Valuable Targets

What are β-lactamase inhibitor and how do you quickly get the latest development progress?

14 November 2023
4 min read

β-lactamase inhibitors are a new type of β-lactam drugs, with the main ones currently in clinical use being clavulanic acid, sulbactam, and tazobactam. These three compounds have a weak antibacterial activity, or no antibacterial activity at all. However, they can inhibit the activity of β-lactamase, protecting β-lactam antibiotics from being hydrolyzed, or at least reducing this hydrolysis. This leads to a significant decrease in the minimum inhibitory concentration (MIC) of penicillins and cephalosporins, potentially enhancing the potency of these drugs several times or even by dozens. When combined with aminopenicillins, these inhibitors can restore the sensitivity to medication in various enzymatic bacterial strains such as staphylococci, streptococci, neisseria, haemophilus, coliform bacteria, klebsiella, legionella, and several pseudomonas strains among others. When used in combination with antipseudomonal penicillins like piperacillin and meropenem, bacterial strains like maltophilic pseudomonas, leuconostoc, acinetobacter, listeria, salmonella, and others can regain sensitivity. It is important to note that these inhibitors are ineffective against methicillin-resistant Staphylococcus aureus (MRSA) infections.

β-lactamase inhibitors can be divided into irreversible and reversible classes. Irreversible inhibitors include clavulanic acid, sulbactam, and tazobactam. These contain a β-lactam ring structure and work by forming a non-covalent bond complex with β-lactamase (this binding is strong and difficult to reverse), causing the enzyme to deactivate and degrade its own structure, hence they are also called suicide enzyme inhibitors or irreversible competitive enzyme inhibitors. They can inhibit most class A β-lactamases except for carbapenemases, but have no inhibitory abilities for the majority of class B, C, and D enzymes.

Reversible inhibitors include avibactam, relebactam, and vaborbactam, which do not contain a β-lactam ring structure. They reversibly bind with the active part of the bacteria's β-lactamase, their structure not being degraded in the process, thus having a long-term inhibitory effect. Avibactam and relebactam belong to the diazabicyclooctanes (DABCOs) structure, being resistant to hydrolysis, demonstrating broader-spectrum β-lactamase inhibitory effects and a reversible inhibition, capable of inhibiting Class A and C β-lactamases including carbapenemases. Avibactam can also inhibit OXA-48 in class D enzymes, but relebactam is unable to inhibit OXA-48. Vaborbactam is a boronic acid derivative, a new generation of enzyme inhibitors, which can inhibit class A and C β-lactamases including carbapenemases, but has no inhibitory effect on the class D carbapenemases including OXA-48.

How do they work?

A β-lactamase inhibitor is a type of drug that is used in combination with certain antibiotics to enhance their effectiveness against bacteria. β-lactamase is an enzyme produced by some bacteria that can break down β-lactam antibiotics, such as penicillins and cephalosporins, rendering them ineffective.

When a β-lactamase inhibitor is combined with a β-lactam antibiotic, it can inhibit the activity of the β-lactamase enzyme, allowing the antibiotic to remain active and kill the bacteria. This combination therapy is particularly useful in treating infections caused by bacteria that produce β-lactamase, as it helps to overcome antibiotic resistance.

By inhibiting the action of β-lactamase, the β-lactamase inhibitor helps to extend the spectrum of activity of the antibiotic, making it effective against a broader range of bacteria. This combination therapy is commonly used in the treatment of various bacterial infections, including respiratory tract infections, urinary tract infections, and skin infections.

Overall, a β-lactamase inhibitor is a valuable tool in combating antibiotic resistance and improving the efficacy of β-lactam antibiotics by preventing the breakdown of these drugs by β-lactamase enzymes produced by bacteria.

List of β-lactamase Inhibitors

The currently marketed β-lactamase inhibitors include:

For more information, please click on the image below.

图形用户界面, 应用程序

描述已自动生成What are β-lactamase inhibitors used for?

β-lactamase inhibitors is commonly used in the treatment of various bacterial infections, including respiratory tract infections, urinary tract infections, and skin infections. For more information, please click on the image below to log in and search.

表格

中度可信度描述已自动生成How to obtain the latest development progress of β-lactamase inhibitors?

In the Synapse database, you can keep abreast of the latest research and development advances of β-lactamase inhibitors anywhere and anytime, daily or weekly, through the "Set Alert" function. Click on the image below to embark on a brand new journey of drug discovery!

图形用户界面, 文本, 应用程序

描述已自动生成

图形用户界面, 应用程序

描述已自动生成

Get a sneak peek at clinical results for ASH2023! New ASH2023 clinical results updated on the Synapse database
Feature Updates
3 min read
Get a sneak peek at clinical results for ASH2023! New ASH2023 clinical results updated on the Synapse database
14 November 2023
New data from the 2023 ASH conference is now available on the Clinical Results section of the Synapse database.
Read →
MoonLake Immunotherapeutics reveals significant outcomes from Phase 2 trials of the Nanobody® medication, sonelokimab, for ongoing psoriatic arthritis
Latest Hotspot
4 min read
MoonLake Immunotherapeutics reveals significant outcomes from Phase 2 trials of the Nanobody® medication, sonelokimab, for ongoing psoriatic arthritis
14 November 2023
MoonLake Immunotherapeutics, a clinical-stage biotech firm, announced encouraging preliminary results from its global Phase 2 ARGO trial. This trial evaluated the efficacy and safety of Nanobody® sonelokimab in patients with active psoriatic arthritis.
Read →
What are Bcl-2 inhibitors and how do you quickly get the latest development progress?
What are Bcl-2 inhibitors and how do you quickly get the latest development progress?
14 November 2023
The overexpression of BCL-2 protein allows tumor cells to evade apoptosis and to become resistant to a variety of anti-tumor drugs. Bcl-2 inhibitors are a new type of anti-cancer drug developed to target the mechanism of apoptosis, promoting cell death.
Read →
SL-172154: Brief Review of its R&D Progress and the Clinical Result in 2023 ASH
5 min read
SL-172154: Brief Review of its R&D Progress and the Clinical Result in 2023 ASH
14 November 2023
At ASH 2023, results of SL-172154 as a single agent and with Azacitidine for relapsed/refractory AML and HR-MDS will be presented, highlighting its safety, pharmacodynamics, and anti-tumor effects.
Read →
Get started for free today!
Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.
Start your data trial now!
Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.