New clinical and preclinical data on Basilea's novel antibiotic BAL30072 against multidrug-resistant Gram-negative superbugs presented at ICAAC

Basel, Switzerland, September 19, 2011 - Detailed results from the successful first phase I study with Basilea's novel antibiotic BAL30072 were presented at the 51st Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) in Chicago, USA. Additional preclinical data underline the strong bactericidal activity and broad coverage of BAL30072 against clinically-relevant multidrug-resistant Gram-negative bacteria. Also, further data on Basilea's anti-MRSA broad-spectrum antibiotic ceftobiprole are presented.

Multidrug-resistant Gram-negative bacteria such as Pseudomonas aeruginosa and Acinetobacter baumannii are causing growing concern as they have become resistant to most marketed antibiotics, leaving only few or no therapeutic options.

Basilea's BAL30072, a beta-lactam antibiotic of the sulfactam class, has the potential to play an essential role in the therapy of life-threatening infections caused by such multidrug-resistant as it is not easily destroyed by bacterial enzymes which cause resistance against many currently marketed anti­biotics. BAL30072 has demonstrated bactericidal activity against a broad range of Gram-negative superbugs.

BAL30072 - a novel sulfactam antibiotic against multidrug-resistant Gram-negative bacteria
Favorable data from the first phase I study, a double-blind, randomized, placebo-controlled, single ascending dose study demonstrate the excellent safety profile of BAL30072. In the study, no clinically relevant drug-related adverse events were observed at any dose level and no dose-limiting toxicities were identified. BAL30072 displayed predictable linear pharmacokinetics with low inter-subject variability, in line with preclinical data and in accordance with the favorable beta-lactam class profile. (Posters A2-572, F1-145 and F1-146) A second, multiple ascending dose phase I study with BAL30072 has been recently initiated and is anticipated to be completed in the first part of 2012.

Further in vitro data presented at ICAAC highlight the potent activity profile of BAL30072 especially against difficult-to-treat multidrug-resistant Gram-negative bacteria.

Data about the strong activity of BAL30072 against multi-resistant Gram-negative bacteria carrying the gene for the NDM-1 enzyme (New Delhi metallo-beta-lactamase) that leads to resistance towards almost all of the currently marketed antibiotics were presented. The test panel included clinical isolates from a recent outbreak of NDM-1 positive Acinetobacter baumannii in the UK. The activity of BAL30072 as a single agent was enhanced by combination with meropenem, suggesting potential synergy. (Poster E-722)

Bacteria resistant against carbapenems, the current most broadly active agents against Gram-negative pathogens, are an emerging threat. The potent activity of BAL30072 against carbapenem-resistant Gram-negative bacteria is therefore of particular importance.
BAL30072 demonstrated the most potent activity against carbapenem-resistant Gram-negative bacteria in a head-to-head comparison with meropenem and aztreonam. In addition, BAL30072 demonstrated bactericidal activity in meropenem- and aztreonam-resistant strains.

(Poster E-737)

Basilea's Head of Biology, Prof. Malcolm Page, was invited to give an oral presentation on BAL30072 and other beta-lactams titled "Monocyclic beta-lactam scaffolds for treatment of multidrug-resistant infections" (Presentation 1073) as part of the symposium "Investigational drugs worth waiting for to treat multidrug-resistant pathogens".

Posters on BAL30072 at ICAAC 2011
Pharmacokinetics and Safety of the Novel Sulfactam Antibiotic BAL30072 after Single Ascending Dose Infusions in Healthy Volunteers - A. SCHMITT-HOFFMANN, B. ROOS,
J. MAARES, J. SAUER, J. SPICKERMANN, I. MEYER, A. KAUFHOLD; A2-572

BAL30072: A Novel Monocyclic Sulfactam Antibiotic - Preclinical Pharmacokinetic Properties - A. SCHMITT-HOFFMANN, K. GEBHARDT, M. WIND, P. HARGREAVES, D. KLAUER, A. BRENDLE,
A. SERAFYN, C. SCHLAEFLE, H. GRUNWALD, C. BUCHER, J. SPICKERMANN; F1-145

BAL30072: A Novel Monocyclic Sulfactam Antibiotic - Preclinical Safety Properties -
A. SCHMITT-HOFFMANN, C. BUCHER, J. SPICKERMANN, H. URWYLER; F1-146

