Delving into the Latest Updates on BEA-2180-BR with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

BEA 2180 BR, BEA-2180

Target

mAChRs

Action

antagonists

Mechanism

mAChRs antagonists(Muscarinic acetylcholine receptor antagonists)

Therapeutic Areas

Respiratory Diseases

Active Indication-

Inactive Indication

Pulmonary Disease, Chronic Obstructive

Originator Organization

Boehringer Ingelheim GmbH

Active Organization-

Inactive Organization

Boehringer Ingelheim GmbH

License Organization-

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC9H16BrNO2

InChIKeyIKDFZBCJDLZSNH-KRIZMXJXSA-M

CAS Registry1508-46-9

A Multinational, Randomised, Double-blind, Placebo- and Active-controlled, Parallel Group Efficacy and Safety Comparison Over 24 Weeks of Three Doses (50µg, 100µg, 200µg) of BEA 2180 BR to Tiotropium 5µg, Delivered by the Respimat Inhaler and Placebo in Patients With Chronic Obstructive Pulmonary Disease (COPD)

The primary objective of this study is to compare the bronchodilator efficacy of three doses (50 µg, 100 µg and 200 µg) of BEA 2180 delivered by the Respimat® once daily to placebo and tiotropium bromide delivered by the Respimat® in patients with COPD. Additional objectives include comparing the effects on dyspnea and health status.

Start Date06 Sep 2007

Sponsor / Collaborator

Boehringer Ingelheim GmbH

NCT02258971

/ CompletedPhase 1

Investigation of the Metabolism and Pharmacokinetics of 1200 μg (Free Cation) [14C] BEA 2180 BR Administered Orally Compared to 500 μg (Free Cation) [14C] BEA 2180 BR Administered Intravenously in Healthy Male Volunteers in an Open Label, Single-dose and Parallel Study Design

Primary objectives: To determine the basic pharmacokinetics of BEA 2180 BR, its metabolites CD 1975 ZW and CD 1976 ZW and radioactivity including excretion mass balance, excretion pathways and metabolism following the oral and intravenous administration of [14C] BEA 2180 BR
Secondary objectives: To determine safety and tolerability following single dose oral and iv administration of BEA 2180 BR in healthy male volunteers.

Start Date01 Mar 2007

Sponsor / Collaborator

Boehringer Ingelheim GmbH

100 Clinical Results associated with BEA-2180-BR

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100 Translational Medicine associated with BEA-2180-BR

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100 Patents (Medical) associated with BEA-2180-BR

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2

Literatures (Medical) associated with BEA-2180-BR

01 Jun 2013·Respiratory medicineQ3 · MEDICINE

Safety and efficacy of the once-daily anticholinergic BEA2180 compared with tiotropium in patients with COPD

Q3 · MEDICINE

Article

Author: Hendrik Schmidt ; Jill Karpel ; Petra Moroni-Zentgraf ; Roger Abrahams ; Joe Ramsdell ; Elizabeth Joseph

BACKGROUND:

To determine the safety and efficacy of BEA2180, an anticholinergic agent in patients with chronic obstructive pulmonary disease (COPD).

METHODS:

Smokers or ex-smokers ≥40 years with COPD and a postbronchodilator forced expiratory volume in 1 s (FEV1) <80% predicted and FEV1/forced vital capacity ≤70% participated in this multinational, randomised, double-blind, parallel study. Patients received BEA2180 (50, 100 or 200 μg), tiotropium (5 μg) or placebo once daily via Respimat Soft Mist™. The primary endpoint was trough FEV1 after 24 weeks. Secondary endpoints included Transition Dyspnoea Index (TDI) focal score, St George's Respiratory Questionnaire (SGRQ) total score, exacerbations and adverse events.

RESULTS:

Patients (n = 2080, 64.5% male) had a mean age of 64.2 years and a baseline FEV1 of 1.2 L. Trough FEV1 at 24 weeks with all BEA2180 doses (0.044-0.087 L) and tiotropium 5 μg (0.092 L) was significantly higher (p < 0.0001) than placebo (-0.034 L) and BEA2180 (200 μg) was noninferior to tiotropium. Mean TDI focal scores were higher with BEA2180 (1.43-1.48) or tiotropium (1.46) versus placebo (0.94; p ≤ 0.01 for all). Mean SGRQ total scores also improved with BEA2180 (40.1-40.7) or tiotropium (39.5) compared with placebo (43.0, p < 0.01 for all). COPD exacerbation rates were reduced for all active treatments, reaching statistical significance for BEA2180 (50 and 200 μg) (p < 0.05, for both).

CONCLUSION:

All study doses of BEA2180 improved lung function, reduced symptoms and exacerbations, and improved health status in COPD; all treatments were well tolerated. Clinical trial identifier: NCT00528996.

01 Mar 1966·British journal of pharmacology and chemotherapy

PHARMACOLOGY OF SCOPINIUM BROMIDE

Article

Author: K. VIDAL‐BERETERVIDE ; J. M. MONTI

Scopinium bromide, in doses ranging from 1 to 50 mg./kg. caused: autonomic ganglionic blockade (more marked for the sympathetic ganglia); autonomic ganglionic stimulation (more marked for the parasympathetic ganglia); arterial hypotension and bradycardia; marked salivation; and mydriasis in mice.Scopinium bromide did not produce chromodacryorrhea or contracture of the isolated intestine, nor did it show atropine-like, adrenergic nerve blocking, or adrenolytic properties.The drug appeared to have a direct constrictor action on vascular smooth muscle.The drug caused irregular, scattered muscle twitches in the cat, rigidity-paresis with coordinated tremor in mice, rats and rabbits, and muscle contracture in pigeons.Tremor in rabbits developed after intracisternal injection of the drug.Electroencephalographic changes in animals with implanted electrodes were not significant.

100 Deals associated with BEA-2180-BR

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pulmonary Disease, Chronic Obstructive	Phase 2	-	Boehringer Ingelheim GmbH	01 Jun 2004

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00528996 (CTgov)	Phase 2	Pulmonary Disease, Chronic Obstructive	2,080	Placebo	xfoexmzzlx(qxedherzru) = clzgutgqlg hrwzobkxwt (bhxgsbjalx, 0.010) View more	-	24 Aug 2021
NCT00528996 (Pubmed \| Respir Med)	Phase 2	Pulmonary Disease, Chronic Obstructive	2,080	BEA2180 50 μg	kdcgmnmwqa(hvwrnyjdhd) = dqkfbkhljv sfxbowjsfl (mumcfazfmv )	-	01 Jun 2013
NCT00528996 (Pubmed \| Respir Med)	Phase 2	Pulmonary Disease, Chronic Obstructive	2,080	BEA2180 100 μg	kdcgmnmwqa(hvwrnyjdhd) = apbflswxmk sfxbowjsfl (mumcfazfmv )	-	01 Jun 2013