ATC Group: J02A Antimycotics for systemic use

Amphotericin B is a macrocyclic, polyene antifungal antibiotic produced by Streptomyces nodosus. The molecule is thought to act by binding to sterols in the fungal cell membrane, with a resulting change in membrane permeability, allowing leakage of a variety of small molecules.

Anidulafungin is a semi-synthetic echinocandin, a lipopeptide synthesised from a fermentation product of Aspergillus nidulans. Anidulafungin selectively inhibits 1,3-β-D glucan synthase, an enzyme present in fungal, but not mammalian cells.

Caspofungin acetate is a semi-synthetic lipopeptide (echinocandin) compound synthesised from a fermentation product of Glarea lozoyensis. Caspofungin acetate inhibits the synthesis of beta (1,3)-D-glucan, an essential component of the cell wall of many filamentous fungi and yeast. Beta (1,3)-D-glucan is not present in mammalian cells.

Fluconazole is a triazole antifungal agent. Its primary mode of action is the inhibition of fungal cytochrome P-450-mediated 14 alpha-lanosterol demethylation, an essential step in fungal ergosterol biosynthesis.

Flucytosine is a fluorinated pyrimidine derivative. It is an antimycotic agent exerting fungistatic and fungicidal activity by interfering with protein and DNA synthesis. Fluorodeoxyuridine interferes with the enzyme thymidylate synthase. Inhibition of thymidylate synthase subsequently causes disruption of DNA synthesis.

Isavuconazole is an active form of isavuconazonium. Isavuconazole inhibits lanosterol 14-alpha demethylase (or CYP51A1) and leads to the accumulation of ergosterol toxic precursors in the fungal cytoplasm. Isavuconazole is indicated for the treatment of invasive aspergillosis and invasive mucormycosis.

Itraconazole is a triazole derivative that inhibits fungal 14α-demethylase, resulting in a depletion of ergosterol and disruption of membrane synthesis by fungi.

Ketoconazole is an imidazole-dioxolane antimycotic, active against yeasts, including Malassezia and dermatophytes.

Micafungin non-competitively inhibits the synthesis of 1,3-β-D-glucan, an essential component of the fungal cell wall. 1,3-β-D-glucan is not present in mammalian cells. Micafungin exhibits fungicidal activity against most Candida species and prominently inhibits actively growing hyphae of Aspergillus species.

Miconazole possesses an antifungal activity against the common dermatophytes and yeasts as well as an antibacterial activity against certain gram-positive bacilli and cocci. Its activity is based on the inhibition of the ergosterol biosynthesis in fungi and the change in the composition of the lipid components in the membrane, resulting in fungal cell necrosis.

Posaconazole inhibits the enzyme lanosterol 14α-demethylase (CYP51), which catalyses an essential step in ergosterol biosynthesis.

Rezafungin selectively inhibits fungal 1,3-β-D-glucan synthase. This results in inhibition of the formation of 1,3-β-D-glucan, an essential component of the fungal cell wall which is not present in mammalian cells. Inhibition of 1,3-β-D-glucan synthesis results in rapid and concentration-dependent fungicidal activity in Candida species (spp.).

Voriconazole is a triazole antifungal agent. The primary mode of action of voriconazole is the inhibition of fungal cytochrome P450-mediated 14 alpha-lanosterol demethylation, an essential step in fungal ergosterol biosynthesis.