foscarnet ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
insecticides, anthelminthics, pesticides etc., phosphorous derivatives 1241 4428-95-9

Description:

MoleculeDescription

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:

DoseUnitRoute
6.50 g P

ADMET properties:

PropertyValueReference
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 ยตM/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:

DateAgencyCompanyOrphan
Sept. 27, 1991 FDA CLINIGEN HLTHCARE
March 26, 2019 PMDA CLINIGEN K.K.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
DNA polymerase catalytic subunit Enzyme INHIBITOR IC50 4.13 CHEMBL CHEMBL
DNA polymerase catalytic subunit Enzyme IC50 5.60 CHEMBL
Reverse transcriptase/RNaseH Enzyme IC50 5.69 CHEMBL
Reverse transcriptase Enzyme IC50 5.60 CHEMBL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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