![\"Novel](\"https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2014\/08\/fmicb-04-00392-g003-e1408842545171.jpg?resize=248%2C135&ssl=1\")
<\/a>combination with an unspecified penem by The Medicines Company. This is a non-betalactam BLI which confers protection against Class A BLs. It does not inactivate Class B (MBLs) or Class D (OXA-type) enzymes. It is devoid of intrinsic antibacterial activity. A Phase 1 SAD and MAD study were completed in 2013; however, safety\/tolerability data have not yet been published.<\/li>\n<\/ul>\nIn summary, boron-containing compounds have made it into the clinic. So far, there are no reports of safety issues but published data are sparse. The demise of GSK \u2018052 was due to problems with efficacy, not safety. Theoretical concerns about the reactivity of boron causing side effects remain for now\u2026well, just theoretical.<\/p>\n
Abbreviations:<\/strong><\/p>\nBL\/BLI \u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0 betalactamase \/ betalactamase-inhibitor
\nMBL\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0 \u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0 Metallo-betalactamase
\nSAD, MAD\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0 single\/multiple ascending dose
\ncUTI\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0\u00a0 complicated urinary tract infection<\/p>\n
References:
\n<\/strong>[1] http:\/\/pipeline.corante.com\/archives\/2012\/03\/05\/trouble_with_a_boroncontaining_drug_candidate.php
\n[2] B. Sekhon. Res Pharm Sci. 2013 Jul-Sep; 8(3): 145\u2013158
\n[3] S. Wring. Parasitology. Jan 2014
\n[4] http:\/\/www.scynexis.com\/pipeline\/scyx-7158\/
\n[5] R. Mendes.\u00a0 AAC. 2013, 57(6):2849
\n[6] See Anacor webside http:\/\/www.anacor.com\/gsk052.php
\n[7] http:\/\/www.clinicaltrials.gov\/ct2\/show\/results\/NCT01381549?term=gsk2251052&rank=5<\/p>\n <\/p>\n","protected":false},"excerpt":{"rendered":"
Why are there so few boron-containing drugs on the market? \u00a0The cancer drug bortezumib (Velcade\u00ae) may be the only better-known drug on the market with a boron atom in its structure.[1]\u00a0 Among antibiotics, there is Kerydin\u2122 (tavaborole), an approved topical solution for the treatment of onychomycosis caused by Trichophyton but Continue reading Not So Boring: \u00a0Boron-Containing Antibiotics Create a Stir<\/span>→<\/span><\/a><\/p>\n","protected":false},"author":1,"featured_media":858,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"jetpack_post_was_ever_published":false,"_jetpack_newsletter_access":"","_jetpack_dont_email_post_to_subs":true,"_jetpack_newsletter_tier_id":0,"_jetpack_memberships_contains_paywalled_content":false,"_jetpack_memberships_contains_paid_content":false,"footnotes":"","jetpack_publicize_message":"","jetpack_publicize_feature_enabled":true,"jetpack_social_post_already_shared":true,"jetpack_social_options":{"image_generator_settings":{"template":"highway","default_image_id":0,"font":"","enabled":false},"version":2}},"categories":[3,18],"tags":[483,478,494,495,498,488,463,482,497,490,492,486,481,499,484,485,491,480,479,493,487,489],"class_list":["post-751","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-the_news","category-the_viewpoint","tag-an3365","tag-anacor","tag-benzoxaborole","tag-betalactamase-inhibitor","tag-boron-antibiotics","tag-bortezumib","tag-carbavance","tag-gsk-052","tag-gsk2251052","tag-kerydin","tag-onychomycosis","tag-oxaborole","tag-rempex","tag-rpx-7009","tag-scyn-7158","tag-scynexis","tag-tavaborole","tag-the-medicines-company","tag-tmc","tag-trichophyton","tag-trypanosomiasis","tag-velcade"],"jetpack_publicize_connections":[],"jetpack_featured_media_url":"https:\/\/allphasepharma.com\/dir\/wp-content\/uploads\/2014\/08\/Bor.jpe","jetpack_shortlink":"https:\/\/wp.me\/p4KWFr-c7","jetpack_sharing_enabled":true,"jetpack-related-posts":[{"id":932,"url":"https:\/\/allphasepharma.com\/dir\/2014\/09\/26\/932\/its-not-a-free-enterprise-market-stupid-part-1\/","url_meta":{"origin":751,"position":0},"title":"It\u2019s Not a Free-Enterprise Market, Stupid!","author":"Harald","date":"September 26, 2014","format":false,"excerpt":"The economics of developing antibacterials is a frustrating topic to address.