Centrally acting analgesic tapentadol - latest phase II data for the treatment of acute postoperative pain presented

Aachen (ots) - At this year's 4th World Congress of the World
Institute of Pain (WIP), the German pharmaceutical company Grunenthal
GmbH presented the latest clinical data on its centrally active
analgesic tapentadol in acute pain. Tapentadol combines two analgesic
principles in one molecule, μ-receptor agonism and noradrenaline
reuptake inhibition, and appears to be well suited for acute as well
as chronic pain conditions.

After promising results in early clinical trials with single-dose
administration of tapentadol (1), the latest Phase II data show the
efficacy and safety of tapentadol in multiple dose studies. An
immediate release (IR) formulation of tapentadol was tested for the
treatment of acute post-surgical pain following bunionectomy, a
standard foot surgery (2). The predictable level of
moderate-to-severe pain for several days make bunionectomy an
excellent model for assessing the efficacy of potent analgesics
(3,4).

Efficacy

268 patients were included in the study and assigned to one of
four treatment groups. Patients received an oral dose of either
tapentadol IR 50 mg, tapentadol IR 100 mg, oxycodone HCl IR 10 mg, or
placebo every 4 to 6 hours over three days. The results demonstrate
that tapentadol IR 50 mg and 100 mg are effective for the relief of
moderate-to-severe pain: both doses showed a significant improvement
in pain relief compared to placebo (tapentadol IR 50 mg p=0.0133;
tapentadol IR 100 mg p=0.0001), as did the active comparator
oxycodone (p=0.0365).

Tolerability

The data suggest that tapentadol exerts an improved tolerability
profile, especially in regard to gastrointestinal side effects like
nausea, vomiting and constipation, compared to oxycodone at
equieffective dosages. Tapentadol IR 50 mg as well as tapentadol IR
100 mg was associated with an incidence of constipation that was less
than half than associated with oxycodone IR 10 mg (6.0% and 7.4%
versus 17.9%, respectively).

"There is a high medical need for pain medication with the
efficacy of strong centrally acting analgesics, but with an improved
tolerability profile", says Prof. Dr. Eric-Paul Pâques, member of the
Executive Board of Grunenthal. "With its combined mode of action
tapentadol is a promising novel treatment approach for both patients
with acute or chronic pain".

Tapentadol Co-Development Partnership

Tapentadol is the latest innovation coming out of Grunenthal's
R&D pipeline. Grunenthal and Ortho-McNeil Pharmaceutical, Inc., based
in Raritan, NJ, United States, began working together on tapentadol
in 2003 with a licensing agreement for the United States and Canada.
The companies are co-developing tapentadol in the United States,
Canada, and the European Union. In January 2007, Grunenthal announced
the extension of the licensing agreement with Ortho-McNeil
Pharmaceutical to include the Japanese market. The companies
currently are conducting a phase III developmental program for
tapentadol for acute and chronic pain conditions.

About WIP

The World Institute of Pain is a worldwide organization which aims
to promote the best practice of pain medicine throughout the world.
It is an internationally recognized organization that brings together
the most recognized experts in the field of pain management for the
benefit of patients and the advancement of pain management.
www.worldinstituteofpain.org

About Grunenthal

Grunenthal is an expert in pain therapy and gynaecology and a
pioneer in intelligent, user-friendly drug delivery technologies.
Founded in 1946, the company employs 1,900 people in Germany and
4,800 worldwide. In 2006, Grunenthal achieved revenues of 813 million
Euro. www.grunenthal.com

References

1. Stegmann JU(1), Engels C(1), Steup A(1), Schwarz HJ(1),
Desjardins PJ(2), Grond S(3): Tapentadol, a Novel Centrally Acting
Analgesic with a Dual Mode of Action: Efficacy and Safety in Clinical
Acute Pain Models (Poster presented at the 5th Congress of the
European Federation of IASP Chapters (EFIC), 2006). (1)Research and
Development, Grunenthal GmbH, Aachen, Germany; (2)Scirex Corporation,
Austin., Texas, United States; (3)Martin-Luther-University
Halle-Wittenberg, Halle, Germany.

2. Stegmann JU(1), Weber H(1), Steup A(1), Upmalis D(2), Link
A(3), Desjardins PJ(3): Efficacy and Tolerability of Tapentadol
Immediate Release for the Treatment of Acute Pain Following
Bunionectomy (Poster presented at the 4th World Congress of the World
Institute of Pain, 2007). (1)Research and Development, Grunenthal
GmbH, Aachen, Germany; (2)Johnson&Johnson Pharmaceutical Research &
Development, L.L. C., Titusville, New Jersey, United States;
(3)Scirex Corporation, Austin, Texas, United States.

3.Desjardins PJ, Black PM, Daniels S, Bird SR, Fitzgerald BJ,
Petruschke RA, Tershakovec A, Chang DJ: Curr Med Res Opin
2004;20:1523-1537.

4. Thipphawong JB, Babul N, Morishige RJ, Findlay HK, Reber KR,
Millward GJ, Otulana BA: Anesthesiology 2003; 99:693-700.

Originaltext: Grünenthal GmbH
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Contact:
Anke Krueger-Hellwig
Phone: +49 241 569-2858,
Fax: +49 241 569-52858
anke.krueger-hellwig@grunenthal.com
Grunenthal GmbH, 52099 Aachen, Germany
www.grunenthal.com