVO2017	Not Applicable	Persistent corneal epithelial defect	9	Nicergoline 10mg	oxsclozrgf(pyldlgugmy) = hkbpqzxskf wimitmfhgl (ntlapnoiak )	-	07 May 2017