\u00a0 There are unique aspects to the antibiotic market which sets it apart from other medicines, esp. the unique societal aspects of antibiotic use which go beyond the benefit to the individual. IDSA has spoken out in various publications (\u201cBad\u2026","rel":"","context":"In "Recent Literature"","block_context":{"text":"Recent Literature","link":"https:\/\/allphasepharma.com\/dir\/category\/recent_literature\/"},"img":{"alt_text":"","src":"https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2014\/09\/freemarket-slider-copy.jpg?fit=640%2C200&ssl=1&resize=350%2C200","width":350,"height":200,"srcset":"https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2014\/09\/freemarket-slider-copy.jpg?fit=640%2C200&ssl=1&resize=350%2C200 1x, https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2014\/09\/freemarket-slider-copy.jpg?fit=640%2C200&ssl=1&resize=525%2C300 1.5x"},"classes":[]},{"id":2660,"url":"https:\/\/allphasepharma.com\/dir\/2016\/08\/27\/2660\/the-epipen-episode-an-epitaph-on-epinephrine-as-we-know-it-an-epilogue-and-an-epiphany\/","url_meta":{"origin":751,"position":1},"title":"The EpiPen Episode, an Epitaph on Epinephrine as we know it, an Epilogue and an Epiphany","author":"Harald","date":"August 27, 2016","format":false,"excerpt":"For a good long time, economists have been thinking about the reimbursement quandary for antibiotics, esp. antibacterials. They are just too cheap, right?\u00a0 Well, with the exception of HCV and some newer HIV drugs, few compounds have ever reached the stratospheric prices that oncology drugs or TNF alpha inhibitors command.\u2026","rel":"","context":"In "The News"","block_context":{"text":"The News","link":"https:\/\/allphasepharma.com\/dir\/category\/the_news\/"},"img":{"alt_text":"EpiPen","src":"https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2016\/08\/EpiPen.jpg?resize=350%2C200","width":350,"height":200,"srcset":"https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2016\/08\/EpiPen.jpg?resize=350%2C200 1x, https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2016\/08\/EpiPen.jpg?resize=525%2C300 1.5x"},"classes":[]},{"id":1332,"url":"https:\/\/allphasepharma.com\/dir\/2015\/03\/28\/1332\/drugs-with-qidp-designation-update-3282015\/","url_meta":{"origin":751,"position":2},"title":"Drugs with QIDP Designation \u2013 Update 4\/8\/2015","author":"Harald","date":"March 28, 2015","format":false,"excerpt":"For the latest QIDP listing, please click HERE Our latest internet search came up with 37 drugs that garnered QIDP status.\u00a0 They are listed in the Table below (if I missed a compound, please leave a comment!!). \u00a0The\u00a0table is searchable so you should be able to massage the data to\u2026","rel":"","context":"In "QIDP Antibiotics"","block_context":{"text":"QIDP Antibiotics","link":"https:\/\/allphasepharma.com\/dir\/category\/qidp_antibiotic\/"},"img":{"alt_text":"APPC + QIDP copy","src":"https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2014\/10\/APPC-QIDP-copy.jpg?resize=350%2C200","width":350,"height":200,"srcset":"https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2014\/10\/APPC-QIDP-copy.jpg?resize=350%2C200 1x, https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2014\/10\/APPC-QIDP-copy.jpg?resize=525%2C300 1.5x"},"classes":[]},{"id":445,"url":"https:\/\/allphasepharma.com\/dir\/2014\/07\/02\/445\/why-the-next-novel-antibiotic-will-cost-40k-or-more\/","url_meta":{"origin":751,"position":3},"title":"Why The Next Novel Antibiotic Will Be A Blockbuster And Cost $40k","author":"Harald","date":"July 2, 2014","format":false,"excerpt":"Looking at all antibiotics in the pipeline, I can\u2019t help but think that \u2013 by 2018 \u2013 there\u00a0will be\u00a0some blockbuster anti-infectives coming to the market. Why do I say this?