Lobucavir
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| Formula | C11H15N5O3 |
| Molar mass | 265.273 g·mol−1 |
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Lobucavir (previously known as BMS-180194, Cyclobut-G) is an antiviral drug that shows broad-spectrum activity against herpesviruses, hepatitis B and other hepadnaviruses, HIV/AIDS and cytomegalovirus.[1][2][3] It initially demonstrated positive results in human clinical trials against hepatitis B with minimal adverse effects but was discontinued from further development following the discovery of increased risk of cancer associated with long-term use in mice.[4] Although this carcinogenic risk is present in other antiviral drugs, such as zidovudine and ganciclovir that have been approved for clinical use, development was halted by Bristol-Myers Squibb, its manufacturer.[5]
Lobucavir has been shown to exhibit antiviral activity against herpesvirus, hepatitis B, HIV/AIDS, and human cytomegalovirus.[6] It reached phase III clinical trials for hepatitis B and herpesvirus, phase II clinical trials for cytomegalovirus, and underwent a pilot study for use in treating AIDs[7][8] prior to discontinuation.
Adverse effects
In early clinical trials, Lobucavir was relatively well tolerated in subjects and was not subject to discontinuation due to adverse effects. Commonly reported effects included headache, fatigue, diarrhea, abdominal pain, and flu-like symptoms common with other nucleoside analogs.[9] Other studies, however, identified Lobucavir-induced carcinogenesis associated with long-term use in mice that led to the drug's discontinuation in clinical trials in 1999.[4]