Effective Entecavir Pharma Raw Materials CAS 142217-69-4 For Treating HBV

Effective Entecavir Pharma Raw Materials CAS 142217-69-4 For Treating HBV

Description:

Entecavir (en tek' a vir) is a guanosine analogue with potent activity against HBV and minimal activity against HIV. Entecavir is phosphorylated intracellularly where it acts by competing with guanosine for uptake by the HBV DNA polymerase and incorporation into the growing HBV DNA molecule, leading to inhibition of the polymerase activity and chain termination. Entecavir was approved by the FDA in 2005 and is currently widely used. Entecavir is indicated for the treatment of chronic hepatitis B and is available in 0.5 and 1 mg tablets under the brand name of Baraclude. An oral solution of 0.05 mg/mL is also available. The recommended dose of entecavir is 0.5 mg orally once daily in adults (and children over the age of 16) with typical chronic hepatitis B and 1.0 mg once daily for patients with lamivudine-resistant HBV infection. Entecavir has slight antiviral activity against HIV which predisposes to antiviral resistance and should not be used alone in patients with HBV-HIV co-infection. Side effects from entecavir are infrequent.

Specifications:

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
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
MP: 249-252°C
Storage temp: -20°C Freezer
Chemical Properties: White to Off-White Crystalline Powder
Usage: An oral antiviral drug used in the treatment of hepatitis B infection. A guanine analogue that inhhibits all three steps in the viral replication process.

2D Stucture:

Medical Uses:

Entecavir is mainly used to treat chronic hepatitis B infection in adults and children 2 years and older with active viral replication and evidence of active disease with elevations in liver enzymes.It is also used to prevent HBV reinfection after liver transplant and to treat HIV patients infected with HBV. Entecavir is weakly active against HIV, but is not recommended for use in HIV-HBV co-infected patients without a fully suppressive anti-HIV regimen as it may select for resistance to lamivudine and emtricitabine in HIV.

The efficacy of entecavir has been studied in several randomized, double-blind, multicentre trials. Entecavir by mouth is effective and generally well tolerated treatment.

Pregnancy and Breastfeeding:

It is considered pregnancy category C in the United States, and currently no adequate and well-controlled studies exist in pregnant women.

Mechanism of Action:

Entecavir is a nucleoside analog,or more specifically, a deoxyguanosine analogue that belongs to a class of carbocyclic nucleosides and inhibits reverse transcription, DNA replication and transcription in the viral replication process.

Dosing:

The recommended dosage of entecavir is a single 0.5 mg tablet once-daily for chronic hepatitis B patients beginning treatment for the first time (nucleoside-na?ve patients), and a single 1 mg tablet once-daily for patients experiencing resistance to lamivudine.

Entecavir comes in tablet and oral suspension forms and is taken by mouth without food. The tablets are film-coated, triangular-shaped and contain 0.5 or 1.0 mg entecavir. The oral solution contains 0.05 mg/ml entecavir in a 260 ml bottle.

Entecavir should be taken 2 hours after a meal and 2 hours before the next meal. Based on the pharmacokinetic profile of entecavir after oral dosing, the estimated apparent volume of distribution is in excess of total body water, suggesting that entecavir is extensively distributed into tissues.

Side Effects:

The majority of people who use entecavir have little to no side effects.The most common side effects include headache, fatigue, dizziness, and nausea.Less common effects include trouble sleeping and gastrointestinal symptoms such as sour stomach, diarrhea, and vomiting.

Serious side effects from entecavir include lactic acidosis, liver problems, liver enlargement, and fat in the liver.

Laboratory tests may show an increase in alanine transaminase (ALT), hematuria, glycosuria, and an increase in lipase. Periodic monitoring of hepatic function and hematology are recommended.

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