A Randomized, Double-Blind, Placebo-Controlled Trial of the Efficacy of Retapamulin as a Topical Decolonizing Agent for Mupirocin Resistant Methicillin Resistant Staphylococcus Aureus (MRSA)

The purpose of this study is to investigate the efficacy of retapamulin to reduce carriage of MRSA via a randomized, double-blind, placebo-controlled clinical study testing retapamulin among patients with confirmed mupirocin-resistant nasal and/or rectal MRSA colonization. The sample size will include 27 subjects in each of the two arms of the study (retapamulin versus placebo) for a total of 54 subjects. Participants who are found to be nasal and/or rectal colonized with MRSA will be randomized to receive either retapamulin or placebo applied nasally and rectally for a total of 5 days. Nasal and rectal swabs will be collected at pre-defined time points during study duration (screening swab, swab one week after completion of topical therapy, swab 4 weeks after completion of topical therapy) to assess MRSA colonization status. The colonization rates of both groups will be assessed via Fisher's Exact Test.

Start Date01 Dec 2017

Sponsor / Collaborator

NYU Langone Health

NCT01812382

/ CompletedPhase 1

A Study to Evaluate the Feasibility of Microdialysis to Determine Skin Concentrations of Retapamulin in Healthy Volunteers

This feasibility study will allow for the determination of the in vivo recovery and time of dialysis to optimize a future thorough microdialysis study. This is a single session, open label study to evaluate the feasibility of microdialysis for Retapamulin in healthy subjects. Three healthy subjects will be enrolled and complete the study procedures. Subjects will be admitted to the research unit on Day 1 and three microdialysis probes will be placed in the thigh of each subject prior to the start of the microdialysis procedure. After normal saline solution infusion for 30 minutes, a Retapamulin solution will be infused for 90 minutes. Saline perfusion will occur during the washout period. Microdialysis sampling will be done for 30 minutes (during the last 30 minutes of drug perfusion) and dialysate sample collection will continue every 30 minutes for 4 hours. The approximate duration of study including follow-up is 4 days.

Start Date02 Apr 2014

Sponsor / Collaborator

GSK Plc

NCT01445600

/ CompletedNot Applicable

An Open Label, Multi-centre, Non-interventional Post-marketing Surveillance (PMS) to Monitor the Safety and Efficacy of ALTARGO(Retapamulin) Administered in Korean Patients According to the Prescribing Information

This is an open label, multi-centre, non-interventional post-marketing surveillance.

Start Date01 Nov 2012

Sponsor / Collaborator

GSK Plc

100 Clinical Results associated with Retapamulin

100 Translational Medicine associated with Retapamulin

100 Patents (Medical) associated with Retapamulin

227

Literatures (Medical) associated with Retapamulin

06 May 2024·JAC-Antimicrobial Resistance

In vitro activity of ozenoxacin against Staphylococcus aureus and Streptococcus pyogenes clinical isolates recovered in a worldwide multicentre study (2020–2022)

Article

Author: García-Castillo, María ; Coppi, Marco ; Hernández-García, Marta ; Sampaio, Jorge ; Correa, Adriana ; Vila, Jordi ; Seifert, Harald ; Pitart, Cristina ; Wootton, Mandy ; Wake, Karen ; Fritsche, Thomas ; Griener, Thomas ; Cantón, Rafael

