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Literature DB >> 28893785

In Vitro Activity of the Novel Pleuromutilin Lefamulin (BC-3781) and Effect of Efflux Pump Inactivation on Multidrug-Resistant and Extensively Drug-Resistant Neisseria gonorrhoeae.

Susanne Jacobsson¹, Susanne Paukner², Daniel Golparian¹, Jörgen S Jensen³, Magnus Unemo⁴.

Abstract

We evaluated the activity of the novel semisynthetic pleuromutilin lefamulin, inhibiting protein synthesis and growth, and the effect of efflux pump inactivation on clinical gonococcal isolates and reference strains (n = 251), including numerous multidrug-resistant and extensively drug-resistant isolates. Lefamulin showed potent activity against all gonococcal isolates, and no significant cross-resistance to other antimicrobials was identified. Further studies of lefamulin are warranted, including in vitro selection and mechanisms of resistance, pharmacokinetics/pharmacodynamics, optimal dosing, and performance in randomized controlled trials.

Entities: Disease

Keywords: MtrCDE efflux pump; antimicrobial resistance; gonorrhea; pleuromutilin; treatment

Mesh：

Substances：

Year: 2017 PMID： 28893785 PMCID： PMC5655042 DOI： 10.1128/AAC.01497-17

Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN： 0066-4804 Impact factor: 5.191

19 in total

1. Antimicrobial activity of the novel pleuromutilin antibiotic BC-3781 against organisms responsible for community-acquired respiratory tract infections (CARTIs).

Authors: Helio S Sader; Susanne Paukner; Zrinka Ivezic-Schoenfeld; Douglas J Biedenbach; Franz J Schmitz; Ronald N Jones
Journal: J Antimicrob Chemother Date: 2012-01-27 Impact factor: 5.790

2. Importance of multidrug efflux pumps in the antimicrobial resistance property of clinical multidrug-resistant isolates of Neisseria gonorrhoeae.

Authors: Daniel Golparian; William M Shafer; Makoto Ohnishi; Magnus Unemo
Journal: Antimicrob Agents Chemother Date: 2014-04-14 Impact factor: 5.191

3. Is Neisseria gonorrhoeae initiating a future era of untreatable gonorrhea?: detailed characterization of the first strain with high-level resistance to ceftriaxone.

Authors: Makoto Ohnishi; Daniel Golparian; Ken Shimuta; Takeshi Saika; Shinji Hoshina; Kazuhiro Iwasaku; Shu-ichi Nakayama; Jo Kitawaki; Magnus Unemo
Journal: Antimicrob Agents Chemother Date: 2011-05-16 Impact factor: 5.191

4. Failure of Dual Antimicrobial Therapy in Treatment of Gonorrhea.

Authors: Helen Fifer; Usha Natarajan; Lucy Jones; Sarah Alexander; Gwenda Hughes; Daniel Golparian; Magnus Unemo
Journal: N Engl J Med Date: 2016-06-23 Impact factor: 91.245

5. Antimicrobial activity of the pleuromutilin antibiotic BC-3781 against bacterial pathogens isolated in the SENTRY antimicrobial surveillance program in 2010.

Authors: Susanne Paukner; Helio S Sader; Zrinka Ivezic-Schoenfeld; Ronald N Jones
Journal: Antimicrob Agents Chemother Date: 2013-07-08 Impact factor: 5.191

6. High-level cefixime- and ceftriaxone-resistant Neisseria gonorrhoeae in France: novel penA mosaic allele in a successful international clone causes treatment failure.

Authors: Magnus Unemo; Daniel Golparian; Robert Nicholas; Makoto Ohnishi; Anne Gallay; Patrice Sednaoui
Journal: Antimicrob Agents Chemother Date: 2011-12-12 Impact factor: 5.191

7. Phase II clinical study of BC-3781, a pleuromutilin antibiotic, in treatment of patients with acute bacterial skin and skin structure infections.

Authors: W T Prince; Z Ivezic-Schoenfeld; C Lell; K J Tack; R Novak; F Obermayr; G H Talbot
Journal: Antimicrob Agents Chemother Date: 2013-02-19 Impact factor: 5.191

8. Phenotypic and genetic characterization of the 2008 WHO Neisseria gonorrhoeae reference strain panel intended for global quality assurance and quality control of gonococcal antimicrobial resistance surveillance for public health purposes.

