Date: 2014-09-08
Type of information: Presentation of results at a congress
phase:
Announcement: presentation of results at the 54th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) in Washington DC
Company: Nabriva Therapeutics (Austria)
Product: lefamulin (BC 3781 - Acetic acid, 2-(((1R,2R,4R)-4-amino-2-hydroxycyclohexyl)thio)-, (3aS,4R,5S,6S,8R,9R,9aR,10R)-6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3ah-cyclopentacycloocten-8-yl ester)
Action
mechanism: antibioctic/pleuromulin derivative. Lefamulin (BC 3781) belongs to the first generation of pleuromutilins to combine excellent systemic bioavailability with substantial activity against Gram-positive pathogens, and fastidious Gram-negative pathogens plus atypical pathogens. Pleuromutilins interfere with bacterial protein synthesis via a specific interaction with the 23S rRNA of the 50S bacterial ribosome subunit. These antibacterials have a distinct anti-bacterial profile. Their unique mechanism of action implies a very low probability of cross resistance with other antibacterials. In an industry first, Nabriva\'s world class medicinal chemistry expertise achieved the development of intravenous and orally available pleuromutilins clearing the way for i.v. and oral therapy with this antibiotic class. This achievement constitutes a significant milestone in providing appropriate medication for the treatment of life-threatening bacterial infections offering a distinctly different class of antibiotics for the treatment of bacterial diseases. Lefamulin is highly active against multi-drug resistant (MDR) pathogens including Methicillin resistant Staphylococcus aureus (MRSA), MDR Streptococcus pneumoniae, Vancomycin resistant Enterococcus faecium.
Disease:
Therapeutic area: Infectious diseases
Country:
Trial details:
Latest
news: * On September 8, 2014, Nabriva Therapeutics, a biotechnology company focused on developing pleuromutilins, a new class of antibiotics for treatment of serious infections caused by resistant pathogens, announced the presentation of a poster on BC 3781, a novel pleuromutilin antibiotic which is being developed for oral and intravenous administration for the treatment of severe infections, at the 54th Interscience Conference on Antimicrobial Agents and Chemotherapy in Washington. The study examines the pharmacokinetics (PK) of BC-3781 in the epithelial lining fluid in comparison to the plasma. Since knowledge of the PK at the site of infection is crucial in the development of antibiotics, for the treatment of respiratory tract infections such as community- and hospital-acquired bacterial pneumonia (CABP & HABP) drug penetration into the pulmonary epithelial lining fluid (ELF) is a pre-requisite. The study, whereby BC-3781 was administered to 12 healthy male subjects, was safe and well tolerated and there were no clinically relevant changes in laboratory values. Main conclusions found were that after a single intravenous dose of BC-3781, exposure levels in ELF were comparable to total plasma levels and considerably exceeded free plasma levels. The individual BC-3781 concentration levels in ELF equilibrated with the plasma rapidly after the end of infusion.