\u00a0 What is going to generate this revenue stream for companies when the new crop of drugs will be restricted by\u2026","rel":"","context":"In "The Viewpoint"","block_context":{"text":"The Viewpoint","link":"https:\/\/allphasepharma.com\/dir\/category\/the_viewpoint\/"},"img":{"alt_text":"pills","src":"https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2014\/07\/pills-300x225.jpg?resize=350%2C200","width":350,"height":200},"classes":[]},{"id":2911,"url":"https:\/\/allphasepharma.com\/dir\/2016\/11\/25\/2911\/prospecting-antibiotics\/","url_meta":{"origin":751,"position":4},"title":"Prospecting for New Antibiotics","author":"Harald","date":"November 25, 2016","format":false,"excerpt":"The QIDP designation was introduced in 2012 to incentivize drug development in antiinfectives. QIDP came with several attractive features, such as prolongation of patent life, FDA\u00a0expedited review and more.\u00a0 In addition, FDA made it quite easy to garner the label.\u00a0 As you can see, there is really no downside to\u2026","rel":"","context":"In "Did you know...?"","block_context":{"text":"Did you know...?","link":"https:\/\/allphasepharma.com\/dir\/category\/interesting_facts\/"},"img":{"alt_text":"engine-qidp-blog","src":"https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2016\/11\/Engine-QIDP-blog.jpg?resize=350%2C200","width":350,"height":200,"srcset":"https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2016\/11\/Engine-QIDP-blog.jpg?resize=350%2C200 1x, https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2016\/11\/Engine-QIDP-blog.jpg?resize=525%2C300 1.5x"},"classes":[]},{"id":1314,"url":"https:\/\/allphasepharma.com\/dir\/2015\/03\/25\/1314\/aerosolized-antibiotics-selling-nebulizers\/","url_meta":{"origin":751,"position":5},"title":"Aerosolized Antibiotics & Selling Nebulizers","author":"Harald","date":"March 25, 2015","format":false,"excerpt":"\u201cThe medicine comes for free, just pay us for the inhaler\u201d should be the marketing slogan for this group of therapeutics.\u00a0 Nebulizers are good business: hard to copy as a delivery system, they are a great opportunity to \u2018evergreen\u2019 off-patent antibiotics. The inhalational route to administer antibiotics is clearly attractive.\u00a0\u2026","rel":"","context":"In "QIDP Antibiotics"","block_context":{"text":"QIDP Antibiotics","link":"https:\/\/allphasepharma.com\/dir\/category\/qidp_antibiotic\/"},"img":{"alt_text":"","src":"","width":0,"height":0},"classes":[]}],"jetpack_likes_enabled":true,"_links":{"self":[{"href":"https:\/\/allphasepharma.com\/dir\/wp-json\/wp\/v2\/posts\/751","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/allphasepharma.com\/dir\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/allphasepharma.com\/dir\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/allphasepharma.com\/dir\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/allphasepharma.com\/dir\/wp-json\/wp\/v2\/comments?post=751"}],"version-history":[{"count":6,"href":"https:\/\/allphasepharma.com\/dir\/wp-json\/wp\/v2\/posts\/751\/revisions"}],"predecessor-version":[{"id":3124,"href":"https:\/\/allphasepharma.com\/dir\/wp-json\/wp\/v2\/posts\/751\/revisions\/3124"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/allphasepharma.com\/dir\/wp-json\/wp\/v2\/media\/858"}],"wp:attachment":[{"href":"https:\/\/allphasepharma.com\/dir\/wp-json\/wp\/v2\/media?parent=751"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/allphasepharma.com\/dir\/wp-json\/wp\/v2\/categories?post=751"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/allphasepharma.com\/dir\/wp-json\/wp\/v2\/tags?post=751"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}
![\"Novel](\"https:\/\/i0.wp.com\/allphasepharma.com\/dir\/wp-content\/uploads\/2014\/08\/fmicb-04-00392-g003-e1408842545171.jpg?ssl=1\")
<\/a>combination with an unspecified penem by The Medicines Company. This is a non-betalactam BLI which confers protection against Class A BLs. It does not inactivate Class B (MBLs) or Class D (OXA-type) enzymes. It is devoid of intrinsic antibacterial activity. A Phase 1 SAD and MAD study were completed in 2013; however, safety\/tolerability data have not yet been published.<\/li>\n<\/ul>\n