Single-Dose Pharmacokinetics, Excretion, and Metabolism of Zoliflodacin, a Novel Spiropyrimidinetrione Antibiotic, in Healthy Volunteers-Reference-Cited by-同舟云学术

Single-Dose Pharmacokinetics, Excretion, and Metabolism of Zoliflodacin, a Novel Spiropyrimidinetrione Antibiotic, in Healthy Volunteers

Published:2019-01 Issue:1 Volume:63 Page:
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

O’Donnell John¹,Lawrence Ken²,Vishwanathan Karthick³,Hosagrahara Vinayak⁴,Mueller John P.¹

Affiliation:

1. Entasis Therapeutics, Inc., Waltham, Massachusetts, USA

2. Tetraphase Pharmaceuticals, Watertown, Massachusetts, USA

3. Clinical Pharmacology, AstraZeneca Pharmaceuticals, Waltham, Massachusetts, USA

4. EMD Serono, Billerica, Massachusetts, USA

Abstract

Zoliflodacin is a novel spiropyrimidinetrione with activity against bacterial type II topoisomerases that inhibits DNA biosynthesis and results in accumulation of double-strand cleavages in bacteria. We report results from two phase 1 studies that investigated the safety, tolerability, and pharmacokinetics (PK) of zoliflodacin and absorption, distribution, metabolism, and excretion (ADME) after single doses in healthy volunteers.

Funder

Entasis Therapeutics, Inc.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.01808-18

Reference18 articles.

1. Emergence of multidrug-resistant, extensively drug-resistant and untreatable gonorrhea

2. Control of Neisseria gonorrhoeae in the Era of Evolving Antimicrobial Resistance

3. US Centers for Disease Control and Prevention. 2015. Sexually transmitted diseases treatment guidelines. CDC, U.S. Department of Health and Human Services, Washington, DC.

4. World Health Organization. 2016. Guidelines for the treatment of Neisseria gonorrhoeae. WHO, Geneva, Switzerland.

5. Discovery of Novel DNA Gyrase Inhibiting Spiropyrimidinetriones: Benzisoxazole Fusion with N-Linked Oxazolidinone Substituents Leading to a Clinical Candidate (ETX0914)

Cited by 22 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. Pharmacodynamics of zoliflodacin plus doxycycline combination therapy against Neisseria gonorrhoeae in a gonococcal hollow-fiber infection model;Frontiers in Pharmacology;2023-12-07

2. An Erythrocyte Membrane‐Derived Nanosystem for Efficient Reversal of Endothelial Injury in Sepsis;Advanced Healthcare Materials;2023-11-12

3. Emerging threat of antimicrobial resistance in Neisseria gonorrhoeae: pathogenesis, treatment challenges, and potential for vaccine development;Archives of Microbiology;2023-09-09

4. Antibiotics with novel mode of action as new weapons to fight antimicrobial resistance;European Journal of Medicinal Chemistry;2023-08

5. The pit latrine paradox in low-income settings: A sanitation technology of choice or a pollution hotspot?;Science of The Total Environment;2023-06