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

Stem definition	Drug id	CAS RN
N-methylated xanthine derivatives	2099	6493-05-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: pentoxifylline azupentat dimethyloxohexylxanthine oxpentifylline pentoxifyllin	A METHYLXANTHINE derivative that inhibits phosphodiesterase and affects blood rheology. It improves blood flow by increasing erythrocyte and leukocyte flexibility. It also inhibits platelet aggregation. Pentoxifylline modulates immunologic activity by stimulating cytokine production. Molecular weight: 278.31 Formula: C13H18N4O3 CLOGP: 0.12 LIPINSKI: 0 HAC: 7 HDO: 0 TPSA: 75.51 ALOGS: -1.73 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

pentoxifylline
azupentat
dimethyloxohexylxanthine
oxpentifylline
pentoxifyllin

A METHYLXANTHINE derivative that inhibits phosphodiesterase and affects blood rheology. It improves blood flow by increasing erythrocyte and leukocyte flexibility. It also inhibits platelet aggregation. Pentoxifylline modulates immunologic activity by stimulating cytokine production.

Molecular weight: 278.31
Formula: C13H18N4O3
CLOGP: 0.12
LIPINSKI: 0
HAC: 7
HDO: 0
TPSA: 75.51
ALOGS: -1.73
ROTB: 5

Status: OFP

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

Drug dosage:

Dose	Unit	Route
1	g	O
0.30	g	P

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	71.86 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	39 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	25 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	191 mg/mL	Benet LZ, Broccatelli F, Oprea TI
Vd (Volume of distribution)	1.80 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.20 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.51 %	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Aug. 30, 1984	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
Body tinea	200.27	18.12	44	5753	1841	63481384
Inhibitory drug interaction	177.05	18.12	43	5754	2806	63480419
Infection susceptibility increased	172.92	18.12	44	5753	3477	63479748
Glucose tolerance impaired	145.71	18.12	44	5753	6533	63476692
Purpura	133.36	18.12	47	5750	11338	63471887
Poor quality sleep	127.73	18.12	53	5744	19882	63463343
Impaired quality of life	117.38	18.12	45	5752	13738	63469487
Bone density decreased	111.31	18.12	44	5753	14568	63468657
Hyperlipidaemia	102.13	18.12	45	5752	19526	63463699
Impaired work ability	100.38	18.12	43	5754	17432	63465793

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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
Acute kidney injury	43.47	17.91	106	4115	304882	34647828
Peripheral artery occlusion	41.06	17.91	13	4208	1699	34951011
Blood lactic acid	39.41	17.91	9	4212	337	34952373
Pleural mass	39.12	17.91	7	4214	73	34952637
Hyperkalaemia	37.50	17.91	44	4177	69345	34883365
Skin hyperpigmentation	36.40	17.91	14	4207	3250	34949460
Biopsy lymph gland	33.15	17.91	6	4215	67	34952643
Heart valve stenosis	32.17	17.91	6	4215	80	34952630
Peripheral ischaemia	31.97	17.91	15	4206	5672	34947038
Drug dependence	31.63	17.91	25	4196	24192	34928518

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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
Body tinea	185.22	15.24	43	9187	1811	79733347
Infection susceptibility increased	155.48	15.24	43	9187	3678	79731480
Glucose tolerance impaired	149.99	15.24	50	9180	8034	79727124
Inhibitory drug interaction	143.43	15.24	42	9188	4411	79730747
Purpura	110.33	15.24	51	9179	19476	79715682
Bone density decreased	101.67	15.24	43	9187	13304	79721854
Poor quality sleep	100.01	15.24	50	9180	22672	79712486
Impaired quality of life	98.56	15.24	43	9187	14343	79720815
Impaired work ability	82.77	15.24	42	9188	19639	79715519
Hyperlipidaemia	79.68	15.24	45	9185	26048	79709110

