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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
S (Water solubility)	24 mg/mL	Bocci G, Oprea TI, Benet LZ

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	485.65	41.40	138	4140	22795	63461949
Pathogen resistance	440.79	41.40	99	4179	6299	63478445
Encephalitis cytomegalovirus	245.78	41.40	41	4237	520	63484224
Cytomegalovirus viraemia	229.27	41.40	57	4221	5592	63479152
Cytomegalovirus infection	221.01	41.40	74	4204	20878	63463866
Nephropathy toxic	195.52	41.40	56	4222	9423	63475321
Off label use	143.14	41.40	199	4079	674263	62810481
Transplant dysfunction	114.99	41.40	32	4246	4840	63479904
Graft versus host disease in gastrointestinal tract	113.09	41.40	29	4249	3212	63481532
Multiple organ dysfunction syndrome	109.38	41.40	60	4218	56692	63428052
Renal impairment	101.58	41.40	67	4211	88288	63396456
Graft versus host disease	83.75	41.40	27	4251	6736	63478008
Cystitis haemorrhagic	83.36	41.40	24	4254	4099	63480645
Pancytopenia	77.71	41.40	59	4219	96874	63387870
Acute graft versus host disease	72.96	41.40	22	4256	4406	63480338
Adenoviral hepatitis	67.34	41.40	13	4265	388	63484356
Haemophagocytic lymphohistiocytosis	64.61	41.40	25	4253	10602	63474142
Adenovirus infection	64.29	41.40	19	4259	3552	63481192
Pneumonia cytomegaloviral	63.69	41.40	17	4261	2197	63482547
Venoocclusive liver disease	62.72	41.40	20	4258	4815	63479929
Cytomegalovirus colitis	62.53	41.40	17	4261	2355	63482389
Cytomegalovirus chorioretinitis	62.33	41.40	16	4262	1777	63482967
Neutropenia	59.81	41.40	66	4212	174939	63309805
Viral haemorrhagic cystitis	57.31	41.40	13	4265	856	63483888
Cytomegalovirus enterocolitis	54.86	41.40	12	4266	669	63484075
Cytomegalovirus infection reactivation	53.91	41.40	17	4261	3946	63480798
Epstein-Barr virus infection reactivation	52.97	41.40	12	4266	786	63483958
Hepatic failure	50.78	41.40	31	4247	35625	63449119
Thrombotic microangiopathy	47.47	41.40	20	4258	10541	63474203
Cytomegalovirus gastrointestinal infection	45.62	41.40	9	4269	301	63484443
Respiratory failure	44.78	41.40	44	4234	101814	63382930
Bronchopulmonary aspergillosis	44.39	41.40	18	4260	8617	63476127
Fatigue	42.78	41.40	5	4273	888023	62596721
Staphylococcal sepsis	41.98	41.40	17	4261	8111	63476633
Disseminated intravascular coagulation	41.84	41.40	22	4256	19029	63465715
Hydrocephalus	41.45	41.40	15	4263	5285	63479459

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	440.46	31.83	160	5100	25767	34925904
Pathogen resistance	248.19	31.83	81	5179	9401	34942270
Cytomegalovirus viraemia	229.49	31.83	72	5188	7358	34944313
Off label use	172.05	31.83	258	5002	419266	34532405
Encephalitis cytomegalovirus	143.47	31.83	30	5230	588	34951083
Pneumonia cytomegaloviral	134.80	31.83	39	5221	3015	34948656
Nephropathy toxic	119.07	31.83	51	5209	12537	34939134
Cytomegalovirus infection	110.48	31.83	61	5199	26074	34925597
Cytomegalovirus chorioretinitis	107.49	31.83	34	5226	3555	34948116
Renal impairment	106.06	31.83	98	5162	94415	34857256
Pancytopenia	94.04	31.83	92	5168	95065	34856606
Acute graft versus host disease in skin	87.62	31.83	32	5228	5169	34946502
Cystitis haemorrhagic	70.63	31.83	28	5232	5651	34946020
Cytomegalovirus infection reactivation	69.88	31.83	27	5233	5091	34946580
Drug ineffective	67.22	31.83	184	5076	456567	34495104
