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lobucavir
- Development stage
- Phase 2
- Lead developer
- Bristol Myers Squibb
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral (investigational)
01
Overview
Lobucavir is a synthetic antiviral drug developed as a carbocyclic nucleoside analogue. It exhibits broad-spectrum activity against several viruses including herpesviruses (such as herpes simplex virus and cytomegalovirus), hepatitis B virus (HBV), HIV/AIDS, and other hepadnaviruses. Lobucavir acts primarily by inhibiting viral DNA polymerase and reverse transcriptase enzymes, thereby blocking viral DNA synthesis and replication. The drug showed promising efficacy in early clinical trials for hepatitis B with minimal adverse effects; however, its development was discontinued after long-term animal studies revealed an increased risk of cancer in mice. Despite this carcinogenic risk also being present in some approved antivirals like zidovudine and ganciclovir, Bristol-Myers Squibb halted further development of lobucavir[10].
- Other names
- BMS-180194BMS180194BMS 180194Cyclobut-G
02
Targets
Human immunodeficiency virus type 1 reverse transcriptaseCMV DNA polymerase (Human cytomegalovirus DNA polymerase)HBV Pol (Hepatitis B virus polymerase)
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