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Second generation 5-HT3 antagonists open new perspectives in emesis prevention

Rome, Italy (ots)

The MASCC (Multinational Association of
Supportive Care in Cancer) 2009 International Symposium opens today 
in Rome, Italy - Chemotherapy-induced nausea and vomiting (CINV), 
treatment of pain, and quality of life in survivors among the key 
topics of the conference
"Supportive care in cancer is a field of increasing relevance for 
both oncology patients and clinical research", said Maurizio Tonato, 
Co-chair of the MASCC 2009 International Symposium, inaugurated in 
Rome today. Tonato explained how supportìve care, in conjunction with
anticancer treatments, may significantly increase quality of life in 
patients especially addressing the most dreaded consequences and 
complications, including pain and emesis.
"MASCC-Multinational Association of Supportive Care in Cancer, 
founded in 1990, is an international, multiprofessional organization 
that encompasses all aspects of cancer care beyond direct 
antineoplastic approaches", echoed Fausto Roila, also Co-chair of the
Rome MASCC 2009. "Significant advances in cancer treatment in the 
last two decades have been made possible by the strides in supportive
care", Roila continued.
Chemotherapy-induced nausea and vomiting (CINV) is among the most 
frequent side effects following therapy in patients with cancer. 
"Despite prophylaxis on the day of chemotherapy, up to 30-45 percent 
of patients experience nausea or vomiting or require rescue therapy 
following administration of certain types of emetogenic 
chemotherapy", said Richard Gralla, Vice President Cancer Services, 
North Shore University Hospital and LIJ Monter Cancer Center, Lake 
Success, NY, USA.
The 5-HT3 receptor plays a pivotal role in the process of emesis, 
and agents that antagonise these receptor subtypes are the basis for 
control of this effect. Following the development of the first 
generation 5-HT3 receptor antagonists, such as ondansetron and 
granisetron, in the late '80s and early '90s, in the recent years new
compounds have been made available for prevention of CINV, including 
palonosetron.
"Controversy continues whether there should be a 
guideline-preferred 5-HT3 antagonist", said Gralla. "5HT3 antagonists
remain the cornerstone of antiemetic regimens for cancer patients 
receiving emetogenic chemotherapy. Guideline groups indicate that no 
significant differences in emesis control are found among any of the 
earlier selective 5HT3 antagonists. But palonosetron has shown 
superior emesis control over earlier agents in several comparison 
studies", he added.
In fact, large trials with palonosetron demonstrated advantages 
over earlier 5-HT3 agents in preventing emesis with chemotherapy, but
these trials used different doses of palonosetron: either 0.25 mg or 
0.75 mg per day.
"We conducted an abstracted-data meta-analysis to see if this 
palonosetron dosings yields differences", explained Gralla. Eight 
trials with 1,926 patients included all randomized double-blind 
studies with these different palonosetron doses - 4 with highly 
emetogenic and 4 with moderately emetogenic chemotherapy (6 with 
intravenous and 2 with oral palonosetron). The findings indicated the
same results with both palonosetron doses for all important 
considerations, including all 5 days complete control and delayed 
emesis, as well as complete control and complete control plus no use 
of rescue medication. "Palonosetron doses of 0.25 mg or 0.75 mg yield
very similar efficacy and safety with both highly and moderately 
emetogenic chemotherapy in our meta-analysis. And these findings 
conclude that whichever dose you administer, the efficacy of 
palonosetron is preserved, and the beneficial results with 
palonosetron compared with each of the older 5-HT3 receptor 
antagonists used so far, can be extended to include all studies using
either of these palonosetron doses", he concluded.
About Palonosetron (Aloxi®, Onicit®, Paloxi®)
Palonosetron (palonosetron hydrochloride) is a selective 5-HT3 
receptor antagonist, developed for the prevention of chemotherapy- 
induced nausea and vomiting (CINV) in patients with cancer, with a 
long half-life of 40 hours and at least 30 times higher receptor 
binding affinity than currently available compounds. Palonosetron is 
a second generation 5-HT3 receptor antagonist, and demonstrates, in 
clinical trials and clinical practice, a unique long-lasting action 
in the prevention of CINV.
The product has shown to be effective in preventing both acute and
delayed CINV in patients receiving moderately emetogenic 
chemotherapies. A single intravenous dose of palonosetron (0.25 mg) 
provides better protection from CINV than first-generation 5-HT3 
receptor antagonists throughout a 5-day post- chemotherapy period. 
This means that a single administration of palonosetron also grants 
protection during the delayed phase of CINV.
Palonosetron 0.075 mg IV is also approved by FDA as a single 
intravenous dose administered immediately before the induction of 
anaesthesia for the prevention of postoperative nausea and vomiting 
(PONV) for up to 24 hours following surgery. Palonosetron is 
contraindicated in patients known to have hypersensitivity to the 
drug or any of its components. The most commonly reported adverse 
reactions (incidence > 2 percent) in CINV trials with palonosetron 
were headache (9 percent) and constipation (5 percent), and they were
similar to the comparators. In PONV trials, the most commonly 
reported adverse reactions were QT prolongation (5 percent), 
bradycardia (4 percent), headache (3 percent), and constipation (2 
percent), similar to placebo. Palonosetron has been developed by 
Helsinn Group of Switzerland and today it is marketed as Aloxi®, 
Onicit®, and Paloxi® in more than 40 countries world-wide. 
Palonosetron, marketed as Aloxi®, is the leading brand in the USA 
within the CINV Day of Chemo segment, and it is steadily growing in 
the European markets. For more information about palonosetron, please
visit the website: www.aloxi.com
About Helsinn Group
Helsinn is a privately owned pharmaceutical group with 
headquarters in Lugano, Switzerland, and subsidiaries in Ireland and 
USA. Helsinn is the worldwide licensor of palonosetron. Helsinn's 
unique business model is focused on the licensing of pharmaceuticals 
and medical devices in therapeutic niche areas. The Group in-licenses
early stage new chemical entities, completes their development from 
the performance of pre-clinical/clinical studies and Chemistry, 
Manufacturing and Control (CMC) development, to the filing for and 
attainment of their market approval worldwide. Helsinn's products are
sold directly, through the Group subsidiaries, or eventually 
out-licensed to its network of local marketing and commercial 
partners, selected for their deep in-market knowledge and know-how, 
and assisted and supported with a full range of product and 
scientific management services, including commercial, regulatory, 
financial, legal and medical marketing advice. The active 
pharmaceutical ingredients and the finished dosage forms are 
manufactured at Helsinn's cGMP facilities in Switzerland and Ireland,
and supplied worldwide to its customers. For more information about 
Helsinn Group, please visit the website: www.helsinn.com

Contact:

Paolo Ferrari
Head of International Marketing
Phone: +41/91/985'21'21
E-Mail: info-hhc@helsinn.com

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