Combination comprising zidovudine and a carbapenem
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Publication Number
US-10888575-B2
Publication Date
2021-01-12
Expiration Date
Abstract
The invention provides a combination comprising zidovudine or a pharmaceutically acceptable derivative thereof and a carbapenem or a pharmaceutically acceptable derivative thereof, optionally with a polymyxin selected from polymyxin E and polymyxin or a pharmaceutically acceptable derivative thereof. This combination is particularly useful for the treatment of microbial infections.
Core Innovation
The described invention provides a synergistic antimicrobial combination that comprises zidovudine or a pharmaceutically acceptable derivative and a carbapenem. The combination optionally further comprises at least one polymyxin selected from polymyxin B or polymyxin E, including polymyxin E/colistin, with examples including colistimethate sodium.
The described problem being solved is treatment of microbial infections, especially Gram-negative infections, including drug-resistant and carbapenemase-resistant infections, by killing multiplying and/or clinically latent microorganisms. The document further frames clinically latent microorganisms and emphasizes clinically relevant drug-resistant Gram-negative bacteria, including NDM-1 carbapenemase-resistant Enterobacteriaceae, with examples such as NDM-1 Escherichia coli and NDM-1 Klebsiella pneumoniae.
The core inventive support in the description is the claimed synergistic antimicrobial activity of zidovudine plus a carbapenem and, optionally, a polymyxin, using chequerboard and time-kill approaches. Synergy is supported using chequerboard (fractional inhibitory concentration index, FICI) with a stated synergy threshold (ΣFICI ≤ 0.5), and time-kill synergy is reported.
The described embodiments also include formulation and administration discussion for the antimicrobial combinations, and chemical structure depictions for zidovudine and other components, including the carbapenem core and an example polymyxin or colistin. The invention is directed to pharmaceutical combinations and compositions for treating microbial infections by administering zidovudine in combination with a carbapenem, optionally further comprising a polymyxin and pharmaceutically acceptable salts or solvates.
Claims Coverage
The document contains three independent claims covering a drug combination, a treatment method, and a pharmaceutical composition. Across the independent claims, the core inventive features include zidovudine combined with a carbapenem, optionally with a polymyxin.
Zidovudine plus carbapenem combination with optional polymyxin
A combination comprising zidovudine or a pharmaceutically acceptable salt and/or solvate thereof and a carbapenem or a pharmaceutically acceptable salt and/or solvate thereof, wherein the combination optionally further comprises at least one polymyxin selected from polymyxin B or polymyxin E, or at least one pharmaceutically acceptable salt and/or solvate thereof.
Administering zidovudine with carbapenem to treat microbial infection with optional polymyxin
A method for treating a microbial infection which comprises administering to a mammal, including man, zidovudine or a pharmaceutically acceptable salt and/or solvate thereof in combination with a carbapenem or a pharmaceutically acceptable salt and/or solvate thereof, optionally with a polymyxin selected from polymyxin E and polymyxin B, or a pharmaceutically acceptable salt and/or solvate thereof.
Pharmaceutical composition of zidovudine and carbapenem with optional polymyxin and adjuvant, diluent or carrier
A pharmaceutical composition comprising zidovudine or a pharmaceutically acceptable salt and/or solvate thereof in combination with a carbapenem or a pharmaceutically acceptable salt and/or solvate thereof, wherein the pharmaceutical composition optionally further comprises at least one polymyxin selected from polymyxin B or polymyxin E, or at least one pharmaceutically acceptable salt and/or solvate thereof, and wherein the pharmaceutical composition contains a pharmaceutically acceptable adjuvant, diluent or carrier.
Overall, the independent claim set consistently covers zidovudine combined with a carbapenem, optionally further including a polymyxin selected from polymyxin B or polymyxin E, expressed as a combination, an administration method for treating microbial infection in a mammal, or as a pharmaceutical composition including an adjuvant, diluent or carrier.
Stated Advantages
Synergistic antimicrobial activity using chequerboard and time-kill approaches.
Treatment of Gram-negative microbial infections, including drug-resistant and carbapenemase-resistant infections, by killing multiplying and/or clinically latent microorganisms.
Documented Applications
Treating a microbial infection in a mammal, including man, by administering zidovudine in combination with a carbapenem, optionally with a polymyxin.
Treating Gram-negative infections, including drug-resistant and NDM-1 carbapenemase-resistant Enterobacteriaceae such as NDM-1 Escherichia coli and NDM-1 Klebsiella pneumoniae.
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