Phase II data show efficacy and tolerability of tapentadol in chronic pain treatment

Aachen (ots) - The German pharmaceutical company Grunenthal GmbH
presented the first clinical evidence for the efficacy and
tolerability of tapentadol ER (extended release) for patients
suffering from chronic pain at the Annual Congress of the European
League Against Rheumatism (EULAR), 13-16 June 2007, Barcelona, Spain.
Tapentadol, a centrally acting analgesic, is the first of its kind,
combining two analgesic principles, mu-receptor agonism and
noradrenaline reuptake inhibition, in one molecule.

The new study results show that tapentadol ER is effective for at
least 4 weeks in the treatment of moderate-to-severe chronic pain due
to osteoarthritis of the knee(1). The broad analgesic efficacy of
tapentadol derived from preclinical models has previously been
confirmed for acute pain conditions in a number of clinical
studies(2). In line with the acute pain data the current findings
confirm tapentadol´s improved tolerability compared to other strong
centrally acting analgesics like oxycodone, and morphine.

"With currently available centrally acting analgesics, many
patients are forced to terminate their treatment due to intolerable
side-effects", comments Prof. Dr. Eric Paul Pâques, member of the
Executive Board of Grunenthal. "Our goal is to provide new treatment
approaches with strong analgesic efficacy and improved tolerability
to these patients. The promising results with tapentadol show that we
are on the right track".

Efficacy

A total of 670 patients were included in this clinical trial, with
a primary objective of evaluating the safety and efficacy at the end
of 4 weeks of treatment with tapentadol. Subjects in this study
underwent a titration period, and were subsequently treated with a
fixed dose of either tapentadol ER 100 mg, 200 mg, oxycodone HCl CR
20 mg, or placebo, all bid (twice daily). Patients who received
tapentadol ER 200 mg bid experienced a significant improvement in
pain intensity compared to patients in the placebo group (p=0.021).
When both dose groups of tapentadol were compared to the oxycodone
arm of the study (added as sensitivity control of the model),
tapentadol ER 100 mg bid was found to be similar to oxycodone HCl CR
20 mg bid, providing further support that the analgesic efficacy of
tapentadol is in the range of other strong centrally acting
analgesics.

Safety and Tolerability

In general, the most common adverse events in all groups were
typical for a treatment with centrally acting analgesics. With
respect to gastrointestinal (e.g. nausea, vomiting, constipation) and
CNS (e.g. somnolence, dizziness) side effects, the data suggest an
improved tolerability of tapentadol compared to oxycodone. The
incidence of constipation with both tapentadol ER 100 mg (7%) and 200
mg (10%) was less than or equal to half of the incidence associated
with oxycodone CR 20 mg (20%).

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.

About Grunenthal

Grunenthal is an expert in pain therapy and gynaecology and a
pioneer in intelligent, user-friendly drug delivery technologies. The
company discovers, develops, produces and markets high therapeutic
value pharmaceuticals that contribute to patients' ability to control
their own lives. Grunenthal is an independent, family-owned German
company operating with affiliates in 27 countries all over the world.
Founded in 1946, the company employs 1,900 people in Germany and
4,800 worldwide. In 2006, Grunenthal achieved revenues of 813 million
Euro.

References

1. C. Rauschkolb-Loeffler1, A.Okamoto1, A. Steup2, C. Lange2:
Efficacy and Tolerability of Tapentadol for Relief of
Moderate-to-Severe Chronic Pain Due to Osteoarthritis of the Knee
(Poster presented at the Annual Congress of the EULAR , 2007).
1Johnson & Johnson Pharmaceutical Research & Development, Titusville,
New Jersey, United States. 2Grunenthal GmbH, Aachen, Germany.

2. J.U. Stegmann1, C. Engels1, A. Steup1, HJ Schwarz1, P.
Desjardins2, S. Grond3. 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 EFIC,
2006). 1Grunenthal GmbH, Aachen, Germany. 2Scirex Corporation,
Austin, Texas, USA. 3Martin-Luther-University Halle-Wittenberg,
Halle, Germany.

Originaltext: Grünenthal GmbH
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Contact:
Anke Krueger-Hellwig
Phone: +49 241 569-2858,
Fax: +49 241 569-1486,
anke.krueger-hellwig@grunenthal.com

Grunenthal GmbH,
52099 Aachen, Germany,
www.grunenthal.com