Delving into the Latest Updates on Doxofylline with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Ansimar, Doxofylline (USAN/INN), Doxofylline Sodium Chloride

+ [30]

Target

A2aR x PDE x PDE2A

Mechanism

A2aR antagonists(Adenosine A2a receptor antagonists), PDE inhibitors, PDE2A inhibitors(Phosphodiesterase 2A inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesRespiratory Diseases

Active Indication

Pulmonary Disease, Chronic ObstructiveBronchitisAsthma+ [1]

Inactive Indication

Bronchiectasis

Originator Organization-

Active Organization

Heilongjiang Fuhe Huaxing Pharmaceutical Group Co. Ltd.

ABC

Inactive Organization

Alitair Pharmaceuticals, Inc.

Drug Highest PhaseApproved

First Approval Date

IT (01 Oct 1988),

AsthmaBronchitis, Chronic

RegulationOrphan Drug (US)

Login to view timeline

Structure

Molecular FormulaC11H14N4O4

InChIKeyHWXIGFIVGWUZAO-UHFFFAOYSA-N

CAS Registry69975-86-6

主要研究目的：研究餐后状态下单次口服受试制剂多索茶碱片（规格：400mg，黑龙江福和制药集团股份有限公司黑龙江福和制药集团股份有限公司）与参比制剂多索茶碱片（商品名：ANSIMAR®，规格：400mg，ABC FARMACEUTICI S.P.A.）在健康成年受试者体内的药代动力学，评价餐后状态下口服两种制剂的生物等效性。次要研究目的: 评价健康受试者餐后单次口服受试制剂（T）多索茶碱片和参比制剂（R）多索茶碱片（商品名：ANSIMAR®）后的安全性。

[Translation]

Main study objectives: To study the pharmacokinetics of the test preparation Doxofylline Tablets (Specification: 400mg, Heilongjiang Fuhe Pharmaceutical Group Co., Ltd. Heilongjiang Fuhe Pharmaceutical Group Co., Ltd.) and the reference preparation Doxofylline Tablets (Trade name: ANSIMAR®, Specification: 400mg, ABC FARMACEUTICI S.P.A.) in healthy adult subjects after a single oral administration in the fed state, and to evaluate the bioequivalence of the two preparations after oral administration in the fed state. Secondary study objectives: To evaluate the safety of the test preparation (T) Doxofylline Tablets and the reference preparation (R) Doxofylline Tablets (Trade name: ANSIMAR®) after a single oral administration in healthy subjects.

Start Date28 Oct 2024

Sponsor / Collaborator

Heilongjiang Fuhe Huaxing Pharmaceutical Group Co. Ltd.

CTR20243683 / RecruitingNot Applicable

多索茶碱片在健康受试者中餐后状态下的单剂量、随机、开放、四周期、完全重复交叉设计的生物等效性试验

[Translation] A single-dose, randomized, open-label, four-period, completely repeated crossover bioequivalence study of doxofylline tablets in healthy volunteers in the fed state

主要研究目的：研究餐后状态下单次口服受试制剂多索茶碱片（规格：400mg，江苏宣泰药业有限公司）与参比制剂多索茶碱片（商品名：ANSIMAR®，规格：400mg，ABC FARMACEUTICI S.P.A.）在健康成年受试者体内的药代动力学，评价餐后状态下口服两种制剂的生物等效性。次要研究目的: 评价健康受试者餐后单次口服受试制剂（T）多索茶碱片和参比制剂（R）多索茶碱片（商品名：ANSIMAR®）后的安全性。

[Translation]

Main study objectives: To study the pharmacokinetics of the test preparation Doxofylline Tablets (Specification: 400mg, Jiangsu Xuantai Pharmaceutical Co., Ltd.) and the reference preparation Doxofylline Tablets (Trade name: ANSIMAR®, Specification: 400mg, ABC FARMACEUTICI S.P.A.) in healthy adult subjects after a single oral administration in the fed state, and to evaluate the bioequivalence of the two preparations after oral administration in the fed state. Secondary study objectives: To evaluate the safety of the test preparation (T) Doxofylline Tablets and the reference preparation (R) Doxofylline Tablets (Trade name: ANSIMAR®) after a single oral administration in healthy subjects.

