Basilea's First-In-Class Antibiotic Ceftobiprole (BAL5788) Unaffected by Resistance and Novel Once-Daily Antifungal (BAL8557) Active Against Resistant Aspergillus


BASEL, Switzerland, Nov. 2, 2004 (PRIMEZONE) -- Basilea Pharmaceutica AG presents sixteen posters at the 44th International Conference on Antimicrobial Agents and Chemotherapy (ICAAC) held in Washington D.C., covering clinical and pre-clinical activity of ceftobiprole, its first-in-class broad-spectrum anti methicillin-resistant Staphylococcus aureus (MRSA) antibiotic, and BAL8557 its broad-spectrum water-soluble anti-fungal.

Poster data confirms that ceftobiprole has potent anti-MRSA activity (Ednie and Appelbaum, 2004; Sader et al., 2004) and is unaffected by endogenous resistance (Bogdanovich et al., 2004; Clark et al., 2004; Rouse et al., 2004; Vaudaux et al., 2004) of a range of pathogens (staphylococci, pneumococci, Haemophilius influenzae, and Enterobacteriaceae). In addition, Kresken and Heep (2004) demonstrate that ceftobiprole has potent activity against Pseudomonas aeruginosa. Clinical data from Heep et al. (2004) confirms that ceftobiprole is a potent anti-MRSA drug for patients with complicated skin and skin structure infections.

The BAL8557 data confirms that Basilea's novel antifungal BAL8557 is active against Aspergillus pathogens resistant to other drugs (Warn et al., 2004) and has a favourable pharmacokinetic profile (Schmitt-Hoffmann et al., 2004).

"The sixteen posters at this year's conference highlight Basilea's position as a leader in both anti-bacterial and anti-fungal research," commented Professor Jutta Heim, Chief Scientific Officer of Basilea.

"The more we study ceftobiprole the more its potential becomes apparent as a first-choice antibiotic for severe hospital infections where MRSA is suspected. Furthermore the new data on BAL8557 shows our commitment to developing anti-infective drugs with strong competitive profiles," commented Dr. Rienk Pypstra, Chief Development Officer of Basilea.

Basilea Data at ICAAC 2004 L-361 BAL5788, the First of a New Class of Anti-MRSA Cephalosporins: Microbiological Results from a Phase II Study in Complicated Skin and Skin Structure Infections. M. HEEP 1), S. QUERNER 1), M. HARSCH 1), W. O'RIORDAN 2); 1) Basilea Pharmaceutica, Basel, Switzerland, 2) Paradise Valley Hospital, San Diego, CA.

A-37 Multiple Ascending Dose Pharmacokinetics of the New Antifungal BAL4815 after Intravenous and Oral Administration of its Prodrug BAL8557 A. SCHMITT-HOFFMANN 1), B. ROOS 1), J. SPICKERMANN 1), E. WEIDEKAMM 1), M. ROEHRLE 2); 1) Basilea Pharmaceutica, Basel, Switzerland, 2) AAI, Neu-Ulm, Germany.

A-134 Monte Carlo Simulations of BAL8557: a New Watersoluble Azole with Antifungal Activity. J. W. MOUTON 1), A. SCHMITT-HOFFMANN 2), N. PUNT 3); 1) Canisius Wilhelmina Hospital, Nijmegen, Netherlands, 2)Basilea, Basel, Switzerland, 3) Medimatics, Maastricht, Netherlands.

B-677 Intensive Therapy with BAL5788 of Experimental Foreign Body Infection due to Methicillin-Resistant Staphylococcus aureus (MRSA) BP. VAUDAUX, A. GJINOVCI, M. BENTO, D. LI, P. FRANCOIS, D. P. LEW, J. SCHRENZEL; Geneva University Hospitals, Geneva, Switzerland.

E-2021 Antistaphylococcal Activity of Ceftobiprole (BAL9141) and Comparators L. EDNIE, P. C. APPELBAUM; Hershey Medical Center, Hershey, PA.

F-842 In Vitro Activity of a New Triazole BAL4815, the Active Component of BAL8557 (the Water-Soluble Prodrug) against Aspergillus spp P. A. WARN, A. SHARP, D. W. DENNING; University of Manchester, Manchester, United Kingdom.

E-2022 In Vitro Activities of BAL9141, the Active Component of BAL5788, and Seven other Beta-Lactams against Selected Strains of Pseudomonas aeruginosa Susceptible or Resistant to Ceftazidime M. KRESKEN 1), M. HEEP 2); 1) Anti-Infectives Intelligence GmbH, Bonn, Germany, 2) Basilea Pharmaceutica Ltd., Basel, Switzerland.

