Basilea's antibiotic BAL30072 shows activity against superbugs expressing the NDM-1 resistance factor
Basel, Switzerland, May 9, 2011 - New research data on Basilea's antibacterial compounds was presented in Milan, Italy, at the European Congress of Clinical Microbiology and Infectious Disease (ECCMID) and the International Congress of Chemotherapy (ICC) joint meeting. Basilea's novel antibiotic BAL30072 was shown to be active against multidrug-resistant Gram-negative bacteria that express the NDM-1 resistance factor.
Multidrug-resistant Gram-negative pathogens are appearing with increasing frequency in hospitals around the world and have been associated with prolonged hospital stays, higher healthcare costs and increased mortality.
Recently, Gram-negative bacteria that harbour the so-called New Delhi metallo-beta-lactamase 1 (NDM-1) alongside with several other resistance mechanisms have triggered increased medical concern. NDM-1 is an enzyme that leads to resistance towards antibiotics that have been the mainstay of treatment of clinically important pathogens such as Escherichia coli or Klebsiella pneumoniae. These bacteria may cause systemic infections including severe lung and complicated urinary tract infections.
Bacteria expressing NDM-1 were discovered only recently but are now being observed with increasing frequency in many countries all over the world.
BAL30072, a novel sulfactam antibiotic currently in phase I clinical testing
In-vitro data presented at ECCMID/ICC show for the first time that BAL30072 is active against multidrug-resistant clinical isolates of Gram-negative bacteria harbouring NDM-1. BAL30072 is resistant to degradation by NDM-1 and was therefore active, at clinically achievable concentrations, against many of the highly resistant isolates tested while standard anti-Gram-negative antibiotics such as meropenem, ceftazidime or aztreonam covered only a minority of the strains. BAL30072 and meropenem combined had enhanced activity and resulted in inhibition of more than 90% of the isolates.
Also at ECCMID/ICC, in-vitro data was presented that demonstrated the potent activity of BAL30072 against meropenem-resistant strains of Acinetobacter baumannii, a clinically important Gram-negative pathogen in hospital-acquired pneumonia, for which only few therapeutic options exist. BAL30072 was tested alongside reference drugs currently used for the treatment of Acinetobacter infections and showed greater activity than all the marketed beta-lactam antibiotics as well as most of the other comparators.
The new data confirm the therapeutic potential of Basilea's phase I compound BAL30072. The drug shows potent activity against a broad range of multidrug-resistant Gram-negative bacteria, including those harbouring NDM-1, and may offer a future treatment option for potentially life-threatening Gram-negative infections where currently only limited therapeutic options exist.
Publications on BAL30072 at the 21st ECCMID / 27th ICC Annual Meetings
· Activity of the novel sulfactam BAL30072, alone and in combination with meropenem, against Enterobacteriaceae harbouring NDM-1 beta-lactamase - T.R. Walsh, J. Weeks, M. Toleman, W.J. Stubbings, M.G.P. Page, M.E. Jones; poster #P1146
· In vitro activity of the siderophore sulfactam BAL30072 against meropenem non-susceptible Acinetobacter baumannii - P.G. Higgins, D. Stefanik, M.G.P. Page, M. Hackel, H. Seifert; poster #P1184
Ceftobiprole, a novel broad-spectrum cephalosporin antibiotic
In addition, new data on ceftobiprole was presented at ECCMID/ICC. Ceftobiprole is a novel cephalosporin antibiotic with broad coverage of both Gram-positive bacteria, including the superbug methicillin-resistant Staphylococcus aureus (MRSA), and many clinically important Gram-negative bacteria.
Publications on ceftobiprole at the 21st ECCMID / 27th ICC Annual Meetings
· Ceftobiprole efficacy in vitro on Panton-Valentine leukocidin production and in vivo in a rabbit community-associated methicillin-resistant Staphylococcus aureus osteomyelitis model - A. Saleh Mghir, A. Dinh, O. Dumitrescu, G. Lina, Y. Boutrad, F. Vandenesch, J. Etienne, A.C. Crémieux; poster #P1068
· In vitro susceptibility of ceftobiprole, vancomycin and fosfomycin against recent clinical bloodstream isolates of methicillin-resistant Staphylococcus aureus in the General Hospital of Vienna - C. Kratzer, C. Dungl, S. Tobudic, K. Karaca, N. Kreischitz, W. Graninger; abstract #R2365
BAL30072 is a novel siderophore (iron-binding) sulfactam antibiotic, currently in phase I of clinical testing, with a unique mode of action, conferring potent bactericidal activity against Gram-negative pathogens. The compound can act like a "Trojan horse" by exploiting natural nutrient uptake systems of pathogens to gain access to its intracellular target. BAL30072 is stable towards many types of beta-lactamase enzymes, including many of the extended-spectrum beta-lactamases (ESBLs), carbapenemases and metallo-beta-lactamases including NDM-1, which can deactivate most of the currently marketed beta-lactam antibiotics such as cephalosporins and carbapenems.
Ceftobiprole is an anti-MRSA broad-spectrum cephalosporin antibiotic exhibiting activity against a wide spectrum of Gram-positive bacteria, including the superbug methicillin-resistant Staphylococcus aureus (MRSA) and penicillin-resistant Streptococcus pneumoniae as well as many clinically important Gram-negative bacteria, including Pseudomonas spp. Ceftobiprole's key features may allow physicians to use it as the first treatment when MRSA is proven or suspected. Basilea owns full global rights to ceftobiprole.
Basilea Pharmaceutica Ltd. is headquartered in Basel, Switzerland, and listed on the SIX Swiss Exchange (SIX:BSLN). Its fully integrated research and development operations are focused on antibiotics, antifungals and oncology drugs, as well as on the development of dermatology drugs, targeting the medical challenge of resistance and non-response to current treatment options in the hospital and specialty care setting. Basilea is currently marketing Toctino® (alitretinoin), the only approved treatment for severe chronic hand eczema unresponsive to potent topical corticosteroids, in Denmark, Finland, France, Germany, Switzerland and the United Kingdom and has appointed distributors for Toctino® in other selected European markets, Canada, Israel and Mexico. Furthermore, a phase III clinical program on alitretinoin for the treatment of severe chronic hand eczema is ongoing in the U.S. For its phase III compound isavuconazole, a potential best-in-class azole antifungal for the treatment of life-threatening invasive fungal infections, the company has entered into a license, co-development and co-promotion agreement with Astellas Pharma Inc. In addition, Basilea is developing ceftobiprole, a late-stage novel anti-MRSA broad-spectrum cephalosporin antibiotic, for the first-line treatment of potentially life-threatening resistant bacterial infections. Ceftobiprole has a broad coverage of both Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), and many clinically important Gram-negative bacteria such as Pseudomonas spp.
This communication expressly or implicitly contains certain forward-looking statements concerning Basilea Pharmaceutica Ltd. and its business. Such statements involve certain known and unknown risks, uncertainties and other factors, which could cause the actual results, financial condition, performance or achievements of Basilea Pharmaceutica Ltd. to be materially different from any future results, performance or achievements expressed or implied by such forward-looking statements. Basilea Pharmaceutica Ltd. is providing this communication as of this date and does not undertake to update any forward-looking statements contained herein as a result of new information, future events or otherwise.
For further information, please contact:
Peer Nils Schröder, Ph.D.
Head Public Relations &
+41 61 606 1102
Barbara Zink, Ph.D., MBA
Head Corporate Development
+41 61 606 1233
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Posted: May 2011