Tìm theo
Telbivudine
Các tên gọi khác (10 ) :
  • 1-(2-Deoxy-beta-L-ribofuranosyl)-5-methyluracil
  • 2'-Deoxy-L-thymidine
  • beta-L-2'-Deoxythymidine
  • Beta-l-thymidine
  • Epavudine
  • L-deoxythymidine
  • L-DT
  • L-thymidine
  • LDT
  • Telbivudin
Thuốc Gốc
Small Molecule
CAS: 3424-98-4
ATC: J05AF11
ĐG : Idenix Pharmaceutical Inc. , http://www.idenix.com
CTHH: C10H14N2O5
PTK: 242.2286
Telbivudine is a synthetic thymidine nucleoside analog with specific activity against the hepatitis B virus. Telbivudine is orally administered, with good tolerance, lack of toxicity and no dose-limiting side effects.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H14N2O5
Phân tử khối
242.2286
Monoisotopic mass
242.090271568
InChI
InChI=1S/C10H14N2O5/c1-5-3-12(10(16)11-9(5)15)8-2-6(14)7(4-13)17-8/h3,6-8,13-14H,2,4H2,1H3,(H,11,15,16)/t6-,7+,8+/m1/s1
InChI Key
InChIKey=IQFYYKKMVGJFEH-CSMHCCOUSA-N
IUPAC Name
1-[(2S,4R,5S)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methyl-1,2,3,4-tetrahydropyrimidine-2,4-dione
Traditional IUPAC Name
telbivudine
SMILES
CC1=CN([C@@H]2C[C@@H](O)[C@H](CO)O2)C(=O)NC1=O
Độ hòa tan
Sparingly soluble in water (>20 mg/mL)
logP
-1.4
logS
-0.56
pKa (strongest acidic)
9.96
pKa (Strongest Basic)
-3
PSA
99.1 Å2
Refractivity
55.41 m3·mol-1
Polarizability
23.25 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Dược Lực Học : Telbivudine is a synthetic thymidine nucleoside analogue with activity against hepatitis B virus (HBV). Telbivudine is the unmodified β–L enantiomer of the naturally occurring nucleoside, thymidine. It undergoes phosphorylation via interaction with cellular kinases to form the active metabolite, telbivudine 5'-triphosphate.
Cơ Chế Tác Dụng : Telbivudine is a synthetic thymidine nucleoside analog with specific activity against the hepatitis B virus. Telbivudine is orally administered, with good tolerance, lack of toxicity and no dose-limiting side effects. Telbivudine 5'–triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, thymidine 5'–triphosphate. This leads to the chain termination of DNA synthesis, thereby inhibiting viral replication. Incorporation of telbivudine 5'–triphosphate into viral DNA also causes DNA chain termination, resulting in inhibition of HBV replication. Telbivudine inhibits anticompliment or second-strand DNA.
Dược Động Học :
▧ Absorption :
Absorbed following oral administration. Telbivudine absorption and exposure were unaffected when a single 600–mg dose was administered with a high–fat (~55 g), high–calorie (~950 kcal) meal.
▧ Protein binding :
In vitro binding of telbivudine to human plasma proteins is low (3.3%).
▧ Metabolism :
No metabolites of telbivudine were detected following administration of [14C]–telbivudine in humans. Telbivudine is not a substrate, or inhibitor of the cytochrome P450 (CYP450) enzyme system.
▧ Route of Elimination :
Telbivudine is eliminated primarily by urinary excretion of unchanged drug.
▧ Half Life :
Approximately 15 hours.
▧ Clearance :
* 7.6 +/- 2.9 L/h [Normal renal function (Clcr>80 mL/min)] * 5.0 +/- 1.2 L/h [Mild renal function impairement (Clcr=50-80 mL/min)] * 2.6 +/- 1.2 L/h [Moderate renal function impairement (Clcr=30-49 mL/min)] * 0.7 +/- 0.4 L/h [Severe renal function impairement (Clcr<30 mL/min)]
Độc Tính : There is no information on intentional overdose of telbivudine, but one subject experienced an unintentional and asymptomatic overdose. Healthy subjects who received telbivudine doses up to 1800 mg/day for 4 days had no increase in or unexpected adverse events. A maximum tolerated dose for telbivudine has not been determined.
Chỉ Định : For the treatment of chronic hepatitis B in adult and adolescent patients ≥16 years of age with evidence of viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease.
Tương Tác Thuốc :
  • Peginterferon alfa-2a Co-administration of Peginterferon alpha-2a and Telbivudine may increase the risk of serious peripheral neuropathy.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Tyzeka 600 mg tablet
    Giá bán buôn : USD >27.26
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Sebivo
  • Công ty :
    Sản phẩm biệt dược : Tyzeka
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01265
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=159269
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508706
ChemSpider
http://www.chemspider.com/Chemical-Structure.140081.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50156567
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0078-0539-85
PharmGKB
http://www.pharmgkb.org/drug/PA164760861
RxList
http://www.rxlist.com/cgi/generic/tyzeka.htm
Drugs.com
http://www.drugs.com/cdi/telbivudine.html
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