E-2035 Comparative Activity of BAL9141, Daptomycin and Linezolid versus S. aureus from Bacteremias in the UK and Ireland R. REYNOLDS 1), D. M. LIVERMORE 2), BSAC Working Party on Bacteraemia Resistance Surveillance; 1)British Society for Antimicrobial Chemotherapy (BSAC), Birmingham, United Kingdom, 2) Health Protection Agency, London, United Kingdom.

E-2036 Effect of Culture Conditions on MICs of BAL9141, Representing a New Class of Cephalosporins Active against MRSA R. REYNOLDS 1), D. M. LIVERMORE 2), BSAC Working Party on Bacteraemia Resistance Surveillance; 1) British Society for Antimicrobial Chemotherapy (BSAC), Birmingham, United Kingdom, 2) Health Protection Agency, London, United Kingdom.

E-2037 Antimicrobial Activity of BAL9141 Tested against Staphylococcal Strains with Selected Resistance Patterns H. S. SADER, D. J. BIEDENBACH, R. N. JONES; JMI Laboratories, Inc., North Liberty, IA.

D-1920 Ceftobiprole (BAL9141): Activity Against Staphylococci and Pneumococci by Microdilution and Etest Methods M. R. JACOBS 1), S. BAJAKSOUZIAN 1), A. WINDAU 1), P. C. APPELBAUM 2); 1) Case Western Reserve Univ./University Hospitals, Cleveland, OH, 2) Hershey Medical Center, Hershey, PA.

E-2018 Resistance Selection Studies on Staphylococci with Ceftobiprole (BAL9141) T. BOGDANOVICH, B. BOZDOGAN, P. C. APPELBAUM; Hershey Med. Ctr., Hershey, PA.

E-2019 Comparative Time-Kill Determination of the Antipneumococcal Activity of Ceftobiprole (BAL9141). G. LIN, P. C. APPELBAUM; Hershey Medical Center, Hershey, PA.

E-2020 Resistance Selection of BAL9141, the Active Component of Prodrug BAL5788, against Pneumococci C. L. CLARK, K. KOSOWSKA, K. CREDITO, P. C. APPELBAUM; Hershey Medical Center, Hershey, PA.

B-1177 Activity of BAL5788 in Haemophilus influenzae, Enterobacter cloacae or Klebsiella pneumoniae Experimental Murine Pneumonia M. ROUSE, P. ANGUITA-ALONSO, M. H. HEIN, J. M. STECKELBERG, R. PATEL; Mayo Clinic, Rochester, MN.

A-1874 Pharmacodynamics of BAL4815: a New Azole Antifungal in a Mouse Model of Systemic Infection D. TE DORSTHORST 1), P. E. VERWEIJ 2), J. F. MEIS 1), J. W. MOUTON 1); 1) Canisius Wilhelmina Hospital, Nijmegen, Netherlands, 2) University Medical Ctr. St. Radboud, Nijmegen, Netherlands.

About Ceftobiprole (BAL5788) Ceftobiprole is the first of a new class of broad-spectrum cephalosporin antibiotics that was specially designed to bind the mutated targets in MRSA resulting in potent bactericidal activity towards MRSA and penicillin-resistant Streptococcus pneumoniae (PRSP). Ceftobiprole has not only maintained a broad-spectrum profile targeting other Gram-positive as well as Gram-negative pathogens, but has also shown a low potential to induce resistance in vitro.

In March 2003 the U.S. Food and Drug Administration granted BAL5788 Fast-Track designation for the treatment of complicated skin and skin structure infections due to methicillin-resistant Staphylococcus species, which has been followed by an additional designation in June 2004 for the treatment of hospital-acquired pneumonia including ventilator-associated pneumonia due to suspected or proven methicillin-resistant Staphylococcus aureus (MRSA). Ceftobiprole has completed phase II clinical development and is anticipated to start phase III this year.

About BAL8557 BAL8557 is a novel water-soluble azole suitable for both oral and intravenous administration for mucocutaneous and invasive fungal infections that has completed phase I clinical development and is anticipated to start phase II this year.

About Basilea Basilea Pharmaceutica AG (BSLN) is an independent biopharmaceutical company headquartered in Basel, Switzerland that is actively engaged in the discovery and development of innovative medicines for the treatment of unmet medical needs.

The company's fully integrated research and development operations are currently focused on new anti-bacterials and anti-fungals to fight drug resistance, and dermatology drugs. Basilea was founded in October 2000 with significant resources to discover, develop and bring innovative medicines to market. Basilea is listed on the SWX Swiss Exchange.

Disclaimer This communication expressly or implicitly contains certain forward-looking statements concerning Basilea Pharmaceutica AG 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 AG to be materially different from any future results, performance or achievements expressed or implied by such forward-looking statements. Basilea Pharmaceutica AG 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 the following: Contact

Basilea Pharmaceutica AG Corporate Information P.O. Pox CH-4005 Basel Switzerland

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