TAKSTATM (CEM-102)
Fusidic acid (TAKSTATM, CEM-102) is an antibiotic with a long history of safety and efficacy outside the United States. Cempra has exclusive rights to the supply of the compound for the U.S. market. Fusidic acid is orally active against gram-positive bacteria, including all S. aureus strains such as HA-MRSA and CA-MRSA. A novel dosing regimen has been successfully evaluated in a Phase II trial in patients with acute bacterial skin and skin structure infections (aBSSSI). We are planning Phase III trials for this indication as well as Phase II trial for prosthetic joint infections.Profile of TAKSTA (CEM-102)
Skin and skin structure infections are most commonly caused by staphylococci and streptococci. Staphylococcus aureus strains resistant to currently available antibiotics are increasingly prevalent. It is estimated that approximately 60% of all skin S. aureus infections in the U.S. are MRSA. MRSA is no longer an infection that is only hospital-acquired; it is found frequently in the community as well. New oral antibiotics that can treat these infections and that are safe and convenient to use are needed.
TAKSTA has shown potent activity against a large number of S. aureus strains, including CA-MRSA, HA-MRSA and linezolid-resistant strains, isolated in the U.S over a 10 year period. Its broad S. aureus coverage makes it useful for a broad range of clinical applications. TAKSTA could be ideal for patients seen in emergency departments with severe skin and skin structure infections who are candidates for oral therapy. Hospital or long-term care patients who are IV intolerant, at high MRSA risk or require transition to oral therapy are also candidates for TAKSTA.
Cempra has developed a unique oral loading dose regimen to optimize key pathogen coverage and minimize drug resistance development. This regimen will be incorporated in our planned Phase III trial that is designed to show non-inferiority to linezolid in patients with acute bacterial skin and skin structure infections as wells as in our planned Phase II trial in prosthetic joint infections.
Research on TAKSTA
Publications
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Update on Fusidic Acid (CEM-102) Tested against Neisseria gonorrhoeae and Chlamydia trachomatis.
R Jones, D Biedenbach, P Roblin, S Kohlhoff, M Hammerschlag
Antimicrobial Agents And Chemotherapy. October 2010 54: 4518-4519
http://aac.asm.org/cgi/content/citation/54/10/4518
Fusidic acid resistance rates and prevalence of resistance mechanisms among Staphylococcus spp. isolated in North America and Australia, 2007-2008
M. Castanheira, A.A. Watters, J.M. Bell, J.D. Turnidge, and R.N. Jones
Antimicrobial Agents and Chemotherapy September 2010 54: 3614-3617
http://www.ncbi.nlm.nih.gov/pubmed/20566766
Spectrum of activity, mutation rates, synergistic interactions, and the effects of pH and serum proteins for fusidic acid (CEM-102)
D Biedenbach, P Rhomberg, R Mendes, R Jones
Diagnostic Microbiology & Infectious Disease. March 2010 66: 301-307
http://www.dmidjournal.com/article/S0732-8893(09)00424-6/abstract
Performance of Fusidic Acid (CEM-102) Susceptibility Testing Reagents: Broth Microdilution, Disk Diffusion, and Etest Methods as Applied to Staphylococcus aureus
R Jones, M Castanheira, P Rhomberg, L Woosley, M Pfaller
Journal of Clinical Microbiology. March 2010 48: 972-976
http://jcm.asm.org/cgi/content/abstract/48/3/972
Evaluation of the activity of fusidic acid tested against contemporary Gram-positive clinical isolates from the USA and Canada
M Pfaller, M Castaneira, H Sader, R Jones
International Journal of Antimicrobial Agents. March 2010 35: 282-287
http://www.ijaaonline.com/article/S0924-8579(09)00510-X/abstract
Activity of Fusidic Acid Against Methicillin-resistant Staphylococcus Aureus (MRSA) Isolated from CF Patients
Prabhavathi Fernandes, Donald Anderson, K. Kosowska-Shick, P. McGhee, L. Beachel and P.C. Appelbaum
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Evaluation of L6 Ribosomal Protein Alterations in Fusidic Acid-Resistant Staphylococcus aureus: Fitness Cost and Time Kill Analysis
M Castanheira, RN Jones, LN Woosley, RE Mendes, GJ Moet, DJ Farrell
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Fusidic Acid Activity and Coverage of Gram-positive Pathogens Associated with Acute Bacterial Skin and Skin Structure Infections (ABSSSI) in the USA (2008-2010)
RN Jones, DJ Farrell, HS Sader, M Castanheira
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Activity of Fusidic Acid Tested Against Contemporary Staphylococcus aureus Collected from United States Hospitals
M. Castanheira, R.E. Mendes, P.R. Rhomberg, R.N. Jones
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Pharmacokinetics-Pharmacodynamics (PK-PD) of CEM- 102 (Sodium Fusidate) Against Streptococcus pyogenes Using In Vitro Pharmacodynamic Models (IVPM)
