2010年12月6日 星期一

Ceftraroline, a 5th. generation cephalosporin

FDA approves Ceftraroline for CABP and cSSSI


Fran Lowry



September 8, 2010 — The Anti-Infective Drugs Advisory Committee of the US Food and Drug Administration (FDA) has heartily endorsed ceftaroline (Cerexa Inc) for the treatment of community-acquired bacterial pneumonia (CABP) and complicated skin and skin structure infections (cSSSI).


At yesterday's meeting, in the morning session, the committee voted 21 to 0 in favor of ceftaroline for CABP, and in the afternoon, a slightly smaller committee voted 18 to 0 in favor of its use for cSSSI. There were no abstentions.


The committee was warm in its praise of the sponsor and the data it presented for both indications.


Ceftaroline is a beta-lactam of the cephalosporin class of antimicrobials with activity against aerobic and anaerobic gram-positive and aerobic gram-negative bacteria associated with skin and respiratory infections. It also has activity against methicillin-resistant Staphylococcus aureus and Streptococcus pneumonia.


Members of the committee said they found it very easy to cast their affirmative votes when asked whether the sponsor had demonstrated safety and efficacy in CABP and cSSSI.


CABP Indication


"I thought this was a relatively easy decision to make," commented Dean Follmann, MD, from the National Institute of Allergy and Infectious Diseases of the National Institutes of Health, Bethesda, Maryland, in explaining his yes vote for the CABP indication.


"It was a very easy decision to make. The noninferiority margin was preserved in instances. In fact, it seemed that cefteroline was strong enough to perhaps star in its own Old Spice commercial," said committee chair Thomas Moore, MD, from Ochsner Health System, New Orleans, Louisiana.


Erica Brittain, PhD, from the National Institute of Allergy and Infectious Diseases of the National Institutes of Health, said she wished all noninferiority trials were this easy to interpret, adding that she was "very impressed that there were hints of superiority all over the place" for ceftaroline.


John E. Bennett, MD, also from the National Institutes of Health, congratulated the manufacturer for a "well-designed, carefully conducted and conservatively analyzed study" and said he was impressed by the quality of the data.


However, he voiced one concern about the generalizability of the data supporting the CABP indication, which were collected in an eastern European population, to patients in the United States. "This population seems to be less sick than patients in this country, but apparently it's impossible to conduct these kinds of studies in the United States. I believe they tried, but I'm not completely assured that we could extrapolate those results to our patients."


One of the pediatricians on the panel, Sheldon L. Kaplan, MD, from Baylor College of Medicine and Texas Children's Hospital, Houston, said he was looking forward to the pediatric studies that the sponsor had promised. "I think this is a potentially fabulous drug for pediatric patients — one that will be very helpful to us — and I hope that we will have much more information on penetration into the [cerebrospinal fluid] because that is always a concern in patients who have pneumococcal bacteremia in particular."


cSSSI Indication


The committee was equally positive about ceftaroline for cSSSI, although some members voiced minor concerns.


Peter Katona, MD, from the David Geffen School of Medicine at the University of California–Los Angeles, said, "I have to admit, I have a weak spot for anything that could replace 2 drugs with 1 drug, which I hope is something that this drug could eventually do."


"I'm impressed at how difficult it is to get a homogeneous group of patients with skin and soft tissue [infections] together," commented Kent A. Sepkowitz, MD, from Memorial Sloan-Kettering Cancer Center, New York City. "The sponsor did a decent job."


Dr. Moore said that cefteroline is now the poster child of how to get through the new FDA endpoints. He also thanked the FDA for their hard work "in crunching the data," adding that this emphasized the effectiveness of the drug.




Medscape Medical News © 2010 WebMD, LLC


[Ceftaroline is a broad-spectrum cephalosporin. Ceftaroline has the ability to bind to penicillin-binding protein (PBP) 2a , an MRSA-specific PBP that has low affinity for most other β-lactam antibacterials. The high binding affinity of ceftaroline to PBP 2a (median inhibitory concentration 0.90μg/mL) correlates well with its low minimum inhibitory concentration for MRSA. Ceftaroline is active in vitro against Gram-positive cocci, including MRSA, meticillin-resistant Staphylococcus epidermidis, penicillin-resistant Streptococcus pneumoniae and vancomycin-resistant Enterococcus faecalis (not E. faecium). The broad-spectrum activity of ceftaroline includes many Gram-negative pathogens but does not extend to extended-spectrum β-lactamase-producing or AmpC-derepressed Enterobacteriaceae or most nonfermentative Gram-negative bacilli. Ceftaroline demonstrates limited activity against anaerobes such as Bacteroides fragilis and non-fragilis Bacteroides spp. Limited data show that ceftaroline has a low propensity to select for resistant subpopulations.


Ceftaroline fosamil (prodrug) is rapidly converted by plasma phosphatases to active ceftaroline. For multiple intravenous doses of 600mg given over 1h every 12 hours for 14 days, the maximum plasma concentration was 19.0μg/mL and 21.0μg/mL for first and last dose, respectively. Ceftaroline has a volume of distribution of 0.37 L /kg ( 28.3 L ), low protein binding (<20%) and a serum half-life of 2.6 hours. No drug accumulation occurs with multiple doses and elimination occurs primarily through renal excretion (49.6%). Based on Monte Carlo simulations, dosage adjustment is recommended for patients with moderate renal impairment (creatinine clearance 30–50mL/min); no adjustment is needed for mild renal impairment.


Currently, limited clinical trial data are available for ceftaroline. A phase II study randomized 100 patients with cSSSI to intravenous ceftaroline 600mg every 12 hours or intravenous vancomycin 1g every 12 hours with or without intravenous aztreonam 1g every 8 hours (standard therapy) for 7–14 days. Clinical cure rates were 96.7% for ceftaroline compared with 88.9% for standard therapy. Adverse events were similar between groups and generally mild in nature. In a phase III trial, 702 patients with cSSSI were randomized to ceftaroline 600mg or vancomycin 1g plus aztreonam 1g, each administered intravenously every 12 hours for 5–14 days. Ceftaroline was noninferior to vancomycin plus aztreonam in treating cSSSI caused by both Gram-positive and -negative pathogens. Adverse event rates were similar between groups.


Ceftaroline is well tolerated, which is consistent with the good safety and tolerability profile of the cephalosporin class. In summary, ceftaroline is a promising treatment for cSSSI and CAP, and has potential to be used as monotherapy for polymicrobial infections because of its broad-spectrum activity. Further clinical studies are needed to determine the efficacy and safety of ceftaroline, and to define its role in patient care.]


 


[Ceftaroline (INN) ( brand name Teflaro) is a fifth-generation cephalosporin antibiotic. It is notable for its activity against methicillin-resistant Staphylococcus aureus (MRSA) and Gram positive bacteria. It retains the activity of later generation cephalosporins having broad spectrum activity against Gram negative bacteria. It is currently being investigated for community-acquired pneumonia and complicated skin and skin structure infection.


Ceftaroline is being developed by Forest Laboratories, under a license from Takeda. Ceftaroline has received approval from the U.S. Food and Drug Administration for the treatment of community-acquired bacterial pneumonia and acute bacterial skin infections on October 29, 2010. In vitro studies show that it has a similar spectrum to ceftobiprole, the only other fifth-generation cephalosporin to date, although no head to head clinical trials have been conducted. Currently, ceftaroline and ceftobiprole are on an unnamed subclass of cephalosporins by the Clinical and Laboratory Standards Institute (CLSI).]



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