Netupitant - MedKoo Biosciences

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MedKoo product information:

Netupitant

MedKoo Code#: 201985
Name: Netupitant
CAS#: 290297-26-6 Synonym: Netupitant 　 IUPAC/Chemical name: 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl]-N-methylisobutyramide.
Chemical structure	Theoretical analysis
	Chemical Formula: C30H32F6N4O Exact Mass: 578.24803 Molecular Weight: 578.59 m/z: 578.24803 (100.0%), 579.25139 (32.4%), 580.25474 (5.1%), 579.24507 (1.5%) Elemental Analysis: C, 62.28; H, 5.57; F, 19.70; N, 9.68; O, 2.77
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Information about this agent

Netupitant is a potent and selective NK-1 receptor antagonist. It is under development for the prevention of chemotherapy-induced nausea and vomiting (CINV). Netupitant is currently in Phase III trial.

Chemotherapy-induced nausea and vomiting, or CINV, is nausea and vomiting that results specifically from treatment with chemotherapy drugs. There can be other causes of nausea or vomiting that are associated with cancer or its treatment. Some examples are treatment with radiation, an obstruction in the intestine caused by a tumor, side effects of pain medications, constipation or imbalances in electrolytes (minerals and salts that keep the body chemistry in equilibrium). [source: http://www.thewellnesscommunity.org/mm/Learn-About/Managing-Side-Effects/Nausea/default.aspx].

Among the NK-1 receptor antagonists, aprepitant has been approved for the treatment of CINV. Currently, several other NK-1 receptor antagonists, including casopitant, vestipitant, netupitant, and SCH619734, are undergoing clinical evaluation for the prevention of CINV in patients with a variety of malignancies. [source: Support Cancer Ther. 2006 Apr 1;3(3):140-2.]

Current developer: Helsinn (Originator) Eisai Co Ltd (Licensee).

References

1: Reddy GK, Gralla RJ, Hesketh PJ. Novel neurokinin-1 antagonists as antiemetics for the treatment of chemotherapy-induced emesis. Support Cancer Ther. 2006 Apr 1;3(3):140-2. PubMed PMID: 18632487.

2: Hoffmann-Emery F, Hilpert H, Scalone M, Waldmeier P. Efficient synthesis of novel NK1 receptor antagonists: selective 1,4-addition of grignard reagents to 6-chloronicotinic acid derivatives. J Org Chem. 2006 Mar 3;71(5):2000-8. PubMed PMID: 16496986.

3: Hoffmann T, Bös M, Stadler H, Schnider P, Hunkeler W, Godel T, Galley G, Ballard TM, Higgins GA, Poli SM, Sleight AJ. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1362-5. Epub 2005 Dec 5. PubMed PMID: 16332435.

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