Saquinavir: Difference between revisions
David Canner (talk | contribs) New page: <applet load="" size="480" color="" frame="true" spin="on" Scene ="Indinavir/Indinavir/1" align="right" caption="Saquinavir, better known as Invirase, (1hsg)"/> ===Better Known as: ... |
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< | <StructureSection load='' size='340' side='right' caption='Saquinavir, better known as Invirase, ([[3d1y]])' scene='Saquinavir/Saquinavir/1'> | ||
===Better Known as: Invirase or Fortovase=== | ===Better Known as: Invirase or Fortovase=== | ||
* Marketed By: Roche<br /> | * Marketed By: Roche<br /> | ||
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* Drug Class: [[HIV Protease]] Inhibitor | * Drug Class: [[HIV Protease]] Inhibitor | ||
* Date of FDA Approval (Patent Expiration): 1995 (2010) <br /> | * Date of FDA Approval (Patent Expiration): 1995 (2010) <br /> | ||
* | * 2004 Sales: $100 Million | ||
* Importance: It was the first [[HIV Protease]] inhibitor to be approved by the FDA. Due to the rapidity with which HIV developed resistance to Saquinavir, Roche halted sales of Saquinavir monotreatments in favor of combination treatments with [[Ritonavir]]. | * Importance: It was the first [[HIV Protease]] inhibitor to be approved by the FDA. Due to the rapidity with which HIV developed resistance to Saquinavir, Roche halted sales of Saquinavir monotreatments in favor of combination treatments with [[Ritonavir]]. | ||
* | * See [[Pharmaceutical Drugs]] for more information about other drugs and diseases. | ||
===Mechanism of Action=== | ===Mechanism of Action=== | ||
When [[HIV]] infects a host, it directs the synthesis of several polyproteins. The maturation of the virus to its infectious form requires that these polyproteins be cleaved to their component proteins by [[HIV Protease]]. The subunits of <scene name=' | When [[HIV]] infects a host, it directs the synthesis of several polyproteins. The maturation of the virus to its infectious form requires that these polyproteins be cleaved to their component proteins by [[HIV Protease]]. The subunits of <scene name='Saquinavir/Hiv_prot/1'>HIV Protease</scene> come together to form a catalytic tunnel capable of binding the nascent peptides and cleaving them into their mature form. Within this tunnel lies <scene name='Saquinavir/Cat/1'>two Asp-Thr-Gly conserved sequences</scene>, which contain the <scene name='Saquinavir/Cat_as/1'>catalytic Asp residues</scene>. These catalytic Asp residues carry out the hydrolytic cleavage of the polyprotein. Saquinavir <scene name='Saquinavir/Cat_asb/1'>binds very precisely</scene> to these conserved sequences within the HIV Protease tunnel, preventing the nascent polyproteins from entering. Unable to actively cleave the nascent proteins into their appropriate form, HIV is unable to mature and proliferate, allowing the patients immune system to fight off the infection more easily.<ref>PMID:1799632</ref><ref>PMID:17243183</ref> | ||
===Drug Resistance=== | ===Drug Resistance=== | ||
The biggest difficulty with treating [[HIV]] is the rapidity at which it mutates and becomes resistant to treatments. To view a comprehensive and interactive analysis of the mutations which confer drug resistance to [[HIV Protease]], See: [[HIV Protease Inhibitor Resistance Profile]] | The biggest difficulty with treating [[HIV]] is the rapidity at which it mutates and becomes resistant to treatments. To view a comprehensive and interactive analysis of the mutations which confer drug resistance to [[HIV Protease]], See: [[HIV Protease Inhibitor Resistance Profile]] | ||
</StructureSection> | |||
===Pharmacokinetics=== | ===Pharmacokinetics=== | ||
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{{:HIV Protease Inhibitor Pharmacokinetics}} | |||
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===References=== | ===References=== | ||