Delving into the Latest Updates on Fluticasone Propionate/Formoterol Fumarate Hydrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Fluticasone/Formoterol, Flutiform 125, Flutiform 50

+ [6]

Target

GR x β2-adrenergic receptor

Mechanism

GR agonists(Glucocorticoid receptor agonists), β2-adrenergic receptor agonists(Beta-2 adrenergic receptor agonists)

Therapeutic Areas

Immune System DiseasesRespiratory Diseases

Active Indication

Asthma

Inactive Indication

Moderate asthmaPersistent asthmaPulmonary Disease, Chronic Obstructive+ [1]

Originator Organization

Vectura Group Ltd.

Active Organization

KYORIN Pharmaceutical Co., Ltd.

Beijing Mengdi Pharmaceutical Co. Ltd.

Napp Pharmaceuticals Ltd.

Inactive Organization

Abbott LaboratoriesSkyePharma AG

Fisons Ltd.

Drug Highest PhaseApproved

First Approval Date

JP (20 Sep 2013),

Asthma

Regulation-

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Structure/Sequence

Molecular FormulaC92H118F6N4O24S2

InChIKeyZLQPBKRHFCHUSM-CNJJYQOESA-N

CAS Registry1818371-29-7

Eurofarma Laboratórios S.A. markets a FDC containing formoterol 12 mcg/fluticasone 250 mcg, in a single capsule for inhalation (Lugano®; reference product). The product is indicated for the treatment of asthma in patients aged ≥ 12 years. The company seeks to register a product with lower concentrations of mono-drugs (6 mcg and 125 mcg, respectively) to enable the dosage step up and step down treatment strategies advocated by the Global Initiative for Asthma for the inhaled maintenance treatment of asthma (GINA, 2022 ) with these combinations.
This Phase 3 study will be carried out for demonstrating the non-inferiority of the investigational drug (FDC of formoterol 6 mcg/fluticasone 125 mcg) compared to the FDC of formoterol 6 mcg/budesonide 200 mcg (Alenia® - Aché Laboratórios Farmacêuticos S.A.) in the maintenance treatment of asthma, allowing its registration as a new concentration of the drug already registered by the company.

Start Date30 Jun 2025

Sponsor / Collaborator

Eurofarma Laboratórios SA

CTR20171144

/ CompletedNot Applicable

一项在中国健康受试者中评估FLUTIFORM pMDI 50/5 μg、125/5 μg和250/10 μg,药代动力学特征的开放性、单剂和单剂加多剂给药研究

[Translation] An open-label, single-dose and single-dose plus multiple-dose study to evaluate the pharmacokinetic characteristics of FLUTIFORM pMDI 50/5 μg, 125/5 μg, and 250/10 μg in healthy Chinese subjects

评估在中国健康受试者中经加压定量吸入器（pMDI）吸入单剂（50/5 μg、125/5 μg和250/10 μg）和多剂（250/10 μg）FLUTIFORM 的药代动力学（PK）特征和安全性特征。

[Translation]

To evaluate the pharmacokinetic (PK) and safety profiles of single (50/5 μg, 125/5 μg, and 250/10 μg) and multiple (250/10 μg) doses of FLUTIFORM inhaled by pressurized metered-dose inhaler (pMDI) in healthy Chinese subjects.

Start Date16 Apr 2018

Sponsor / Collaborator

Beijing Mengdi Pharmaceutical Co. Ltd.

