{"id":4157,"date":"2021-12-29T17:49:29","date_gmt":"2021-12-29T17:49:29","guid":{"rendered":"https:\/\/biotechsa.com\/2\/?p=4157"},"modified":"2026-03-10T13:01:24","modified_gmt":"2026-03-10T19:01:24","slug":"new-resistance-busting-antibiotic-combination-could-extend-the-use-of-last-resort-antibiotics","status":"publish","type":"post","link":"https:\/\/biotechsa.com\/2\/noticias\/new-resistance-busting-antibiotic-combination-could-extend-the-use-of-last-resort-antibiotics\/","title":{"rendered":"New resistance-busting antibiotic combination could extend the use of ‘last-resort’ antibiotics"},"content":{"rendered":"\n
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Science Daily recently published an article on the discovery of a class of enzyme blockers called indole carboxylates that have the potential to extend and protect the efficacy of vital \u201clast-resort\u201d antibiotics called carbapenems. Carbapenems are a class of antibiotics often used to treat \u201cserious, multi-drug resistant infections when other antibiotics, such as penicillin, have failed.\u201d These drugs work by blocking the formation of new cell walls during multiplication, which kills bacteria. However, some bacteria have developed the ability to survive this treatment by producing metallo-beta-lactamases (MBL) enzymes that break down carbapenem antibiotics and render them ineffective.<\/p>\n

The Ineos Oxford Institute (IOI) for Antimicrobial research collaborated with several institutes across Europe to screen and test \u201chundreds of thousands\u201d of chemicals that could inhibit MBL\u2019s that lead to resistance in bacteria that cause conditions such as sepsis, pneumonia and UTIs. Using a process called crystallography, scientists found that indole carboxylates interact with MBL\u2019s using a \u201cTrojan Horse\u201d method that imitates antibiotics and allows them to attach to MBL enzymes to inactivate them. After this initial discovery, researchers engineered the drug to make it as effective as possible and ran both in-vitro and mice experiments. They found that this potential new drug in combination with carbapenems was \u201c5 times more potent at treating severe bacterial infections than carbapenems alone, and at a less concentrated dose.\u201d<\/p>\n

Currently there is no licensed drug that targets MBL\u2019s and only one in clinical trials; and with antimicrobial resistance-related deaths projected to overtake the number of annual cancer-related deaths by the year 2050, there is an urgent need to find treatments that overcome resistance and preserve these vital antibiotics. Professor Christopher Schofield, Academic Lead of the study encourages that his team is \u201cactively progressing this new drug type towards clinical trials in people, most importantly in lower and middle income countries where resistance to carbapenem antibiotics is widespread.\u201d<\/p>\n

Click here to read the full article.<\/a><\/p>\n

December 2021<\/p>\n

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TRADUCCI\u00d3N DE GOOGLE:<\/span><\/strong><\/p>\n

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Una nueva combinaci\u00f3n de antibi\u00f3ticos que destruyen la resistencia podr\u00eda extender el uso de antibi\u00f3ticos de ‘\u00faltimo recurso’<\/h3>\n

Science Daily public\u00f3 recientemente un art\u00edculo sobre el descubrimiento de una clase de bloqueadores enzim\u00e1ticos llamados indol carboxilatos que tienen el potencial de extender y proteger la eficacia de antibi\u00f3ticos vitales de \u201c\u00faltimo recurso\u201d llamados carbapen\u00e9micos. Los carbapen\u00e9micos son una clase de antibi\u00f3ticos que a menudo se utilizan para tratar “infecciones graves resistentes a m\u00faltiples f\u00e1rmacos cuando otros antibi\u00f3ticos, como la penicilina, han fallado”. Estos medicamentos act\u00faan bloqueando la formaci\u00f3n de nuevas paredes celulares durante la multiplicaci\u00f3n, lo que mata las bacterias. Sin embargo, algunas bacterias han desarrollado la capacidad de sobrevivir a este tratamiento al producir enzimas metalo-beta-lactamasas (MBL) que descomponen los antibi\u00f3ticos carbapen\u00e9micos y los vuelven ineficaces.<\/p>\n

El Instituto Ineos Oxford (IOI) de investigaci\u00f3n antimicrobiana colabor\u00f3 \u200b\u200bcon varios institutos de Europa para detectar y probar “cientos de miles” de sustancias qu\u00edmicas que podr\u00edan inhibir las MBL que provocan resistencia en las bacterias que causan afecciones como sepsis, neumon\u00eda e infecciones urinarias. Usando un proceso llamado cristalograf\u00eda, los cient\u00edficos encontraron que los carboxilatos de indol interact\u00faan con MBL usando un m\u00e9todo de “caballo de Troya” que imita a los antibi\u00f3ticos y les permite unirse a las enzimas MBL para inactivarlos. Despu\u00e9s de este descubrimiento inicial, los investigadores dise\u00f1aron el f\u00e1rmaco para hacerlo lo m\u00e1s eficaz posible y realizaron experimentos tanto in vitro como con ratones. Descubrieron que este nuevo f\u00e1rmaco potencial en combinaci\u00f3n con carbapen\u00e9micos era “5 veces m\u00e1s potente para tratar infecciones bacterianas graves que los carbapen\u00e9micos solos, y en una dosis menos concentrada”.<\/p>\n

Actualmente no existe ning\u00fan f\u00e1rmaco con licencia que se dirija a las MBL y solo uno se encuentra en ensayos cl\u00ednicos; y dado que se prev\u00e9 que las muertes relacionadas con la resistencia a los antimicrobianos superen el n\u00famero de muertes anuales relacionadas con el c\u00e1ncer para el a\u00f1o 2050, existe una necesidad urgente de encontrar tratamientos que superen la resistencia y preserven estos antibi\u00f3ticos vitales. El profesor Christopher Schofield, l\u00edder acad\u00e9mico del estudio, alienta que su equipo est\u00e1 “progresando activamente con este nuevo tipo de f\u00e1rmaco hacia ensayos cl\u00ednicos en personas, sobre todo en pa\u00edses de ingresos bajos y medios donde la resistencia a los antibi\u00f3ticos carbapen\u00e9micos est\u00e1 generalizada”.<\/p>\n

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Haga clic aqu\u00ed para ver este art\u00edculo.<\/a><\/p>\n

Diciembre de 2021<\/p>\n

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