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

Stem definition	Drug id	CAS RN
insecticides, anthelminthics, pesticides etc., phosphorous derivatives	156	20537-88-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: amifostine aminopropylaminoethyl thiophosphate ethiofos gammaphos WR-2721 amifostine trihydrate	A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia. Molecular weight: 214.22 Formula: C5H15N2O3PS CLOGP: -1.85 LIPINSKI: 0 HAC: 5 HDO: 4 TPSA: 95.58 ALOGS: -1.06 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

amifostine
aminopropylaminoethyl thiophosphate
ethiofos
gammaphos
WR-2721
amifostine trihydrate

A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.

Molecular weight: 214.22
Formula: C5H15N2O3PS
CLOGP: -1.85
LIPINSKI: 0
HAC: 5
HDO: 4
TPSA: 95.58
ALOGS: -1.06
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
1.70	g	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	30.65 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	18.70 mg/mL	Bocci G, Oprea TI, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose)	105 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.69 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	0.15 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.09 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 8, 1995	FDA	CLINIGEN HLTHCARE

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
Pyrexia	46.77	41.04	41	721	470437	63017823

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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
Mucosal inflammation	132.10	36.08	55	1688	38567	34916621
Laryngeal pain	126.50	36.08	29	1714	2735	34952453
Pyrexia	90.91	36.08	96	1647	332917	34622271
Chills	67.99	36.08	45	1698	80998	34874190
Hypotension	65.71	36.08	67	1676	221582	34733606
Soft tissue disorder	63.15	36.08	13	1730	737	34954451
Rash	54.74	36.08	61	1682	222691	34732497
Dehydration	53.08	36.08	47	1696	129922	34825266
Nausea	47.06	36.08	70	1673	339838	34615350
Dermatitis	44.48	36.08	17	1726	9451	34945737

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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
Laryngeal pain	154.95	33.94	36	2328	6078	79735946
Mucosal inflammation	117.46	33.94	53	2311	75527	79666497
Pyrexia	112.93	33.94	118	2246	678591	79063433
Hypotension	80.90	33.94	81	2283	440236	79301788
Chills	77.67	33.94	52	2312	160182	79581842
Dehydration	63.48	33.94	55	2309	248132	79493892
Radiation skin injury	61.48	33.94	13	2351	1421	79740603
Soft tissue disorder	59.69	33.94	15	2349	3500	79738524
Nausea	59.37	33.94	103	2261	957093	78784931
Rash	58.11	33.94	78	2286	578280	79163744

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	V03AF05	VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Detoxifying agents for antineoplastic treatment
CHEBI has role	CHEBI:22586	antioxidants
CHEBI has role	CHEBI:50266	Prodrugs
CHEBI has role	CHEBI:66987	radiation protective drugs
MeSH PA	D020011	Protective Agents
MeSH PA	D011837	Radiation-Protective 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
Prevention of Xerostomia Secondary to Radiation Therapy	indication
Prevention of Cancer Chemotherapy-Induced Renal Impairment	indication
Myelodysplastic syndrome	off-label use	109995007
Drug-induced mucositis	off-label use	403666006
Chemotherapy-induced neutropenia	off-label use	425229001
Prevention of Chemotherapy-Induced Neurotoxicity	off-label use
Prevention of Radiation Therapy-Induced Mucositis	off-label use
Hypocalcemia	contraindication	5291005
Hypovolemia	contraindication	28560003
Dehydration	contraindication	34095006

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.67	acidic
pKa2	10.06	Basic
pKa3	8.46	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	6.18		DRUG MATRIX
Alkaline phosphatase, tissue-nonspecific isozyme	Enzyme	P05186	PPBT_HUMAN					WOMBAT-PK

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External reference:

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ID	Source
005536	NDDF
108823002	SNOMEDCT_US
112901-68-5	SECONDARY_CAS_RN
133029	MMSL
1545987	RXNORM
2141	PUBCHEM_CID
386923005	SNOMEDCT_US
4020970	VUID
4020970	VANDF
4164	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ethyol	HUMAN PRESCRIPTION DRUG LABEL	1	76310-017	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	500 mg	INTRAVENOUS	NDA	20 sections
Ethyol	HUMAN PRESCRIPTION DRUG LABEL	1	76310-017	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	500 mg	INTRAVENOUS	NDA	20 sections

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