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C04AD03	CARDIOVASCULAR SYSTEM PERIPHERAL VASODILATORS PERIPHERAL VASODILATORS Purine derivatives
FDA EPC	N0000175895	Blood Viscosity Reducer
FDA PE	N0000009065	Hematologic Activity Alteration
MeSH PA	D000975	Antioxidants
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D016166	Free Radical Scavengers
MeSH PA	D006401	Hematologic Agents
MeSH PA	D010726	Phosphodiesterase Inhibitors
MeSH PA	D010975	Platelet Aggregation Inhibitors

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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
Peripheral vascular disease	indication	400047006
Osteoradionecrosis	off-label use	109333005
Alcoholic hepatitis	off-label use	235875008
Retinal hemorrhage	contraindication	28998008
Blood coagulation disorder	contraindication	64779008	DOID:1247
Kidney disease	contraindication	90708001	DOID:557
Bleeding	contraindication	131148009
Hemorrhagic cerebral infarction	contraindication	230706003

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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	1.43	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])	Bioact source	MoA source
Adenosine receptor A2b	GPCR	P29275	AA2BR_HUMAN	ANTAGONIST	Ki	5.29	CHEMBL	CHEMBL
cAMP-specific 3',5'-cyclic phosphodiesterase 4B	Enzyme	Q07343	PDE4B_HUMAN	INHIBITOR			WOMBAT-PK	CHEMBL
cGMP-specific 3',5'-cyclic phosphodiesterase	Enzyme	O76074	PDE5A_HUMAN	INHIBITOR			DRUGBANK	CHEMBL
Acetylcholinesterase	Enzyme	P22303	ACES_HUMAN		IC50	5.18	CHEMBL

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External reference:

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ID	Source
PNX	PDB_CHEM_ID
002098	NDDF
10203	MMSL
3309	INN_ID
387522004	SNOMEDCT_US
4018468	VUID
4018468	VANDF
41909	MMSL
4740	PUBCHEM_CID
5257	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
BETAMETHASONE DIPROPIONATE 0.05% / MINOXIDIL 5% / NIACINAMIDE 2% / PENTOXIFYLLINE 0.5%	HUMAN PRESCRIPTION DRUG LABEL	4	72934-4024	SOLUTION	2 g	TOPICAL	unapproved drug other	4 sections
PENTOXIFYLLINE	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8305	TABLET, EXTENDED RELEASE	400 mg	ORAL	ANDA	17 sections
PENTOXIFYLLINE	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8305	TABLET, EXTENDED RELEASE	400 mg	ORAL	ANDA	17 sections
PENTOXIFYLLINE	HUMAN PRESCRIPTION DRUG LABEL	1	0904-5448	TABLET, EXTENDED RELEASE	400 mg	ORAL	ANDA	17 sections
PENTOXIFYLLINE	HUMAN PRESCRIPTION DRUG LABEL	1	16590-856	TABLET, EXTENDED RELEASE	400 mg	ORAL	ANDA	19 sections
PENTOXIFYLLINE	HUMAN PRESCRIPTION DRUG LABEL	1	33261-992	TABLET, EXTENDED RELEASE	400 mg	ORAL	ANDA	17 sections
Pentoxifylline	HUMAN PRESCRIPTION DRUG LABEL	1	43353-123	TABLET, EXTENDED RELEASE	400 mg	ORAL	ANDA	19 sections
Pentoxifylline	HUMAN PRESCRIPTION DRUG LABEL	1	53808-0516	TABLET, FILM COATED, EXTENDED RELEASE	400 mg	ORAL	ANDA	19 sections
Pentoxifylline	HUMAN PRESCRIPTION DRUG LABEL	1	53808-0757	TABLET, EXTENDED RELEASE	400 mg	ORAL	ANDA	19 sections
Pentoxifylline	HUMAN PRESCRIPTION DRUG LABEL	1	53808-0758	TABLET, FILM COATED, EXTENDED RELEASE	400 mg	ORAL	ANDA	19 sections

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