Start Date08 Oct 2024

Sponsor / Collaborator

Jiangsu Xuantai Pharmaceutical Co., Ltd

CTRI/2024/08/071763 / Not yet recruitingNot ApplicableIIT

Comparative study of Oral Doxophylline along with Triple drug therapy versus Triple Drug Therapy in Stable Severe Chronic Obstructive Pulmonary Disease Patients A Randomised control Trial. - NIL

Start Date11 Aug 2024

Sponsor / Collaborator

SRM Hospital

100 Clinical Results associated with Doxofylline

Login to view more data

100 Translational Medicine associated with Doxofylline

Login to view more data

100 Patents (Medical) associated with Doxofylline

Login to view more data

125

Literatures (Medical) associated with Doxofylline

01 Oct 2024·Science Progress

Development of a rapid method for the simultaneous determination of aminophylline, doxofylline, bromhexine, and ambroxol by HPLC

Article

Author: Meng, Xia ; Feng, Yunxia ; Chen, Fuchao ; Fang, Baoxia ; Shi, Ming

Introduction: Antitussive and expectorant drugs such as aminophylline (APL), doxofylline (DXL), bromhexine hydrochloride (BXH), and ambroxol hydrochloride (AXH), either individually or in combination, are widely used in the prevention and treatment of respiratory diseases. The study aimed to establish a high-performance liquid chromatography (HPLC) method for the simultaneous determination of these four drugs and to investigate their stability in 0.9% sodium chloride injection or 5% glucose injection over 48 hours. Methods: An InertSustain C18 column (150 mm × 4.6 mm, 5 μm) was used. The mobile phase consisted of acetonitrile and 50 mmol·L−1 potassium dihydrogen phosphate solution (pH 4.0) with gradient elution. The flow rate was 0.8 mL·min−1, and the column temperature was maintained at 30°C. The stability of APL, DXL, BXH, and AXH in 0.9% sodium chloride and 5% glucose injections over 48 h was determined using HPLC. Results: APL, DXL, BXH, and AXH showed good linearity within the ranges of 0.01 to 0.20, 0.003–0.06, 0.015–0.30, and 0.016–0.16 mg·mL−1, respectively (r > 0.999). The intraday and interday relative standard deviations were <2%, with recovery rates between 98.4% and 102.2%. The four drugs remained colorless and clear in infusion mixtures. The pH value fluctuated within ±0.3 over 48 hours, and the relative percentage content of the drugs ranged from 95.0% to 105.0%. Conclusion: The established HPLC method is simple, reliable, and stable, allowing for the simultaneous determination of the four antitussive and expectorant drugs. APL, DXL, BXH, and AXH were stable within 48 hours when mixed with 0.9% sodium chloride and 5% glucose injections.

02 Jun 2024·Journal of Asthma

Doxofylline as a steroid-sparing treatment in Mexican children with asthma

Article

Author: Ansotegui, Ignacio J. ; de la Cruz-de la Cruz, Carlos ; Acuña-Ortega, Natalhie ; González-Díaz, Sandra Nora ; Macouzet-Sánchez, Carlos

