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Development Status

Investigational

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Primary Target

Penicillin-binding protein 1B

2

UDP-N-acetylglucosamine--N-acetylmuramyl-(pentapeptide) pyrophosphoryl-undecaprenol N-acetylglucosamine transferase

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Approval Year

Unknown

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Originator

Gruppo Lepetit S.p.A.

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Mixture

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FDA UNII

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Showing 1 - 2 of 2 results

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RAMOPLANIN

0WX9996O2G

Status:

Investigational

Class:

MIXTURE

Targets:

UDP-N-acetylglucosamine--N-acetylmuramyl-(pentapeptide) pyrophosphoryl-undecaprenol N-acetylglucosamine transferase

Penicillin-binding protein 1B

Ramoplanin is a glycolipodepsipeptide antibiotic obtained from the fermentation of Actinoplanes sp. ATCC 33076 that exhibits activity against clinically important multi-drug-resistant, Gram-positive pathogens including vancomycin-resistant Enterococc...

us (VRE), methicillin-resistant Staphylococcus aureus (MRSA), and vancomycin-intermediate resistant Clostridium difficile. Ramoplanin was first isolated as a complex of three closely related components A1, A2, and A3. Preclinical studies have also demonstrated that ramoplanin exerts a rapid bactericidal effect on S. aureus biofilms and that a clinical vancomycin-resistant S. aureus strain containing the vanA gene was susceptible to ramoplanin. Ramoplanin blocks bacterial cell wall biosynthesis by interfering with peptidoglycan production. Ramoplanin inhibits the N-acetylglucosaminyltransferase-catalysed conversion of lipid intermediate I to lipid intermediate II, a step that occurs before the transglycosylation and transpeptidation reactions. Ramoplanin’s mechanism of action is distinct from that of glycopeptides. Unlike glycopeptides, ramoplanin does not complex with the D-Ala–D-Ala sequence of cell wall precursors. Ramoplanin is being developed for the targeted prophylaxis of recently treated patients with C. difficile infection (CDI) at high risk for infection relapse. Twelve Phase I studies, two Phase II studies (one in CDI and one in VRE) as well as one Phase III study (in VRE) have been conducted

RAMOPLANIN DIHYDROCHLORIDE

3W6BAN6R4E

Status:

Investigational

Class:

MIXTURE

Targets:

UDP-N-acetylglucosamine--N-acetylmuramyl-(pentapeptide) pyrophosphoryl-undecaprenol N-acetylglucosamine transferase

Penicillin-binding protein 1B

Ramoplanin is a glycolipodepsipeptide antibiotic obtained from the fermentation of Actinoplanes sp. ATCC 33076 that exhibits activity against clinically important multi-drug-resistant, Gram-positive pathogens including vancomycin-resistant Enterococc...

us (VRE), methicillin-resistant Staphylococcus aureus (MRSA), and vancomycin-intermediate resistant Clostridium difficile. Ramoplanin was first isolated as a complex of three closely related components A1, A2, and A3. Preclinical studies have also demonstrated that ramoplanin exerts a rapid bactericidal effect on S. aureus biofilms and that a clinical vancomycin-resistant S. aureus strain containing the vanA gene was susceptible to ramoplanin. Ramoplanin blocks bacterial cell wall biosynthesis by interfering with peptidoglycan production. Ramoplanin inhibits the N-acetylglucosaminyltransferase-catalysed conversion of lipid intermediate I to lipid intermediate II, a step that occurs before the transglycosylation and transpeptidation reactions. Ramoplanin’s mechanism of action is distinct from that of glycopeptides. Unlike glycopeptides, ramoplanin does not complex with the D-Ala–D-Ala sequence of cell wall precursors. Ramoplanin is being developed for the targeted prophylaxis of recently treated patients with C. difficile infection (CDI) at high risk for infection relapse. Twelve Phase I studies, two Phase II studies (one in CDI and one in VRE) as well as one Phase III study (in VRE) have been conducted

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