Multiple organ dysfunction syndrome	66.34	31.83	69	5191	76497	34875174
Retinal detachment	65.02	31.83	26	5234	5365	34946306
Acute graft versus host disease	63.62	31.83	27	5233	6476	34945195
Graft versus host disease	56.86	31.83	29	5231	10540	34941131
Renal tubular disorder	54.64	31.83	22	5238	4621	34947050
Myelosuppression	52.70	31.83	34	5226	19231	34932440
Encephalitis	51.24	31.83	24	5236	7253	34944418
Botulism	49.66	31.83	10	5250	161	34951510
Product use issue	49.47	31.83	54	5206	63162	34888509
Retinal scar	48.87	31.83	11	5249	307	34951364
Aplastic anaemia	47.49	31.83	25	5235	9691	34941980
BK virus infection	46.92	31.83	21	5239	5717	34945954
Acute graft versus host disease in intestine	46.86	31.83	17	5243	2691	34948980
Thrombotic microangiopathy	42.65	31.83	24	5236	10606	34941065
Hypokalaemia	42.56	31.83	48	5212	58166	34893505
Acute kidney injury	41.77	31.83	120	5140	304868	34646803
Disseminated cytomegaloviral infection	41.25	31.83	9	5251	217	34951454
Bone marrow failure	39.99	31.83	34	5226	29219	34922452
Cytomegalovirus colitis	39.11	31.83	15	5245	2769	34948902
Necrotising retinitis	38.24	31.83	11	5249	831	34950840
Glomerulonephropathy	35.80	31.83	8	5252	216	34951455
Chronic graft versus host disease	35.74	31.83	16	5244	4357	34947314
Cytomegalovirus test positive	34.27	31.83	15	5245	3871	34947800
Meningoencephalitis herpetic	33.90	31.83	10	5250	825	34950846
Bacterial toxaemia	33.05	31.83	7	5253	146	34951525
Aspergillus infection	31.97	31.83	21	5239	12233	34939438

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	920.20	32.13	293	8803	41920	79693372
Pathogen resistance	646.00	32.13	175	8921	14167	79721125
Cytomegalovirus viraemia	406.71	32.13	119	8977	12702	79722590
Encephalitis cytomegalovirus	369.98	32.13	70	9026	1080	79734212
Cytomegalovirus infection	296.28	32.13	128	8968	42516	79692776
Off label use	291.97	32.13	430	8666	906785	78828507
Nephropathy toxic	290.18	32.13	103	8993	20316	79714976
Renal impairment	197.78	32.13	155	8941	157628	79577664
Pneumonia cytomegaloviral	188.24	32.13	53	9043	4916	79730376
Pancytopenia	166.10	32.13	143	8953	165602	79569690
Cytomegalovirus chorioretinitis	148.10	32.13	45	9051	5445	79729847
Multiple organ dysfunction syndrome	133.24	32.13	110	8986	120136	79615156
Cystitis haemorrhagic	125.42	32.13	45	9051	9127	79726165
Transplant dysfunction	124.05	32.13	42	9054	7179	79728113
Graft versus host disease	123.89	32.13	51	9045	14975	79720317
Cytomegalovirus infection reactivation	123.86	32.13	44	9052	8672	79726620
Graft versus host disease in gastrointestinal tract	117.23	32.13	39	9057	6317	79728975
Acute graft versus host disease	113.62	32.13	43	9053	10124	79725168
Cytomegalovirus colitis	95.46	32.13	31	9065	4654	79730638
Acute graft versus host disease in skin	84.16	32.13	32	9064	7626	79727666
Myelosuppression	83.77	32.13	54	9042	40242	79695050
Renal tubular disorder	81.86	32.13	30	9066	6456	79728836
Thrombotic microangiopathy	76.61	32.13	40	9056	20129	79715163
Adenovirus infection	74.16	32.13	30	9066	8417	79726875
Acute kidney injury	73.44	32.13	174	8922	519230	79216062
BK virus infection	72.96	32.13	30	9066	8774	79726518
Fatigue	68.39	32.13	12	9084	929715	78805577
Haemophagocytic lymphohistiocytosis	68.11	32.13	38	9058	21799	79713493
Drug ineffective	66.94	32.13	271	8825	1080642	78654650
