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Alovudine is a nucleoside reverse transcriptase inhibitor (NRTI) that was investigated as an antiretroviral for HIV infection and, in a fluorine-18 labeled form, is used as a PET imaging tracer for cell proliferation.
- Retains antiviral activity against many NRTI-resistant HIV-1 strains in laboratory studies
- Also developed as an F-18 labeled PET tracer (FLT-PET) for imaging cell proliferation in cancer research
- Bone marrow suppression was the main dose-limiting toxicity in early trials
- Hematologic and liver toxicity signals appeared at doses tested
Overview
It works, but the same NRTI toxicity that sank it in the 1990s (bone marrow suppression) kept resurfacing when researchers tried to bring it back.
Mechanism
Alovudine (3'-deoxy-3'-fluorothymidine) is a synthetic thymidine analog. Once inside cells it is phosphorylated to its active triphosphate form, which is incorporated by HIV reverse transcriptase into the growing viral DNA chain and terminates further chain elongation because it lacks the 3'-hydroxyl group needed to continue DNA synthesis. It retains activity against many HIV-1 strains resistant to other NRTIs, including zidovudine-resistant virus and strains with multiple thymidine-associated mutations.
receptor fingerprint
HIV reverse transcriptaseInhibitor
Safetyrisks and cautions, not medical advice
The dose-limiting toxicity identified in early trials was bone marrow suppression (myelosuppression), along with hematologic and liver toxicity signals; this narrow therapeutic window and lack of clear advantage over already-approved NRTIs led to discontinued development in the 1990s and again in later attempts to revive the compound at lower doses.
Subjective profileweighing the evidence above
Development stopped for good reason; the bone-marrow and liver toxicity showed up at the doses needed to work, and better NRTIs already existed. Its lasting value is as an F-18 PET tracer, not as a drug anyone should take.
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 Alovudine used for?
It was investigated as a treatment for drug-resistant HIV infection; a radiolabeled version (FLT) is also used as a PET imaging tracer in cancer research, unrelated to its antiviral use.
How does Alovudine work?
As a thymidine analog, it gets built into HIV's growing DNA chain by reverse transcriptase and then stops the chain from growing any further, halting viral replication.
Is Alovudine well-researched?
It has real clinical trial history in HIV patients dating back to the early 1990s, but development was repeatedly stopped because of bone marrow toxicity, so it was never approved.
Adverse effects
- Bone marrow suppression was the main dose-limiting toxicity in early trials
- Hematologic and liver toxicity signals appeared at doses tested
Notes and cautions
- Never approved for HIV treatment due to its narrow safety margin