48 Week Data on Investigational Antiretroviral TMC125 From Tibotec

Toronto (ots/PRNewswire) -

- TMC125 a Next-Generation NNRTI

Tibotec Pharmaceuticals Ltd. presented 48 week efficacy and safety
data on TMC125, a next-generation non-nucleoside reverse
transcriptase inhibitor (NNRTI), at the 16th International AIDS
conference (IAC), AIDS 2006, in Toronto, Canada this week. TMC125 is
currently being investigated in phase 3 trials (DUET 1 and 2) in
treatment-experienced adult patients.

TMC125 showed activity against NNRTI-resistant virus

The presented data were the final 48 week analysis of study
TMC125-C223, a phase 2b dose-finding, randomized, partially-blinded
study in HIV-1 infected adult patients with substantial treatment
experience, documented evidence of NNRTI resistance and 3 or more PI
mutations. A total of 199 patients were randomized to TMC125 (400 mg
or 800 mg bid) (n=159) plus background regimen or best available
control regimen (n=40). Ninety eight percent of control group
patients had discontinued treatment by 48 weeks, compared with 38% of
TMC125 patients.

Intent to treat analysis showed that the mean change from baseline
in viral load at week 48 was -0.88, -1.01 and -0.14 log10 copies/ml
in the TMC125 400mg and 800 mg bid and active control groups
respectively. A decrease from baseline in plasma viral load of at
least 1 log10 copies/ml was achieved by 31%, 34% and 8% of patients
respectively. In these patients with NNRTI resistance, the viral load
reduction in patients receiving TMC125 400mg or 800mg bid in
combination with an optimized background regimen (OBR) was
significantly greater than in the active control at 48 weeks, p=0.018
and p=0.002 respectively.

"These 48 week results in patients with NNRTI-resistance with
limited treatment options are encouraging," said Dr Cal Cohen,
Research Director, CRI New England and Harvard Vanguard Medical
Associates, Boston, MA.

The comparison of adverse events (AEs) and serious AEs (SAEs)
between the TMC125 arms and the control group is confounded because
by 48 weeks 98% of patients in the control group had discontinued,
the majority for poor virologic response. The most common adverse
events (AEs) were diarrhea, pyrexia and rash which were 22%, 20% and
20%, respectively, for the TMC125 groups compared with 15%, 10% and
8% for the active control group. Overall, 27% of TMC125 and 18% of
control patients reported at least one serious adverse event; 4 of
these SAEs were classified as possibly related to TMC125.

Sixteen presentations by Tibotec Pharmaceuticals Ltd. and its
collaborators provided new safety and efficacy, pharmacokinetic and
drug interaction data on the Tibotec compounds -- including the
investigational agents TMC125, TMC278 and TMC120.

For further information, please visit: http://www.tibotec.com

Tibotec Pharmaceuticals Ltd.

Tibotec Pharmaceuticals Ltd., based in Cork, Ireland, is a
pharmaceutical research and development company. The Company's main
research and development facilities are in Mechelen, Belgium with
offices in Yardley, PA. Tibotec is dedicated to the discovery and
development of innovative HIV/AIDS drugs and anti-infectives for
diseases of high unmet medical need.

Tibotec is developing a Global Access Program to facilitate access
to its antiretrovirals for patients living with HIV/AIDS in
developing countries. The Global Access Program for PREZISTA(TM)
(darunavir, also known TMC114) includes access, pricing,
registration, medical education for appropriate use and voluntary
licensing.

IAC Presentations

Cal Cohen, et al. 48-week efficacy and safety results of TMC125 in
HIV patients with NNRTI and PI resistance - study TMC125-C223

Howard Grossman, et al. Prediction of clinical benefits of TMC125
from treatment effects on CD4 counts and HIV RNA

Monika Scholler, et al. Lack of interaction between TMC125 and
methadone

Monika Scholler, et al. TMC125 bioavailability is not affected by
ranitidine and omeprazole

Julio Montaner, et al. Combination of TMC114/ritonavir and TMC125
in patients with multidrug resistant HIV

Thomas Kaduda, et al. The pharmacokinetic interaction between
TMC125 and TMC114/rtv in HIV-negative volunteers

Rolf Van Heeswijk, et al. The pharmacokinetic interaction between
ketoconazole and TMC278, an investigational non-nucleoside reverse
transcriptase inhibitor (NNRTI), in healthy HIV-negative subjects

J. Romano, et al. Characterization of in vitro release and in vivo
delivery of TMC120 with an intravaginal ring: implications for
microbicide delivery

Web site: http://www.tibotec.com

ots Originaltext: Tibotec Pharmaceuticals Ltd.
Im Internet recherchierbar: http://www.presseportal.de

Contact:
Karen Manson, cell: +32-479-89-47-99, for Tibotec Pharmaceuticals
Ltd.