Delving into the Latest Updates on Fluticasone Propionate/Formoterol fumarate/Glycopyrrolate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

AIRZ-FF, Fluticasone propionate/glycopyrrolate/formoterol fumarate, Glycopyrrolate/formoterol fumarate/fluticasone propionate

Target

GR x cPLA2α x mAChRs x β2-adrenergic receptor

Mechanism

GR agonists(Glucocorticoid receptor agonists), cPLA2α agonists(Cytosolic phospholipase A2 agonists), mAChRs antagonists(Muscarinic acetylcholine receptor antagonists)

+ [1]

Therapeutic Areas

Respiratory Diseases

Active Indication

Pulmonary Disease, Chronic Obstructive

Inactive Indication-

Originator Organization

Glenmark Pharmaceuticals Ltd.

Active Organization

Glenmark Pharmaceuticals Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

IN (01 May 2020),

Pulmonary Disease, Chronic Obstructive

Regulation-

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Structure

Molecular FormulaC25H31F3O5S

InChIKeyWMWTYOKRWGGJOA-CENSZEJFSA-N

CAS Registry80474-14-2

View All Structures (2)

Several studies have demonstrated the benefits of the LAMA (Long-Acting Muscarinic Antagonists) + LABA (Long-Acting Beta-Agonists) + IC (inhaled corticosteroids) combination in the treatment of chronic obstructive pulmonary disease (COPD). The use of the triple combination in patients with severe airflow obstruction and a history of flares has been associated with improved lung function, improved patient-reported endpoints and prevention of flares, when compared to LABA, LABA + LAMA and LABA + IC. Furthermore, when compared to dual therapies LABA + IC and LABA + LAMA, triple therapy has been able to reduce all-cause deaths among chronic obstructive pulmonary disease (COPD) patients.
Previously published studies have demonstrated that the triple combination of Fluticasone 250 mcg/Formoterol 12 mcg/Glycopyrronium 12.5 mcg was able to improve lung function in chronic obstructive pulmonary disease (COPD) patients with a history of flares. There was also a significant improvement in the mMRC (modified-Medical Research Council) which began in the 2nd week of treatment and continued up to week 12. The association was considered safe and well tolerated, with only mild to moderate adverse events recorded in approximately 25% of the subjects treated in the study.
Furthermore, bioavailability studies performed with the components of the combination proposed as experimental drug - Fluticasone/Formoterol/Glycopyrronium - indicated that there is no pharmacokinetic interaction between the 3 active ingredients when they were administered concomitantly to healthy individuals under fasting conditions.

Start Date28 Feb 2026

Sponsor / Collaborator

Eurofarma Laboratórios SA

NCT02666287 / CompletedPhase 1

An Open Label, Six-period Cross-over, Single and Repeat Dose Study to Determine the Pharmacokinetics of Fluticasone Furoate and GSK961081 When Administered Alone, in Combination, or Concurrently Via the ELLIPTA

Batefenterol (BAT) is a novel bifunctional molecule that combines muscarinic antagonism and beta2-agonism in a single molecule and is in development for the treatment of chronic obstructive pulmonary disease (COPD). FF is a corticosteroid approved as the inhaled corticosteroid (ICS) component of a combination product, with vilanterol (VI), a long-acting beta2-agonist for COPD. In the current study FF will be investigated as an inhaled product in combination with BAT, for treatment of COPD.
This study is an open-label, six-way crossover, single and repeat dose study to evaluate the systemic pharmacokinetics, safety and tolerability of FF and BAT when administered via the ELLIPTA™ alone, in combination, or concurrently at 3 times the clinical dose, following a single dose, and at the proposed clinical dose, following repeat doses.
This study will consist of screening period, 6 treatment periods, and a follow-up visit. Each subject will have 3 periods in which they receive a single dose treatment regimen (3 inhalations on Day 1 of each single dose study period) and 3 periods in which they receive a single dose treatment regimen followed by a 7-day, once-daily, repeated dose. On Day 1 of those periods, subjects will receive their single dose as 3 inhalations. On Days 2-8, subjects will receive 1 inhalation per day for the repeated dose regimen. There will be a minimum of 7-day washout between each treatment periods. All subjects will receive 9 treatments and follow-up procedures will be done 7 14 days after the last dose.
Forty eight healthy subjects will be enrolled into the study, such that approximately 40 subjects complete dosing and PK assessments. The total duration of participation for each subject in this study will be up to 15 weeks. ELLIPTA is a registered trademark of the GlaxoSmithKline [GSK] group of companies.