AbstractObjectivesWe performed a multicentre study (2020–2022) to compare the in vitro activity of ozenoxacin and comparator agents against Staphylococcus aureus and Streptococcus pyogenes clinical isolates from skin and soft-tissue infections (SSTI).MethodsA total of 1725 isolates (1454 S. aureus and 271 S. pyogenes) were collected in 10 centres from eight countries between January 2020 and December 2022. Antimicrobial susceptibility testing was determined (microdilution-SENSITITRE). Results were interpreted following European Committee on Antimicrobial Susceptibility Testing (EUCAST) 2023 (clinical breakpoints, ECOFF) and CLSI criteria.ResultsOzenoxacin exhibited high in vitro activity against S. aureus (MIC50/90 = 0.002/0.12 mg/L) and S. pyogenes (MIC50/90 = 0.015/0.03 mg/L), inhibiting 99% of the isolates at MIC ≤ 0.5 mg/L and at MIC ≤ 0.06, respectively. The most active comparators against S. aureus were retapamulin (MIC90 = 0.12 mg/L), fusidic acid (MIC90 = 0.25 mg/L) and mupirocin (MIC90 = 0.5 mg/L); and against S. pyogenes were retapamulin (MIC90 = 0.03 mg/L), clindamycin (MIC90 = 0.12 mg/L) and mupirocin (MIC90 = 0.25 mg/L). Ciprofloxacin and methicillin resistant rates for S. aureus were 31.3% (455/1454) and 41% (598/1454), respectively. Additionally, 62% (373/598) of the MRSA were also ciprofloxacin non-susceptible, whereas only 10% (23/271) of the MSSA were ciprofloxacin resistant. Ozenoxacin was more active against ciprofloxacin-susceptible S. aureus than against ciprofloxacin-resistant isolates, and showed a slightly higher MIC in MRSA isolates than in MSSA. However, ozenoxacin activity was comparable in both ciprofloxacin-resistant MSSA and MRSA subsets. On the other hand, ozenoxacin had similar activity in ciprofloxacin-susceptible and resistant S. pyogenes isolates.ConclusionsOzenoxacin is a potent antimicrobial agent of topic use against Gram-positive bacteria causing SSTI, including MRSA isolates non-susceptible to ciprofloxacin.

01 Oct 2023·Molecular Pharmacology

Induced Fit Describes Ligand Binding to Membrane-Associated Cytochrome P450 3A4

Article

Author: Sweeney, David Tyler ; Hackett, John C ; Stokowa-Sołtys, Kamila ; Zárate-Pérez, Francisco

Cytochrome P450 3A4 (CYP3A4) is the dominant P450 involved in human xenobiotic metabolism. Competition for CYP3A4 therefore underlies several adverse drug-drug interactions. Despite its clinical significance, the mechanisms CYP3A4 uses to bind diverse ligands remain poorly understood. Highly monodisperse CYP3A4 embedded in anionic lipoprotein nanodiscs containing an equal mixture of 1-palmitoyl-2-oleoyl-glycero-3-phosphocholine and 1-palmitoyl-2-oleoyl-sn-glycero-3-phospho-(1'-rac-glycerol) were used to determine which of the limiting kinetic schemes that include protein conformational change, conformational selection (CS) or induced fit (IF), best described the binding of four known irreversible inhibitors. Azamulin, retapamulin, pleuromutilin, and mibrefadil binding to CYP3A4 nanodiscs conformed to a single-site binding model. Exponential fits of stopped-flow UV-visible absorption spectroscopy data supported multiple-step binding mechanisms. Trends in the rates of relaxation to equilibrium with increasing ligand concentrations were ambiguous as to whether IF or CS was involved; however, global fitting and consideration of the rate constants favored an IF mechanism. In the case of mibrefadil, a transient complex was observed in the stopped-flow UV-visible experiment, definitively assigning the presence of IF in ligand binding. While these studies only consider a small region of CYP3A4's vast ligand space, they provide kinetic evidence that CYP3A4 can use an IF mechanism. SIGNIFICANCE STATEMENT: CYP3A4 is capable of oxidizing numerous xenobiotics, including many drugs. Such promiscuity could not be achieved without conformational changes to accommodate diverse substrates. It is unknown whether conformational heterogeneity is present before (conformational selection) or after (induced fit) ligand binding. Stopped-flow measurements of suicide inhibitors binding to nanodisc-embedded CYP3A4 combined with sophisticated numerical analyses support that induced fit better describes ligand binding to this important enzyme.

08 Jun 2023·ACS medicinal chemistry letters

Design, Synthesis, and Biological Activity of Thioguanine-Modified Pleuromutilin Derivatives.

