Maraviroc, CCR5 Co- Receptor Antagonists

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Clinical Use
:Ø ART experienced patients with CCR5 tropic HIV-1 virus and withdetectable viral resistance to multiple ARTs
Ø Should not be used in treatment naïve patient
Failure:• Tropism for conversion from CCR 5 to CXCR 4 or dual or mixedtropism of HIV-1
• v3 loop mutation in gp120
Recommended Maraviroc Dose:1) 150mg oral BD in combination with CYP3A inhibitors (proteaseinhibitors,azole itraconazol/ ketoconazol, clarithromycin).2) 300mg oral BD in combination with ritonavir boosted tipranavir, NRTI,enfuvirtide, nevirapine or other drugs without CYP3A effect.3) 600mg oral BD with CYP 3A inducers efavirenz, entravirin, rifampicin,st. jone`s wart.Metabolism :Primarily by liverToxicities: Diarrhoea, nausea, fatigue, headache and derangement ofliver function testVicriviroc:Plasma half life markedly increased by CYP 3A4 inhibitorsPlasma half life >24 hrsNo food effectDurable antiretroviral activity in CCR5 tropic strainUnder Phase III trialAlpraviroc: Hepatotoxic, so trial was terminated.Apretinant: neurokinin 1 receptor antagonistApproved antiemetic, downregulates CCR5 expression on macrophages invitro- under investigation.

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Unknown said…
BOC Sciences provides a wide range of research chemicals and biochemicals including inhibitors, building blocks, Maraviroc
November 16, 2018 at 8:51 PM
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