| 词条 | Foscarnet |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 461113374 | IUPAC_name = phosphonoformic acid | image = Foscarnet.svg | width = 160 | image2 = Foscarnet ball-and-stick model.png | tradename = Foscavir | Drugs.com = {{drugs.com|monograph|foscavir}} | MedlinePlus = a601144 | pregnancy_AU = B3 | pregnancy_US = C | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = POM | legal_US = Rx only | legal_status = | routes_of_administration = Intravenous | bioavailability = NA | protein_bound = 14–17% | metabolism = | elimination_half-life = 3.3–6.8 hours | IUPHAR_ligand = 5497 | CAS_number_Ref = {{cascite|changed|CAS}} | CAS_number = 4428-95-9 | CAS_supplemental = (trisodium salt) | ATC_prefix = J05 | ATC_suffix = AD01 | PubChem = 3415 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB00529 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 3297 | UNII_Ref = {{fdacite|changed|FDA}} | UNII = 364P9RVW4X | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = C06456 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 127780 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 666 | C=1 | H=3 | O=5 | P=1 | molecular_weight = 126.005 g/mol 300.1 g/mol (foscarnet trisodium hexahydrate) | SMILES = O=C(O)P(=O)(O)O | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/CH3O5P/c2-1(3)7(4,5)6/h(H,2,3)(H2,4,5,6) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = ZJAOAACCNHFJAH-UHFFFAOYSA-N | synonyms = phosphonomethanoic acid, dihydroxyphosphinecarboxylic acid oxide }} Foscarnet (phosphonomethanoic acid) is an antiviral medication which is primarily used to treat viral infections involving the Herpesviridae family. It is classified as a pyrophosphate analog DNA polymerase inhibitor. Foscarnet is the conjugate base of a chemical compound with the formula HO2CPO3H2. Foscarnet was approved for medical use in 1991.[1] Medical useThis phosphonic acid derivative (marketed by Clinigen as foscarnet sodium under the trade name Foscavir) is an antiviral medication used to treat herpes viruses, including drug-resistant cytomegalovirus (CMV) and herpes simplex viruses types 1 and 2 (HSV-1 and HSV-2). It is particularly used to treat CMV retinitis. Foscarnet can be used to treat highly treatment-experienced patients with HIV as part of salvage therapy.[2][3][4] Mechanism of actionFoscarnet is a structural mimic of the anion pyrophosphate[5] that selectively inhibits the pyrophosphate binding site {{Citation needed|date=October 2010}} on viral DNA polymerases at concentrations that do not affect human DNA polymerases. In individuals treated with the DNA polymerase inhibitors acyclovir or ganciclovir, HSV or CMV particles can develop mutant protein kinases (thymidine kinase or UL97 protein kinase, respectively) that make them resistant to these antiviral drugs. However, unlike acyclovir and ganciclovir, foscarnet is not activated by viral protein kinases, making it useful in acyclovir- or ganciclovir-resistant HSV and CMV infections. However, acyclovir- or ganciclovir-resistant mutants with alterations in viral DNA polymerase may also be resistant to foscarnet.[6][7] AdministrationIntravenous infusion or intravitreous injection. Side effects
References1. ^{{cite book|last1=Long|first1=Sarah S.|last2=Pickering|first2=Larry K.|last3=Prober|first3=Charles G.|title=Principles and Practice of Pediatric Infectious Disease|date=2012|publisher=Elsevier Health Sciences|isbn=1437727026|page=1502|url=https://books.google.com/books?id=nQ7-o8JAH7kC&pg=PA1502|language=en}} 2. ^{{cite journal |vauthors=Canestri A, Ghosn J, Wirden M |title=Foscarnet salvage therapy for patients with late-stage HIV disease and multiple drug resistance |journal=Antivir. Ther. (Lond.) |volume=11 |issue=5 |pages=561–6 |year=2006 |pmid=16964823 |doi=|display-authors=etal}} 3. ^{{cite journal |vauthors=Mathiesen S, Dam E, Roge B |title=Long-term foscarnet therapy remodels thymidine analogue mutations and alters resistance to zidovudine and lamivudine in HIV-1 |journal=Antivir. Ther. (Lond.) |volume=12 |issue=3 |pages=335–43 |year=2007 |pmid=17591023 |doi=|display-authors=etal}} 4. ^{{cite journal |vauthors=Meyer PR, Rutvisuttinunt W, Matsuura SE, So AG, Scott WA |title=Stable complexes formed by HIV-1 reverse transcriptase at distinct positions on the primer-template controlled by binding deoxynucleoside triphosphates or foscarnet |journal=J. Mol. Biol. |volume=369 |issue=1 |pages=41–54 |year=2007 |pmid=17400246 |doi=10.1016/j.jmb.2007.03.006 |url=http://linkinghub.elsevier.com/retrieve/pii/S0022-2836(07)00335-X |pmc=1986715}} 5. ^{{cite journal |vauthors=Meyer PR, Rutvisuttinunt W, Matsuura SE, So AG, Scott WA |title=Stable complexes formed by HIV-1 reverse transcriptase at distinct positions on the primer-template controlled by binding deoxynucleoside triphosphates or foscarnet |journal=J. Mol. Biol. |volume=369 |issue=1 |pages=41–54 |date=May 2007 |pmid=17400246 |pmc=1986715 |doi=10.1016/j.jmb.2007.03.006 |url=http://linkinghub.elsevier.com/retrieve/pii/S0022-2836(07)00335-X}} 6. ^{{cite journal |vauthors=Bonnafous P, Naesens L, Petrella S |title=Different mutations in the HHV-6 DNA polymerase gene accounting for resistance to foscarnet |journal=Antivir. Ther. (Lond.) |volume=12 |issue=6 |pages=877–88 |year=2007 |pmid=17926642 |doi=|display-authors=etal}} 7. ^{{cite journal |vauthors=Tchesnokov EP, Gilbert C, Boivin G, Götte M |title=Role of helix P of the human cytomegalovirus DNA polymerase in resistance and hypersusceptibility to the antiviral drug foscarnet |journal=J. Virol. |volume=80 |issue=3 |pages=1440–50 |date=February 2006 |pmid=16415021 |pmc=1346920 |doi=10.1128/JVI.80.3.1440-1450.2006 |url=http://jvi.asm.org/cgi/pmidlookup?view=long&pmid=16415021}} Sources
External links
5 : Anti-herpes virus drugs|Antiretroviral drugs|Phosphonic acids|Carboxylic acids|Nephrotoxins |
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