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Lefamulin, sold under the brand name Xenleta, is an
antibiotic An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting pathogenic bacteria, bacterial infections, and antibiotic medications are widely used in the therapy, ...
medication used it to treat adults with community-acquired bacterial
pneumonia Pneumonia is an inflammatory condition of the lung primarily affecting the small air sacs known as alveoli. Symptoms typically include some combination of productive or dry cough, chest pain, fever, and difficulty breathing. The severi ...
. It is taken by mouth or by injection into a vein. Relatively common side effects include diarrhea, nausea, pain at the site of injection, and liver inflammation. It is a
pleuromutilin antibiotic Pleuromutilin and its derivatives are antibacterial drugs that inhibit protein synthesis in bacteria by binding to the peptidyl transferase component of the 50S subunit of ribosomes. This class of antibiotics includes the licensed drugs lefamu ...
that inhibits the
large subunit In structural biology, a protein subunit is a polypeptide chain or single protein molecule that assembles (or "''coassembles''") with others to form a protein complex. Large assemblies of proteins such as viruses often use a small number of ty ...
of bacterial ribosomes. Lefamulin was approved for medical use in the United States in August 2019, and in the European Union in July 2020.


Medical uses

Lefamulin is used to treat adults with community-acquired bacterial
pneumonia Pneumonia is an inflammatory condition of the lung primarily affecting the small air sacs known as alveoli. Symptoms typically include some combination of productive or dry cough, chest pain, fever, and difficulty breathing. The severi ...
. It was also investigated for treatment of
acute bacterial skin and skin-structure infection Skin and skin structure infections (SSSIs), also referred to as skin and soft tissue infections (SSTIs), or acute bacterial skin and skin structure infections (ABSSSIs), are infections of skin and associated soft tissues (such as loose connective ti ...
s (ABSSSI).


Spectrum of activity

Lefamulin has ''
in vitro ''In vitro'' (meaning in glass, or ''in the glass'') studies are performed with microorganisms, cells, or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in biology and ...
'' activity against ''
Streptococcus pneumoniae ''Streptococcus pneumoniae'', or pneumococcus, is a Gram-positive, spherical bacteria, alpha-hemolytic (under aerobic conditions) or beta-hemolytic (under anaerobic conditions), aerotolerant anaerobic member of the genus Streptococcus. They a ...
'', '' viridans group Streptococci'', ''
Moraxella catarrhalis ''Moraxella catarrhalis'' is a fastidious, nonmotile, Gram-negative, aerobic, oxidase-positive diplococcus that can cause infections of the respiratory system, middle ear, eye, central nervous system, and joints of humans. It causes the i ...
'', ''
Enterococcus faecium ''Enterococcus faecium'' is a Gram-positive, gamma-hemolytic or non- hemolytic bacterium in the genus '' Enterococcus''. It can be commensal (innocuous, coexisting organism) in the gastrointestinal tract of humans and animals, but it may als ...
'', methicillin-resistant ''Staphylococcus aureus'' (MRSA), among other bacteria.


History

It was developed by Nabriva Therapeutics and approved in the United States in 2019. It was granted
fast track The fast track is an informal English term meaning "the quickest and most direct route to achievement of a goal, as in competing for professional advancement". By definition, it implies that a less direct, slower route also exists. Fast track or F ...
status by the US
Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food ...
(FDA) in 2014. Although pleuromutilin antibiotics were first developed in the 1950s, lefamulin is the first to be used for systemic treatment of bacterial infections in humans.


Society and culture


Legal status

Lefamulin was approved for medical use in the United States in August 2019, and in the European Union in July 2020.


References


External links

* Pleuromutilin antibiotics Vinyl compounds {{antibiotic-stub