Adefovir

Bezeichnung:Adefovir

CAS-Nr106941-25-7

Englisch Name:Adefovir

CBNumberCB2698137

SummenformelC8H12N5O4P

Molgewicht273.19

MOL-Datei106941-25-7.mol

Adefovir physikalisch-chemischer Eigenschaften

Schmelzpunkt	>260°C
Siedepunkt	632.5±65.0 °C(Predicted)
Dichte	1.88
storage temp.	-20°C
Löslichkeit	0.1 M NaOH: ≥5mg/mL
pka	pKa1 2.0, pKa2 6.8(at 25℃)
Aggregatzustand	powder
Farbe	white to beige
InChIKey	SUPKOOSCJHTBAH-UHFFFAOYSA-N
CAS Datenbank	106941-25-7(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25
S-Sätze:	45
RIDADR	2811
WGK Germany	3
RTECS-Nr.	SZ6563500
HazardClass	6.1
PackingGroup	Ⅲ
HS Code	29339900
Giftige Stoffe Daten	106941-25-7(Hazardous Substances Data)

Gefahreninformationscode (GHS)

Adefovir Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften
Pale Brown Solid
Verwenden
Adefovir has been used to study its anti-retro viral effect on porcine endogenous retrovirus (PERV) activity.
Verwenden
Used as an antiviral
Definition
ChEBI: Adefovir is a member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection. It has a role as a HIV-1 reverse transcriptase inhibitor, a drug metabolite, an antiviral drug, a nephrotoxic agent and a DNA synthesis inhibitor. It is a member of 6-aminopurines, an ether and a member of phosphonic acids. It is functionally related to an adenine. It is a conjugate acid of an adefovir(1-).
Acquired resistance
It has a lower propensity to induce drug resistance than lamivudine. Clinical trials of patients receiving 48 weeks of therapy did not identify any cases of resistance. Longer courses yield resistant strains of HBV with mutations in the DNA polymerase gene; other rare variants of resistant strains have been identified. Lamivudine-resistant strains of HBV retain susceptibility to adefovir.
Pharmazeutische Anwendungen
A nucleotide analog of adenosine monophosphate, administered orally as its prodrug, adefovir dipivoxil.
Biochem/physiol Actions
Adefovir is an antiviral drug that after intracellular conversion to adefovir diphosphate inhibits hepatitis B virus (HBV) DNA polymerase (reverse transcriptase).
Pharmakokinetik
Oral absorption： c. 60%
C_max 10 mg/kg oral： 18.4 ng/mL
Plasma half-life： c. 7.5 h.
Volume of distribution： 392 mL/kg
Plasma protein binding： Not known
The prodrug is metabolized to adefovir, which is excreted by the kidneys and therefore requires dose adjustment in patients with impaired renal function. It does not induce cytochrome P₄₅₀ at standard doses and does not influence the metabolism or plasma concentrations of the other licensed medications used in the treatment of hepatitis B.
Clinical Use
Treatment of chronic hepatitis B virus infection in patients >12 years of age
Nebenwirkungen
It is generally well tolerated, with headache, pharyngitis, abdominal pain and peripheral neuropathy being the most common side effects. Nephrotoxicity has been observed in some patients, with those receiving higher doses and longer courses of therapy at greater risk. Exacerbation of hepatitis has been reported in patients immediately following discontinuation of treatment. Most exacerbations occur within 12 weeks of stopping therapy, and elevations of alanine aminotransferase (ALT) up to 10 times the upper limit of normal can be observed in over 25% of patients. Lactic acidosis has been reported in a few patients and is an indication for immediate discontinuation.

Adefovir Upstream-Materialien And Downstream Produkte

Adefovir Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

106941-25-7, Adefovir Verwandte Suche:

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