Natural Product-Inspired Antifungal Drugs Introduced for Human Use from 1872 to August 2026

This review provides a comprehensive account of 30 natural product (NP)-inspired antifungal therapeutic agents introduced for human use between 1872 and August 2026. These comprise 14 NPs (47%) and 16 NP-derived (NP-D; 53%) agents, the latter encompassing semisynthetic derivatives and synthetic analogues of NP scaffolds. These antifungal drugs are organised into eight structural classes, many of which share modes of action (MoA), and are individually classified as NP or NP-D, with accompanying structures illustrating the chemical modifications that link NP-D agents to their progenitor NPs. We summarise the first introduction or approval of each agent for human use by country and year, documented antifungal spectrum, routes of administration, usage status, MoA and key historical, chemical and clinical context. Analysis of the assembled dataset documents the historical importance and enduring clinical impact of these agents, while also revealing a recent concentration of approvals among NP-D inhibitors of β-1,3-D-glucan synthase. These findings underscore the enduring value of NPs as antifungal leads and highlight the need for greater chemical and mechanistic diversity in antifungal discovery, particularly through agents directed at new fungal targets.