B. T. Tsuji, A. Forrest, P. A. Kelchlin, T. Brown, P. N. Holden, O. O. Okusanya, S. M. Bhavnani, P. Fernandes, P. G. Ambrose
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Activity of CEM-102 (sodium fusidate) against 40 MRSA from Cystic Fibrosis Patients
Cynthia Todd, Pamela Mcghee, and Peter Appelbaum
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Ability of CEM-102 (Fusidic Acid), Linezolid, Daptomycin to Select Resistant S.aureus Mutants at Steady-state Serum Levels
K. Kosowska-Shick, P. Mcghee, L. Beachel, P. C. Appelbaum;
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CEM-102 (Fusidic Acid) Maintains Potency against Resistant MRSA and Prevalent Hospital Acquired, Community Acquired,and Epidemic MRSA Clones
C.M. Pillar, M.K. Torres, D.F. Sahm and P. Fernandes
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In Vitro Activity Of Fusicic Acid (CEM-102) Against Resistant Strains Of Staphylococcus aureus
J. dubois, P. Fernandes
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Efficacy and Safety of CEM-102 in a Phase 2, Randomized, Double-Blind Study in Patients with Acute Bacterial Skin and Skin Structure Infections (ABSSSI)
S. R. Moriarty, K. Clark, D. Scott, T. P. Degenhardt, P. Fernandes, J.C. Craft, G.R. Corey, J.G. Still; A Das
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CEM-102 (fusidic acid) in vitro activity and evaluation of molecular resistance mechanisms among European Gram-positive isolates, 2008-2009
M. Castanheira, D. Farrell, M. Janechek, R. Jones
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CEM-102 (Sodium Fusidate) Dosage Regimen Decision Support Using Population Pharmacokinetic (PPK) and Mechanism-Based Pharmacokinetic-Pharmacodynamic (PK-PD) Models
OO OKUSANYA, JB. BULITTA, A FORREST, BT TSUJI, SM BHAVNANI, J GORDON STILL, P FERNANDES, PG AMBROSE
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Contemporary Antimicrobial Activity of CEM-102 (Fusidic Acid [FA)]) Against Canadian Isolates of Staphylococci and Streptococci (2001-2006)
P. R. Rhomberg, L.N. Woosley, H.S. Sader, R. N. Jones
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Update on the Spectrum of CEM-102 (Fusidic Acid [FA)]) Against Contemporary Wildtype (WT) Bacterial Species Including Mutational Resistance (R) Analysis, and Synergy Testing
P. R. Rhomberg, R. E. Mendes, H. K. Becker, K. A. Fedler, H. S. Sader, R. N.
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Performance of CEM-102 (Fusidic Acid [FA)]) Susceptibility Testing Reagents; Broth Microdilution, Disk Diffusion and Etest Methods.
P. R. Rhomberg, L.N. Woosley, H.S. Sader, R. N. Jones
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Relevance of Protein Binding of CEM-102 (Fusidic acid) and its pH-dependent Effect on in vitro Activity
TP Degenhardt, PR Rhomberg, RN Jones, P Fernandes, D Johnson
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Contrasting Effect of Acidic pH on the Bactericidal Activities of CEM-102 (Fusidic Acid) vs. Linezolid and Clindamycin Towards Staphylococcus aureus
PM Tulkens, S Lemaire, F Van Bambeke
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Pharmacokinetics-Pharmacodynamics (PK-PD) of CEM-102 against Methicillin-Resistant Staphylococcus aureus (MRSA) using an In Vitro PD Model (IVPM) and Mechanism-Based (MB) Modeling
BT Tsuji, JB Bulitta, A Forrest, PA Kelchlin, T Brown, PN Holden, MP Pai, SM Bhavnani, P Fernandes, RN Jones, PG Ambrose
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Low CEM-102 (Fusidic Acid [FA]) Resistance (R) Rates and High Prevalence of Acquired (acq) Genes Among Staphylococcus spp. (SSP) from North America and Australia
M Castanheira, AA Watters, JM Bell, RN Jones, JD Turnidge
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Assessment of In Vivo Activity of CEM-102 (Fusidic Acid) in Murine Infection Models
T Murphy, S Little, R Wu, A Slee, P Fernandes
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Initial Quality Control (QC) Ranges for Fusidic Acid (FA) Using the CLSI Multi-Laboratory M23-A3 Study Design
RN Jones, JE Ross
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Population Pharmacokinetics (PPK) of CEM-102 in Healthy Subjects
JB Bulitta, OO Okusanya, A Forrest, SM Bhavnani, D Reynolds, MP Pai, JG Still, PB Fernandes, PG Ambrose
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Pharmacokinetics and Safety of Single, Multiple, and Loading Doses of CEM-102 in Healthy Subjects
JG Still, K Clark, TP Degenhardt, D Scott, P Fernandes, MJ Gutierrez
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From Mouse to Man: The Pharmacokinetics of CEM-102 (Fusidic acid)
TP Degenhardt, JG Still, K Clark, P Fernandes
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