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Atevirdine is an investigational non-nucleoside reverse transcriptase inhibitor (NNRTI) from the bis(heteroaryl)piperazine (BHAP) chemical class, studied in the 1990s for HIV-1 infection, typically combined with zidovudine (AZT).
- Raised CD4 lymphocyte counts in a portion of treated patients in early combination trials
- Well tolerated alongside zidovudine in Phase 1 testing
- Helped establish the BHAP chemical class that led to the approved drug delavirdine
Overview
An early HIV drug candidate that got outcompeted; its chemical lineage led to delavirdine, which did reach market.
Mechanism
Atevirdine binds directly to HIV-1 reverse transcriptase at a site distinct from the enzyme's active site (a non-nucleoside binding pocket), blocking the conformational changes the enzyme needs to convert viral RNA into DNA. This action does not require intracellular activation, unlike nucleoside analogues such as zidovudine.
receptor fingerprint
HIV-1 reverse transcriptaseInhibitor
Dosingtypical ranges, not medical advice
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Safetyrisks and cautions, not medical advice
In Phase 1 combination trials with zidovudine, atevirdine was generally well tolerated, and a meaningful proportion of treated patients had increases in CD4 lymphocyte counts. Resistance-conferring mutations, notably at reverse transcriptase codons 103 and 181, emerged during monotherapy and combination regimens, limiting durability of response. It was never approved and was superseded in its developer's pipeline by the more potent successor compound delavirdine.
Subjective profileweighing the evidence above
Of historical interest only. It was tolerable and moved CD4 counts in some patients, but resistance mutations appeared quickly and its own developer replaced it with delavirdine. Modern HIV therapy is in a different league, so there is no reason to seek this out.
Resources
This entry is here for reference.
Research
1 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
FAQ
What is Atevirdine used for?
It was investigated in the 1990s as a treatment for HIV-1 infection, usually paired with zidovudine (AZT).
How does Atevirdine work?
It's a non-nucleoside reverse transcriptase inhibitor; it binds HIV's reverse transcriptase enzyme directly and blocks it from converting viral RNA into DNA.
Is Atevirdine well-researched?
It has published Phase 1 clinical data, but it was never approved and was replaced in development by its more effective successor, delavirdine.
Limitations of the evidence
- Resistance mutations emerged relatively quickly during monotherapy
Notes and cautions
- Never approved; superseded by delavirdine
- Outdated relative to modern antiretroviral regimens