Netupitant - CAS 290297-26-6
Catalog number: 290297-26-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C30H32F6N4O
Molecular Weight:
578.603
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.
Purity:
>98%
Appearance:
Solid powder
Synonyms:
AGE94200; AGE-94200; AGE 94200;Ro 67-3189; Ro-67-3189; Ro67-3189; CHEBI441603; CID6451149; D05152; UNII-7732P08TIR, CHEMBL206253, AG-E-94200, Netupitant
MSDS:
Inquire
InChIKey:
WAXQNWCZJDTGBU-UHFFFAOYSA-N
InChI:
InChI=1S/C30H32F6N4O/c1-19-8-6-7-9-23(19)24-17-26(40-12-10-38(4)11-13-40)37-18-25(24)39(5)27(41)28(2,3)20-14-21(29(31,32)33)16-22(15-20)30(34,35)36/h6-9,14-18H,10-13H2,1-5H3
Canonical SMILES:
CC1=CC=CC=C1C2=CC(=NC=C2N(C)C(=O)C(C)(C)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)N4CCN(CC4)C
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Neurokinin Receptor Products


CAS 170729-80-3 Aprepitant

Aprepitant
(CAS: 170729-80-3)

Aprepitant is a specific NK-1R antagonist, used as an antiemetic agent.

CAS 63968-82-1 Kassinin

Kassinin
(CAS: 63968-82-1)

Kassinin, a tachykinin peptide derived from the Kassina frog, is secreted as a defense response, and is involved in neuropeptide signalling and shows selectivit...

CAS 135306-85-3 MEN 10376

MEN 10376
(CAS: 135306-85-3)

MEN 10376 is a selective NK2 receptor antagonist.

CAS 122063-01-8 [bAla8]-Neurokinin A(4-10)

[bAla8]-Neurokinin A(4-10)
(CAS: 122063-01-8)

An agonist of neurokinin 2 (NK2) receptor

CAS 160492-56-8 Osanetant

Osanetant
(CAS: 160492-56-8)

Osanetant is a non-peptide neurokinin 3 (NK3) receptor antagonist. It is developed for the treatment of schizophrenia and other central nervous system (CNS) dis...

CAS 145148-39-6 CP 99994 dihydrochloride

CP 99994 dihydrochloride
(CAS: 145148-39-6)

The hydrochloride salt form of CP 99994, which is a high affinity NK1 antagonist and could attenuate endothelium-dependent contraction induced by substance P.

CAS 188923-01-5 L760735

L760735
(CAS: 188923-01-5)

L760735 is a high-affinity NK1 receptor antagonist with IC50 value of 0.19 nM. It is selective over NK2 and NK3 receptors. It is used in the synthetic preparati...

CAS 2990-43-4 Eledoisin-Related Peptide

Eledoisin-Related Peptide
(CAS: 2990-43-4)

Eledoisin-Related Peptide is a tachykinin receptor ligand.

Chemical Structure

CAS 290297-26-6 Netupitant

Quick Inquiry

Verification code

Featured Items