[+2]

JPRN-UMIN000029379

/ CompletedNot ApplicableIIT

Rapid effect of Flutiform on pulmonary function compared with Relvar and Symbicort - Rapid effect of Flutiform on pulmonary function compared with Relvar and Symbicort

Start Date02 Oct 2017

Sponsor / Collaborator-

100 Clinical Results associated with Fluticasone Propionate/Formoterol Fumarate Hydrate

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100 Translational Medicine associated with Fluticasone Propionate/Formoterol Fumarate Hydrate

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100 Patents (Medical) associated with Fluticasone Propionate/Formoterol Fumarate Hydrate

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24

Literatures (Medical) associated with Fluticasone Propionate/Formoterol Fumarate Hydrate

01 Apr 2023·Journal of Aerosol Medicine and Pulmonary Drug Delivery

Pharmacokinetic and Pharmacodynamic Comparison of Fluticasone Propionate/Formoterol Fumarate Administered via a Pressurized Metered-Dose Inhaler and a Novel Breath-Actuated Inhaler in Healthy Volunteers

Article

Author: Dissanayake, Sanjeeva ; Lomax, Mark ; Mundin, Gill ; Dalvi, Prashant ; Woodward, Jo

Introduction: Fluticasone propionate/formoterol fumarate (fluticasone/formoterol) exposures, following administration of Flutiform^® K-haler^®, a breath-actuated inhaler (BAI), were compared with the Flutiform pressurized metered-dose inhaler (pMDI) with/without spacer in two healthy volunteer studies. In addition, formoterol-induced systemic pharmacodynamic (PD) effects were examined in the second study. Methods: Study 1: single-dose, three-period, crossover pharmacokinetic (PK) study with oral charcoal administration. Fluticasone/formoterol 250/10 μg was administered via BAI, pMDI, or pMDI with spacer (pMDI+S). Pulmonary exposure for BAI was deemed no less than for pMDI (primary comparator) if the lower limit of 94.12% confidence intervals (CIs) for BAI:pMDI maximum plasma concentration (Cmax) and area under the plasma concentration-time curve (AUCt) ratios was ≥80%. Study 2: two-stage adaptive design, both stages being single-dose, crossover without charcoal administration. The PK stage compared fluticasone/formoterol 250/10 μg via BAI, pMDI, or pMDI+S. The primary comparisons were as follows: BAI versus pMDI+S for fluticasone and BAI versus pMDI for formoterol. Systemic safety with BAI was deemed no worse than primary comparator if the upper limit of 94.12% CIs for Cmax and AUCt ratios was ≤125%. PD assessment was to be conducted if BAI safety was not confirmed in the PK stage. Based on PK results, only formoterol PD effects were evaluated. The PD stage compared fluticasone/formoterol 1500/60 μg via BAI, pMDI, or pMDI+S; fluticasone/formoterol 500/20 μg pMDI; and formoterol 60 μg pMDI. The primary endpoint was maximum reduction in serum potassium within 4 hours postdose. Equivalence was defined as 95% CIs for BAI versus pMDI+S and pMDI ratios within 0.5-2.0. Results: Study 1: lower limit of 94.12% CIs for BAI:pMDI ratios >80%. Study 2, PK stage: upper limit of 94.12% CIs for fluticasone (BAI:pMDI+S) ratios <125%; upper limit of 94.12% CIs for formoterol (BAI:pMDI) ratios >125% (for Cmax, not AUCt). Study 2, PD stage: 95% CIs for serum potassium ratios 0.7-1.3 (BAI:pMDI+S) and 0.4-1.5 (BAI:pMDI). Conclusions: Fluticasone/formoterol BAI performance was within the range observed for the pMDI with/without a spacer. Sponsor: Mundipharma Research Ltd. EudraCT 2012-003728-19 (Study 1) and 2013-000045-39 (Study 2).

01 Jan 2020·Arerugi = [Allergy]

[A PHASE III STUDY TO EVALUATE SAFETY AND EFFICACY OF FLUTICASONE/FORMOTEROL COMBINATION (FLUTIFORM^® AEROSOL) IN LONG-TERM ADMINISTRATION (24 WEEKS) IN JAPANESE PEDIATRIC PATIENTS WITH BRONCHIAL ASTHMA].

