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

Stem definition	Drug id	CAS RN
insecticides, anthelminthics, pesticides etc., phosphorous derivatives	1241	4428-95-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: foscavir foscarnet phosphonocarboxylic acid phosphonoformic acid foscarnet sodium foscarnet sodium hydrate	An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV. Molecular weight: 126.00 Formula: CH3O5P CLOGP: -2.17 LIPINSKI: 0 HAC: 5 HDO: 3 TPSA: 94.83 ALOGS: -0.88 ROTB: 1 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

foscavir
foscarnet
phosphonocarboxylic acid
phosphonoformic acid
foscarnet sodium
foscarnet sodium hydrate

An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.

Molecular weight: 126.00
Formula: CH3O5P
CLOGP: -2.17
LIPINSKI: 0
HAC: 5
HDO: 3
TPSA: 94.83
ALOGS: -0.88
ROTB: 1

Status: OFP

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

Drug dosage:

Dose	Unit	Route
6.50	g	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	82 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	952.34 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	9 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.50 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.10 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.85 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	4.70 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Sept. 27, 1991	FDA	CLINIGEN HLTHCARE
March 26, 2019	PMDA	CLINIGEN K.K.

FDA Adverse Event Reporting System (Female)

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
Drug resistance	413.77	39.62	120	3726	18869	50582409
Pathogen resistance	413.47	39.62	94	3752	5595	50595683
Encephalitis cytomegalovirus	242.29	39.62	41	3805	501	50600777
Cytomegalovirus viraemia	212.61	39.62	53	3793	4656	50596622
Cytomegalovirus infection	199.71	39.62	68	3778	17894	50583384
Nephropathy toxic	180.11	39.62	52	3794	7977	50593301
Off label use	121.11	39.62	163	3683	474263	50127015
Transplant dysfunction	112.44	39.62	32	3814	4652	50596626
Multiple organ dysfunction syndrome	95.78	39.62	55	3791	50282	50550996
Graft versus host disease in gastrointestinal tract	94.62	39.62	25	3821	2756	50598522
Renal impairment	84.49	39.62	59	3787	75602	50525676
Graft versus host disease	74.97	39.62	25	3821	6141	50595137
Acute graft versus host disease	72.79	39.62	22	3824	3936	50597342
Pancytopenia	72.30	39.62	56	3790	83974	50517304
Adenoviral hepatitis	72.01	39.62	13	3833	235	50601043
Cystitis haemorrhagic	69.90	39.62	21	3825	3681	50597597
Venoocclusive liver disease	62.84	39.62	20	3826	4241	50597037
Adenovirus infection	59.94	39.62	18	3828	3150	50598128
Pneumonia cytomegaloviral	59.16	39.62	16	3830	1925	50599353
Neutropenia	58.90	39.62	64	3782	147901	50453377
Cytomegalovirus chorioretinitis	58.27	39.62	15	3831	1492	50599786
Haemophagocytic lymphohistiocytosis	55.99	39.62	22	3824	8611	50592667
Cytomegalovirus enterocolitis	55.57	39.62	12	3834	557	50600721
Cytomegalovirus colitis	54.61	39.62	15	3831	1912	50599366
Hepatic failure	50.19	39.62	31	3815	32252	50569026
Thrombotic microangiopathy	45.32	39.62	19	3827	8772	50592506
Epstein-Barr virus infection reactivation	45.16	39.62	10	3836	522	50600756
Cytomegalovirus gastrointestinal infection	45.02	39.62	9	3837	285	50600993
Staphylococcal sepsis	42.38	39.62	17	3829	7019	50594259
Cytomegalovirus test positive	41.68	39.62	13	3833	2579	50598699
Venous haemorrhage	41.57	39.62	8	3838	207	50601071
Disseminated intravascular coagulation	41.55	39.62	22	3824	17113	50584165
Cytomegalovirus infection reactivation	41.49	39.62	13	3833	2618	50598660
Hydrocephalus	41.18	39.62	15	3831	4773	50596505
Bronchopulmonary aspergillosis	41.13	39.62	17	3829	7575	50593703
Myelosuppression	40.45	39.62	20	3826	13497	50587781

FDA Adverse Event Reporting System (Male)

