Palonosetron Hydrochloride, a potent and highly selective 5-HT3 receptor antagonist, was developed for the prevention of chemotherapy-induced nausea and vomiting (CINV).

Helsinn Healthcare SA completed an extensive and FDA-compliant development plan and obtained FDA approval for marketing palonosetron in USA (ALOXI®) with the following unique indications:

• the prevention of acute nausea and vomiting associated with initial and repeat courses of moderately and highly emetogenic cancer chemotherapy,
• the prevention of delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy,

following a single intravenous (IV) administration.

In March 2005, Palonosetron HCl was approved in Europe by the EMEA, through a centralized procedure, with the following indications:

• the prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy,
• the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy,

following single intravenous (IV) administration.

Palonosetron HCl, a potent and highly selective 5-HT3-receptor antagonist , is a pure non-racemic isomer, able to block the action of serotonin (5-hydroxytryptamine), a neurotransmitter produced by gastrointestinal cells under the stimulus of chemotherapeutic agents. Serotonin induces nausea and vomiting via a cascade of neuronal activation involving both the gastrointestinal tract and the central nervous system. By blocking the action of serotonin, palonosetron is able to control nausea and vomiting induced by administration of chemotherapy.

Palonosetron HCl showed to be effective in the control of undesired symptoms of nausea and vomiting as from the first day of chemotherapy administration in both highly and moderately emetogenic chemotherapy. It maintains control over nausea and emesis up to 5 days following the moderately emetogenic chemotherapy administration.
The capability of this compound to be highly effective and to maintain efficacy in the delayed phase, gives palonosetron the chance to satisfy the need for a new therapy with a strong and prolonged efficacy following a single administration, while offering a safety profile comparable with that of the class.

Helsinn is completing the Post Operative Nausea and Vomiting development program and investigating further indications and dosage forms for palonosetron with the aim to complete its clinical profile.
ALOXI® was launched in USA in September 2003, few months after its approval by the FDA by Helsinn's US partner, MGI PHARMA Inc. The product is successfully used in this market since then, with a great market penetration in the clinics and in the hospital settings.

In Europe, Aloxi® has been launched in over 20 countries so far. The list of Helsinn partners who are commercializing the product is available on the web site www.aloxi.com.
In Latin America, Palonosetron HCl is commercialized under the tradename Onicit®. Helsinn’s partner Schering Plough launched the product in 14 countries.
In Asia Palonosetron HCl has been launched in Indonesia (brandname PaloxiTM) and other countries will follow soon. In Japan the product is still under development.