Tìm theo
Raltegravir
Các tên gọi khác (2) :
  • MK-0518
  • RAL
anti hiv agents
Thuốc Gốc
Small Molecule
CAS: 518048-05-0
CTHH: C20H21FN6O5
PTK: 444.4163
Raltegravir is an antiretroviral drug produced by Merck & Co., used to treat HIV infection. It received approval by the U.S. Food and Drug Administration (FDA) on 12 October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H21FN6O5
Phân tử khối
444.4163
Monoisotopic mass
444.155746017
InChI
InChI=1S/C20H21FN6O5/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30)
InChI Key
InChIKey=CZFFBEXEKNGXKS-UHFFFAOYSA-N
IUPAC Name
N-[(4-fluorophenyl)methyl]-5-hydroxy-1-methyl-2-{2-[(5-methyl-1,3,4-oxadiazol-2-yl)formamido]propan-2-yl}-6-oxo-1,6-dihydropyrimidine-4-carboxamide
Traditional IUPAC Name
raltegravir
SMILES
CN1C(=O)C(O)=C(N=C1C(C)(C)NC(=O)C1=NN=C(C)O1)C(=O)NCC1=CC=C(F)C=C1
logP
-0.39
pKa (strongest acidic)
5.62
pKa (Strongest Basic)
-1.5
PSA
150.02 Å2
Refractivity
112.59 m3·mol-1
Polarizability
42.47 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
7
H Bond Donor Count
3
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Cơ Chế Tác Dụng : Raltegravir is an antiretroviral drug produced by Merck & Co., used to treat HIV infection. It received approval by the U.S. Food and Drug Administration (FDA) on 12 October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval. [Wikipedia] Raltegravir targets integrase, an HIV enzyme that integrates the viral genetic material into human chromosomes, a critical step in the pathogenesis of HIV. The drug is metabolized away via glucuronidation.
Dược Động Học :
▧ Absorption :
Absorbed from the gastrointestinal tract.
▧ Volume of Distribution :
Approximately 83% bound to human plasma protein and is minimally distributed into red blood cells (blood-to-plasma partitioning ratio of 0.6).
▧ Protein binding :
83%
▧ Metabolism :
Hepatic (UGT1A1)
▧ Route of Elimination :
Feces and urine
▧ Half Life :
9 hours
▧ Clearance :
The major mechanism of clearance of raltegravir in humans is glucuronidation mediated by UGT1A1, the renal clearance of unchanged drug is a minor pathway of elimination of raltegravir (9% of total dose).
Chỉ Định : For the treatment of HIV-1 infection in conjunction with other antiretrovirals.
Tương Tác Thuốc :
  • Telaprevir Telaprevir increases the exposure of raltegravir by up to 31% but this interaction is considered as not clinically relevant.
Liều Lượng & Cách Dùng : Tablet, chewable - Oral - 100mg
Tablet, chewable - Oral - 25mg
Tablet, film coated - Oral - 400mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Merck
    Sản phẩm biệt dược : Isentress
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06817
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D06676
Wikipedia
http://en.wikipedia.org/wiki/Raltegravir
Drugs.com
http://www.drugs.com/monograph/isentress.html
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