Start Date27 Jan 2016

Sponsor / Collaborator

GSK Plc

[+1]

NCT02483975 / CompletedPhase 3

A Randomized, Double-blind, Placebo-controlled, Parallel Group Study of Once-daily Inhaled Fluticasone Furoate Inhalation Powder for Six Weeks on the Hypothalamic-pituitary-adrenocortical Axis of Children Aged 5-11 Years With Asthma

Inhaled corticosteroids (ICS) have a number of known class effects including hypothalamic-pituitary-adrenocortical (HPA) axis suppression. Although the safety of inhaled Fluticasone Furoate (FF) on the HPA axis of adults and adolescent asthmatic patients has been established, it is important to assess the risk of suppression in children so as to establish whether this medicine can be safely used in this young population. This study aims to evaluate the effect of inhaled FF on the HPA axis of children 5-11 years of age (inclusive) with persistent asthma compared with placebo. Approximately 143 subjects will be enrolled. Subjects will enter a 7 to 14 day run-in period on oral montelukast 4 milligrams (mg) (5 year old subjects) or 5 mg (6-11 year old subjects) once daily. Eligible subjects will be randomized to receive once-daily FF inhalation powder 50 micrograms (mcg) or once-daily placebo inhalation powder in the morning via the ELLIPTA™ inhaler for 42 days. Subjects will continue to receive open label montelukast during the treatment period. All subjects will be provided albuterol/salbutamol inhalation aerosol, to use as needed to treat acute asthma symptoms throughout the study.
ELLIPTA is a registered trademark of the GlaxoSmithKline group of companies.

Start Date09 Oct 2015

Sponsor / Collaborator

GSK Plc

100 Clinical Results associated with Fluticasone Propionate/Formoterol fumarate/Glycopyrrolate

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100 Translational Medicine associated with Fluticasone Propionate/Formoterol fumarate/Glycopyrrolate

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100 Patents (Medical) associated with Fluticasone Propionate/Formoterol fumarate/Glycopyrrolate

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5

Literatures (Medical) associated with Fluticasone Propionate/Formoterol fumarate/Glycopyrrolate

01 Jan 2019·Nigerian Journal of Clinical PracticeQ4 · MEDICINE

3-D mapping of cortical bone thickness in subjects with different face form and arch form: A CBCT analysis

Q4 · MEDICINE

Article

Author: Alfarsi, M A ; Chaturvedi, S

OBJECTIVETo determine the relationship between face form (FF), arch form (AF), and cortical bone thickness in anterior and posterior region of the mandibular jaws, using cone beam computed tomography (CBCT).PATIENTS AND METHODSTotal 90 subjects were selected. For each subject FF (euryprosopic, mesoprosopic, and leptoprosopic) was determined using Prosopic Index. CBCT scans were done for each subject to determine mandibular AF (as tapered, oval, or square in horizontal sections) and cortical bone thickness (at two vertical levels 4 and 7 mm from the alveolar crest in the anterior and posterior region of mandible in sagittal sections). Numerical data so obtained were analyzed using descriptive statistics, analysis of variance followed by Tukey HSD (honestly significant difference) test at a statistical significance level of 5%.RESULTSSignificant difference in thickness of cortical bone was noted between various AF and face. In square AF, mean value of thickness of cortical bone was highest both at 4 and 7 mm vertical level and tapered AF had minimum mean values at 4 mm and oval at 7 mm in anterior region and posterior region on buccal and lingual sides, in all the three-FF.CONCLUSIONSignificant effects of FF and AF on cortical bone thickness were seen both on buccal and lingual side and the effect of AF was more compared to FF. The availability of the cortical bone in euryprosopic FF and square AF patients was more; therefore, implants with a shorter length may be used in these clinical cases.

25 Sep 2007·Journal of Assisted Reproduction and GeneticsQ3 · MEDICINE

Sperm motility stimulation and preservation with various concentrations of follicular fluid

Q3 · MEDICINE

Article

Author: Suwadee Wirotkarun ; Chatpavit Getpook

PURPOSEThe purpose of this study is to evaluate the optimal concentrations of follicular fluid (FF) for sperm motility stimulation and preservation.METHODSThirty normal semen samples and FF from women in an in vitro fertilization programme were used in an experiment. The semen was processed and incubated in Earle culture media with 20, 50, 80, and 100% FF (v/v) with controls. Sperm motility was evaluated and followed up for 48 h.RESULTSFF could stimulate progressive sperm motility at all concentrations and last for at least 12 h. However, at more than 50% v/v of FF, sperm demonstrated a rapid decline in progressive motility after 12 h of incubation compared to other concentrations and the control group.CONCLUSIONFF can stimulate the sperm motility properly at not more than 50% (v/v) concentration.

01 Dec 1984·Indian journal of experimental biology

Effect of follicular atresia on in vitro uptake of acetate-1-14C by granulosa cells of preovulatory follicles in rat ovary.

Article

Author: Parshad, R K ; Guraya, S S

100 Deals associated with Fluticasone Propionate/Formoterol fumarate/Glycopyrrolate

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