Taksta

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Taksta (previously CEM-102) is a front-loaded oral dosing regimen of sodium fusidate under development in the U.S. as an antibiotic for gram-positive infections including drug-resistant strains such as methicillin-resistant Staphylococcus aureus (MRSA). [1]

Methicillin-resistant <i>Staphylococcus aureus</i> bacterium responsible for difficult-to-treat infections in humans

Methicillin-resistant Staphylococcus aureus (MRSA) refers to a group of gram-positive bacteria that are genetically distinct from other strains of Staphylococcus aureus. MRSA is responsible for several difficult-to-treat infections in humans. MRSA is any strain of S. aureus that has developed, through horizontal gene transfer and natural selection, multiple drug resistance to beta-lactam antibiotics. β-lactam antibiotics are a broad spectrum group which includes some penams – penicillin derivatives such as methicillin and oxacillin, and cephems such as the cephalosporins. Strains unable to resist these antibiotics are classified as methicillin-susceptible S. aureus, or MSSA.

Contents

Clinical trials

Jan 2010: Taksta has completed enrollment in a Phase 2 trial (due to run until March 2010) and is preparing for Phase 3 studies in the U.S. for acute bacterial skin structure infections (being compared with Linezolid). [2]

A skin and skin structure infection (SSSI), also referred to as skin and soft tissue infection (SSTI) or acute bacterial skin and skin structure infection (ABSSSI), is an infection of skin and associated soft tissues. The pathogen involved is usually a bacterial species. Such infections often requires treatment by antibiotics.

Linezolid chemical compound

Linezolid is an antibiotic used for the treatment of infections caused by Gram-positive bacteria that are resistant to other antibiotics. Linezolid is active against most Gram-positive bacteria that cause disease, including streptococci, vancomycin-resistant enterococci (VRE), and methicillin-resistant Staphylococcus aureus (MRSA). The main uses are infections of the skin and pneumonia although it may be used for a variety of other infections including drug resistant tuberculosis. It is used either by injection into a vein or by mouth.

Sep 2010: Taksta demonstrated comparable clinical success rates compared to linezolid in a Phase 2 trial in the U.S. for acute bacterial skin and skin structure infections. [3]

Jun 2011: Taksta may be effective in the treatment of chronic prosthetic joint infections and osteomyelitis. [4]

Dec 2015: Cempra Doses First Patient in Phase 3 Clinical Trial of Taksta(TM) in Acute Bacterial Skin and Skin Structure Infections. (2015) [5]

Nov 2016: Cempra completes Phase 3 Clinical Trial of Taksta(TM) in Acute Bacterial Skin and Skin Structure Infections. Results remain pending. (2016) [6]

Feb 2017: Cempra achieves the primary endpoint of a 10% non-inferiority margin. The microbiological success in each ME population with methicillin-resistant S. aureus (MRSA) infection is 100 percent (99/99) at both the EOT and PTE visits. (2017) [7]

See also

Related Research Articles

<i>Staphylococcus aureus</i> species of bacterium

Staphylococcus aureus is a Gram-positive, round-shaped bacterium that is a member of the Firmicutes, and it is a usual member of the microbiota of the body, frequently found in the upper respiratory tract and on the skin. It is often positive for catalase and nitrate reduction and is a facultative anaerobe that can grow without the need for oxygen. Although S. aureus usually acts as a commensal of the human microbiota it can also become an opportunistic pathogen, being a common cause of skin infections including abscesses, respiratory infections such as sinusitis, and food poisoning. Pathogenic strains often promote infections by producing virulence factors such as potent protein toxins, and the expression of a cell-surface protein that binds and inactivates antibodies. The emergence of antibiotic-resistant strains of S. aureus such as methicillin-resistant S. aureus (MRSA) is a worldwide problem in clinical medicine. Despite much research and development, no vaccine for S. aureus has been approved.

Fusidic acid chemical compound

Fusidic acid is an antibiotic that is often used topically in creams and eyedrops but may also be given systemically as tablets or injections. The global problem of advancing antimicrobial resistance has led to a renewed interest in its use recently.

Glycopeptide antibiotics are a class of drugs of microbial origin that are composed of glycosylated cyclic or polycyclic nonribosomal peptides. Significant glycopeptide antibiotics include the anti-infective antibiotics vancomycin, teicoplanin, telavancin, ramoplanin and decaplanin, and the antitumor antibiotic bleomycin. Vancomycin is used if infection with methicillin-resistant Staphylococcus aureus (MRSA) is suspected.

Tigecycline chemical compound

Tigecycline is an antibiotic for a number of bacterial infections. It is a glycylcycline administered intravenously. It was developed in response to the growing rate of antibiotic resistant bacteria such as Staphylococcus aureus, Acinetobacter baumannii, and E. coli. As a tetracycline derivative antibiotic, its structural modifications has expanded its therapeutic activity to include Gram-positive and Gram-negative organisms, including those of multi-drug resistance.

Flucloxacillin chemical compound

Flucloxacillin (INN) or floxacillin (USAN) is a narrow-spectrum beta-lactam antibiotic of the penicillin class. It is used to treat infections caused by susceptible Gram-positive bacteria. Unlike other penicillins, flucloxacillin has activity against beta-lactamase-producing organisms such as Staphylococcus aureus as it is beta-lactamase stable. However, it is ineffective against methicillin-resistant Staphylococcus aureus (MRSA). It is very similar to dicloxacillin; they are considered interchangeable. Flucloxacillin is supplied under a variety of trade names including Floxapen, Flopen (CSL), Staphylex (Alphapharm), Softapen, Flubex, and Flupen. It is no longer available in the United States.

