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Foscarnet

Catalog No. DB00529 Name DrugBank
CAS Number 63585-09-1 Website http://www.ualberta.ca/
M. F. CH3O5P Telephone (780) 492-3111
M. W. 126.005281 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 411

SYNONYMS

IUPAC name
phosphonoformic acid
IUPAC Traditional name
foscarnet
Brand Name
Foscavir
Foscarmet
Triapten
Synonyms
Dihydroxyphosphinecarboxylic acid oxide
Forscarnet sodium
PFA
Phosphonoformic acid
Foscarnet sodium
Carboxyphosphonic acid
Phgosphonocarboxylic acid
Phosphonoformate

DATABASE IDS

PubChem CID 3415
CAS Number 63585-09-1
PubChem SID 46507873

PROPERTIES

Hydrophobicity(logP) -2.1
Solubility Complete

DETAILS

Description (English)
Item Information
Drug Groups approved
Description An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV. [PubChem]
Indication For the treatment of CMV retinitis in patients with acquired immunodeficiency syndrome (AIDS) and for treatment of acyclovir-resistant mucocutaneous HSV infections in immunocompromised patients.
Pharmacology Foscarnet is an organic analogue of inorganic pyrophosphate that inhibits replication of herpes viruses in vitro including cytomegalovirus (CMV) and herpes simplex virus types 1 and 2 (HSV-1 and HSV-2). Foscarnet does not require activation (phosphorylation) by thymidine kinase or other kinases and therefore is active in vitro against HSV TK deficient mutants and CMV UL97 mutants. Thus, HSV strains resistant to acyclovir or CMV strains resistant to ganciclovir may be sensitive to foscarnet. However, acyclovir or ganciclovir resistant mutants with alterations in the viral DNA polymerase may be resistant to foscarnet and may not respond to therapy with foscarnet. The combination of foscarnet and ganciclovir has been shown to have enhanced activity in vitro.
Toxicity Oral, rat LD50: >2,000 mg/kg. Signs of overdose include renal impairment.
Affected Organisms
Human Herpes Virus
Biotransformation Not metabolized.
Absorption Poorly absorbed after oral administration (bioavailability from 12 to 22%).
Half Life 3.3-6.8 hours
Protein Binding 14-17%
Clearance * 2.13 +/- 0.71 mL/min/kg [patients had normal renal function (CrCl > 80 mL/min]
* 68 +/- 8 mL/min/kg [CrCl was 50-80 mL/min]
* 34 +/- 9 mL/min/kg [CrCl was 25-49 mL/min]
* 20 +/- 4 mL/min/kg [CrCl was 10 - 24 mL/min]
External Links
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REFERENCES