Name: | Foscarnet |
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PubChem Compound ID: | 169569 |
Description: | An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV. |
Molecular formula: | CH12Na3O11P |
Molecular weight: | 300.042 g/mol |
Synonyms: |
34156-56-4; D02267; Trisodium phosphonoformte hexahydrate; Dihydroxyphosphinecarboxylic acid oxide trisodium salt hexahydrate; Formic acid, phosphono-, trisodium salt, hexahydrate; Foscarnet sodium hydrate; Foscarnet; Foscavir; Foscavir (TN); Phosphinecarboxylic acid, dihydroxy-, oxide, trisodium salt, hexahydrate.
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Name: | Foscarnet |
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Name (isomeric): | DB00529 |
Drug Type: | small molecule |
Description: | An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV. |
Synonyms: |
Phosphonoformate; Forscarnet sodium; Carboxyphosphonic acid; Foscarnet sodium; Dihydroxyphosphinecarboxylic acid oxide; Phgosphonocarboxylic acid; PFA; Phosphonoformic acid
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Brand: | Triapten, Foscavir, Foscarmet |
Category: | Antiviral Agents, Reverse Transcriptase Inhibitors |
CAS number: | 63585-09-1 |
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. |
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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...
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Mechanism of Action: | Foscarnet exerts its antiviral activity by a selective inhibition at the pyrophosphate binding site on virus-specific DNA polymerases at concentrations that do not affect cellular DNA polymerases. |
Absorption: | Poorly absorbed after oral administration (bioavailability from 12 to 22%). |
Protein binding: | 14-17% |
Biotransformation: | Not metabolized. |
Half Life: | 3.3-6.8 hours |
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] |
Toxicity: | Oral, rat LD50: >2,000 mg/kg. Signs of overdose include renal impairment. |
Affected organisms: | Human Herpes Virus |
Drug interaction: |
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