Tìm theo
Entecavir
Các tên gọi khác (2) :
  • Entecavir
  • Entecavirum
Thuốc Gốc
Small Molecule
CAS: 142217-69-4
ATC: J05AF10
ĐG : Bristol-Myers Squibb Co. , http://www.bms.com
CTHH: C12H15N5O3
PTK: 277.2792
Entecavir is an oral antiviral drug used in the treatment of hepatitis B infection. It is marketed under the trade name Baraclude (BMS). Entecavir is a guanine analogue that inhibits all three steps in the viral replication process, and the manufacturer claims that it is more efficacious than previous agents used to treat hepatitis B (lamivudine and adefovir). It was approved by the U.S. Food and Drug Administration (FDA) in March 2005.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
277.2792
Monoisotopic mass
277.117489371
InChI
InChI=1S/C12H15N5O3/c1-5-6(3-18)8(19)2-7(5)17-4-14-9-10(17)15-12(13)16-11(9)20/h4,6-8,18-19H,1-3H2,(H3,13,15,16,20)/t6-,7-,8-/m0/s1
InChI Key
InChIKey=QDGZDCVAUDNJFG-FXQIFTODSA-N
IUPAC Name
2-amino-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-6,9-dihydro-3H-purin-6-one
Traditional IUPAC Name
entecavir
SMILES
NC1=NC(=O)C2=C(N1)N(C=N2)[[email protected]]1C[[email protected]](O)[[email protected]@H](CO)C1=C
Độ hòa tan
Slightly soluble (2.4 mg/mL at pH 7.9, 25 °C)
logP
-0.8
logS
-1.6
pKa (strongest acidic)
8
pKa (Strongest Basic)
2.77
PSA
125.76 Å2
Refractivity
71 m3·mol-1
Polarizability
27.31 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
7
H Bond Donor Count
4
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Dược Lực Học : Entecavir is a guanosine nucleoside analogue with selective activity against hepatitis B virus (HBV). It is designed to selectively inhibit the Hepatitis B virus, blocking all three steps in the replication process. Entecavir is more efficient than an older Hepatitis B drug, lamivudine.
Cơ Chế Tác Dụng : Entecavir is an oral antiviral drug used in the treatment of hepatitis B infection. It is marketed under the trade name Baraclude (BMS). Entecavir is a guanine analogue that inhibits all three steps in the viral replication process, and the manufacturer claims that it is more efficacious than previous agents used to treat hepatitis B (lamivudine and adefovir). It was approved by the U.S. Food and Drug Administration (FDA) in March 2005. By competing with the natural substrate deoxyguanosine triphosphate, entecavir functionally inhibits all three activities of the HBV polymerase (reverse transcriptase, rt): (1) base priming, (2) reverse transcription of the negative strand from the pregenomic messenger RNA, and (3) synthesis of the positive strand of HBV DNA. Upon activation by kinases, the drug can be incorporated into the DNA which has the ultimate effect of inhibiting the HBV polymerase activity.
Dược Động Học :
▧ Absorption :
Absorption Following oral administration in healthy subjects, entecavir peak plasma concentrations occurred between 0.5 and 1.5 hours. In healthy subjects, the bioavailability of the tablet is 100% relative to the oral solution.
▧ Protein binding :
Binding of entecavir to human serum proteins in vitro is approximately 13%.
▧ Metabolism :
Entecavir is not a substrate, inhibitor, or inducer of the cytochrome P450 (CYP450) enzyme system. Entecavir is efficiently phosphorylated to the active triphosphate form.
▧ Half Life :
After reaching peak concentration, entecavir plasma concentrations decreased in a bi-exponential manner with a terminal elimination half-life of approximately 128-149 hours. The phosphorylated metabolite has a half-life of 15 hours.
▧ Clearance :
* renal cl=383.2 +/- 101.8 mL/min [Unimpaired renal function] * renal cl=197.9 +/- 78.1 mL/min [Mild impaired renal function] * renal cl=135.6 +/- 31.6 mL/min [Moderate impaired renal function] * renal cl=40.3 +/- 10.1 mL/min [severe impaired renal function] * apparent oral cl=588.1 +/- 153.7 mL/min [Unimpaired renal function] * apparent oral cl=309.2 +/- 62.6 mL/min [Mild impaired renal function] * apparent oral cl=226.3 +/- 60.1 mL/min [Moderate impaired renal function] * apparent oral cl=100.6 +/- 29.1 mL/min [severe impaired renal function] * apparent oral cl=50.6 +/- 16.5 mL/min [severe impaired renal function amnaged with Hemodialysis] * apparent oral cl=35.7 +/- 19.6 mL/min [severe impaired renal function amnaged with CAPD]
Độc Tính : Healthy subjects who received single entecavir doses up to 40 mg or multiple doses up to 20 mg/day for up to 14 days had no increase in or unexpected adverse events. If overdose occurs, the patient must be monitored for evidence of toxicity, and standard supportive treatment applied as necessary.
Chỉ Định : For the treatment of chronic hepatitis B virus infection in adults with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Baraclude 0.5 mg tablet
    Giá bán buôn : USD >28.94
    Đơn vị tính : tablet
  • Biệt dược thương mại : Baraclude 1 mg tablet
    Giá bán buôn : USD >28.94
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Sản phẩm biệt dược : Baraclude
  • Công ty : Incepta
    Sản phẩm biệt dược : Barcavir
  • Công ty : PMP
    Sản phẩm biệt dược : Caavirel
  • Sản phẩm biệt dược : Entaliv
  • Công ty : ACI
    Sản phẩm biệt dược : Teviral
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