Yardley, Pa. -- Tibotec, Inc. announced today it plans to initiate an expanded access program (EAP) for its investigational protease inhibitor, TMC114, in the autumn of this year for people with HIV/AIDS who need the compound to construct a viable treatment regimen. The company also announced that it plans to seek accelerated approval for TMC114 in the United States and Europe through regulatory submissions filed by early 2006 based principally on the 24-week primary analyses of the company's two phase IIB trials.

Initiation of enrollment into the expanded access program -- which will be for heavily treatment-experienced adults living with HIV/AIDS -- is contingent on the approval of local health authorities and recruitment of pivotal phase III trials. Expanded access programs provide people with severe or life-threatening illnesses with access to treatments currently being evaluated in clinical trials.

"We know that many people living with HIV/AIDS have run out of treatment options because of the increasingly significant issue of viral resistance, and we are working to provide them with access to TMC114 as soon as possible through this program," said Paul Stoffels, M.D., President of Tibotec.

TMC114 belongs to a class of antiretroviral agents known as protease inhibitors. Protease inhibitors are commonly used in combination with other classes of anti-HIV drugs to prevent the replication of HIV in the body.

The TMC114 expanded access program will be administered by local operating entities within Johnson & Johnson, and will be supported by i3 Research in the U.S. and Parexel outside the U.S. Pending local regulatory approvals, the product will be commercialized by Tibotec Therapeutics in the U.S. and Janssen-Cilag and other affiliates outside the U.S.

Data Presented at CROI, Boston, February 22-25, 2005

Data from a 24-week combined interim analysis of the phase IIB trials of TMC114 were presented at the 12th Conference on Retroviruses and Opportunistic Infections (CROI). That analysis included two phase IIB (dose-finding), randomized trials of TMC114 boosted with ritonavir (TMC114/RTV) in patients with experience of at least three classes of antiretrovirals and with one or more primary protease inhibitor mutations. Patients in the highest dose group, 600mg/100mg BID, experienced a mean reduction in plasma HIV RNA of -1.85 log₁₀, compared to a reduction of -0.27 log₁₀ in the control group. Patients were randomized to receive optimized background regimen (OBR) plus one of four doses of TMC114/RTV (400mg/100mg QD; 800mg/100mg QD; 400mg/100mg BID; 600mg/100mg BID) or optimized background regimen (OBR) plus investigator-selected control protease inhibitor(s). The interim analysis was performed after 150 patients had reached 24 weeks in each of the two studies; a total of 497 patients were included in the analysis.

After 24 weeks, the percentage of patients reaching undetectable virus levels (<50 copies/ml) ranged from 30% (lowest dose group) to 47% (highest dose group) in the TMC114/RTV arms, compared with 10% in the control arm. The most common adverse events were headache and diarrhea, which were 17% and 14% respectively across all TMC114/RTV arms compared with 23% and 20% in the control arm. 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.

Tibotec Inc., Janssen-Cilag and Tibotec Therapeutics are members of the Johnson & Johnson family of companies.