Palonosetron HCl (135729-62-3)

The API expertise for producing Palonosetron hcl is High Potent.

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Palonosetron, the active ingredient of palonosetron hydrochloride, belongs to the class of substances termed antiemetics, which are used to treat nausea and vomiting.

There are two distinct types of CINV: acute, which occurs within 24 hours of initiation of chemotherapy and delayed, which begins afterwards and may continue for several days. Palonosetron is prescribed for both acute and delayed CINV in patients receiving moderately emetogenic chemotherapy.

It is approved for acute CINV alone in patients receiving highly emetogenic chemotherapy, or in children from the age of one month to less than 17 years. It is the first such treatment approved for use in ages one to six months. For treatment of PONV, palonosetron may be used during the first 24 hours following surgery. 

Palonosetron was approved by the FDA in 2003 and by the EMA in 2005. An oral formulation was approved by the FDA in 2008, but is no longer marketed. It is produced through a multi-step chemical process.

The serotonin 5-HT3 receptor plays a critical role in the process of emesis. Palonosetron is an antagonist of the 5-HT3 receptor (blocking its activity) with a strong binding affinity for this receptor and little or no affinity for other receptors.

It is thought that chemotherapeutic agents produce nausea and vomiting by causing the release of serotonin from cells in the small intestine. The released serotonin then activates 5-HT3 receptors located on vagal afferents. Palonosetron competitively blocks the action of serotonin at 5-HT3 receptors located on vagal afferents in the chemoreceptor trigger zone.