Article

Author: Ishikawa, Yasuyuki ; Kamata, Miho ; Katsunuma, Toshio

BACKGROUNDThe combination drug of inhaled corticosteroid (ICS)/long-acting β2 agonist is being used as a long-term control medication for pediatric asthma patients for those who are poorly controlled by ICS alone. Long-term efficacy and safety of Fluticasone propionate/formoterol fumarate hydrate (FP/FM) was evaluated in pediatric patients with bronchial asthma.METHODSTwo inhales of FP/FM (50/5μg) at one time, twice daily were administered for 24 weeks to Japanese asthma patients aged 5 to ＜16 years who had asthma symptoms during the observation period while using the same dosage of ICS during a certain period of time. Adverse drug reactions, morning peak flow (mPEF) and asthma symptoms were evaluated 24 weeks after administration.RESULTSFP/FM was administered to 53 subjects. 52 subjects completed the 24 week administration. The incidence of adverse drug reactions was 9.4% (5 of 53), and all of the adverse drug reactions were mild. The mPEF increased from the starting value and was maintained through the treatment period. The average change from baseline in the mPEF after 24 weeks of treatment was 21.39±2.93L/min (Least squares mean±standard error). Changes in asthma symptoms were similar to that of morning peak flow.CONCLUSIONIt was considered that FP/FM could be useful for long-term control of pediatric asthma.

01 Jan 2020·DrugsQ1 · MEDICINE

Comparative Safety Profile of the Fixed-Dose Combination Corticosteroid and Long-acting β2-Agonist Fluticasone Propionate/Formoterol Fumarate: A 36-Month Longitudinal Cohort Study in UK Primary Care

Q1 · MEDICINE

Article

Author: Carter, Victoria ; Martin, Jessica ; Yang, Sen ; Hoffman, Matthias ; Cooper, Andrew J ; Skinner, Derek ; Price, David B ; Gardener, Elizabeth A ; Willis, Jenna C

OBJECTIVEThe inhaled corticosteroid/long-acting β₂-agonist (ICS/LABA) fluticasone propionate/formoterol fumarate (FP/FORM; Flutiform^®) has been available as fixed-dose combination (FDC) therapy for asthma patients aged ≥ 12 years in the UK since 2012. This post-authorisation safety study examined adverse outcomes and prescribing practices for FP/FORM and other FDC ICS/LABA therapies in a real-life clinical setting over 36 months.METHODSHistorical, longitudinal cohort database study using UK primary care data from the Clinical Practice Research Datalink (CPRD) database, for patients initiated on or switched to an FDC ICS/LABA (ENCePP study number: EUPAS12330). The main cohort was adults aged ≥ 18 years with asthma. The primary outcome was incidence of new adverse outcomes after initiation of ICS/LABA; hazard ratios (HRs) and 95% confidence intervals were estimated for FP/FORM versus other FDC ICS/LABAs using Cox regression models.RESULTSA total of 241,007 patients with an FDC ICS/LABA prescription were identified. In the adult asthma cohort (N = 41,609), the incidence rate of new adverse outcomes [in 100 patient-years (py)] was significantly lower for FP/FORM (24.75) versus fluticasone/salmeterol metered-dose inhaler [8.86; HR 1.14 (1.04, 1.25)], fluticasone/salmeterol dry powder inhaler [31.19; HR 1.18 (1.08, 1.29)], budesonide/formoterol [25.16; HR: 1.13 (1.03, 1.25)] and beclometasone/formoterol [25.47; HR 1.14 (1.04, 1.25)]. The overall prescribing rate was lower for FP/FORM (13.85 per 1000/py) than licensed FDC ICS/LABA comparators (20.30-28.13 per 1000/py). Of those prescribed FP/FORM, 80.8% were adults with asthma and < 7% were prescribed FP/FORM "off-label".CONCLUSIONSThe results suggest that FP/FORM was associated with an overall lower adverse outcome rate than the licensed comparators.

