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Drug Development

HEPT Analog Moves Forward in Preclinical Tests

Published in AIDS Weekly, July 10th, 1995

An unusual member of the family of anti-HIV-1 drugs known as HEPT derivatives has pharmacokinetic properties that may permit its use as an AIDS therapy.

The acyclic nucleoside analog 1-[(2-hyroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) and its derivatives are potent inhibitors of HIV-1. Like the diverse group of drugs known as non-nucleoside reverse transcriptase inhibitors (NNRTIs), most HEPT derivatives inhibit HIV-1, but not HIV-2, reverse transcriptase (RT). In fact, HEPT and the NNRTIs are sometimes referred to as HIV-1-specific RT inhibitors. But in addition to NNRTI-like noncompetitive RT inhibition, the HEPT compounds also inhibit HIV RT by competing with...

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