“As resistance is now a leading cause of HIV treatment failure and a major concern for people living with HIV/AIDS, these are important data,” said Professor Brian Gazzard of Chelsea and Westminster Hospital, London. “There is widely overlapping cross-resistance among the currently approved NNRTIs which can render the class ineffective once resistance has developed. From the data collected so far, TMC125 seems to be quite different from existing NNRTIs in that it continues to be active in the presence of NNRTI-resistant virus.”
The ability of HIV to develop mutant strains that are resistant to HIV drugs is one of the main reasons why people living with HIV experience treatment failure. A recent study in North America showed that nearly 80% of people with HIV infection, who have detectable concentrations of the virus in their bloodstream, are carrying mutated versions of the virus that are resistant to at least one of the currently available antiretroviral medications.
This study (C207) was a phase IIa open label trial. Sixteen treated-experienced HIV patients with documented evidence of highly NNRTI-resistant virus and currently failing on a NNRTI regimen received TMC125, as a substitute for their failing NNRTI, for one week. NNRTI therapy continued unchanged.
NNRTI mutations found among study participants included L100I, K103N, Y181C, Y188L and G190A/S, with 12 patients having multiple NNRTI mutations. None of the subjects experienced any rebound in viral load and there was no genotypic or phenotypic evidence of the development of resistance to TMC125 during the one week trial. TMC125 was well tolerated during this study.
“We are delighted that TMC125 has performed well in this study,” commented Neil Graham MD, Vice President of the Medical Department, Tibotec-Virco. “TMC125, one of a series of DAPY derivatives, was selected for clinical development on the basis of its novel in vitro antiviral profile and its in vitro potency against NNRTI resistant HIV. These early clinical data confirm our view that TMC125 is a next generation NNRTI and suggest that TMC125 could become a major contributor to more effective HIV therapy in the future.”
In response to the emerging needs for new HIV therapeutics, Tibotec-Virco has developed and implemented a unique parallel drug profiling strategy to accelerate drug discovery and development.
About Tibotec-Virco
Tibotec-Virco is a biopharmaceutical company with headquarters in Belgium and operating subsidiaries in the United States and Ireland.
Tibotec-Virco is dedicated to the development of novel, new drugs for HIV/AIDS and hepatitis C with the ultimate aim of enhancing and extending peoples’ lives. The Company is focusing on the discovery and development of HIV/AIDS compounds that are active against both wild-type and drug resistant strains of HIV; HIV drug resistance is a major cause of treatment failure.
Tibotec-Virco has two novel antiretroviral compounds in phase II clinical development; TMC125, a non-nucleoside reverse transcriptase inhibitor (NNRTI) and TMC114, a protease inhibitor (PI).
The Company is widely regarded as a world leader in HIV resistance testing. It has built the world’s largest relational database of more than 120,000 HIV genotypes and phenotypes and has developed unique HIV disease management tools such as the VirtualPhenotype™. Combining the strengths of genotyping and phenotyping, the VirtualPhenotype™ provides physicians with comprehensive, accurate and cost-effective HIV resistance information for improved patient management.
The company was formed from the merger of Virco Group NV and Tibotec Group NV on March 14, 2001 and brings together the complementary expertise of Tibotec in drug discovery and development and that of Virco in pharmacogenomics and molecular diagnostics.
For further information, please visit Tibotec-Virco’s website: http://www.tibotec-virco.com
Contacts: Peter Vigliarolo, Cooney Waters – 212/886-2200
Karen Manson, VP Corporate Communications
+32 479 89 47 99 (mobile)
Dr. Neil Graham, VP Medical Department – 919/201-1915 (mobile)