Pleuromutilins were discovered as natural-product antibiotics in 1950. The modifications of pleuromutilin lead to the successful development of veterinary medicines such as tiamulin and valnemulin. Retapamulin became the first pleuromutilin approved for use in human skin infections. Recent advances have led to the synthesis of pleuromutilins that combine potent antibacterial activity with favorable pharmaceutical properties, and three new pleuromutilins, BC-3781, BC-3205 and BC-7013, have entered clinical trials. In this review, the key pleuromutilin derivatives, as well as related novel derivatives during 2009-2013, and its antibacterial activities, are presented. Moreover, the antibacterial and resistance mechanism are discussed.

01 Oct 2012·Journal of Clinical MicrobiologyQ2 · MEDICINE

Disk Diffusion and MIC Quality Control Ranges for BC-3205 and BC-3781, Two Novel Pleuromutilin Antibiotics

Q2 · MEDICINE

Article

Author: Sader, Helio S. ; Ivezic-Schoenfeld, Zrinka ; Paukner, Susanne ; Jones, Ronald N. ; Ross, James E.

ABSTRACT MIC and disk diffusion quality control (QC) ranges were established for two new pleuromutilin antimicrobials (BC-3205 and BC-3781) in an eight-laboratory study performed according to Clinical and Laboratory Standards Institute M23-A3 guidelines. Staphylococcus aureus ATCC 29213 and 25923, Streptococcus pneumoniae ATCC 49619, and Haemophilus influenzae ATCC 4927 strains were evaluated. The proposed QC ranges would aid clinical laboratories in testing these compounds following their development for treatment of respiratory and cutaneous infections.

01 Feb 2010·Current opinion in investigational drugs (London, England : 2000)

The pleuromutilin antibiotics: a new class for human use.

Review

Author: Shlaes, David M ; Novak, Rodger

Pleuromutilins were discovered as natural-product antibiotics in 1950. Tiamulin was the first pleuromutilin compound to be approved for veterinary use in 1979, followed by valnemulin in 1999. It was not until 2007 that retapamulin became the first pleuromutilin approved for use in humans. However, retapamulin is limited to topical application. Recent advances in lead optimization have led to the synthesis of pleuromutilins that combine potent antibacterial activity with favorable pharmaceutical properties, making these compounds suitable for oral and intravenous delivery. Most pleuromutilins have an antibacterial spectrum that spans the common pathogens involved in both skin and respiratory tract infections. Two new pleuromutilins, BC-3205 and BC-7013 (both Nabriva Therapeutics AG), have entered clinical trials. In this review, the key properties of pleuromutilin derivatives, designed primarily through modifications at the C(14) side chain, are presented, and the potential of these compounds in systemic therapy in humans is discussed.

100 Deals associated with BC-3205

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Phase 1	AT	Nabriva Therapeutics Plc	-
Complicated skin and soft tissue infection	Phase 1	AT	Nabriva Therapeutics Plc	-
Pneumonia	Phase 1	AT	Nabriva Therapeutics Plc	-

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