Cempra Pharmaceuticals, Inc. Profiles the Broad Spectrum and Potent Activity Profile of Solithromycin (CEM-101) at the 5th Annual PHEMCE Stakeholders Workshop and BARDA Industry Day

CHAPEL HILL, N.C., Jan. 12, 2011 /PRNewswire/ -- Cempra Pharmaceuticals presented the broad spectrum and potent activity profile of solithromycin (CEM-101), the first fluoroketolide antibiotic, at the 5th Annual PHEMCE stakeholders workshop and Biomedical Advanced Research and Development Authority (BARDA) industry day on January 10 to 12 in Washington D.C.

Solithromycin is a clinical-stage fluoroketolide antibiotic with potent and broad-spectrum activity against gram-positive and gram-negative pathogens, including multidrug-resistant strains, non-bacterial pathogens such as Plasmodium falciparum and a variety of bio-defense pathogens including Bacillus anthracis, Yersiniapestis, Burkholderiamallei and Francisellatularensis. Phase 1 clinical studies with the oral formulation have shown excellent safety and tolerability and a pharmacokinetic profile that will enable once-daily dosing. The oral formulation is undergoing a Phase 2 clinical trial in patients with community-acquired bacterial pneumonia (CABP). An intravenous (IV) formulation of solithromycin is undergoing a safety and tolerability evaluation in a Phase 1 single and multiple dose escalation trial in healthy volunteers. An oral pediatric suspension is also under development.

The presentation, delivered on January 12 by Jennifer Schranz, M.D., vice president of clinical affairs at Cempra Pharmaceuticals, described the potential utility of solithromycin as a bio-defense agent due to its broad antimicrobial spectrum, safety and tolerability, once-daily dosing, high tissue penetration, intracellular accumulation, and compound stability. Data from mouse models were presented on the activity of once-daily solithromycin compared to an optimal dosing regimen of ciprofloxacin against B. anthracis and gentamicin against F. tularensis. Solithromycin demonstrated activity comparable to ciprofloxacin against B. anthracis, despite a less than optimal dose. Solithromycin also delayed mortality in mice for days after dosing against F. tularensis. Future studies will evaluate optimal doses of solithromycin based on PK/PD modeling and the current therapeutic regimen being tested in Phase 2.

“Solithromycin is emerging as a very promising broad spectrum, well-tolerated antibiotic,” said Prabhavathi Fernandes, Ph.D., Chief Executive Officer of Cempra Pharmaceuticals. “Pre-clinical and clinical data collected to date show it to have a broad activity spectrum and to be well tolerated in healthy volunteers. Its flexibility of administration including once-daily oral, oral suspension and intravenous, its high tissue penetration, especially in blood and lung including lung macrophages, and its ability to target intracellular pathogens, demonstrate its significant potential for both civilian and bio-defense applications. Building a safety and efficacy database for civilian bacterial pneumonia coupled with meeting the animal rule, which is a unique regulatory mechanism to gain FDA approval based on animal data when well-controlled efficacy studies in humans is not ethical or feasible, could be a path forward for approval for bio-defense indications.”

About solithromycin (CEM-101)

Solithromycin is the first fluoroketolide with a number of attributes that may provide clinically important advantages over several comparator products:

• 8 to 16 times more potent than azithromycin and is active against organisms that have become resistant to azithromycin
• Potent in vitro activity against all important respiratory pathogens, including pneumococci, beta-hemolytic streptococci, staphylococci, Hemophilus, Legionella, Mycoplasma, Moraxella and Chlamydophila
• Potent in vitro activity against other medically significant pathogens including CA-MRSA, M. avium, malaria, enterococci and gonococci
• Good tolerability to date as demonstrated in phase 1 trials of the oral formulation
• Low resistance frequency in vitro
• Unlike telithromycin, solithromycin does not inhibit the 7 acetylcholine nicotinic receptor; such inhibition is believed responsible for certain adverse effects observed with telithromycin (Ketek®).
• Excellent tissue distribution and intracellular tissue concentrations including lung epithelial lining fluid and alveolar macrophages
• Oral and IV formulations concurrently in development
• Once-daily dosing
• Potential for indications beyond CABP, including urethritis and other urogenital infections, bioterrorism targets, malaria, M. avium infections and tuberculosis.

About Cempra Pharmaceuticals

Founded in 2006, Cempra Pharmaceuticals is a privately-held, clinical-stage biotechnology company focused on developing antibacterials to address critical medical needs. Two lead products, both in late-stage clinical trials, address the urgent and increasing need for new treatments targeting drug-resistant bacterial infections in the hospital and in the community. Cempra is well-funded and is committed to developing commercially viable products through consideration of pricing and reimbursement issues throughout its products’ lifecycles. The company is also utilizing its proprietary chemistry technology to develop macrolides without antibacterial activity for non-antibiotic uses in motilin receptor activity, anti-inflammatory activity and GnRH receptor antagonism. Additional information about Cempra can be found at www.cempra.com.

SOURCE Cempra Pharmaceuticals