Caspofungin

Antifungal

Also known as: Cancidas, Caspofungin Acetate, MK-0991

EchinocandinsResearch phase: FDA-approvedRegulatory: FDA-approved (2001) for invasive aspergillosis (salvage), invasive candidiasis, empiric therapy in febrile neutropenia, and esophageal candidiasis (Cancidas).

Mechanism

Caspofungin is an IV antifungal drug derived from a fungal natural product. It works by blocking the enzyme that builds fungal cell walls (1,3-beta-D-glucan synthase), causing the fungal cell to become fragile and die. It is a first-line treatment for invasive candidiasis and aspergillosis and has an excellent safety profile because human cells do not have the target enzyme.

Technical detail

Caspofungin is a semisynthetic lipopeptide echinocandin derived from pneumocandin B0 (a metabolite of Glarea lozoyensis). It non-competitively inhibits 1,3-beta-D-glucan synthase (encoded by FKS1/FKS2), the enzyme responsible for synthesizing 1,3-beta-D-glucan — a critical structural polysaccharide in fungal cell walls absent in mammalian cells. Glucan depletion leads to osmotic instability and fungal cell lysis. Fungicidal against Candida spp. and fungistatic against Aspergillus spp. (where it causes aberrant hyphal growth). Resistance arises via FKS1 hot-spot mutations reducing drug-target interaction.

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