TMC125 Can Be Used in Combination with Most Antiretrovirals

Glasgow, Scotland, November 14 (ots/PRNewswire) -

- Also Found Compatible with Other Medicines Used by HIV/AIDS
Patients

A review of 17 drug-drug interaction studies involving the
investigational non-nucleoside reverse transcriptase inhibitor
(NNRTI) TMC125 was presented today as a plenary oral paper at the
Eighth International Congress on Drug Therapy in HIV Infection (HIV8)
in Glasgow, Scotland. The data indicate that TMC125, a
next-generation NNRTI active against NNRTI-resistant strains of HIV
can be combined, without dose adjustment, with most other marketed
antiretrovirals. However as TMC125 has not yet received regulatory
approval this needs to be confirmed by the relevant authorities.

The data suggest that antiretrovirals that can be used in
combination with TMC125 without requiring dosage adjustments include
nucleoside reverse transcriptase inhibitors and most ritonavir
boosted protease inhibitors including darunavir (TMC114).
Tipranavir/ritonavir, nevirapine and efavirenz reduced TMC125
exposures by 76%, 55% and 41% and should not be used in combination
with TMC125. TMC125 increased fosamprenavir/ritonavir (FPV/r)
exposure 69% and thus FPV/r dosing may need to be adjusted.

No dose adjustments may be required when TMC125 is co-administered
with contraceptive hormones, proton-pump inhibitors, H2 blockers or
methadone. TMC125 reduced the exposure of sildenafil 69% and
therefore doses of sildenafil may need to be adjusted.

TMC125 may be used with rifabutin and clarithromycin without dose
adjustment in most situations however it is recommended to use an
alternative drug to clarithromycin, when treating Mycobacterium avium
complex (MAC).

TMC125 is an inducer of CYP3A and an inhibitor of CYP2C19. TMC125
is currently being investigated in phase 3 trials (DUET 1 and 2) in
treatment-experienced adult patients.

TMC125 Expanded Access Program

The expanded access program (EAP) for TMC125 is now open in a
number of European countries, more will follow shortly, Canada and
the US where 46 clinical trial sites have initiated the program.
TMC125 is available to HIV-1 infected adults, at least 18 years old,
who have limited treatment options either due to virological failure
or intolerance to multiple ARV regimens. Patients must be three-class
experienced, having received licensed treatment from each of the 3
major oral classes of anti-HIV drugs (NRTIs, NNRTIs, and PIs), and
must have received at least two PI-based regimens.

For more about the program, healthcare professionals and people
living with HIV/AIDS may obtain information by visiting
http://www.clinicaltrials.gov.

About Tibotec

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.

For more information, visit http://www.tibotec.com

TMC125 Presentations at HIV 8 conference in Glasgow.

Oral presentations:

1. TMC125 in combination with other medications: summary of
drug-drug interaction studies. Thomas Kakuda et al.

Plenary 5/Session 5, Tuesday 14 Nov, 10:45-11am

2. Impact of NNRTI and NRTI resistance on the response to the
regimen of TMC125 plus two NRTIs in Study TMC125-C227. B. Woodfall et
al.

Plenary 5/Session 6, Tuesday 14 Nov, 11:45-12:00pm

Poster presentations:
    1. No frequent reporting of neurological or psychiatric events during
       TMC125 treatment
       B. Woodfall et al.
    2. No Effect of TMC125 on the Pharmacokinetics of Oral Contraceptives
       M. Scholler-Gyure et al
    3. Pharmacokinetics of TMC125, with atazanavir and atazanavir/ritonavir
      (ATV/r)
       M. Scholler-Gyure et al

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

Rückfragehinweis:
Karen Manson, +32-479-89-4799

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