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
Drug resistance	383.37	32.56	139	4489	21401	29548498
Pathogen resistance	245.09	32.56	78	4550	8038	29561861
Cytomegalovirus viraemia	221.16	32.56	68	4560	6252	29563647
Off label use	175.97	32.56	224	4404	300576	29269323
Pneumonia cytomegaloviral	124.82	32.56	36	4592	2646	29567253
Encephalitis cytomegalovirus	119.62	32.56	25	4603	469	29569430
Renal impairment	105.39	32.56	93	4535	81240	29488659
Cytomegalovirus chorioretinitis	101.27	32.56	32	4596	3206	29566693
Nephropathy toxic	98.21	32.56	43	4585	10713	29559186
Cytomegalovirus infection	82.35	32.56	49	4579	23166	29546733
Acute graft versus host disease in skin	82.31	32.56	30	4598	4634	29565265
Pancytopenia	75.14	32.56	78	4550	83090	29486809
Multiple organ dysfunction syndrome	71.50	32.56	67	4561	63049	29506850
Retinal detachment	64.02	32.56	25	4603	4661	29565238
Acute graft versus host disease	62.10	32.56	26	4602	5798	29564101
Graft versus host disease	58.35	32.56	29	4599	9599	29560300
Renal tubular disorder	55.19	32.56	22	4606	4330	29565569
Encephalitis	53.19	32.56	24	4604	6406	29563493
Botulism	49.33	32.56	10	4618	160	29569739
Thrombotic microangiopathy	46.34	32.56	24	4604	8657	29561242
Cystitis haemorrhagic	46.26	32.56	20	4608	4822	29565077
Hypokalaemia	45.10	32.56	47	4581	50156	29519743
Retinal scar	44.22	32.56	10	4618	274	29569625
Cytomegalovirus infection reactivation	42.63	32.56	17	4611	3347	29566552
Drug ineffective	41.99	32.56	138	4490	363032	29206867
Disseminated cytomegaloviral infection	41.60	32.56	9	4619	200	29569699
Acute graft versus host disease in intestine	41.07	32.56	15	4613	2326	29567573
Aplastic anaemia	40.76	32.56	21	4607	7489	29562410
Cytomegalovirus colitis	40.30	32.56	15	4613	2454	29567445
Necrotising retinitis	38.82	32.56	11	4617	757	29569142
Bone marrow failure	38.67	32.56	33	4595	27416	29542483
Product use issue	37.23	32.56	43	4585	51401	29518498
Glomerulonephropathy	36.43	32.56	8	4620	191	29569708
Chronic graft versus host disease	36.40	32.56	16	4612	4013	29565886
Meningoencephalitis herpetic	34.33	32.56	10	4618	759	29569140
Bacterial toxaemia	32.78	32.56	7	4621	146	29569753

FDA Adverse Event Reporting System (Geriatric)

