foscarnet 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

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

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 617.86 45.43 175 5585 30274 90592413
Pathogen resistance 470.70 45.43 108 5652 8007 90614680
Encephalitis cytomegalovirus 279.03 45.43 47 5713 675 90622012
Cytomegalovirus infection 278.09 45.43 92 5668 26510 90596177
Cytomegalovirus viraemia 259.52 45.43 66 5694 7520 90615167
Nephropathy toxic 252.66 45.43 72 5688 12616 90610071
Off label use 202.21 45.43 294 5466 1101958 89520729
Viral haemorrhagic cystitis 172.07 45.43 35 5725 1458 90621229
Renal impairment 153.72 45.43 91 5669 105330 90517357
Transplant dysfunction 151.69 45.43 40 5720 5242 90617445
Cytomegalovirus infection reactivation 136.26 45.43 40 5720 7760 90614927
Multiple organ dysfunction syndrome 134.92 45.43 72 5688 68264 90554423
Graft versus host disease in gastrointestinal tract 120.13 45.43 32 5728 4356 90618331
BK virus infection 109.97 45.43 30 5730 4468 90618219
Pancytopenia 104.31 45.43 75 5685 120188 90502499
Graft versus host disease 100.58 45.43 32 5728 8112 90614575
Chronic graft versus host disease 98.37 45.43 27 5733 4112 90618575
Pneumonia cytomegaloviral 96.25 45.43 25 5735 3086 90619601
Acute graft versus host disease 95.31 45.43 28 5732 5440 90617247
Cystitis haemorrhagic 95.08 45.43 28 5732 5485 90617202
Cytomegalovirus gastrointestinal infection 92.89 45.43 17 5743 401 90622286
Venoocclusive liver disease 92.78 45.43 28 5732 5965 90616722
Retinitis viral 92.03 45.43 16 5744 279 90622408
Haemophagocytic lymphohistiocytosis 91.14 45.43 35 5725 15424 90607263
Neutropenia 84.88 45.43 87 5673 224817 90397870
Hypouricaemia 80.21 45.43 14 5746 250 90622437
Adenoviral hepatitis 78.92 45.43 15 5745 437 90622250
Cytomegalovirus chorioretinitis 77.55 45.43 20 5740 2399 90620288
Epstein-Barr virus infection reactivation 74.89 45.43 18 5742 1619 90621068
Human herpesvirus 6 infection 70.62 45.43 20 5740 3412 90619275
Acute kidney injury 70.62 45.43 94 5666 320293 90302394
Adenovirus infection 68.99 45.43 21 5739 4601 90618086
Cytomegalovirus colitis 66.38 45.43 19 5741 3367 90619320
Acidosis hyperchloraemic 62.99 45.43 14 5746 892 90621795
Myelosuppression 59.60 45.43 39 5721 53552 90569135
Renal tubular injury 58.51 45.43 14 5746 1235 90621452
Bladder hypertrophy 58.44 45.43 12 5748 523 90622164
Infection reactivation 57.16 45.43 15 5745 1925 90620762
Cerebral toxoplasmosis 56.87 45.43 14 5746 1391 90621296
Respiratory failure 56.21 45.43 52 5708 118366 90504321
Graft versus host disease in skin 55.35 45.43 17 5743 3836 90618851
Hepatic failure 54.43 45.43 33 5727 39695 90582992
Fatigue 52.72 45.43 6 5754 1154017 89468670
Cytomegalovirus enterocolitis 52.57 45.43 12 5748 862 90621825
Hypomagnesaemia 52.49 45.43 31 5729 35557 90587130
Nephrogenic diabetes insipidus 51.33 45.43 12 5748 958 90621729
Thrombotic microangiopathy 50.15 45.43 23 5737 15720 90606967
Staphylococcal sepsis 47.39 45.43 19 5741 9364 90613323
Bronchopulmonary aspergillosis 47.12 45.43 20 5740 11378 90611309
Disseminated intravascular coagulation 46.15 45.43 24 5736 21514 90601173
Venous haemorrhage 46.12 45.43 9 5751 302 90622385

