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Chimerix's Antiviral CMX157 Demonstrates Positive Phase 1 Clinical Results With Favorable Pharmacokinetics, Safety and Tolerability
Date:12/13/2010

157. PBMC levels of TFV-PP remained detectable for six days after the single 400 mg dose of CMX157, suggesting the possibility of a convenient, once-weekly dosing regimen.

CMX157 In Vitro Activity

The in vitro antiviral activity of CMX157 was evaluated in PBMCs for wild-type and nucleotide reverse transcriptase inhibitors (NRTI)-resistant HIV strains.  CMX157 was effective and highly potent against all clinically-important HIV strains, including drug resistant isolates that are known to be unresponsive to tenofovir.  CMX157 was observed to have highly potent antiviral activity against XMRV in vitro, with an EC50 approximately 20-fold more potent than the anti-retroviral drug azidothymidine (AZT) and 800-fold more potent than tenofovir.  Data were also presented that showed CMX157 is not a substrate in vitro for human Organic Anion Transporter 1 (hOAT1), which actively transports tenofovir into renal proximal tubule cells of the kidney and is linked to tenofovir-induced nephrotoxicity.  Consequently, CMX157 has significantly reduced potential to cause nephrotoxicity.

CMX157 findings were featured in an oral presentation, CMX157 (Hexadecyloxypropyl Tenofovir), a Clinical Stage Antiretroviral with In Vitro Activity against HIV and XMRV, by Randall Lanier, Ph.D., Senior Director of Virology of Chimerix, at the HIV DART 2010 Frontiers in Drug Development for Antiretroviral Therapies conference.  A copy of Dr. Lanier's oral presentation and poster are available on the Chimerix website at www.chimerix.com.  

About CMX157

CMX157 is a new chemical entity created by applying Chimerix's PIM (Phospholipid Intramembrane Microfluidization) Conjugate Technology to chemically modify tenofovir, marketed as the prodrug Viread, an antiviral agent approved for the treatment of HIV and chronic hepatitis B. Chimerix's propr
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SOURCE Chimerix, Inc.
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