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
Drug resistance	789.51	31.93	255	7799	34847	64455831
Pathogen resistance	625.44	31.93	169	7885	12374	64478304
Cytomegalovirus viraemia	389.24	31.93	113	7941	10715	64479963
Encephalitis cytomegalovirus	341.63	31.93	65	7989	940	64489738
Off label use	269.94	31.93	360	7694	632446	63858232
Nephropathy toxic	254.70	31.93	92	7962	17422	64473256
Cytomegalovirus infection	246.63	31.93	111	7943	37088	64453590
Renal impairment	178.43	31.93	142	7912	134875	64355803
Pneumonia cytomegaloviral	176.94	31.93	50	8004	4289	64486389
Pancytopenia	138.55	31.93	126	7928	143183	64347495
Cytomegalovirus chorioretinitis	132.01	31.93	41	8013	4871	64485807
Multiple organ dysfunction syndrome	126.06	31.93	103	7951	101310	64389368
Transplant dysfunction	123.37	31.93	42	8012	6666	64484012
Graft versus host disease	116.85	31.93	49	8005	13764	64476914
Acute graft versus host disease	110.93	31.93	42	8012	9042	64481636
Graft versus host disease in gastrointestinal tract	98.76	31.93	34	8020	5578	64485100
Cytomegalovirus colitis	89.85	31.93	29	8025	3899	64486779
Cystitis haemorrhagic	87.18	31.93	34	8020	7922	64482756
Renal tubular disorder	81.56	31.93	30	8024	5957	64484721
Cytomegalovirus infection reactivation	79.00	31.93	29	8025	5727	64484951
Acute graft versus host disease in skin	77.61	31.93	30	8024	6825	64483853
Thrombotic microangiopathy	77.49	31.93	39	8015	16616	64474062
Adenoviral hepatitis	73.87	31.93	16	8038	452	64490226
Adenovirus infection	72.47	31.93	29	8025	7226	64483452
Retinal detachment	63.14	31.93	27	8027	7949	64482729
Fatigue	61.58	31.93	10	8044	748720	63741958
Haemophagocytic lymphohistiocytosis	61.37	31.93	34	8020	17575	64473103
Cytomegalovirus test positive	56.41	31.93	22	8032	5122	64485556
Acute graft versus host disease in intestine	56.33	31.93	20	8034	3589	64487089
Acute kidney injury	55.18	31.93	151	7903	449089	64041589
Hypocalcaemia	55.16	31.93	44	8010	41709	64448969
Hypomagnesaemia	55.03	31.93	42	8012	37334	64453344
Epstein-Barr virus infection reactivation	54.68	31.93	15	8039	1151	64489527
Genital ulceration	53.22	31.93	13	8041	630	64490048
Human herpesvirus 6 encephalitis	53.09	31.93	12	8042	414	64490264
Meningoencephalitis herpetic	52.83	31.93	16	8038	1745	64488933
Myelosuppression	51.86	31.93	34	8020	23796	64466882
Venoocclusive liver disease	51.17	31.93	25	8029	9990	64480688
Bone marrow failure	49.83	31.93	44	8010	47908	64442770
Chronic graft versus host disease	48.86	31.93	21	8033	6255	64484423
Encephalitis	48.59	31.93	26	8028	12545	64478133
Bronchopulmonary aspergillosis	48.41	31.93	30	8024	19055	64471623
Hepatic failure	48.17	31.93	46	8008	55348	64435330
Neutropenia	47.29	31.93	97	7957	239527	64251151
Staphylococcal sepsis	45.20	31.93	25	8029	12874	64477804
Hypokalaemia	44.73	31.93	65	7989	121838	64368840
Toxic epidermal necrolysis	44.52	31.93	37	8017	37129	64453549
Human herpesvirus 6 infection	44.40	31.93	18	8036	4636	64486042
Botulism	44.07	31.93	10	8044	351	64490327
Cytomegalovirus enterocolitis	43.62	31.93	13	8041	1342	64489336
Cytopenia	43.56	31.93	26	8028	15445	64475233
Aplastic anaemia	43.42	31.93	25	8029	13895	64476783
Retinal scar	43.15	31.93	10	8044	386	64490292
Cytomegalovirus gastritis	42.54	31.93	10	8044	411	64490267
Disseminated intravascular coagulation	42.53	31.93	34	8020	32314	64458364
Disseminated cytomegaloviral infection	42.45	31.93	10	8044	415	64490263
Respiratory failure	41.35	31.93	73	7981	161110	64329568
Electrolyte imbalance	40.79	31.93	30	8024	25213	64465465
Fall	40.64	31.93	3	8051	416823	64073855
Product use issue	38.00	31.93	68	7986	151647	64339031
Necrotising retinitis	37.73	31.93	11	8043	1052	64489626
Renal failure	37.53	31.93	75	7979	181613	64309065
Viral haemorrhagic cystitis	37.10	31.93	12	8042	1623	64489055
Pneumonia pseudomonal	36.84	31.93	16	8038	4887	64485791
Venous haemorrhage	35.91	31.93	8	8046	258	64490420
Neurological decompensation	35.05	31.93	15	8039	4421	64486257
Glomerulonephropathy	34.95	31.93	8	8046	292	64490386
Bacterial toxaemia	33.91	31.93	7	8047	156	64490522
Drug ineffective	33.21	31.93	198	7856	840049	63650629
Aspergillus infection	32.33	31.93	22	8032	16357	64474321

