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

Stem definition	Drug id	CAS RN
neurokinin NK1 (substance P) receptor antagonist	4470	172673-20-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ivemend fosaprepitant fosaprepitant dimeglumine fosaprepitant meglumine	a pro-drug form of aprepitant Molecular weight: 614.41 Formula: C23H22F7N4O6P CLOGP: 2.19 LIPINSKI: 1 HAC: 10 HDO: 3 TPSA: 123.93 ALOGS: -4.99 ROTB: 9 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ivemend
fosaprepitant
fosaprepitant dimeglumine
fosaprepitant meglumine

a pro-drug form of aprepitant

Molecular weight: 614.41
Formula: C23H22F7N4O6P
CLOGP: 2.19
LIPINSKI: 1
HAC: 10
HDO: 3
TPSA: 123.93
ALOGS: -4.99
ROTB: 9

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	2.20 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	18.60 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	100 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution)	0.07 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
March 27, 2003	FDA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	474.00	16.45	359	20895	118090	63349678
Flushing	156.16	16.45	157	21097	74930	63392838
Erythema	145.85	16.45	232	21022	175519	63292249
Febrile bone marrow aplasia	131.18	16.45	59	21195	7266	63460502
Mucosal inflammation	118.05	16.45	109	21145	46819	63420949
Neutropenia	117.22	16.45	210	21044	174795	63292973
Nausea	110.98	16.45	570	20684	853901	62613867
Pyrexia	108.94	16.45	375	20879	470103	62997665
Computerised tomogram thorax abnormal	100.40	16.45	33	21221	1730	63466038
Neutrophil count decreased	99.41	16.45	108	21146	56298	63411470

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	194.63	20	231	11188	136618	34808894
Hiccups	117.58	20	60	11359	10022	34935490
Erythema	111.54	20	141	11278	88639	34856873
Neutropenia	96.93	20	179	11240	156599	34788913
Neutrophil count decreased	83.68	20	93	11326	51011	34894501
Nausea	77.61	20	265	11154	339643	34605869
Anaphylactic reaction	73.16	20	70	11349	32231	34913281
Drug ineffective	65.51	20	34	11385	456717	34488795
Hypersensitivity	64.29	20	89	11330	60946	34884566
Thrombocytopenia	61.02	20	148	11271	156099	34789413

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	592.14	15.99	563	28672	230436	79484717
Erythema	244.55	15.99	352	28883	222938	79492215
Neutropenia	178.73	15.99	352	28883	287358	79427795
Flushing	173.80	15.99	187	29048	88081	79627072
Neutrophil count decreased	167.60	15.99	189	29046	93770	79621383
Febrile bone marrow aplasia	156.06	15.99	82	29153	12938	79702215
Nausea	143.51	15.99	710	28525	956486	78758667
Pyrexia	141.50	15.99	556	28679	678153	79037000
Encephalopathy	133.01	15.99	143	29092	67254	79647899
Drug ineffective	109.66	15.99	142	29093	1080771	78634382

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:50919	antiemetico
CHEBI has role	CHEBI:55350	neurokinin-1 receptor antagonists
FDA EPC	N0000175786	Substance P/Neurokinin-1 Receptor Antagonist
FDA MoA	N0000010262	Neurokinin 1 Antagonists
MeSH PA	D000932	Antiemetics
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D005765	Gastrointestinal Agents
MeSH PA	D064729	Neurokinin-1 Receptor Antagonists
MeSH PA	D018377	Neurotransmitter Agents

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

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Disease	Relation	SNOMED_ID	DOID
Chemotherapy-induced nausea and vomiting	indication	236084000
Hepatic failure	contraindication	59927004

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	0.87	acidic
pKa2	6.2	acidic
pKa3	8.25	acidic
pKa4	10.36	acidic
pKa5	3.99	Basic
pKa6	1.47	Basic

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Orange Book patent data (new drug applications)

None

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 115MG BASE/VIAL Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons	EMEND	MERCK AND CO INC	N022023	Jan. 25, 2008	DISCN	POWDER	INTRAVENOUS	May 2, 2025	ADDITION OF A 3-DAY FOSAPREPITANT FOR INJECTION INTRAVENOUS DOSING REGIMEN IN PEDIATRIC PATIENTS FOR THE CURRENTLY APPROVED PREVENTION OF CHEMOTHERAPY-INDUCED NAUSEA AND VOMITING
EQ 150MG BASE/VIAL	EMEND	MERCK AND CO INC	N022023	Nov. 12, 2010	RX	POWDER	INTRAVENOUS	May 2, 2025	ADDITION OF A 3-DAY FOSAPREPITANT FOR INJECTION INTRAVENOUS DOSING REGIMEN IN PEDIATRIC PATIENTS FOR THE CURRENTLY APPROVED PREVENTION OF CHEMOTHERAPY-INDUCED NAUSEA AND VOMITING

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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	IC50	8.92		IUPHAR	CHEMBL

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External reference:

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ID	Source
012534	NDDF
012535	NDDF
135413538	PUBCHEM_CID
1731071	RXNORM
25045	MMSL
265121-04-8	SECONDARY_CAS_RN
322336	MMSL
4027246	VANDF
4027247	VUID
4027247	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
EMEND	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3061	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	150 mg	INTRAVENOUS	NDA	29 sections
EMEND	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3061	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	150 mg	INTRAVENOUS	NDA	29 sections
EMEND	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3061	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	150 mg	INTRAVENOUS	NDA	29 sections
EMEND	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3061	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	150 mg	INTRAVENOUS	NDA	29 sections
EMEND	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3884	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	115 mg	INTRAVENOUS	NDA	29 sections
EMEND	HUMAN PRESCRIPTION DRUG LABEL	1	0006-3941	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	150 mg	INTRAVENOUS	NDA	29 sections
Fosaprepitant	HUMAN PRESCRIPTION DRUG LABEL	1	0338-0008	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	150 mg	INTRAVENOUS	ANDA	29 sections
Fosaprepitant	HUMAN PRESCRIPTION DRUG LABEL	1	0338-0008	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	150 mg	INTRAVENOUS	ANDA	29 sections
Fosaprepitant	HUMAN PRESCRIPTION DRUG LABEL	1	0591-4385	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	150 mg	INTRAVENOUS	NDA	27 sections
Fosaprepitant	HUMAN PRESCRIPTION DRUG LABEL	1	0591-4385	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	150 mg	INTRAVENOUS	NDA	27 sections

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