OBJECTIVEThe aim of this pilot study was to assess the efficacy of doxofylline as an ICS-sparing agent in the treatment of Mexican children with asthma.METHODS10-week, open-label, crossover, pilot study, we examined the steroid-sparing effect of doxofylline in Mexican children with asthma. Patients aged 6-16 years treated with inhaled corticosteroids (ICS) for at least 8 wk before enrollment were divided randomly into two groups at the baseline visit. Group A (n = 31) received doxofylline (18 mg/kg/day) plus standard-dose budesonide (D + SDB) for the first 4-week period followed by doxofylline plus reduced-dose budesonide (D + RDB) for the second 4-week period. Group B (n = 30) received D + RDB followed by D + SDB. Clinical outcomes assessed included lung function (forced expiratory volume; in 1 s, FEV1), fractional exhaled nitric oxide (FeNO), asthma control, number of exacerbations and use of rescue medication (salbutamol).RESULTSIt was shown that combined use of doxofylline and ICS may allow children with asthma to reduce their daily dose of ICS while maintaining lung function and improving asthma control (p = 0.008). There were few asthma exacerbations and only one patient required treatment with systemic corticosteroids. Rescue medication use decreased significantly in patients receiving D + SDB during the first 4-week period.CONCLUSIONSOur results suggest that doxofylline may be a steroid-sparing treatment in asthma, but longer-term, controlled studies are needed to confirm these observations.

01 May 2024·Journal of Thoracic Disease

A narrative review of theophylline: is there still a place for an old friend?

Review

Author: Scurek, Martin ; Brat, Kristian

Background and ObjectiveTheophylline has been used for decades in human medicine for its psychostimulant, anti-inflammatory, and bronchodilator effects. Historically, in pulmonary medicine, theophylline has been used in the treatment of obstructive pulmonary diseases such as bronchial asthma (BA) or chronic obstructive pulmonary disease (COPD). This review aims to determine whether theophylline still has its place in the therapy of obstructive pulmonary diseases or whether we can even extend its use to other diagnoses such as atropine-resistant cardiac arrests, apnea of prematurity, or others. Moreover, we also aim to determine if there is a rationale for using low-dose theophylline due to its immunomodulatory and anti-inflammatory effect, or if the future of methylxanthines lies in newly synthesized derivates of theophylline such as bamifylline, or doxofylline.MethodsThe narrative review is based on a literature search of the articles indexed in the PubMed database in 2023. We searched the database since the year 2009 using the MeSH terms "theophylline", "aminophylline", and "methylxanthines" and we included original articles in the English language.Key Content and FindingsTheophylline has a number of adverse drug reactions (ADRs), the most serious of which is its effect on the cardiovascular system. It can cause severe arrhythmias or even cardiac arrest when overdosed. On the other hand, there is still a substantial amount of its applications in current clinical practice.ConclusionsThere is considerable controversy associated with its use in current medicine, which can be attributed both to its narrow therapeutic range and its mentioned cardiotoxic effect. Herein, we summarize the current state-of-art of theophylline and its use in human medicine.

100 Deals associated with Doxofylline

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D03898	Doxofylline	R03DA11	DB09273

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Pulmonary Disease, Chronic Obstructive	PH	-	27 Apr 2007
Bronchitis	IT	ABC	10 Dec 2001
Asthma	IT	-	01 Oct 1988
Bronchitis, Chronic	IT	-	01 Oct 1988

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Bronchiectasis	Discovery	US	Alitair Pharmaceuticals, Inc.	-

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ERS2014	Not Applicable	Van Der Woude Syndrome	-	Doxofylline	gowfspagps(dhttfxxvqo) = xtwhiazken wyskxtqlcy (pamlecibqg )	-	01 Sep 2014
				Montelukast	gowfspagps(dhttfxxvqo) = ezkpzyhusm wyskxtqlcy (pamlecibqg )
ERS2011	Not Applicable	Pulmonary Disease, Chronic Obstructive	30	Doxofylline 400 mg bid + inhaled bronchodilators	vxfauxwlev(uxygtpidey) = uxpcriqpod xofaqbgfca (aiivvslhvk )	Positive	01 Sep 2011
				inhaled bronchodilators only	vxfauxwlev(uxygtpidey) = hmomzjithz xofaqbgfca (aiivvslhvk )