TMC-114 to be submitted for registration based on Phase 2b trial results: expanded access expected in UK in Autumn 2005

Based on the results from Phase 2 studies, and supported by safety data in a rapidly enrolled group of 300 additional patients, Tibotec announced on 15 June that it plans to submit its new protease inhibitor (TMC114) for early approval. This is the first time in ten years (since indinavir) that Phase 2 data have been sufficiently impressive, in a population with currently unmet treatment needs, to justify accelerating approval even more quickly than current Fast Track system. TMC-114 has activity against a broad range of currently PI-resistant virus.

Importantly, an expanded access programme will start in the Autumn 2005, that will provide guaranteed access to TMC-114 for people in greatest need of life-saving treatment. This will be an international programme (initially 24,000 places worldwide) for heavily treatment-experienced adults, with CD4 count <100 cells/mm3. The planned phase 3 studies will continue to recruit and enroll patients with higher CD4 counts.

The results from the 24-week combined interim analysis of the phase IIB trials of TMC114 were presented at the 12th Conference on Retroviruses and Opportunistic Infections (CROI) in February this year and were covered in HTB April 2005. [1]

Patients in the highest dose group, 600mg/100mg BID, plus optimised background regimen, experienced a mean reduction in plasma HIV RNA of -1.85 log, compared to a reduction of -0.27 log in the control group. These studies will continue to 144 weeks.

Based on these 24-week results, the selected dose of TMC114/RTV for treatment-experienced patients in phase III trials is 600mg/100mg BID. TMC114 will be studied in both treatment-experienced and -naive patients in phase III trials.