Clinical Trial to Assess the Protective Effect of the Fixed Drug Combination of Disodium Cromoglycate Plus Reproterol in Comparison to the Single Components and Placebo in Adults With Exercise Induced Asthma Randomised, Placebo-controlled, Double-blind, Crossover, Multicentre Study

This is a multicentre, randomised, double-blind, placebo-controlled, 4-way cross-over study. At each study visit a standardised treadmill test will be performed to provoke EIA. Before and after the challenge test pulmonary function variables (e.g. forced expiratory volume in one second (FEV1)) will be measured in order to assess the protective effect of the study medication.

Start Date01 Nov 2007

Sponsor / Collaborator

MEDA Pharma GmbH & Co. KG

[+2]

100 Clinical Results associated with Reproterol Hydrochloride

100 Translational Medicine associated with Reproterol Hydrochloride

100 Patents (Medical) associated with Reproterol Hydrochloride

Literatures (Medical) associated with Reproterol Hydrochloride

01 Jun 2023·Journal of medical virology

Novel SARS-CoV-2 entry inhibitors, 2-anilinoquinazolin-4(3H)-one derivatives, show potency as SARS-CoV-2 antivirals in a human ACE2 transgenic mouse model.

Article

Author: Ko, Meehyun ; Myung, Subeen ; Park, Hyeung-Geun ; Kim, Hyoung Rae ; Shin, Young Sup ; Kim, Seungtaek ; Song, Jong Hwan ; Jang, Min Seong ; Jeon, Sangeun ; Lee, Jun Young ; Park, Chul Min ; Cho, Jung-Eun

The ongoing COVID-19 has not only caused millions of deaths worldwide, but it has also led to economic recession and the collapse of public health systems. The vaccines and antivirals developed in response to the pandemic have improved the situation markedly; however, the pandemic is still not under control with recurring surges. Thus, it is still necessary to develop therapeutic agents. In our previous studies, we designed and synthesized a series of novel 2-anilinoquinazolin-4(3H)-one derivatives, and demonstrated inhibitory activity against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and MERS-CoV in vitro. We then conducted in vivo studies using modified compounds that are suitable for oral administration. These compounds demonstrated no toxicity in rats and inhibited viral entry. Here, we investigated the in vivo efficacy of these drug candidates against SARS-CoV-2. Three candidate drugs, 7-chloro-2-((3,5-dichlorophenyl)amino)quinazolin-4(3H)-one (1), N-(7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-N-(3,5-dichlorophenyl)acetamide (2), and N-(7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)-N-(3,5-difluorophenyl)acetamide (3) were administered orally to hACE2 transgenic mice at a dose of 100 mg/kg. All three drugs improved survival rate and reduced the viral load in the lungs. These results show that the derivatives possess in vivo antiviral efficacy similar to that of molnupiravir, which is currently being used to treat COVID-19. Overall, our data suggest that 2-anilinoquinazolin-4(3H)-one derivatives are promising as potential oral antiviral drug candidates against SARS-CoV-2 infection.

01 May 2021·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Design, synthesis and biological evaluation of 2-aminoquinazolin-4(3H)-one derivatives as potential SARS-CoV-2 and MERS-CoV treatments

Q4 · MEDICINE

Article

Author: Jeon, Sangeun ; Lee, Se In ; Kim, Seungtaek ; Lee, Jun Young ; Kim, Hyoung Rae ; Jang, Min Seong ; Song, Jong Hwan ; Cho, Jung-Eun ; Park, Chul Min ; Shin, Young Sup ; Noh, Soojin

Despite the rising threat of fatal coronaviruses, there are no general proven effective antivirals to treat them. 2-Aminoquinazolin-4(3H)-one derivatives were newly designed, synthesized, and investigated to show the inhibitory effects on SARS-CoV-2 and MERS-CoV. Among the synthesized derivatives, 7-chloro-2-((3,5-dichlorophenyl)amino)quinazolin-4(3H)-one (9g) and 2-((3,5-dichlorophenyl)amino)-5-hydroxyquinazolin-4 (3H)-one (11e) showed the most potent anti-SARS-CoV-2 activities (IC₅₀ < 0.25 μM) and anti-MERS-CoV activities (IC₅₀ < 1.1 μM) with no cytotoxicity (CC₅₀ > 25 μM). In addition, both compounds showed acceptable results in metabolic stabilities, hERG binding affinities, CYP inhibitions, and preliminary PK studies.

01 Dec 2012·Sleep and BreathingQ3 · MEDICINE

Cromoglycate, reproterol, or both—what’s best for exercise-induced asthma?

Q3 · MEDICINE

Article

Author: N. C. Netzer ; K. Goebbels ; T. Küpper ; L. N. Kennes

OBJECTIVEInternational guidelines recommend short- (SABA) or long-acting b-agonists for the prevention of bronchoconstriction after exercise (EIB) in patients with exercise-induced asthma (EIA). However, other drugs are still in discussion for the prevention of EIB. We investigated the efficacy of a combination of inhaled sodium cromoglycate and the β-mimetic drug reproterol versus inhaled reproterol alone and both versus inhaled placebo in subjects with exercise-induced asthma (EIA).METHODSThe study aimed to prove the preventive effect of a combination of 1-mg reproterol and 2-mg disodium cromoglycate (DSCG) and its single components vs. placebo, measuring the decrease of FEV1 after a standardized treadmill test in 11 patients with recorded EIA. The study medication was twice as high as those of drugs which are commercially available (e.g., Allergospasmin®, Aarane®).RESULTSThe results revealed that the combination of reproterol and DSCG was significantly effective against a decrease of FEV1 after a standardized exercise challenge test (ECT) compared to placebo. The short-acting b-agonist reproterol alone had almost the same effectiveness as the combination of reproterol and DNCG. The difference between the combination with DNCG and reproterol alone was less than 10% and insignificant (p 0.48). DNCG alone did not show a difference in the effectiveness compared to placebo.CONCLUSIONPrevention of EIA with the combination of reproterol and DSCG or with reproterol only is effective. An exclusive recommendation in favor of the combination cannot be given due to the low difference in the effectiveness versus reproterol alone. Due to the limited number of subjects and some probands showing protection under DSCG, it cannot be completely excluded that there is some preventive power of DSCG in individual cases.

100 Deals associated with Reproterol Hydrochloride

External Link

KEGG	Wiki	ATC	Drug Bank
D05718	Reproterol Hydrochloride	R03AC15 R03CC14	DB12846

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Asthma	-	-	-
Pulmonary Disease, Chronic Obstructive	-	-	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma, Exercise-Induced	Discovery	DE	MEDA Pharma GmbH & Co. KG	01 Nov 2007

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