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 605.56 32.38 224 6930 34024 42580157
Nephropathy toxic 307.47 32.38 113 7041 16725 42597456
Cytomegalovirus viraemia 267.33 32.38 90 7064 10287 42603894
Cystitis haemorrhagic 255.66 32.38 80 7074 7249 42606932
Pathogen resistance 250.96 32.38 88 7066 11362 42602819
Cytomegalovirus infection reactivation 241.50 32.38 85 7069 11093 42603088
Off label use 228.10 32.38 391 6763 637944 41976237
BK virus infection 205.90 32.38 71 7083 8713 42605468
Epstein-Barr viraemia 203.78 32.38 52 7102 2237 42611944
Pancytopenia 195.77 32.38 160 6994 117583 42496598
Myelosuppression 179.06 32.38 101 7053 40360 42573821
Encephalitis cytomegalovirus 175.97 32.38 41 7113 1198 42612983
Pneumonia cytomegaloviral 156.30 32.38 48 7106 4078 42610103
Drug ineffective 156.01 32.38 331 6823 629866 41984315
Cytomegalovirus chorioretinitis 134.68 32.38 44 7110 4567 42609614
Cytomegalovirus infection 133.08 32.38 77 7077 32229 42581952
Generalised oedema 122.34 32.38 57 7097 15279 42598902
Acute kidney injury 106.86 32.38 207 6947 367130 42247051
Acute graft versus host disease in skin 103.59 32.38 41 7113 7383 42606798
Renal impairment 103.39 32.38 109 7045 110119 42504062
Respiratory distress 100.60 32.38 71 7083 41749 42572432
Retinal detachment 67.16 32.38 29 7125 6496 42607685
Acute graft versus host disease 63.83 32.38 30 7124 8185 42605996
Necrotising retinitis 61.19 32.38 17 7137 1013 42613168
Aplastic anaemia 60.38 32.38 33 7121 12351 42601830
Multiple organ dysfunction syndrome 59.16 32.38 77 7077 96958 42517223
Graft versus host disease 59.06 32.38 33 7121 12892 42601289
Renal tubular disorder 57.78 32.38 24 7130 4885 42609296
Thrombotic microangiopathy 57.55 32.38 34 7120 14748 42599433
Lung disorder 57.01 32.38 54 7100 47869 42566312
Product use issue 56.56 32.38 67 7087 76684 42537497
Acute graft versus host disease in intestine 52.25 32.38 21 7133 3930 42610251
Botulism 51.61 32.38 11 7143 211 42613970
Retinal scar 50.89 32.38 12 7142 369 42613812
Encephalitis 46.30 32.38 25 7129 9133 42605048
Graft versus host disease in gastrointestinal tract 43.74 32.38 20 7134 5123 42609058
Disseminated cytomegaloviral infection 43.48 32.38 10 7144 275 42613906
Drug ineffective for unapproved indication 42.01 32.38 45 7109 46118 42568063
Cytomegalovirus colitis 41.97 32.38 18 7136 3963 42610218
Fatigue 39.70 32.38 12 7142 435629 42178552
Haemophagocytic lymphohistiocytosis 39.34 32.38 29 7125 18193 42595988
Lymphopenia 35.01 32.38 29 7125 21534 42592647
Glomerulonephropathy 34.41 32.38 8 7146 231 42613950
Cytomegalovirus test positive 34.25 32.38 16 7138 4303 42609878
Meningitis viral 34.10 32.38 11 7143 1094 42613087
Aspergillus infection 33.72 32.38 25 7129 15812 42598369
Hypokalaemia 33.34 32.38 50 7104 71671 42542510
Bone marrow failure 33.21 32.38 34 7120 33059 42581122
Bacterial toxaemia 32.56 32.38 7 7147 140 42614041