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	J05AD01	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Phosphonic acid derivatives
FDA MoA	N0000000087	Chelating Activity
FDA MoA	N0000020060	DNA Polymerase Inhibitors
FDA EXT	N0000175469	Pyrophosphate Analog
FDA EPC	N0000175470	Pyrophosphate Analog DNA Polymerase Inhibitor
CHEBI has role	CHEBI:36044	antiviral drugs
CHEBI has role	CHEBI:53756	reverse transcriptase inhibitors
CHEBI has role	CHEBI:63330	Na-Pi inhibitor
CHEBI has role	CHEBI:176497	geroprotectors
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000998	Antiviral Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D019384	Nucleic Acid Synthesis Inhibitors
MeSH PA	D018894	Reverse Transcriptase Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Encephalitis caused by human herpesvirus 6 infection	indication	441512004
Acyclovir-Resistant Mucocutaneous HSV in Immunocompromised Patients	indication
CMV Retinitis in AIDS Patients	indication
Herpes zoster associated with AIDS	off-label use	422127002
Acyclovir-Resistant HSV Infections	off-label use
CMV-Related Polyradiculopathy in AIDS Patients	off-label use
Prevention of Cytomegalovirus Disease	off-label use
Hypophosphatemia	contraindication	4996001
Hypocalcemia	contraindication	5291005
Hyperphosphatemia	contraindication	20165001	DOID:0050459
Torsades de pointes	contraindication	31722008
Dehydration	contraindication	34095006
Hypokalemia	contraindication	43339004
Epilepsy	contraindication	84757009	DOID:1826
Kidney disease	contraindication	90708001	DOID:557
Prolonged QT interval	contraindication	111975006
Hypomagnesemia	contraindication	190855004
Anemia	contraindication	271737000	DOID:2355
Neutropenic disorder	contraindication	303011007	DOID:1227
Granulocytopenic disorder	contraindication	417672002
Congenital long QT syndrome	contraindication	442917000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	0.44	acidic
pKa2	3.41	acidic
pKa3	5.49	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
DNA polymerase catalytic subunit	Enzyme	DPOL_HHV11	INHIBITOR	IC50	4.13	CHEMBL	CHEMBL
DNA polymerase catalytic subunit	Enzyme	DPOL_HCMVA		IC50	5.60	CHEMBL
Reverse transcriptase/RNaseH	Enzyme	Q72547_9HIV1		IC50	5.69	CHEMBL
Reverse transcriptase	Enzyme	Q9WKE8_9HIV1		IC50	5.60	CHEMBL

External reference:

ID	Source
D00579	KEGG_DRUG
34156-56-4	SECONDARY_CAS_RN
4020530	VANDF
C0070895	UMLSCUI
CHEBI:127780	CHEBI
PPF	PDB_CHEM_ID
CHEMBL666	ChEMBL_ID
3415	PUBCHEM_CID
DB00529	DRUGBANK_ID
CHEMBL754	ChEMBL_ID
D017245	MESH_DESCRIPTOR_UI
5497	IUPHAR_LIGAND_ID
364P9RVW4X	UNII
225811	RXNORM
306	MMSL
4764	MMSL
74819	MMSL
d00065	MMSL
003605	NDDF
006662	NDDF
372902006	SNOMEDCT_US
96099004	SNOMEDCT_US
96100007	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Foscarnet Sodium	HUMAN PRESCRIPTION DRUG LABEL	1	25021-189	INJECTION, SOLUTION	24 mg	INTRAVENOUS	ANDA	25 sections
Foscarnet	HUMAN PRESCRIPTION DRUG LABEL	1	63323-875	INJECTION, SOLUTION	24 mg	INTRAVENOUS	ANDA	23 sections
Foscarnet Sodium	Human Prescription Drug Label	1	68083-389	INJECTION, SOLUTION	24 mg	INTRAVENOUS	ANDA	21 sections
Foscavir	HUMAN PRESCRIPTION DRUG LABEL	1	76310-024	INJECTION, SOLUTION	24 mg	INTRAVENOUS	NDA	24 sections
Foscavir	HUMAN PRESCRIPTION DRUG LABEL	1	76310-024	INJECTION, SOLUTION	24 mg	INTRAVENOUS	NDA	24 sections
Foscavir	HUMAN PRESCRIPTION DRUG LABEL	1	76310-024	INJECTION, SOLUTION	24 mg	INTRAVENOUS	NDA	24 sections