The company added that the CINVANTI (aprepitant) injectable emulsion for intravenous (IV) use is the first and only polysorbate 80-free, IV formulation of an NK1 receptor antagonist
(RA) indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV).
Aprepitant is an oral NK1 receptor antagonist
approved as Emend more than a decade ago for prevention of chemotherapy-induced nausea and vomiting.
The filing of the NDA for CINVANTI is an important milestone, bringing us one step closer to a new NK1 receptor antagonist
treatment option for cancer patients suffering from the debilitating side effects of chemotherapy, said Kimberly J.
Aprepitant is a highly selective NK1 receptor antagonist
with little to no affinity for other neurokinin receptors [10,11].
"Effects of CP-99, 994, a tachykinin NK1 receptor antagonist
, on abdominal afferent vagal activity in ferrets: Evidence for involvement of NK1 and 5-HT3 receptors." European Journal of Pharmacology 428.2 (2001): 215-220.
Akynzeo targets two critical signaling pathways associated with CINV by combining netupitant, an NK1 receptor antagonist
, and palonosetron, a 5-HT3 receptor antagonist, in a single capsule for the prevention of CINV.
It is composed of a highly-selective NK1 receptor antagonist
, netupitant, and palonosetron, the pharmacologically and clinically distinct 5-HT3 receptor antagonist which prevents nausea and vomiting during both the acute and delayed phase after cancer chemotherapy.
Privately held Menlo Therapeutics is focused on the development of serlopitant, a once-daily oral NK1 receptor antagonist
, for the treatment of pruritus associated with various underlying dermatological conditions, and for refractory chronic cough.
It combines palonosetron with netupitant, the new highly selective NK1 receptor antagonist
, in a single capsule.