Article

Author: Lai, Peng ; Wang, Zhouyu ; Yong, Can ; Zhang, Xiujuan ; Li, Yun ; He, Xiaolong ; Zhang, Yuanyuan ; Yu, Jianglin ; Xie, Chuan ; Wu, Chunxia ; Liu, Dongfang

Antibiotic overuse has caused the increasingly serious problem of bacterial drug resistance, with numerous marketed antibiotics exhibiting significantly reduced activity against drug-resistant bacteria.Therefore, there is urgent demand for the development of novel antibiotics.Pleuromutilin is a tricyclic diterpene exhibiting antibacterial activity against Gram-pos. bacteria and is currently considered the most promising natural antibiotic.In this study, novel pleuromutilin derivatives were designed and synthesized by introducing thioguanine units, and their antibacterial activities against drug-resistant strains were evaluated in vitro and in vivo.Compound 6j was observed to have a rapid bactericidal effect, low cytotoxicity, and potent antibacterial activity.The in vitro results suggest that 6j has a significant therapeutic effect on local infections, and its activity is equal to that of retapamulin, an anti-Staphylococcus aureus pleuromutilin derivative

News (Medical) associated with Retapamulin

22 Jun 2022

·www.prnewswire.com

Acute Bacterial Skin and Skin Structure Infections (ABSSSI) Market to Surpass US$ 20,450.6 Million by 2030 - Coherent Market Insights

