Tenofovir_nov - Tuesday Case Conference Introduction What...

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Unformatted text preview: Tuesday Case Conference Introduction What is Tenofovir disoproxil fumarte (TDF)? How Nucleotide RTI work Nephrotoxicity of NtRTI Is TDF Nephrotoxic? In vitro evidence Epidemiologic evidence What is tenofovir disoproxil fumarate (TDF)? Orally administered pro-drug of tenofovir Tenofovir is a nucleotide analogue inhibitor of reverse transcriptase (NtRTI) Others in the family are Adefovir and Cidofovir, well described nephrotoxins Tenofovir similar to Adefovir The only NtRTI used for treatment of HIV TDF Single Agent Viread marketed for the treatment of HIV since 2001 Combination Truvada Fixed-dose combination TDF and emtricitabine (NRTI), 2004 Atripla Fixed-dose triple combination of TDF, emtricitabine (NRTI) and efavirenz (NNRTI), 2006 Reverse Transcriptase Inhibitors Competitive substrate inhibitors Nucleoside RTI (NRTI) Nucleotide RTI (NtRTI) Non-competitive substrate inhibitor Non-nucleoside RTI (NNRTI) www.web-books.com/.../Images/HIV_Cycle.jpg How does NtRI work? Nucleoside+Phosphate Prolonged action Low resistance profile TDF Compete with normal substrate for viral DNA polymerase (HIV-1 RT) Minimally interfere with nuclear DNA synthesis Clercq-Holy_Acyclic nuc phosphonates_Nat Rev Pharm_2005 TDF in treatment of HIV infection Clercq-Holy_Acyclic nuc phosphonates_Nat Rev Pharm_2005 Regimen with TDF >80% of patients with HIV RNA (<50 copies per ml) at 48 weeks Is TDF nephrotoxic? Potential for nephrotoxicity Similar structure to Adefovir, known nephrotoxin Accumulation in renal proximal tubule Vd of 0.8 L/kg Minimally protein bound (<8%) Mainly excreted in urine,...
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This note was uploaded on 12/24/2011 for the course STEP 1 taught by Professor Dr.aslam during the Fall '11 term at Montgomery College.

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Tenofovir_nov - Tuesday Case Conference Introduction What...

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