Product information

Entecavir Basic information

Hepatitis B treatment first-line drug mechanism of action side effect usage and dosage Adefovir dipivoxilGenotoxicity

Product Name:	Entecavir
Synonyms:	ENTECAVIR;Entecavi;ENTECAVIR, 98-102%;entecavir Baraclude;2-Amino-9-[4-hydroxy-3-(hydroxymethyl)-2-methylidene-cyclopentyl]-3H-purin-6-one,Baraclude;2-Amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one;2-Amino-9-[4-hydroxy-3-(hydroxymethyl)-2-methylidene-cyclopentyl]-3H-purin-6-one;Baraclude
CAS:	142217-69-4
MF:	C12H15N5O3
MW:	277.283
EINECS:
Product Categories:	Antiviral Agents;Nucleotides and Nucleosides;Bases & Related Reagents;Intermediates & Fine Chemicals;Nucleotides;Pharmaceuticals;API;Anti-virals;Heterocycles;The latest anti hepatitis b anti-aids drugs;Inhibitors
Mol File:	142217-69-4.mol

Entecavir Chemical Properties

mp	249-252°C
storage temp.	-20°C Freezer
CAS DataBase Reference	142217-69-4(CAS DataBase Reference)

Safety Information

Hazardous Substances Data

142217-69-4(Hazardous Substances Data)

 

Entecavir Usage And Synthesis

Hepatitis B treatment first-line drug	Entecavir is a new generation of guanine nucleoside analogues oral medicine for treatment of hepatitis B virus infection in, mainly for the treatment of adult patients with viral replication activity and serum transaminase continued to increase, or liver tissue for pathological activity of chronic hepatitis B, is currently down virus the fastest and the most powerful, the mutation rate lowest nucleoside analogues. Data show that different in patients with chronic hepatitis B, including nucleoside naive and nucleoside treated and liver cirrhosis patients, using well entecavir tablets in the treatment can control the disease rapidly and easily reach the treatment of reality end, namely the hepatitis B virus unmeasured; through adherence to treatment, a considerable portion of patients can be arrived at the end of treatment satisfaction, namely e antigen serology conversion, some patients can even reach the ideal for the treatment of end, namely surface antigen negative.
mechanism of action	This product is guanosine analogue, having inhibiting effect to hepatitis B virus (HBV) polymerase. It can change to the active phosphorylation by three phosphate, the half-life of three phosphate in cells is 15 hours. The natural substrate DNA guanine nucleoside and HBV polymerase three phosphate competition, entecavir three phosphate can inhibite of viral polymerase (reverse transcriptase) of all three activities: (1) HBV polymerase promoter; (2) the formation of before genomic mRNA reverse transcription negative strand; (3) HBV DNA chain is synthetised. Entecavir three phosphate on the inhibition constant HBV DNA polymerase (Ki) 0.0012 μM. entecavir three phosphate on cell entecavir α, β, δ DNA polymerase and mitochondrial DNA polymerase inhibition. Ki value is 18 to 160μM.
side effect	In the treatment of hepatitis B, entecavir as first-line antiviral drugs in the treatment of hepatitis B virus on the effect is worthy of recognition, have a significant treatment effect of serum transaminase ALT increased or liver lesions for active viral replication in patients with chronic hepatitis B in adults,. However, the clinical application of entecavir is affected due to the side effects of entecavir. The most common side effects of entecavir: the increase of ALT, fatigue, dizziness, nausea, abdominal pain, abdominal discomfort, abdominal discomfort, liver, muscle, insomnia, rubella and indigestion, also be found in neutrophils decreased slightly. These adverse reactions were mild to moderate. In trials with lamivudine controls, the incidence of adverse events is equivalent to lamivudine. According to the study, it also found that, as the same type of antiviral drugs, entecavir and the first generation of antiviral drugs have similar side effects, such as acid poisoning, hepatomegaly, liver fatty degeneration in the withdrawal will appear rebound phenomenon. In these studies, using entecavir of the patients in the treatment process, ALT increased to 10 times of the normal value upper limit and baseline values of 2 times, the generally continue to medication for a period of time, the ALT returned to normal; prior to or concurrently with viral load 2 on the numerical decline. So during the treatment, regular liver function should be tested. In the side effects of entecavir, most not easy to accept the resistance for patients, resistance will increase the difficulty of treatment, medication time to grow, for patients, psychological pressure and economic pressure will increase, half-way stopping may cause illness rebound. Although existing nucleoside analogues inhibited viral force of entecavir is strong, and mutation rate is lowest (newly diagnosed 4 years less than 1%), but the price is also the most expensive, more suitable for economic conditions, long-term treatment. Because of the side effects of entecavir, patients with hepatitis B should be taken entecavir under the guidance of specialized subject doctor, once appear uncomfortable to reflect to the doctor. In the necessary condition, timely adjustment of treatment. And the use entecavir therapy does not reduce hepatitis B through sexual contact or blood transmission of hepatitis B virus risk. Therefore, it is necessary to take appropriate protective measures.
usage and dosage	Patients with chronic hepatitis B should be under the guidance of experienced doctors taking this product. Recommended dosage: adult and over the age of 16 young oral this product, once a day, each 0.5 mg. lamivudine treatment viremia or patients with lamivudine resistant mutants to once a day, each 1.0 mg (0.5mg two pieces), taken on an empty stomach (a meal or a meal after at least 2 hours).

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