SEATTLE, June 22, 2022 /PRNewswire/ -- According to Coherent Market Insights, the global acute bacterial skin and skin structure infections (ABSSSI) market is estimated to be valued at US$ 10,263.5 million in 2022 and is expected to exhibit a CAGR of 9.0% over the forecast period (2022-2030). Key Trends and Analysis of the Global Acute Bacterial Skin and Skin Structure Infections (ABSSSI) Market: Key trends in market include widespread presence of acute bacterial skin and skin structure infections (ABSSSI); increasing approval of novel drugs for acute bacterial skin and skin structure infections (ABSSSI), and increasing collaborations, acquisitions, and partnerships among key players. These key trends are expected to aid in growth of the global acute bacterial skin and skin structure infections (ABSSSI) market. According to an article published in the PLOS One journal, a peer-reviewed open access scientific journal in July 2020, the lifetime prevalence of skin and soft tissue infections (SSTI), a type of ABSSSI in people who inject drugs (PWID) in London was found to be 64% (abscess and/or cellulitis), on the basis of data collected between October 2017 and March 2019. Moreover, rapid research and development in the field of acute bacterial skin and skin structure infections (ABSSSI) for development of novel treatment for the same is expected to fuel market growth over the forecast period. For instance, in January 2022, Paladin Labs Inc., a subsidiary of Endo International plc launched Xydalba (dalbavancin for injection), in Canada. Xydalba is a 30-minute intravenous (IV) therapy, which can be administered as a single- or two-dose regimen for treatment of acute bacterial skin and skin structure infections (ABSSSI) in adults. Furthermore, key players operating in the global acute bacterial skin and skin structure infections (ABSSSI) market are focusing on adoption of inorganic growth strategies such as partnerships, acquisitions, collaborations, and others in order to expand their market presence in the global market. For instance, in May 2020, Advanz Pharma, a U.K.-based pharmaceutical company, announced that it had completed the acquisition of Correvio Pharma Corp., a Canada-based specialty pharmaceutical company whose product portfolio includes licensed medicines such as XYDALBA (dalbavancin hydrochloride) indicated for the treatment of acute bacterial skin and skin structure infections (ABSSSI) in adults. Request Sample Copy of this Report @ Key Market Takeaways: Global acute bacterial skin and skin structure infections (ABSSSI) market is expected to exhibit a CAGR of 9.0% over the forecast period, owing to rising focus of market players on regulatory approvals for novel acute bacterial skin and skin structure infections (ABSSSI) therapeutics. For instance, in July 2021, AbbVie Inc. ., a U.S. based pharmaceutical company announced that it has received the U.S. Food and Drug Administration (USFDA) approval for its drug Dalvance (dalbavancin), administered as an intravenous (IV) infusion for the treatment of pediatric patients with ABSSSI caused by methicillin-resistant Staphylococcus aureus (MRSA) and other gram-positive bacteria. Among infection type, community acquired ABSSSI segment is expected to account for the largest market share in 2022, owing to rising drug launches by market players for treatment of community acquired acute bacterial skin and skin structure infections (ABSSSI). For instance, in February 2021, Paratek Pharmaceuticals, Inc., a U.S.-based pharmaceutical company announced that it is expanding commercial launch of its tetracycline-class oral antibiotic Nuzyra (omadacycline) into the community setting. Nuzyra is indicated for the treatment of adults with acute skin and skin structure infections (ABSSSI). Key players operating in the global acute bacterial skin and skin structure infections (ABSSSI) market include Merck & Co., Inc., Pfizer, Inc., GlaxoSmithKline plc., Teva Pharmaceutical Industries Ltd., Paratek Pharmaceuticals, Inc., Melinta Therapeutics, Inc., Arrevus, Inc., AbbVie, Inc., Aurobindo Pharma Ltd., Amneal Pharmaceuticals LLC, Sun Pharmaceutical Industries Ltd., Accord Healthcare Ltd., Intas Pharmaceuticals Ltd., Fresenius SE & Co. KGaA, Sandoz Inc., Glenmark Pharmaceuticals Ltd, and Cadila Healthcare Ltd. Request for Customization @ Detailed Segmentation: Global Acute Bacterial Skin and Skin Structure Infections (ABSSSI) Market, By Drug Type: Oral & Parenteral Antibiotics Vancomycin Linezolid Clindamycin Ceftaroline Daptomycin Dalbavancin Tedizolid Others (Rifampin, Doxycycline, Minocycline, and Trimethoprim-Sulfa Methoxazol, among others) Topical Antibiotics Hydrogen Peroxide Fusidic Acid Mupirocin Retapamulin Povidone-Iodine Global Acute Bacterial Skin and Skin Structure Infections (ABSSSI) Market, By Infection Type: Hospital Acquired ABSSSI Community Acquired ABSSSI Global Acute Bacterial Skin and Skin Structure Infections (ABSSSI) Market, By Route of Administration: Oral Parenteral Topical Global Acute Bacterial Skin and Skin Structure Infections (ABSSSI) Market, By Distribution Channel: Hospital Pharmacies Retail Pharmacies Online Pharmacies Global Acute Bacterial Skin and Skin Structure Infections (ABSSSI) Market, By Region: North America By Country: U.S. Canada Europe By Country: U.K. Germany Italy France Spain Russia Rest of Europe Asia Pacific By Country: China India Japan ASEAN Australia South Korea Rest of Asia Pacific Latin America By Country: Brazil Mexico Argentina Rest of Latin America Middle East & Africa By Country: GCC Countries Israel South Africa Rest of Middle East & Africa Buy this Complete Report Now @ Find related trending report below: North America and Europe Acute Bacterial Skin and Skin Structure Infections (ABSSSI) Market , by Drug Type (Oral & Parenteral Antibiotics (Vancomycin, Linezolid, Clindamycin, Ceftaroline, Daptomycin, Dalbavancin, Tedizolid, and Others) and Topical Antibiotics (Hydrogen Peroxide, Fusidic Acid, Mupirocin, Retapamulin, and Povidone-Iodine)), by Infection Type (Hospital Acquired ABSSSI and Community Acquired ABSSSI), by Route of Administration (Oral, Parenteral, and Topical), by Distribution Channel (Hospital Pharmacies, Retail Pharmacies, and Online Pharmacies), and by Region (North America, and Europe) - Size, Share, Outlook, and Opportunity Analysis, 2020 - 2027 About Us: Coherent Market Insights is a global market intelligence and consulting organization focused on assisting our plethora of clients achieve transformational growth by helping them make critical business decisions. We are headquartered in India, having sales office at global financial capital in the U.S. and sales consultants in United Kingdom and Japan. Our client base includes players from across various business verticals in over 57 countries worldwide. We create value for clients through our highly reliable and accurate reports. We are also committed in playing a leading role in offering insights in various sectors post-COVID-19 and continue to deliver measurable, sustainable results for our clients. Contact Us: Mr. Shah Senior Client Partner – Business Development Coherent Market Insights Phone: US: +1-206-701-6702 UK: +44-020-8133-4027 Japan: +81-050-5539-1737 India: +91-848-285-0837 Email: [email protected] Website: Follow Us: LinkedIn | Twitter Logo: SOURCE Coherent Market Insights

