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Ciclofilin Pharmaceuticals to Present at HEP DART 2015 Research Shows CPI-431-32 Drug Candidate Completely Suppresses HBV HBsAg Production and Reduces Liver Fibrosis
November 30, 2015 09:30 ET | Source: Ciclofilin Pharmaceuticals Inc.
SAN DIEGO, Nov. 30, 2015 (GLOBE NEWSWIRE) -- Ciclofilin Pharmaceuticals Inc. ("Ciclofilin" or the "Company"), a privately held biotech, announced today that it will discuss the antiviral and anti-fibrotic effects of its lead drug candidate for chronic hepatitis B, CPI-431-32, during a presentation at the HEP DART 2015 conference in Wailea, Hawaii, on December 6-10.
Entitled "The Cyclophilin Inhibitor, CPI-431-32, is a Hepatitis B Oral Drug Candidate with Antiviral and Antifibrotic Activities," the presentation will review the recent results of a series of experiments conducted by Ciclofilin in partnership with Dr. Philippe Gallay's research laboratory at The Scripps Research Institute, the National Institutes of Health, and Stelic Institute (Japan). With a broad scope, the studies examined: 1) in vitro determination of HBsAg and HBeAg in infected and transfected Huh7 cells; 2) transgenic mouse model; 3) NASH mouse model; 4) HBV transport of sodium taurocholate co-transporting polypeptide ("NTCP"); 5) single oral dose rat pharmacokinetics; 6) PgP and MRP transporter studies; and 7) cytotoxicity in human cell lines and primary liver cells.
Now concluded, the study results demonstrate that: 1) CPI-431-32 can completely suppress both HBsAg (100%) and HBeAg; 2) HBV DNA in the mouse liver is reduced by oral administration of CPI-431-32; 3) oral dosing of CPI-431-32 significantly reduced fibrosis scores in the NASH mouse model; 4) CPI-431-32 blocks HBV cellular entry; 5) oral bioavailability of CPI-431-32 is approximately double that of cyclosporine ("CsA"); 6) CPI-431-32 demonstrates reduced inhibition of PgP and MRP compared with CsA; and 7) there is a clear separation between in vitro CC50 and IC50 values. Taken together, these results validate the important role that cyclophilins play in HBV and fibrosis, and underscore the therapeutic potential of CPI-431-32.
"To date, our research has shown that CPI-431-32 inhibits virus transport into cells via NTCP, and completely suppresses HBsAg and HBeAg production," explained Dr. Robert Foster, Ciclofilin's CEO. "Our lead drug candidate demonstrated efficacy at concentrations that were well below those exhibiting signs of cytotoxicity in a number of cell lines. We also determined that CPI-431-32 is efficacious and safe in animal models, and that its pharmacokinetics are completely in line with the necessary requirements to move toward the clinic. Finally, CPI-431-32 dosing in a NASH model suggests there may be added, anti-fibrotic benefits from the drug."
"It is becoming increasingly important to find drugs that suppress HBsAg while possessing other beneficial properties, and CPI-431-32 clearly fulfills this criteria," commented Dr. Philippe Gallay. "As others have pointed out, cyclophilins will play a major role in the HBV life cycle in hepatocytes. These studies were largely carried out at the Scripps Research Institute in my laboratory, and the results are compelling. CPI-431-32 deserves our focused attention."
Dr. Tarek Hassanein,Professor of Medicine, UCSD School of Medicine commented, "The data looks very impressive in dropping the surface antigen and it would be of great importance if we can duplicate it in our patients."
About Ciclofilin:
Ciclofilin is a privately held life sciences company based in San Diego, California, with R&D facilities in Edmonton, Canada.The company's lead drug candidate, CPI-431-32, is being developed as a treatment for chronic HBV infection. CPI-431-32 interferes with the ability of the HBV to infect cells, propogate, and cause disease primarily by preventing HBV interaction with host cell cyclophilins. CPI-431-32 also demonstrates anti-fibrotic activity in the liver, and may offer clinical benefits to patients in addition to anti-HBV activity.
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发表于 2015-12-1 09:43
