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amphotericin B + flucytosine
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous, Oral, Intrathecal
01
Overview
Amphotericin B + flucytosine is a combination antifungal therapy primarily used for the treatment of severe systemic fungal infections, most notably cryptococcal meningitis. Amphotericin B is a polyene antifungal that binds to ergosterol in fungal cell membranes, creating pores that lead to cell death. Flucytosine is an antimetabolite antifungal; it enters fungal cells via cytosine permease and is converted into 5-fluorouracil, which disrupts both DNA and RNA synthesis by inhibiting thymidylate synthase and incorporating into RNA. The combination exhibits synergistic or additive effects against susceptible fungi, improving efficacy compared to monotherapy and reducing the risk of resistance development[2][5][6][7]. This regimen is considered the standard of care for initial induction therapy in cryptococcal meningitis, especially in immunocompromised patients such as those with HIV/AIDS[2][3].
- Brand names
- FungizoneAncotil
- Other names
- 5-FC + amphotericin Bflucytosine + amphotericin B
02
Targets
ErgosterolTS (Thymidylate synthase)
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