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

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 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 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 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 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 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:

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 (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 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