NXL-103, a combination of flopristin and linopristin, for the potential treatment of bacterial infections including community-acquired pneumonia and MRSA

Amani Politano, Robert G. Sawyer

Research output: Contribution to journalReview article

18 Citations (Scopus)

Abstract

Novexel is developing the novel, orally active, semisynthetic streptogramin NXL-103, which has potential therapeutic application in the treatment of community-acquired pneumonia, community- or hospital-acquired MRSA, vancomycin-resistant enterococcus, and acute bacterial skin and soft tissue infections. NXL-103 is a combination of streptogramin A:streptogramin B components, initially developed in a 70:30 dose ratio. In multiple in vitro studies, NXL-103 demonstrated potent activity against different types of bacteria, such as Staphylococcus aureus (including MRSA), Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecium, Enterococcus faecalis, Haemophilus influenzae and Haemophilus parainfluenzae. NXL-103 was not affected by the resistance profiles of bacteria against other commonly used antibiotics. In phase I clinical trials, NXL-103 achieved bactericidal levels in plasma and was generally well tolerated, with side effects primarily on the gastrointestinal system. The first phase II trial conducted to evaluate the efficacy of NXL-103 against community-acquired pneumonia revealed that the compound was comparable with amoxicillin. NXL-103 has promise to become an important agent in the treatment of community-acquired pneumonia and complex skin and soft tissue infections, pending further development.

Original languageEnglish (US)
Pages (from-to)225-236
Number of pages12
JournalCurrent Opinion in Investigational Drugs
Volume11
Issue number2
StatePublished - Feb 1 2010
Externally publishedYes

Fingerprint

Methicillin-Resistant Staphylococcus aureus
Bacterial Infections
Pneumonia
Soft Tissue Infections
Streptogramin A
Streptogramin B
Haemophilus parainfluenzae
Streptogramins
Bacteria
Enterococcus faecium
Skin
Clinical Trials, Phase I
Enterococcus faecalis
Streptococcus pyogenes
Amoxicillin
Community Hospital
Haemophilus influenzae
Streptococcus pneumoniae
linopristin drug combination flopristin
Staphylococcus aureus

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

Cite this

@article{0989b89f2c6e41b7b349d8b30a415787,
title = "NXL-103, a combination of flopristin and linopristin, for the potential treatment of bacterial infections including community-acquired pneumonia and MRSA",
abstract = "Novexel is developing the novel, orally active, semisynthetic streptogramin NXL-103, which has potential therapeutic application in the treatment of community-acquired pneumonia, community- or hospital-acquired MRSA, vancomycin-resistant enterococcus, and acute bacterial skin and soft tissue infections. NXL-103 is a combination of streptogramin A:streptogramin B components, initially developed in a 70:30 dose ratio. In multiple in vitro studies, NXL-103 demonstrated potent activity against different types of bacteria, such as Staphylococcus aureus (including MRSA), Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecium, Enterococcus faecalis, Haemophilus influenzae and Haemophilus parainfluenzae. NXL-103 was not affected by the resistance profiles of bacteria against other commonly used antibiotics. In phase I clinical trials, NXL-103 achieved bactericidal levels in plasma and was generally well tolerated, with side effects primarily on the gastrointestinal system. The first phase II trial conducted to evaluate the efficacy of NXL-103 against community-acquired pneumonia revealed that the compound was comparable with amoxicillin. NXL-103 has promise to become an important agent in the treatment of community-acquired pneumonia and complex skin and soft tissue infections, pending further development.",
author = "Amani Politano and Sawyer, {Robert G.}",
year = "2010",
month = "2",
day = "1",
language = "English (US)",
volume = "11",
pages = "225--236",
journal = "Current Opinion in Investigational Drugs",
issn = "1472-4472",
publisher = "Current Drugs Ltd.",
number = "2",

}

TY - JOUR

T1 - NXL-103, a combination of flopristin and linopristin, for the potential treatment of bacterial infections including community-acquired pneumonia and MRSA

AU - Politano, Amani

AU - Sawyer, Robert G.

PY - 2010/2/1

Y1 - 2010/2/1

N2 - Novexel is developing the novel, orally active, semisynthetic streptogramin NXL-103, which has potential therapeutic application in the treatment of community-acquired pneumonia, community- or hospital-acquired MRSA, vancomycin-resistant enterococcus, and acute bacterial skin and soft tissue infections. NXL-103 is a combination of streptogramin A:streptogramin B components, initially developed in a 70:30 dose ratio. In multiple in vitro studies, NXL-103 demonstrated potent activity against different types of bacteria, such as Staphylococcus aureus (including MRSA), Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecium, Enterococcus faecalis, Haemophilus influenzae and Haemophilus parainfluenzae. NXL-103 was not affected by the resistance profiles of bacteria against other commonly used antibiotics. In phase I clinical trials, NXL-103 achieved bactericidal levels in plasma and was generally well tolerated, with side effects primarily on the gastrointestinal system. The first phase II trial conducted to evaluate the efficacy of NXL-103 against community-acquired pneumonia revealed that the compound was comparable with amoxicillin. NXL-103 has promise to become an important agent in the treatment of community-acquired pneumonia and complex skin and soft tissue infections, pending further development.

AB - Novexel is developing the novel, orally active, semisynthetic streptogramin NXL-103, which has potential therapeutic application in the treatment of community-acquired pneumonia, community- or hospital-acquired MRSA, vancomycin-resistant enterococcus, and acute bacterial skin and soft tissue infections. NXL-103 is a combination of streptogramin A:streptogramin B components, initially developed in a 70:30 dose ratio. In multiple in vitro studies, NXL-103 demonstrated potent activity against different types of bacteria, such as Staphylococcus aureus (including MRSA), Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecium, Enterococcus faecalis, Haemophilus influenzae and Haemophilus parainfluenzae. NXL-103 was not affected by the resistance profiles of bacteria against other commonly used antibiotics. In phase I clinical trials, NXL-103 achieved bactericidal levels in plasma and was generally well tolerated, with side effects primarily on the gastrointestinal system. The first phase II trial conducted to evaluate the efficacy of NXL-103 against community-acquired pneumonia revealed that the compound was comparable with amoxicillin. NXL-103 has promise to become an important agent in the treatment of community-acquired pneumonia and complex skin and soft tissue infections, pending further development.

UR - http://www.scopus.com/inward/record.url?scp=77649133971&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=77649133971&partnerID=8YFLogxK

M3 - Review article

C2 - 20112172

AN - SCOPUS:77649133971

VL - 11

SP - 225

EP - 236

JO - Current Opinion in Investigational Drugs

JF - Current Opinion in Investigational Drugs

SN - 1472-4472

IS - 2

ER -