1

News (Medical) associated with Fluticasone Propionate/Formoterol Fumarate Hydrate

02 Nov 2009

·www.pharmatimes.com

SkyePharma boosted by Flutiform trial success

SkyePharma’s shares were given a hefty boost yesterday after the company announced that a late-stage trial of Flutiform was a success, paving the way for the drug’s filing in Europe during the first quarter of next year. The group’s stock had already jumped more than 22% by mid-morning trading on the London Stock Exchange as investors welcomed news that development and marketing partner Mundipharma has completed the final Phase III clinical trial of the European development programme for its flagship asthma combination drug Flutiform (fluticasone and formoterol), and that the higher dose strength study hit its primary targets. Flutiform HFA-MDI has been designed to bring together the most commonly prescribed inhaled anti-inflammatory corticosteroid (fluticasone propionate) and a long-acting beta-agonist (formoterol fumarate) in one product, delivered via "an environmentally-friendly aerosol propellant hydrofluoroalkane" and through a metered dose inhaler, with which the companies will be hoping to gain a significant share of the multi-billion-euro asthma market. In the multi-centre study, 529 patients with severe, persistent and reversible asthma were randomised to receive either Flutiform (fluticasone 500 _g/formoterol 20 _g); a mix of (Flixotide (fluticasone 500 _g) and Foradil (formoterol 24 _g); a lower dose form of Flutiform (fluticasone 100 _g /formoterol 10 _g); or Flixotide alone. The results showed that Flutiform was at least as effective as the Flixotide/Foradil combination in improving pre- and post-dose FEV1 (Forced Expiratory Volume in the first second) over the eight week duration of the study, and also that the drug was well tolerated in patients, enabling a European Marketing Authorisation Application to be filed in Q1 2010, confirmed SkyePharma’s chief executive Dr Ken Cunningham. The news will be particularly welcome given the delays the drug, the success of which is crucial to the company’s future, is facing across the pond. Back in September SkyePharma’s stock was given a knock after it was announced the US regulators have requested more dosing data on the drug, requiring additional clinical work and delaying its potential approval for at least a couple of years.

100 Deals associated with Fluticasone Propionate/Formoterol Fumarate Hydrate

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External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Asthma	JP	KYORIN Pharmaceutical Co., Ltd.	20 Sep 2013

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Moderate asthma	Discovery	CN	Beijing Mengdi Pharmaceutical Co. Ltd.	19 Apr 2017
Moderate asthma	Discovery	CN	Napp Pharmaceuticals Ltd.	19 Apr 2017
Pulmonary Disease, Chronic Obstructive	Discovery	CN	Fisons Ltd.	04 Mar 2015
Pulmonary Disease, Chronic Obstructive	Discovery	CN	Beijing Mengdi Pharmaceutical Co. Ltd.	04 Mar 2015
Pulmonary Disease, Chronic Obstructive	Discovery	CN	Napp Pharmaceuticals Ltd.	04 Mar 2015
Asthma	Discovery	DE	SkyePharma AG	01 Mar 2006
Asthma	Discovery	HU	SkyePharma AG	01 Mar 2006
Asthma	Discovery	GB	SkyePharma AG	01 Mar 2006
Asthma	Discovery	PL	SkyePharma AG	01 Mar 2006
Asthma	Discovery	RO	SkyePharma AG	01 Mar 2006

