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Foscarnet


ACCESSION NB: DB00529 (APRD00669)


TYPE: small molecule


GROUP: approved


DESCRIPTION:
An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV. [PubChem]

CATEGORIES:
Antiviral Agents Reverse Transcriptase Inhibitors

ABSORPTION: Poorly absorbed after oral administration (bioavailability from 12 to 22%).

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.

PHARMACODYNAMICS:
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.

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.

PROTEIN BINDING:
14-17%

METABOLISM:
Not metabolized.

TOXICITY:
Oral, rat LD50: >2,000 mg/kg. Signs of overdose include renal impairment.

AFECTED ORGANISMS:
Human Herpes Virus