fosnetupitant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
neurokinin NK1 (substance P) receptor antagonist	5283	1703748-89-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: fosnetupitant 07-PNET 08-PNET fosnetupitant chloride fosnetupitant chloride hydrochloride arokaris	Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. 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. Molecular weight: 689.62 Formula: C31H36F6N4O5P CLOGP: 2.66 LIPINSKI: 1 HAC: 9 HDO: 2 TPSA: 103.20 ALOGS: -6.64 ROTB: 10 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

fosnetupitant
07-PNET
08-PNET
fosnetupitant chloride
fosnetupitant chloride hydrochloride
arokaris

Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. 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.

Molecular weight: 689.62
Formula: C31H36F6N4O5P
CLOGP: 2.66
LIPINSKI: 1
HAC: 9
HDO: 2
TPSA: 103.20
ALOGS: -6.64
ROTB: 10

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
S (Water solubility)	1.40 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
April 19, 2018	FDA	HELSINN HLTHCARE
March 28, 2022	PMDA	Taiho Pharmaceutical Co., Ltd.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

None

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Chemotherapy-induced nausea and vomiting	indication	236084000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.75	acidic
pKa2	3.93	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML)	AKYNZEO	HELSINN HLTHCARE	N210493	May 27, 2020	RX	SOLUTION	INTRAVENOUS	9186357	Nov. 18, 2030	USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML)	AKYNZEO	HELSINN HLTHCARE	N210493	May 27, 2020	RX	SOLUTION	INTRAVENOUS	10828297	Dec. 17, 2030	USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML)	AKYNZEO	HELSINN HLTHCARE	N210493	May 27, 2020	RX	SOLUTION	INTRAVENOUS	10208073	May 23, 2032	USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML)	AKYNZEO	HELSINN HLTHCARE	N210493	May 27, 2020	RX	SOLUTION	INTRAVENOUS	8895586	May 23, 2032	USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML)	AKYNZEO	HELSINN HLTHCARE	N210493	May 27, 2020	RX	SOLUTION	INTRAVENOUS	9403772	May 23, 2032	USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL	AKYNZEO	HELSINN HLTHCARE	N210493	April 19, 2018	RX	POWDER	INTRAVENOUS	9186357	Nov. 18, 2030	USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL	AKYNZEO	HELSINN HLTHCARE	N210493	April 19, 2018	RX	POWDER	INTRAVENOUS	10828297	Dec. 17, 2030	USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL	AKYNZEO	HELSINN HLTHCARE	N210493	April 19, 2018	RX	POWDER	INTRAVENOUS	10208073	May 23, 2032	USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL	AKYNZEO	HELSINN HLTHCARE	N210493	April 19, 2018	RX	POWDER	INTRAVENOUS	8895586	May 23, 2032	USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL	AKYNZEO	HELSINN HLTHCARE	N210493	April 19, 2018	RX	POWDER	INTRAVENOUS	9403772	May 23, 2032	USE IN COMBINATION WITH DEXAMETHASONE IN ADULTS FOR THE PREVENTION OF ACUTE AND DELAYED NAUSEA AND VOMITING ASSOCIATED WITH INITIAL AND REPEAT COURSES OF HIGHLY EMETOGENIC CANCER CHEMOTHERAPY

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 235MG BASE/20ML (EQ 11.75MG BASE/ML);EQ 0.25MG BASE/20ML (EQ 0.0125MG BASE/ML)	AKYNZEO	HELSINN HLTHCARE	N210493	May 27, 2020	RX	SOLUTION	INTRAVENOUS	April 19, 2023	NEW CHEMICAL ENTITY
EQ 235MG BASE/VIAL;EQ 0.25MG BASE/VIAL	AKYNZEO	HELSINN HLTHCARE	N210493	April 19, 2018	RX	POWDER	INTRAVENOUS	April 19, 2023	NEW CHEMICAL ENTITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Substance-P receptor	GPCR	P25103	NK1R_HUMAN	ANTAGONIST	Ki	9.02		SCIENTIFIC LITERATURE	DRUG LABEL

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External reference:

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ID	Source
017511	NDDF
017512	NDDF
10146	INN_ID
1643757-72-5	SECONDARY_CAS_RN
2044416	RXNORM
34267	MMSL
4037545	VANDF
71544786	PUBCHEM_CID
781258008	SNOMEDCT_US
C4691680	UMLSCUI

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
AKYNZEO	HUMAN PRESCRIPTION DRUG LABEL	2	69639-102	INJECTION	260 mg	INTRAVENOUS	NDA	26 sections
AKYNZEO	HUMAN PRESCRIPTION DRUG LABEL	2	69639-102	INJECTION	260 mg	INTRAVENOUS	NDA	26 sections
AKYNZEO	HUMAN PRESCRIPTION DRUG LABEL	2	69639-102	INJECTION	260 mg	INTRAVENOUS	NDA	26 sections
AKYNZEO	HUMAN PRESCRIPTION DRUG LABEL	2	69639-105	INJECTION	260 mg	INTRAVENOUS	NDA	26 sections
AKYNZEO	HUMAN PRESCRIPTION DRUG LABEL	2	69639-105	INJECTION	260 mg	INTRAVENOUS	NDA	26 sections
AKYNZEO	HUMAN PRESCRIPTION DRUG LABEL	2	69639-105	INJECTION	260 mg	INTRAVENOUS	NDA	26 sections
AKYNZEO	HUMAN PRESCRIPTION DRUG LABEL	2	69639-106	INJECTION	260 mg	INTRAVENOUS	NDA	26 sections

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