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ERS2018	Phase 3	-	4,102	Fluticasone propionate/formoterol pMDI	urgvqjfrxx(sjncbasbtf) = siesgdsqio qigmwykyng (uqldngjbcn )	-	15 Sep 2018
EudraCT number: 2015-000744-42 (ERS2017)	Not Applicable	-	36	fluticasone propionate/formoterol	phgaqelmmy(qrtgxpqrrg) = oeplojsajq eivtdosvof (viuyibpoag )	-	01 Sep 2017
				fluticasone propionate/formoterol	phgaqelmmy(qrtgxpqrrg) = hyfxaeubwq eivtdosvof (viuyibpoag )
EUPAS4072 (ERS2017)	Not Applicable	Asthma	2,539	Fluticasone propionate/formoterol (FP/FORM)	bqthgqljld(aeioqrmkkp) = dcrcsticza yhffqqdmzx (ndckuzmgar )	Positive	01 Sep 2017
ERS2017	Not Applicable	Asthma	6	Flutiform	czduaoefxy(eroqqcchms) = qprzhipslf ausazbjauq (ciyzhpnuyr )	-	01 Sep 2017
ENCePP/SDPP/3702 (ERS2016)	Not Applicable	Asthma	1,563	Fluticasone propionate/formoterol combination (FP/FORM)	(hfudqqbakr) = 160 patients (10.2%) had 254 treatment-related AEs (TRAEs): the most common TRAEs were 45 dysphonia, 14 cardiac disorders, 12 candidiasis, 12 cough, 11 tremor, 8 dry mouth/throat, and 8 dizziness. Other TRAEs included four patients (0.3%) who had 5 asthma exacerbations requiring systemic steroids xtdrkwkvih (bgknnuxdzo )	Positive	01 Sep 2016
NCT01978145 (CTgov)	Phase 3	Pulmonary Disease, Chronic Obstructive	665	Placebo+Salbutamol+FSC (FSC Capsule-Based Unit Dose DPI)	ksbzcmlage(jxslbfayce) = ubhupctwkt wtmbsjvsaa (iuagyctxzo, bnctxmjykq - fobjhhdtwr) View more	-	18 Jan 2016
				Placebo+Salbutamol+FSC (FSC Multi-Dose DPI)	ksbzcmlage(jxslbfayce) = mehgxvckdk wtmbsjvsaa (iuagyctxzo, jnffsdhuur - zdgzgnoodc) View more
NCT01978119 (CTgov)	Phase 3	Asthma	124	Placebo+Salbutamol+FSC (FSC Capsule-Based Unit Dose DPI)	rznevmoqjf(kbaukbgzxi) = rpqxnwsnes uxnhkrqvgq (dqpwzwcozz, tldlhddkje - htydemaupb) View more	-	08 Oct 2015
				Placebo+Salbutamol+FSC (FSC Multi-Dose DPI)	rznevmoqjf(kbaukbgzxi) = nmnfwcalkf uxnhkrqvgq (dqpwzwcozz, gaswoizhsf - xsqqccbngd) View more
ERS2014	Not Applicable	Asthma	512	Fluticasone propionate/formoterol (FP/FORM) 100/10µg BID	dhxkkulgsq(vbkwsmyrtk) = kcdeliyybc odvkadqqsz (eixbpkqvpe )	Positive	01 Sep 2014
				Fluticasone propionate/salmeterol (FP/SAL) 100/50µg BID	dhxkkulgsq(vbkwsmyrtk) = ugedjtjzqi odvkadqqsz (eixbpkqvpe ) View more
ERS2014	Not Applicable	-	-	Fluticasone propionate/formoterol (FP/FORM)	bbpxqxnwqz(dpjmrswwls) = smvddjvppz ejwwxijatg (gfwdhosgqq, 0.07)	-	01 Sep 2014
				Beclometasone/formoterol (BDP/FORM)	bbpxqxnwqz(dpjmrswwls) = canvkxpplt ejwwxijatg (gfwdhosgqq, 0.14)
ERS2014	Not Applicable	-	-	Fluticasone propionate/formoterol 125/5μg (FP/FORM)	lanblyiajq(yclkhmmhey) = thiuamgtgb fdwytvswfg (ohaahrlgyf ) View more	-	01 Sep 2014
				Fluticasone propionate/salmeterol 125/25μg (FP/SAL)	lanblyiajq(yclkhmmhey) = pjixufcnpf fdwytvswfg (ohaahrlgyf ) View more