Netupitant and Palonosetron — Competitive Intelligence Brief

Netupitant and Palonosetron (Netupitant and Palonosetron) competitive landscape: 3 comparators, recent regulatory actions, upcoming PDUFA, patent timeline. Class: Substance P/Neurokinin-1 Receptor Antagonist [EPC]. Area: Oncology.

discontinued Substance P/Neurokinin-1 Receptor Antagonist [EPC] Oncology Small molecule

Target snapshot

Netupitant and Palonosetron (Netupitant and Palonosetron) — Helsinn Healthcare SA. 12.1 Mechanism of Action Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. Palonosetron is a 5-HT 3 receptor antagonist with a strong binding affinity for this receptor and little or no affinity for other receptors. Cancer chemotherapy may be associated with a high incidence of nausea and vomiting, particularly when certain agents, such as cisplatin, are used. 5-HT 3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. Chemotherapeutic agents produce nausea and vomiting by stimulating the release of serotonin from the enterochromaffin cells of the small intestine. Serotonin then activates 5-HT 3 receptors located on vagal afferents to initiate the vomiting reflex. The development of acute emesis is known to depend on serotonin and its 5-HT 3 receptors have been demonstrated to selectively stimulate the emetic response. Delayed emesis has been largely associated with the activation of tachykinin family neurokinin 1 (NK-1) receptors (broadly distributed in the central and peripheral nervous systems) by substance P. As shown in in vitro and in vivo studies, netupitant inhibits substance P mediated responses.

Comparator set (3 drugs)

Drug	Generic	Sponsor	Phase	Class	Target	Approval / PDUFA
Netupitant and Palonosetron TARGET	Netupitant and Palonosetron	Helsinn Healthcare SA	discontinued	Substance P/Neurokinin-1 Receptor Antagonist [EPC]
Varubi	ROLAPITANT	Tersera	marketed	Substance P/Neurokinin-1 Receptor Antagonist	Substance-P receptor	2015-01-01
Emend	APREPITANT	Merck & Co.	marketed	Substance P/Neurokinin-1 Receptor Antagonist [EPC]	Substance-P receptor	2003-01-01
Emend	FOSAPREPITANT		marketed	Substance P/Neurokinin-1 Receptor Antagonist	Substance-P receptor	2003-01-01

Recent regulatory actions (last 90 days)

No regulatory actions in the last 90 days for this set.

Upcoming PDUFA dates (next 180 days)

No PDUFA dates in the next 180 days for this set.

Patent timeline (forward window)

No upcoming patent expiries for this set.

Sponsor landscape (Substance P/Neurokinin-1 Receptor Antagonist [EPC] class)

1. Helsinn Healthcare SA · 1 drug in this class
2. Merck & Co. · 1 drug in this class