Pristinamycin group of chemical compounds

Pristinamycin (INN), also spelled pristinamycine, is an antibiotic used primarily in the treatment of staphylococcal infections, and to a lesser extent streptococcal infections. It is a streptogramin group antibiotic, similar to virginiamycin, derived from the bacterium Streptomyces pristinaespiralis. It is marketed in Europe by Sanofi-Aventis under the trade name Pyostacine.

Oritavancin pharmaceutical drug

Oritavancin is a novel semisynthetic glycopeptide antibiotic for the treatment of serious Gram-positive bacterial infections. Its chemical structure as a lipoglycopeptide is similar to vancomycin.

Ceftobiprole chemical compound

Ceftobiprole (Zevtera/Mabelio) is a new 5th-generation cephalosporin for the treatment of hospital-acquired pneumonia and community-acquired pneumonia (CAP). It is marketed by Basilea Pharmaceutica in the United Kingdom, Germany, Switzerland and Austria under the trade name Zevtera, in France and Italy under the trade name Mabelio. Like other cephalosporins, ceftobiprole exerts its antibacterial activity by binding to important penicillin-binding proteins and inhibiting their transpeptidase activity which is essential for the synthesis of bacterial cell walls. Ceftobiprole has high affinity for PBP2a of methicillin-resistant Staphylococcus aureus (MRSA) strains and retains its activity against strains that express divergent mecA gene homologues. Ceftobiprole also binds to PBP2b in Streptococcus pneumoniae (penicillin-intermediate), to PBP2x in S. pneumoniae, and to PBP5 in Enterococcus faecalis.

Targanta Therapeutics Corporation was a biopharmaceutical company headquartered in Cambridge, Massachusetts. The company also had operations in Indianapolis, Montreal and Toronto. Targanta completed its initial public offering on October 9, 2007 and traded on the Nasdaq market under the symbol: TARG. Targanta was acquired by The Medicines Company in 2009.

Dalbavancin chemical compound

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Delafloxacin chemical compound

Delafloxacin is a fluoroquinolone antibiotic used to treat acute bacterial skin and skin structure infections.

Tedizolid chemical compound

Tedizolid, is an oxazolidinone-class antibiotic. Tedizolid phosphate is a phosphate ester prodrug of the active compound tedizolid. It was developed by Cubist Pharmaceuticals, following acquisition of Trius Therapeutics, and is marketed for the treatment of acute bacterial skin and skin structure infections.

Ceftaroline fosamil chemical compound

Ceftaroline fosamil (INN), brand name Teflaro in the US and Zinforo in Europe, is a cephalosporin antibiotic with anti-MRSA activity. It is active against methicillin-resistant Staphylococcus aureus (MRSA) and other Gram-positive bacteria. It retains some activity of later-generation cephalosporins having broad-spectrum activity against Gram-negative bacteria, but its effectiveness is relatively much weaker. It is currently being investigated for community-acquired pneumonia and complicated skin and skin structure infection.

NXL103 is an experimental drug candidate under development by Novexel. It is an oral streptogramin antibiotic that has potent in vitro activity against certain Gram positive bacteria including methicillin resistant Staphylococcus aureus (MRSA) as well as the important respiratory pathogens including penicillin-, macrolide- and quinolone-resistant strains. It is a combination of linopristin and flopristin.

Lipoglycopeptides are a class of antibiotic that have lipophilic side-chains linked to glycopeptides. The class includes oritavancin, telavancin and dalbavancin.

Omadacycline chemical compound

Omadacycline is a broad spectrum antibiotic belonging to the aminomethylcycline subclass of tetracycline antibiotics. In the United States, it was approved in October 2018 for the treatment of community-acquired bacterial pneumonia and acute skin and skin structure infections.

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References

  1. ↑ "Cempra Announces Expansion of Clinical Management Team to Advance Leading Antibacterial Clinical Programs TAKSTA(TM) and CEM-101".
  2. ↑ "Safety and Efficacy of CEM-102 Compared to Linezolid in Acute Bacterial Skin Infections".
  3. ↑ Craft JC, Moriarty SR, Clark K, Scott D, Degenhardt TP, Still JG, Corey GR, Still JG, Das A, Fernandes P (2011). "A randomized, double-blind Phase 2 study comparing the efficacy and safeety of an oral fusidic acid loading-dose regimen to oral linezolid in the treatment of acute bacterial skin and skin structure infections." Clinical Infectious Diseases 52(Supplement 7):S520-S226.
  4. ↑ Wolfe CR. (2011) "Case report: treatment of chronic osteomyelitis." Clinical Infectious Diseases 52(Supplement 7):S538-S541.
  5. ↑ Cempra Press Release. Cempra Company http://investor.cempra.com/releasedetail.cfm?releaseid=946010 . Retrieved 17 December 2016.Missing or empty |title= (help)
  6. ↑ "Oral Sodium Fusidate (CEM-102) Versus Oral Linezolid for the Treatment of Acute Bacterial Skin and Skin Structure Infections". ClinicalTrials.gov. FDA. Retrieved 17 December 2016.
  7. ↑ "Cempra's Fusidic Acid Achieves Primary Endpoint in Phase 3 Study of ABSSSI". Cempra.com. Cempra. Retrieved 4 April 2017.


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