Last update 21 Nov 2024

YU-253911

Last update 21 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

non-beta-lactam penicillin binding protein inhibiting core(Domillin/ Case Western Reserve University of Medicine), oxopyrazole antibiotics(Domillin/ Case Western Reserve University of Medicine)

+ [1]

Target

PBP3

Mechanism

PBP3 inhibitors(Penicillin-binding protein 3 inhibitors)

Therapeutic Areas

Infectious Diseases

Active Indication

Acinetobacter InfectionsKlebsiella InfectionsPseudomonas Infections

Inactive Indication-

Originator Organization

Domillion

Active Organization

Case Western Reserve University School of Medicine

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

100 Clinical Results associated with YU-253911

100 Translational Medicine associated with YU-253911

100 Patents (Medical) associated with YU-253911

Literatures (Medical) associated with YU-253911

01 Aug 2021·The Lancet Regional Health - Europe

Paediatric outpatient prescriptions in France between 2010 and 2019: A nationwide population-based study

Article

Author: Weill, Alain ; Dray-Spira, Rosemary ; Taine, Marion ; Offredo, Lucile ; Zureik, Mahmoud ; Chalumeau, Martin

BACKGROUNDPaediatric outpatient prescription (POP) monitoring is pivotal to identify inadequate prescriptions and optimize drug use. We aimed at describing recent trends in POPs in France.METHODSAll reimbursed dispensations of outpatient prescribed drugs (excluding vaccines) were prospectively collected for the paediatric population (<18 years old) in the French national health database in 2010-2011 and 2018-2019 (mean 117,356,938/year). POP prevalence (proportion of children receiving ≥1 drug prescriptions/year) was calculated by age groups and compared by prevalence rate ratios (PRRs). Given the large sample size, 95% confidence intervals of POP prevalences and PRRs did not differ from estimates.FINDINGSAmong the 14,510,023 children resident in France in 2018-2019, mean POP prevalence was 857‰ children. Most prescribed therapeutic classes were analgesics (643‰), antibiotics (405‰), nasal corticosteroids (328‰), nonsteroidal anti-inflammatory drugs (NSAIDs) (244‰), antihistamines (246‰) and systemic corticosteroids (210‰). POPs decreased with age from 976‰ for infants to 782‰ for adolescents. Children <6 years old were notably more exposed to inhaled corticosteroids (PRR=3.06), non-penicillin beta-lactam antibacterial agents (PRR=3.05) and systemic corticosteroids (PRR=2.11) than older ones. The POP prevalence was slightly higher (PRR=1.04) during 2018-2019 than 2010-2011, with marked increases for anti-emetics (PRR=1.84), vitamin D (PRR=1.49), proton pump inhibitors (PRR=1.42), systemic contraceptives (PRR=1.24) and nasal corticosteroids (PRR=1.21) and decreases for propulsive/prokinetic agents (PRR=0.09), NSAIDs (PRR=0.73) and systemic antibiotics (PRR=0.88).INTERPRETATIONPOP remained highly prevalent in France throughout the 2010s, especially for children <6 years old, with only a few improvements for selected therapeutic classes. These findings should prompt clinical guidance campaigns and/or regulatory policies.FUNDINGInternal funding.

01 Aug 2021·European Journal of Medicinal ChemistryQ1 · MEDICINE

A γ-lactam siderophore antibiotic effective against multidrug-resistant Pseudomonas aeruginosa, Klebsiella pneumoniae, and Acinetobacter spp.

Q1 · MEDICINE

Article

Author: Perez, Federico ; van Duin, David ; Hoyer, Denton ; Spencer, Elizabeth J ; Papp-Wallace, Krisztina M ; Goldberg, Joel A ; Kumar, Vijay ; Bethel, Christopher R ; Kreiswirth, Barry N ; Plummer, Mark S ; Marshall, Steven H ; Hujer, Kristine M ; van den Akker, Focco ; Bonomo, Robert A ; Hujer, Andrea M ; Jacobs, Michael R

Serious infections caused by multidrug-resistant (MDR) organisms (Klebsiella pneumoniae, Pseudomonas aeruginosa, Acinetobacter baumannii) present a critical need for innovative drug development. Herein, we describe the preclinical evaluation of YU253911, 2, a novel γ-lactam siderophore antibiotic with potent antimicrobial activity against MDR Gram-negative pathogens. Penicillin-binding protein (PBP) 3 was shown to be a target of 2 using a binding assay with purified P. aeruginosa PBP3. The specific binding interactions with P. aeruginosa were further characterized with a high-resolution (2.0 Å) X-ray structure of the compound's acylation product in P. aeruginosa PBP3. Compound 2 was shown to have a concentration >1 μg/ml at the 6 h time point when administered intravenously or subcutaneously in mice. Employing a meropenem resistant strain of P. aeruginosa, 2 was shown to have dose-dependent efficacy at 50 and 100 mg/kg q6h dosing in a mouse thigh infection model. Lastly, we showed that a novel γ-lactam and β-lactamase inhibitor (BLI) combination can effectively lower minimum inhibitory concentrations (MICs) against carbapenem resistant Acinetobacter spp. that demonstrated decreased susceptibility to 2 alone.

11 Jun 2020·Journal of Medicinal ChemistryQ1 · MEDICINE

A γ-Lactam Siderophore Antibiotic Effective against Multidrug-Resistant Gram-Negative Bacilli

Q1 · MEDICINE

Article

Author: Jacobs, Michael R ; Cmolik, Anna ; Marshall, Steven H ; Kumar, Vijay ; Hujer, Andrea M ; Bethel, Christopher R ; Goldberg, Joel A ; Papp-Wallace, Krisztina M ; Perez, Federico ; Hujer, Kristine M ; Rudin, Susan D ; Hoyer, Denton ; Marshall, Emma K ; Nguyen, Ha ; van Duin, David ; van den Akker, Focco ; O'Shea, Margaret ; Plummer, Mark S ; Bonomo, Robert A ; Domitrovic, T Nicholas ; Logan, Latania K ; Kreiswirth, Barry M ; Spencer, Elizabeth J

Treatment of multidrug-resistant Gram-negative bacterial pathogens represents a critical clinical need. Here, we report a novel γ-lactam pyrazolidinone that targets penicillin-binding proteins (PBPs) and incorporates a siderophore moiety to facilitate uptake into the periplasm. The MIC values of γ-lactam YU253434, 1, are reported along with the finding that 1 is resistant to hydrolysis by all four classes of β-lactamases. The druglike characteristics and mouse PK data are described along with the X-ray crystal structure of 1 binding to its target PBP3.

100 Deals associated with YU-253911

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acinetobacter Infections	Preclinical	US	Case Western Reserve University School of Medicine	-
Klebsiella Infections	Preclinical	US	Case Western Reserve University School of Medicine	-
Pseudomonas Infections	Preclinical	US	Case Western Reserve University School of Medicine	-

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YU-253911

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R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

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Regulation