AcquisitionCollaborate

100 Deals associated with Retapamulin

External Link

KEGG	Wiki	ATC	Drug Bank
D05720	Retapamulin	D06AX13	DB01256

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Skin Diseases, Bacterial	Preclinical	India	GSK Plc	01 May 2008
Skin Diseases, Bacterial	Preclinical	United States	GSK Plc	01 May 2008
Skin Diseases, Bacterial	Preclinical	Argentina	GSK Plc	01 May 2008
Skin Diseases, Bacterial	Preclinical	South Africa	GSK Plc	01 May 2008
Impetigo	Preclinical	United States	Almirall LLC	12 Apr 2007

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01591785 (CTgov)	Not Applicable	Eczema, Dyshidrotic	60	Retapamulin 1% ointment (Retapamulin 1% Ointment)	zvqczavpxq(whnqcanfsu) = sigvxlfzwa kfqplgumjn (eunwjriwam, kcbnumibmo - vozvhjnrpr) View more	-	03 Dec 2020
				Placebo (Placebo Ointment)	zvqczavpxq(whnqcanfsu) = lorjenuqnp kfqplgumjn (eunwjriwam, mphqcgunyi - guoxqwlhvz) View more
NCT03304873 (CTgov)	Phase 3	-	47	Retapamulin (Retapamulin)	xnvwquhgte(zdabfvxybl) = rzpbtrxrbq mdpizlkhyi (gtufpccjcd, ldpmclmbsm - relrhzzgdz) View more	-	19 Mar 2020
				Placebo Ointment (Placebo)	xnvwquhgte(zdabfvxybl) = kdeayngpqp mdpizlkhyi (gtufpccjcd, btbfklppek - eqzlujwejm) View more
NCT01461668 (CTgov)	Phase 4	MRSA - Methicillin resistant Staphylococcus aureus infection	53	Retapamulin (Retapamulin)	hqkhrrhgwv(varvcmnylg) = syoywgbssi ewpphwhybz (mzkhrtotsa, xbvgxfsfxh - qcjuxuxayo) View more	-	02 Apr 2018
				Placebo (Placebo)	hqkhrrhgwv(varvcmnylg) = yxqdlsilrb ewpphwhybz (mzkhrtotsa, jbzcewlncq - xxlyuesxse) View more
NCT00852540 (CTgov)	Phase 3	Impetigo	410	Placebo+Retapamulin (Retapamulin Ointment, 1% (Weight/Weight) Plus Oral Placebo)	sjuwttvllu(nmhfgbxgll) = hxhsmkutzg gfevmcursz (khjqpptbbm, uhbvxzmpuq - fcvngztyie) View more	-	26 Aug 2011
				Placebo+Linezolid (Linezolid Plus Placebo Ointment)	sjuwttvllu(nmhfgbxgll) = ksdcbotugp gfevmcursz (khjqpptbbm, adblizmcca - qomiurpghj) View more
NCT00555061 (CTgov)	Phase 4	Skin Diseases, Bacterial \| Skin and skin structure infections	60	Retapamulin	oxbtuignej(thypcmzvgl) = rrjtryjvlh ogptwibbuz (ckexrymucw, dvttbcoecm - shilklkcgd) View more	-	30 Apr 2010

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