ETX0914 Publications and Presentations

Damião Gouveia, A.C., Unemo, M. and Jensen, J.S.
In vitro activity of zoliflodacin (ETX0914) against macrolide-resistant fluoroquinolone-resistant and antimicrobial-susceptible Mycoplasma genitalium strains
J Antimicrobial Chemotherapy doi:10.1093/jac/dky022 (2018)


Presentation Title: Microbiological Cure Rates and Antimicrobial Susceptibility of Neisseria gonorrhoeaeto ETX0914 (AZD0914) in a Phase II Treatment Trial for Urogenital Gonorrhea
Presented by: Stephanie N. Taylor, MD; LSU-Crescent Care Sexual Health Center
Meeting: ID Week, 2016


Papp JR,  Lawrence K, Sharpe S, Mueller J, Kirkcaldy  R
In vitro growth of multidrug-resistant Neisseria gonorrhoeae isolates is inhibited by ETX0914, a novel spiropyrimidinetrione
International Journal of Antimicrobial Agents (2016)


Giacobbe R, Huband M, deJonge B, Bradford P
Effect of Susceptibility Testing Conditions on the In Vitro Antibacterial Activity of ETX0914
Diagnostic Microbiology and Infectious Disease (2016)


Guo J, Joubran C, Luzietti RA Jr, Basarab GS, Grimm SW, Vishwanathan K
Absorption, distribution, metabolism and elimination of 14C-ETX0914, a novel inhibitor of bacterial type-II topoisomerases in rodents
Xenobiotica (2016)


Foerster S, Golparian D, Jacobsson S, Hathaway L, Low N, Shafer W, Althaus C, Unemo M
Genetic resistance determinants, in vitro time-kill curve analysis and pharmacodynamic functions for the novel topoisomerase II inhibitor ETX0914 (AZD0914) in Neisseria gonorrhoeae
Frontiers in Microbiology (2015)


Su XH, Wang BX, Le WJ, Liu YR, Wan C, Li S, Alm RA, Mueller JP, Rice PA
Multidrug resistant Neisseria gonorrhoeae from Nanjing are sensitive to killing by a novel DNA gyrase inhibitor, ETX0914 (AZD0914)
Antimicrobial Agents Chemotherapy (2015)


Biedenbach DJ, Huband MD, Hackel M, de Jonge BL, Sahm DF, Bradford PA
In vitro Activity of AZD0914, a Novel Bacterial DNA Gyrase/Topoisomerase IV Inhibitor, Against Clinically Relevant Gram-positive and Fastidious Gram-negative Pathogens
Antimicrobial Agents and Chemotherapy (2015)


Basarab GS, Kern G, McNulty J, Mueller JP, Lawrence K, Vishwanathan K, Alm RA, Barvian K, Doig P, Galullo V, Gardner H, Gowravaram M, Huband M, Kimzey A, Morningstar M, Kutschke A, Lahiri SD, Perros M, Singh R, Schuck V, Tommasi R, Walkup G, Newman J
Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases
Nature Scientific Reports (2015)


Kern G , Palmer T, Ehmann DE, Shapiro AB, Andrews B, Basarab GS, Doig P, Fan J, Gao N, Mills SD, Mueller J, Sriram S, Thresher J, Walkup G
Inhibition of Neisseria gonorrhoeae type II Topoisomerases by the Novel Spiropyrimidinetrione AZD0914
Journal of Biological Chemistry (2015)


Basarab GS, Doig P, Galullo V, Kern G, Kimzey A, Kutschke ANewman J, Morningstar M, Mueller J, Otterson L, Vishwanathan KZhou F, Gowravaram M
Discovery of Novel DNA Gyrase Inhibiting Spiropyrimidinetriones – Benzisoxazole Fusion with N-Linked Oxazolidinone Substituents Leading to a Clinical Candidate (ETX0914)
Journal of Medicinal Chemistry (2015)


Waites KB, Crabb DM, Duffy LB, Huband MD
In Vitro Antibacterial Activity of AZD0914 Against Human Mycoplasmas and Ureaplasmas
Antimicrobial Agents and Chemotherapy (2015)


Unemo M, Ringlander J, Wiggins C, Fredlund H, Jacobsson S, Cole M
High in vitro susceptibility to the novel spiropyrimidinetrione ETX0914 (also known as AZD0914) among 873 contemporary clinical Neisseria gonorrhoeae isolates in 21 European countries during 2012-2014.
Antimicrobial Agents and Chemotherapy (2015)


Alm R, Lahiri S, Kutschke A, Otterson L, McLaughlin R, Whiteaker J, Lewis L, Su X, Huband M, Gardner H, Mueller J
Characterization of the novel DNA gyrase inhibitor AZD0914: Low resistance potential and lack of cross-resistance in Neisseria gonorrhoeae
Antimicrobial Agents and Chemotherapy (2014)


Jacobsson S, Golparian D, Alm RA, Huband M, Mueller J, Skov Jensen J, Ohnishi M, Unemoa M
High in vitro activity of the novel spiropyrimidinetrione AZD0914, a DNA gyrase inhibitor, against multidrug resistant Neisseria gonorrhoeae isolates suggests a new effective option for oral treatment of gonorrhea
Antimicrobial Agents and Chemotherapy (2014)


Kohlhoff S, Huband M, Hammerschlag M
In vitro activity of AZD0914, a novel DNA gyrase inhibitor, against Chlamydia trachomatis and Chlamydia pneumoniae
Antimicrobial Agents and Chemotherapy (2014)


Huband M, Bradford P, Otterson L, Basarab G, Kutschke A, Giacobbe R, Patey S, Alm R, Johnstone M, Potter M, Miller P, Mueller J
In Vitro Antibacterial Activity of AZD0914: A New Spiropyrimidinetrione DNA Gyrase/Topoisomerase Inhibitor with Potent Activity against Gram-Positive, Fastidious Gram-Negative, and Atypical Bacteria
Antimicrobial Agents and Chemotherapy (2014)


Basarab GS, Brassil P, Doig P, Galullo V, Haimes HB, Kern G, Kutschke A, McNulty J, Schuck VJ, Stone G, Gowravaram M
Novel DNA Gyrase Inhibiting Spiropyrimidinetriones with a Benzisoxazole Scaffold: SAR and in Vivo Characterization
Journal of Medicinal Chemistry (2014)


Basarab G, Galullo V, DeGrace N, Hauck S, Joubran C, Wesolowski S
Synthesis of a Tetrahydronaphthyridine Spiropyrimidinetrione DNA Gyrase Inhibiting Antibacterial Agent – Differential Substitution at all Five Carbon Atoms of Pyridine
Organic Letters (2014)

“Our scientific approach and expertise, coupled with Entasis’ strong pipeline of programs, really make us stand out in the field of antibacterial drug discovery and development.”

— Satenig Guler, Senior Scientist