Abacavir sulfate Chemical Properties |
Melting point |
222-225°C |
storage temp. |
2-8°C |
solubility |
H2O: ≥17mg/mL |
form |
powder |
color |
white to tan |
optical activity |
[α]/D -30 to -40°, c = 0.5 in methanol |
Water Solubility |
1.68ug/L(32 ºC) |
CAS DataBase Reference |
188062-50-2(CAS DataBase Reference) |
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Abacavir sulfate Usage And Synthesis |
Description |
Abacavir sulfate was first launched as Ziagen in the US for the treatment of human immunodeficiency virus (HIV) infection, in combination with other antiretroviral drugs. Abacavir is a carbocyclic nucleoside reverse transcriptase inhibitor (nRTI); it is one of the most potent anti-HIV agents to date. The compound can be prepared by an enantioselective synthesis involving palladium-catalyzed coupling of a chloropurine with a carbocyclic allylic diacetate. In vitro, Abacavir is a potent and selective inhibitor of HIV-1 and HIV-2 replication. Resistance to Abacavir develops more slowly than for other anti-HIV agents. Abacavir is highly synergistic with protease inhibitors such as Amprenavir. In clinical trials for HIV infections in adults, it produced durable suppression in viral load. Combinations with different protease inhibitors such as Nelfinavir, Saquinavir or Indinavir markedly reduced plasma viral load to undetectable levels for at least 48 weeks, and significantly raised CD4+ cell counts in adults with HIV infection, especially nRTI-naive patients. Abacavir has a good oral availability and its penetration into CSF is much more significant than for other anti-HIV drugs. The two major metabolites identified in humans were the 5'-carboxylate and the 5'-glucuronide, mainly excreted via the renal route. |
Chemical Properties |
White Solid |
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