Global first-in-class drugs approved in 2023-2024: Breakthroughs and insights

First-in-class (FIC) drugs are considered the main drivers of new drug discovery and have novel targets and mechanisms. The proportion of FIC drugs among new drugs provides fundamental guidance for both academic and pharmaceutical research. From a global perspective, 81 FIC drugs were approved in 2023 and 2024. Among them, small-molecule drugs account for a greater percentage (51.9%), illustrating the discovery of new chemical entities. Macromolecule drugs (48.1%), which mainly consist of antibody analogs, represent a growing trend as new biotechnology techniques have emerged. In terms of FIC drug indications, cancer remained the top priority (22.0%) with 18 FIC therapies, revealing the high patient need in this context. As for innovations regarding mechanism-based therapies, diverse enzymes were the most common FIC drugs (32.1%), with 26 novel targets identified. In this review, the performance and characteristics of FIC drug approvals in 2023 and 2024 will be presented, providing information on breakthroughs and insights for global drug discovery.