Activity of the Novel Sulfactam BAL30072, Alone and in Combination with Meropenem, Against Diverse Gram-Negative Isolates Carrying NDM-1 Beta-Lactamase Gene -
T. R. WALSH, J. WEEKS, M. TOLEMAN, R. HOWE, M. WOOTTON, V. DANIEL, W. J. STUBBINGS,
M. E. JONES; E-722

Bactericidal Activity of BAL30072 Compared to Other Agents against Multi-Resistant Gram-Negative Bacteria by Time-Kill - G. A. PANKUCH, C. CLARK, G. LIN, W. STUBBINGS,
P. C. APPELBAUM, K. KOSOWSKA-SHICK; E-737

Expression of Fe-Uptake Systems in Pseudomonas aeruginosa PAO1 and Susceptibility to the Siderophore Sulfactam BAL30072 - T. KOEHLER, M. G. P. PAGE, C. VAN DELDEN; F1-144

For further information please visit www.icaac.org


Ceftobiprole - a novel broad-spectrum anti-MRSA antibiotic targeting Gram-positive and Gram-negative bacteria for the treatment of severe infections such as hospital-acquired pneumonia
Furthermore, additional preclinical data on Basilea's anti-MRSA broad-spectrum antibiotic ceftobiprole are presented at ICAAC.

Ceftobiprole is a novel broad-spectrum cephalosporin antibiotic, tested in several phase III studies, for the first-line treatment of severe multidrug-resistant bacterial infections. It has demonstrated activity against a wide range of Gram-positive bacteria, including the methicillin-resistant Staphylococcus aureus (MRSA) superbug, as well as clinically-relevant Gram-negative bacteria such as Pseudomonas aeruginosa, against which ceftobiprole has a broader spectrum than other drugs, for example piperacillin/tazobactam or ceftazidime.

Posters on ceftobiprole at ICAAC 2011
Comparison of In Vitro Activity of Ceftobiprole (BPR) with Ceftriaxone (CRO), Ceftazidime (TAZ), and Cefepime (FEP) Against Isolates of Rapidly Growing Microbacteria (RGM) and Nocardia (NOC) - R. J. WALLACE JR., B. A. BROWN-ELLIOT, K. KRIEL, T. MARTIN, L. BRIDGE,
R. VASIREDDY; E-118

Investigating Ceftobiprole (Cef) Alone and in Combination with Daptomycin (Dap), Linezolid (Lin) and Vancomycin (Van) Against Methicillin-Resistant Staphylococcus aureus (MRSA) in an In Vitro Infection Model - N. ALKURDI, A. KUMAR, R. ARIANO, S. ZELENITSKY; E-1335

New Cephalosporins against Gram-Positive and Gram-Negative Bacteria Have No Significant Ecological Impact on the Human Intestinal Microflora - M. RASHID, A. WEINTRAUB, C. NORD; K-1415

For further information please visit www.icaac.org

About Basilea
Basilea Pharmaceutica Ltd. is headquartered in Basel, Switzerland, and listed on the SIX Swiss Exchange (SIX:BSLN). Basilea Pharmaceutica International Ltd.'s 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 adults with severe chronic hand eczema unresponsive to potent topical corticosteroids, in Denmark, Finland, France, Germany, Norway, Switzerland and the United Kingdom and has appointed distributors for Toctino® in other selected European markets, Canada, Israel, Mexico and the Republic of Korea. 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 (methicillin-resistant Staphylococcus aureus) 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 MRSA, and many clinically important Gram-negative bacteria such as Pseudomonas spp.

Basilea's BAL30072, a novel antibiotic for the treatment of resistant Gram-negative infections, and the oncology drug BAL101553 for the treatment of drug-resistant cancers are in phase I clinical testing.

Disclaimer
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:

Media Relations
Investor Relations

Peer Nils Schröder, Ph.D.

Head Public Relations &

Corporate Communications

+41 61 606 1102

media_relations@basilea.com
Barbara Zink, Ph.D., MBA

Head Corporate Development

 

+41 61 606 1233

investor_relations@basilea.com
 


This press release can be downloaded from www.basilea.com.

 

 

 

Posted: September 2011

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