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 1325.06 33.50 414 12148 55960 110520777
Pathogen resistance 682.53 33.50 191 12371 17481 110559256
Nephropathy toxic 570.54 33.50 184 12378 27294 110549443
Cytomegalovirus viraemia 473.39 33.50 144 12418 17620 110559117
Off label use 433.56 33.50 674 11888 1499511 109077226
Encephalitis cytomegalovirus 405.13 33.50 82 12480 1828 110574909
Cytomegalovirus infection reactivation 401.88 33.50 128 12434 18205 110558532
Cytomegalovirus infection 377.46 33.50 163 12399 54281 110522456
BK virus infection 331.05 33.50 102 12460 13004 110563733
Cystitis haemorrhagic 325.31 33.50 99 12463 12110 110564627
Pancytopenia 296.77 33.50 221 12341 209392 110367345
Renal impairment 254.00 33.50 193 12369 188252 110388485
Myelosuppression 236.34 33.50 142 12420 94198 110482539
Pneumonia cytomegaloviral 218.21 33.50 64 12498 6890 110569847
Epstein-Barr viraemia 210.53 33.50 54 12508 3525 110573212
Drug ineffective 204.21 33.50 496 12066 1520044 109056693
Cytomegalovirus chorioretinitis 194.98 33.50 59 12503 7069 110569668
Acute kidney injury 190.22 33.50 292 12270 635138 109941599
Viral haemorrhagic cystitis 155.41 33.50 42 12520 3357 110573380
Graft versus host disease 152.48 33.50 63 12499 18743 110557994
Multiple organ dysfunction syndrome 152.47 33.50 131 12431 151579 110425158
Graft versus host disease in gastrointestinal tract 149.70 33.50 51 12511 8917 110567820
Transplant dysfunction 149.42 33.50 50 12512 8278 110568459
Acute graft versus host disease 138.82 33.50 53 12509 12828 110563909
Generalised oedema 125.85 33.50 64 12498 30640 110546097
Respiratory distress 118.71 33.50 82 12480 68792 110507945
Chronic graft versus host disease 109.46 33.50 41 12521 9416 110567321
Acute graft versus host disease in skin 107.92 33.50 42 12520 10698 110566039
Cytomegalovirus colitis 101.80 33.50 36 12526 7025 110569712
Aplastic anaemia 100.58 33.50 51 12511 24257 110552480
Renal tubular disorder 100.01 33.50 36 12526 7393 110569344
Haemophagocytic lymphohistiocytosis 98.87 33.50 55 12507 31504 110545233
Thrombotic microangiopathy 97.38 33.50 53 12509 29096 110547641
Human herpesvirus 6 infection 92.78 33.50 33 12529 6548 110570189
Fatigue 92.69 33.50 14 12548 1215944 109360793
Adenovirus infection 89.68 33.50 37 12525 10957 110565780
Epstein-Barr virus infection reactivation 83.22 33.50 27 12535 4057 110572680
Retinitis viral 81.44 33.50 17 12545 442 110576295
Arthralgia 75.70 33.50 3 12559 779629 109797108
Acute graft versus host disease in intestine 74.68 33.50 27 12535 5612 110571125
Adenoviral hepatitis 73.09 33.50 18 12544 994 110575743
Retinal detachment 72.79 33.50 32 12530 11068 110565669
Necrotising retinitis 69.59 33.50 19 12543 1577 110575160
Cytomegalovirus gastritis 69.24 33.50 16 12546 672 110576065
Neutropenia 64.92 33.50 136 12426 374484 110202253
Drug ineffective for unapproved indication 63.59 33.50 68 12494 102770 110473967
Venoocclusive liver disease 63.18 33.50 32 12530 15175 110561562
Epstein-Barr virus infection 62.38 33.50 34 12528 18704 110558033
Hypomagnesaemia 62.33 33.50 53 12509 60317 110516420
Bone marrow failure 62.22 33.50 52 12510 57796 110518941
Hypouricaemia 61.15 33.50 14 12548 564 110576173
Post transplant lymphoproliferative disorder 59.50 33.50 31 12531 15582 110561155
Dyspnoea 57.59 33.50 27 12535 1106845 109469892
Human herpesvirus 6 encephalitis 57.31 33.50 15 12547 1059 110575678
Respiratory failure 57.20 33.50 94 12468 215238 110361499
Cytomegalovirus test positive 55.09 33.50 23 12539 7013 110569724
Aspergillus infection 55.01 33.50 35 12527 25581 110551156
Bronchopulmonary aspergillosis 54.85 33.50 37 12525 29826 110546911
