Netupitant - CAS 290297-26-6
Catalog number:
290297-26-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
Neurokinin Receptor
Description:
Netupitant is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity. Netupitant competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). SP is found in neurons of vagal afferent fibers innervating the brain-stem nucleus tractus solitarii and the area postrema, which contains the chemoreceptor trigger zone (CTZ), and may be elevated in response to chemotherapy. The NK-receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema. Check for active clinical trials or closed clinical trials using this agent. On 10/10 2014 FDA approved netupitant for the treatment of nausea and vomiting in patients undergoing cancer chemotherapy.
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Purity:
>98%
Appearance:
Solid powder
Synonyms:
CHEBI441603; CID6451149; D05152; UNII-7732P08TIR, CHEMBL206253, AG-E-94200, Netupitant
MSDS:
Inquire
Current Developer:
Helsinn Group and Eisai Inc
1.Safety of an Oral Fixed Combination of Netupitant and Palonosetron (NEPA): Pooled Data From the Phase II/III Clinical Program.
Aapro M1, Hesketh PJ2, Jordan K3, Gralla RJ4, Rossi G5, Rizzi G5, Palmas M5. Oncologist. 2016 Apr;21(4):494-502. doi: 10.1634/theoncologist.2015-0301. Epub 2016 Mar 21.
BACKGROUND: Standard prophylaxis for chemotherapy-induced nausea and vomiting (CINV) with highly emetogenic and anthracycline-cyclophosphamide-based chemotherapy includes a 5-hydroxytryptamine-3 receptor antagonist, a neurokinin-1 receptor antagonist (NK1RA), and corticosteroid therapy. NEPA is a fixed combination of netupitant and palonosetron. The primary objective of this analysis was to document the safety profile, including cardiac safety, of NEPA + dexamethasone in comparison with current therapies across all phase II/III trials.
2.Netupitant/Palonosetron: A Review in the Prevention of Chemotherapy-Induced Nausea and Vomiting.
Keating GM1. Drugs. 2015 Dec;75(18):2131-41. doi: 10.1007/s40265-015-0512-9.
An oral fixed combination of netupitant/palonosetron (NEPA; Akynzeo(®)) is available for use in the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV). Netupitant is a highly selective neurokinin-1 receptor antagonist and palonosetron is a serotonin 5-HT3 receptor antagonist with a distinct pharmacological profile. Complete response rates during the delayed, acute and overall phases were significantly higher with single-dose netupitant 300 mg plus palonosetron 0.5 mg than with single-dose palonosetron 0.5 mg in cycle 1 of cisplatin-based highly emetogenic chemotherapy (HEC) in a phase II trial and with single-dose netupitant/palonosetron 300/0.5 mg than with single-dose palonosetron 0.5 mg in cycle 1 of anthracycline-cyclophosphamide (AC) moderately emetogenic chemotherapy (MEC) in a phase III trial; the greater efficacy of netupitant/palonosetron was maintained over repeated cycles of AC MEC in the phase III trial.
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