Authors: Magnus Unemo; Oskar Fasth; Hans Fredlund; Athena Limnios; John Tapsall
Journal: J Antimicrob Chemother Date: 2009-03-24 Impact factor: 5.790

9. Molecular characterization of two high-level ceftriaxone-resistant Neisseria gonorrhoeae isolates detected in Catalonia, Spain.

Authors: Jordi Cámara; Judit Serra; Josefina Ayats; Teresa Bastida; Dolors Carnicer-Pont; Antònia Andreu; Carmen Ardanuy
Journal: J Antimicrob Chemother Date: 2012-05-07 Impact factor: 5.790

10. A novel pleuromutilin antibacterial compound, its binding mode and selectivity mechanism.

Authors: Zohar Eyal; Donna Matzov; Miri Krupkin; Susanne Paukner; Rosemarie Riedl; Haim Rozenberg; Ella Zimmerman; Anat Bashan; Ada Yonath
Journal: Sci Rep Date: 2016-12-13 Impact factor: 4.379

17 in total

Review 1. Leave it to Lefamulin: A Pleuromutilin Treatment Option in Community-Acquired Bacterial Pneumonia.

Authors: Young Ran Lee; Katy Louise Jacobs
Journal: Drugs Date: 2019-11 Impact factor: 9.546

2. Low Prevalence of Gram-Positive Isolates Showing Elevated Lefamulin MIC Results during the SENTRY Surveillance Program for 2015-2016 and Characterization of Resistance Mechanisms.

Authors: Rodrigo E Mendes; Susanne Paukner; Timothy B Doyle; Steven P Gelone; Robert K Flamm; Helio S Sader
Journal: Antimicrob Agents Chemother Date: 2019-03-27 Impact factor: 5.191

3. In Vitro Activity of Lefamulin against Sexually Transmitted Bacterial Pathogens.

Authors: Susanne Paukner; Astrid Gruss; Jørgen Skov Jensen
Journal: Antimicrob Agents Chemother Date: 2018-04-26 Impact factor: 5.191

Review 4. Optimising treatments for sexually transmitted infections: surveillance, pharmacokinetics and pharmacodynamics, therapeutic strategies, and molecular resistance prediction.

Authors: Arlene C Seña; Laura Bachmann; Christine Johnston; Teodora Wi; Kimberly Workowski; Edward W Hook; Jane S Hocking; George Drusano; Magnus Unemo
Journal: Lancet Infect Dis Date: 2020-06-19 Impact factor: 25.071

Review 5. World Health Organization Global Gonococcal Antimicrobial Surveillance Program (WHO GASP): review of new data and evidence to inform international collaborative actions and research efforts.

Authors: Magnus Unemo; Monica M Lahra; Michelle Cole; Patricia Galarza; Francis Ndowa; Irene Martin; Jo-Anne R Dillon; Pilar Ramon-Pardo; Gail Bolan; Teodora Wi
Journal: Sex Health Date: 2019-09 Impact factor: 2.706

Review 6. Ten decadal advances in fungal biology leading towards human well-being.

Authors: Ausana Mapook; Kevin D Hyde; Khadija Hassan; Blondelle Matio Kemkuignou; Adéla Čmoková; Frank Surup; Eric Kuhnert; Pathompong Paomephan; Tian Cheng; Sybren de Hoog; Yinggai Song; Ruvishika S Jayawardena; Abdullah M S Al-Hatmi; Tokameh Mahmoudi; Nadia Ponts; Lena Studt-Reinhold; Florence Richard-Forget; K W Thilini Chethana; Dulanjalee L Harishchandra; Peter E Mortimer; Huili Li; Saisamorm Lumyong; Worawoot Aiduang; Jaturong Kumla; Nakarin Suwannarach; Chitrabhanu S Bhunjun; Feng-Ming Yu; Qi Zhao; Doug Schaefer; Marc Stadler
Journal: Fungal Divers Date: 2022-09-15 Impact factor: 24.902