Cytopenia 52.19 33.50 36 12526 30080 110546657
Graft versus host disease in skin 51.56 33.50 23 12539 8231 110568506
Product use issue 51.47 33.50 111 12451 311584 110265153
Lymphopenia 51.45 33.50 40 12522 40130 110536607
Dizziness 50.92 33.50 9 12553 698184 109878553
Malaise 50.46 33.50 8 12554 671811 109904926
Pain 50.09 33.50 23 12539 954932 109621805
Mucosal inflammation 49.86 33.50 58 12504 96083 110480654
Disseminated cytomegaloviral infection 49.58 33.50 12 12550 616 110576121
Meningitis viral 49.45 33.50 16 12546 2383 110574354
Meningoencephalitis herpetic 49.43 33.50 16 12546 2386 110574351
Cerebral toxoplasmosis 49.05 33.50 17 12545 3125 110573612
Hepatic failure 48.87 33.50 49 12513 68690 110508047
Encephalitis 48.76 33.50 29 12533 18810 110557927
Fall 48.09 33.50 6 12556 603476 109973261
Retinal scar 47.46 33.50 11 12551 468 110576269
Bladder hypertrophy 47.24 33.50 13 12549 1111 110575626
Hypocalcaemia 47.22 33.50 47 12515 65319 110511418
Acidosis hyperchloraemic 47.13 33.50 14 12548 1572 110575165
Disseminated intravascular coagulation 46.24 33.50 38 12524 41248 110535489
Botulism 46.21 33.50 11 12551 526 110576211
Asthenia 45.86 33.50 11 12551 688988 109887749
Staphylococcal sepsis 45.52 33.50 27 12535 17427 110559310
Genital ulceration 44.10 33.50 14 12548 1961 110574776
Pain in extremity 43.70 33.50 3 12559 487115 110089622
Cytomegalovirus gastrointestinal infection 42.94 33.50 11 12551 713 110576024
Renal failure 42.43 33.50 85 12477 226489 110350248
Nausea 42.29 33.50 47 12515 1235643 109341094
Septic shock 42.12 33.50 69 12493 157459 110419278
Cytomegalovirus enterocolitis 42.12 33.50 14 12548 2267 110574470
Renal tubular injury 41.60 33.50 15 12547 3093 110573644
Toxic epidermal necrolysis 41.36 33.50 41 12521 56686 110520051
Neurological decompensation 39.25 33.50 18 12544 6865 110569872
Venous haemorrhage 39.18 33.50 9 12553 368 110576369
Acute graft versus host disease in liver 37.74 33.50 13 12549 2346 110574391
Infection reactivation 37.63 33.50 15 12547 4066 110572671
Hypokalaemia 37.25 33.50 71 12491 182377 110394360
Electrolyte imbalance 37.17 33.50 32 12530 36996 110539741
Multiple-drug resistance 35.89 33.50 21 12541 13214 110563523
Headache 35.47 33.50 29 12533 882348 109694389
Pruritus 35.46 33.50 11 12551 581549 109995188
Drug hypersensitivity 35.00 33.50 5 12557 454085 110122652
Herpes simplex test positive 34.44 33.50 9 12553 631 110576106
Bacterial toxaemia 34.11 33.50 7 12555 167 110576570
Glomerulonephropathy 34.10 33.50 8 12554 359 110576378
Abdominal discomfort 33.70 33.50 3 12559 393855 110182882

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
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000998 Antiviral Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018894 Reverse Transcriptase Inhibitors
MeSH PA D019384 Nucleic Acid Synthesis Inhibitors
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:36044 antiviral drug
CHEBI has role CHEBI:53756 HIV-1 reverse transcriptase inhibitor
CHEBI has role CHEBI:63330 sodium-dependent Pi-transporter inhibitor
CHEBI has role CHEBI:176497 geroprotector

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




🐶 Veterinary Drug Use

None

🐶 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 0143-9192 INJECTION, SOLUTION 24 mg INTRAVENOUS ANDA 23 sections
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 65145-191 INJECTION, SOLUTION 24 mg INTRAVENOUS ANDA 20 sections
Foscarnet Sodium Human Prescription Drug Label 1 68083-389 INJECTION, SOLUTION 24 mg INTRAVENOUS ANDA 21 sections
Foscarnet Sodium HUMAN PRESCRIPTION DRUG LABEL 1 70121-1744 INJECTION 24 mg INTRAVENOUS ANDA 20 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