Tìm theo
Trifluridine
Các tên gọi khác (12 ) :
  • 5-(Trifluoromethyl)deoxyuridine
  • 5-Trifluoromethyl-2-deoxyuridine
  • F₃T
  • TFT
  • Trifluoromethyldeoxyuridine
  • Trifluorothymidine
  • Trifluorothymine deoxyriboside
  • Trifluridin
  • Trifluridina
  • Trifluridine
  • Trifluridinum
  • Viroptic
antiviral agents, antimetabolites
Thuốc Gốc
Small Molecule
CAS: 70-00-8
ATC: S01AD02
ĐG : Alcon Laboratories , http://www.alcon.com
CTHH: C10H11F3N2O5
PTK: 296.1999
An antiviral derivative of thymidine used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p557)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H11F3N2O5
Phân tử khối
296.1999
Monoisotopic mass
296.062006087
InChI
InChI=1S/C10H11F3N2O5/c11-10(12,13)4-2-15(9(19)14-8(4)18)7-1-5(17)6(3-16)20-7/h2,5-7,16-17H,1,3H2,(H,14,18,19)/t5-,6+,7+/m0/s1
InChI Key
InChIKey=VSQQQLOSPVPRAZ-RRKCRQDMSA-N
IUPAC Name
1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-(trifluoromethyl)-1,2,3,4-tetrahydropyrimidine-2,4-dione
Traditional IUPAC Name
trifluridine
SMILES
OC[C@H]1O[C@H](C[C@@H]1O)N1C=C(C(=O)NC1=O)C(F)(F)F
Độ tan chảy
186-189 °C
Độ hòa tan
1560 mg/L
logP
-0.46
logS
-1.6
pKa (strongest acidic)
7.6
pKa (Strongest Basic)
-3
PSA
99.1 Å2
Refractivity
56.34 m3·mol-1
Polarizability
23.07 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
pKa
7.95
Dược Lực Học : Trifluridine is a fluorinated pyrimidine nucleoside with in vitro and in vivo activity against herpes simplex virus, types 1 and 2 and vacciniavirus. Some strains of adenovirus are also inhibited in vitro. Trifluridine is also effective in the treatment of epithelial keratitis that has not responded clinically to the topical administration of idoxuridine or when ocular toxicity or hypersensitivity to idoxuridine has occurred. In a smaller number of patients found to be resistant to topical vidarabine, trifluridine was also effective. Trifluridine interferes with DNA synthesis in cultured mammalian cells. However, its antiviral mechanism of action is not completely known.
Cơ Chế Tác Dụng : An antiviral derivative of thymidine used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p557) The mechanism of action of trifluridine has not been fully determined, but appears to involve the inhibition of viral replication. Trifluridine does this by incorporating into viral DNA during replication, which leads to the formation of defective proteins and an increased mutation rate. This drug also reversibly inhibits thymidylate synthetase, an enzyme that is necessary for DNA synthesis.
Dược Động Học :
▧ Absorption :
Systemic absorption of trifluridine following therapeutic dosing with trifluridine ophthalmic appears to be negligible.
▧ Metabolism :
One major metabolite, 5-carboxy-2'-deoxyuridine found on the endothelial side of the cornea, indicating localized metabolism.
▧ Half Life :
Approximately 12 to 18 minutes following ophthalmic administration.
Độc Tính : Overdosage by ocular instillation is unlikely because any excess solution should be quickly expelled from the conjunctival sac. Acute overdosage by accidental oral ingestion has not occurred. However, should such ingestion occur, the 75 mg dosage of trifluridine in a 7.5 mL bottle of trifluridine is not likely to produce adverse effects. Single intravenous doses of 1.5 to 30 mg/kg/day in children and adults with neoplastic disease produce reversible bone marrow depression as the only potentially serious toxic effect and only after three to five courses of therapy. The acute oral LD50 in the mouse and rat was 4379 mg/kg or higher.
Chỉ Định : Ophthalmic solution for the treatment of primay keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex virus, types 1 and 2.
Liều Lượng & Cách Dùng : Solution - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Pharmex
    Sản phẩm biệt dược : Thilol
  • Công ty : Dr. Gerhard Mann
    Sản phẩm biệt dược : Triflumann
  • Công ty : Alcon
    Sản phẩm biệt dược : Trifluridine
  • Công ty : Medivis
    Sản phẩm biệt dược : Triherpine
  • Công ty : Horus
    Sản phẩm biệt dược : Virophta
  • Công ty : Monarch
    Sản phẩm biệt dược : Viroptic
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00432
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6256
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506192
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00391
ChemSpider
http://www.chemspider.com/Chemical-Structure.6020.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50132298
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/61570-037-75
PharmGKB
http://www.pharmgkb.org/drug/PA451775
Wikipedia
http://en.wikipedia.org/wiki/Trifluridine
RxList
http://www.rxlist.com/cgi/generic2/trifluridine.htm
Drugs.com
http://www.drugs.com/cdi/trifluridine-drops.html
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