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Oral Reverse Transcriptase Inhibitor Adefovir Dipivoxil CAS 142340-99-6
Product Name: Adefovir Dipivoxil
Synonyms: BIS POM PMEA;BIS(PIVALOYLOXYMETHYL)-9-[2-(PHOSPHONOMETHOXY)ETHYL]ADENINE;9-[2-[bis[(pivaloyloxy)methoxy]phosphinyl]methoxy]ethyl]adenine;ADEFOVIR DIPIVOXIL;ADEFOVIR PIVOXIL;Adefovir Dipivoxyl;Bis(Pivaloyloxymethyl)-9-[(R)-2-(Phosphonomethoxy)Ethyl]Adenine;AdefovirDipivoxl 98.5%Min
Product Categories: Active Pharmaceutical Ingredients;Adefovir;APIs;Other Products;Bases & Related Reagents;Inhibitors;Intermediates & Fine Chemicals;Nucleotides;Pharmaceuticals;Pharmaceutical raw material;API;Bis-POM PMEA, Preveon, Hepsera
Melting point : 98-102°C
Storage temp. : −20°C
Merck : 14,151
Chemical Properties : White Solid
Usage : Adefovir Dipivoxil(Preveon, Hepsera) works by blocking reverse transcriptase, an enzyme that is crucial for the hepatitis B virus (HBV) to reproduce in the body. It is approved for the treatment of chronic hepatitis B in adults with evidence of active vir
Usage : A nucleotide analog, useful as an oral reverse transcriptase inhibitor (ntRTI) .
Regulating human immune system
Adefovir dipivoxil regulates the immune system and let the immune system to attack liver cells of the intrusion of HBV , and clear the virus, but this method will develop resistance, at the same time for patients with renal dysfunction or potential renal dysfunction risk, the use of adefovir dipivoxil chronic treatment will lead to renal toxicity. If eating 1 mg every day, in the three months will produce nephrotoxicity, this will lead to severe renal failure. These patients should be closely monitoring renal function and making appropriate dosage adjustments.
Bisphosphonates is quick conversion of adefovir dipivoxil in vivo, adefovir dipivoxil is a kind of single adenosine monophosphate acyclic nucleoside analogues, became to activity of the metabolites of adefovir in cellular kinases by phosphorylation in cellular kinases. A Duff Vee two phosphate through the following two ways to suppress HBV DNA polymerase (reverse transcriptase); one is with the natural substrate of deoxyadenosine triphosphate competition, the second is the integration of viral DNA and induce DNA chain elongation terminated. A Duff Vee two phosphate to HBV DNA polymerase inhibition constant (KI) is 0.1μM, but of human DNA polymeraseα and γ is weak and Ki values were 1.18μM and 0.97 μM.
Anti-viral activity: in the human hepatoma cell line transfected with HBV, the concentration of A Duff Vee inhibited 50% viral DNA replication (IC50) is from 0.2 to 2.5uM.
Adefovir dipivoxil applies for the treatment of hepatitis B virus replication activity and serum amino acid transfer enzyme and persistently elevated liver decompensation adult patients with chronic hepatitis B patients.
Liver injury is often encountered in the course of hepatitis B treatment, hepatitis B therapy is inappropriate, as well as long-term use of drugs on the liver damage, will lead to the occurrence of liver damage.
After long-term taking adefovir dipivoxil tablets, once the withdrawal will aggravate the damage of liver function. Therefore, for stopping taking the patients should be monitored for liver function.
Adefovir dipivoxil is more moderate suitable for long-term use, suitable for patients with lamivudine resistant patients, their chances of producing drug resistance is small, because the amount is less, side effects are small.
Entecavir is new, antiviral effect is also strong, if not treated with lamivudine, the possible resistance is the smallest, but it and lamivudine have cross resistance, if treated with lamivudine to take entecavir produced resistance rate is much greater.
Adefovir dipivoxil Uses
Has a broad spectrum of antiviral activity, can be used for the treatment of chronic hepatitis B .
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