{"id":1152,"date":"2025-10-23T20:35:35","date_gmt":"2025-10-23T19:35:35","guid":{"rendered":"https:\/\/microregistrar.com\/?p=1152"},"modified":"2025-10-23T20:35:37","modified_gmt":"2025-10-23T19:35:37","slug":"beta-lactamase-inhibitors","status":"publish","type":"post","link":"https:\/\/microregistrar.com\/?p=1152","title":{"rendered":"Beta-lactamase inhibitors"},"content":{"rendered":"\n

Clavams (Classical \u03b2-lactam-structured inhibitors)<\/h2>\n\n\n\n
Inhibitor<\/th>Structure type<\/th>Mechanism<\/th>Effective vs \u03b2-lactamase class<\/th>Unique features<\/th><\/tr><\/thead>
Clavulanic acid<\/strong><\/td>\u03b2-lactam (oxazolidine ring)<\/td>Irreversible suicide substrate<\/strong><\/td>Class A (TEM, SHV); weak vs C\/D<\/td>Only natural<\/strong> inhibitor (from Streptomyces clavuligerus<\/em>); first marketed (1981)<\/td><\/tr>
Sulbactam<\/strong><\/td>\u03b2-lactam (penicillanic acid sulfone)<\/td>Irreversible acyl-enzyme<\/td>Class A > C (limited)<\/td>Has intrinsic antibacterial activity<\/strong> vs Acinetobacter<\/em> spp.<\/td><\/tr>
Tazobactam<\/strong><\/td>\u03b2-lactam (triazolylmethyl sulfone)<\/td>Irreversible<\/td>Class A; weak vs C\/D<\/td>Broader than clavulanate; used with piperacillin, cefepime<\/td><\/tr><\/tbody><\/table><\/figure>\n\n\n\n

Diazabicyclooctane (DBO) inhibitors \u2014 non-\u03b2-lactam, reversible<\/strong><\/h2>\n\n\n\n
Inhibitor<\/th>Mechanism<\/th>Effective vs Class<\/th>Partner Drug(s)<\/th>Key Distinction<\/th><\/tr><\/thead>
Avibactam<\/strong><\/td>Reversible covalent acyl-enzyme<\/strong> (non-\u03b2-lactam DBO)<\/td>A, C, some D (e.g., OXA-48)<\/td>Ceftazidime (CZA)<\/td>First clinically used non-\u03b2-lactam inhibitor<\/td><\/tr>
Relebactam<\/strong><\/td>Reversible DBO<\/td>A, C (not D)<\/td>Imipenem + cilastatin (IMI\/REL)<\/td>Improved stability vs avibactam<\/td><\/tr>
Nacubactam<\/strong><\/td>DBO<\/td>A, C (+ intrinsic PBP inhibition)<\/td>Meropenem (in trials)<\/td>Has dual mechanism<\/strong> (\u03b2-lactamase + PBP)<\/td><\/tr>
Zidebactam<\/strong><\/td>DBO<\/td>A, C (+ PBP2 binding)<\/td>Cefepime ( FEP-ZID, in development)<\/td>Potent synergy via PBP2 affinity<\/td><\/tr>
Enmetazobactam<\/strong><\/td>DBO-like (penicillanic sulfone + triazole)<\/td>A (incl. ESBL)<\/td>Cefepime (approved EU 2024)<\/td>Modified sulfone, faster kinetics<\/td><\/tr><\/tbody><\/table><\/figure>\n\n\n\n

Boronate inhibitors (Transition-state analogues)<\/h2>\n\n\n\n
Inhibitor<\/th>Mechanism<\/th>Effective vs Class<\/th>Partner<\/th>Notes<\/th><\/tr><\/thead>
Vaborbactam<\/strong><\/td>Reversible boronate transition-state mimic<\/strong><\/td>A (esp. KPC), not C\/D<\/td>Meropenem (\u2192 MER\/VAB)<\/td>Potent against KPC carbapenemases<\/td><\/tr>
Taniborbactam<\/strong><\/td>Cyclic boronate<\/td>A, C, D, some B (NDM)<\/td>Cefepime (\u2192 phase 3 trials)<\/td>Broadest coverage (incl. MBL NDM partial)<\/td><\/tr>
QPX7728<\/strong><\/td>Ultrawide-spectrum boronate<\/td>A, C, D, some B<\/td>In development (oral \u03b2-lactams)<\/td>Designed for oral combinations<\/td><\/tr><\/tbody><\/table><\/figure>\n\n\n\n

Miscellaneous or Investigational<\/h2>\n\n\n\n
Inhibitor<\/th>Type<\/th>Stage<\/th>Coverage<\/th><\/tr><\/thead>
LN-1-255<\/strong><\/td>Monobactam-based inhibitor<\/td>Pre-clinical<\/td>A > C<\/td><\/tr>
ETX0282<\/strong><\/td>Oral prodrug of DBO (ETX1317)<\/td>Phase 2<\/td>A, C<\/td><\/tr><\/tbody><\/table><\/figure>\n\n\n\n

<\/p>\n","protected":false},"excerpt":{"rendered":"

Clavams (Classical \u03b2-lactam-structured inhibitors) Inhibitor Structure type Mechanism Effective vs \u03b2-lactamase class Unique features Clavulanic acid \u03b2-lactam (oxazolidine ring) Irreversible […]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"site-sidebar-layout":"default","site-content-layout":"","ast-site-content-layout":"default","site-content-style":"default","site-sidebar-style":"default","ast-global-header-display":"","ast-banner-title-visibility":"","ast-main-header-display":"","ast-hfb-above-header-display":"","ast-hfb-below-header-display":"","ast-hfb-mobile-header-display":"","site-post-title":"","ast-breadcrumbs-content":"","ast-featured-img":"","footer-sml-layout":"","ast-disable-related-posts":"","theme-transparent-header-meta":"","adv-header-id-meta":"","stick-header-meta":"","header-above-stick-meta":"","header-main-stick-meta":"","header-below-stick-meta":"","astra-migrate-meta-layouts":"default","ast-page-background-enabled":"default","ast-page-background-meta":{"desktop":{"background-color":"var(--ast-global-color-5)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"tablet":{"background-color":"","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"mobile":{"background-color":"","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""}},"ast-content-background-meta":{"desktop":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"tablet":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"mobile":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""}},"ngg_post_thumbnail":0,"footnotes":""},"categories":[9],"tags":[28],"class_list":["post-1152","post","type-post","status-publish","format-standard","hentry","category-antibiotic","tag-antibiotic"],"_links":{"self":[{"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/posts\/1152","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/microregistrar.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=1152"}],"version-history":[{"count":1,"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/posts\/1152\/revisions"}],"predecessor-version":[{"id":1153,"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/posts\/1152\/revisions\/1153"}],"wp:attachment":[{"href":"https:\/\/microregistrar.com\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=1152"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/microregistrar.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=1152"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/microregistrar.com\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=1152"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}