Epstein-Barr virus infection reactivation	66.31	32.13	19	9077	1873	79733419
Retinal detachment	64.90	32.13	28	9068	9219	79726073
Adenoviral hepatitis	64.43	32.13	16	9080	911	79734381
Acute graft versus host disease in intestine	63.53	32.13	22	9074	4019	79731273
Aplastic anaemia	60.92	32.13	33	9063	17872	79717420
Viral haemorrhagic cystitis	60.34	32.13	18	9078	2043	79733249
Cytomegalovirus test positive	55.25	32.13	22	9074	5925	79729367
Bone marrow failure	54.94	32.13	46	9050	51061	79684231
Product use issue	53.38	32.13	90	9006	209732	79525560
Arthralgia	53.20	32.13	3	9093	571800	79163492
Encephalitis	52.44	32.13	28	9068	14732	79720560
Venoocclusive liver disease	52.43	32.13	26	9070	11745	79723547
Meningoencephalitis herpetic	52.34	32.13	16	9080	1973	79733319
Hypocalcaemia	51.74	32.13	44	9052	49880	79685412
Respiratory failure	50.60	32.13	81	9015	180830	79554462
Human herpesvirus 6 infection	50.35	32.13	20	9076	5350	79729942
Hypomagnesaemia	49.96	32.13	42	9054	46869	79688423
Hepatic failure	49.69	32.13	47	9049	61165	79674127
Chronic graft versus host disease	49.13	32.13	21	9075	6760	79728532
Bronchopulmonary aspergillosis	49.11	32.13	31	9065	22263	79713029
Human herpesvirus 6 encephalitis	48.62	32.13	12	9084	666	79734626
Cytomegalovirus gastritis	47.74	32.13	11	9085	454	79734838
Disseminated cytomegaloviral infection	47.51	32.13	11	9085	464	79734828
Genital ulceration	47.46	32.13	13	9083	1087	79734205
Cytopenia	46.55	32.13	29	9067	20354	79714938
Cytomegalovirus enterocolitis	46.49	32.13	14	9082	1641	79733651
Necrotising retinitis	45.87	32.13	13	9083	1232	79734060
Neutropenia	44.49	32.13	100	8996	287610	79447682
Staphylococcal sepsis	44.22	32.13	25	9071	14701	79720591
Botulism	44.18	32.13	10	9086	381	79734911
Retinal scar	43.28	32.13	10	9086	418	79734874
Aspergillus infection	43.10	32.13	27	9069	19134	79716158
Hypokalaemia	42.34	32.13	66	9030	143974	79591318
Electrolyte imbalance	42.18	32.13	32	9064	30849	79704443
Disseminated intravascular coagulation	42.16	32.13	34	9062	35808	79699484
Toxic epidermal necrolysis	41.57	32.13	37	9059	44544	79690748
Fall	41.24	32.13	4	9092	487625	79247667
Renal failure	39.38	32.13	77	9019	200891	79534401
Product use in unapproved indication	38.66	32.13	87	9009	250272	79485020
Malaise	36.63	32.13	6	9090	489863	79245429
Dyspnoea	36.29	32.13	27	9069	856998	78878294
Pneumonia pseudomonal	35.36	32.13	16	9080	5895	79729397
Glomerulonephropathy	35.18	32.13	8	9088	311	79734981
Bacterial toxaemia	34.54	32.13	7	9089	156	79735136
Venous haemorrhage	34.36	32.13	8	9088	346	79734946
Dizziness	34.11	32.13	9	9087	526432	79208860
Pain	34.11	32.13	19	9077	703783	79031509
Neurological decompensation	33.91	32.13	15	9081	5238	79730054
Post transplant lymphoproliferative disorder	33.17	32.13	19	9077	11445	79723847
Septic shock	32.96	32.13	54	9042	122747	79612545

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	23155-771	INJECTION, SOLUTION	24 mg	INTRAVENOUS	ANDA	20 sections
Foscarnet Sodium	HUMAN PRESCRIPTION DRUG LABEL	1	25021-189	INJECTION, SOLUTION	24 mg	INTRAVENOUS	ANDA	25 sections
FOSCARNET SODIUM	HUMAN PRESCRIPTION DRUG LABEL	1	43066-089	INJECTION, SOLUTION	6000 mg	INTRAVENOUS	ANDA	22 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
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