FDA-Approved Drugs Containing Amide Functionality in the Last Five Years (2021–2025): Pharmaceutical Use, Trends and Synthetic Approaches
- 1Laboratory of Molecular Logic Gates, Department of Chemistry, Faculty of Science, University of Malta, MSD 2080 Msida, Malta
Abstract
The amide functional group remains a cornerstone of medicinal chemistry, serving as an indispensable scaffold in the design of modern therapeutics. This review presents an analysis of FDA-approved drugs (small molecules and peptides with MW < 1300 Da) containing amide functionality between 2021 and 2025, highlighting its continued and evolving role in addressing contemporary medical challenges. An analysis of these novel therapeutics reveals the remarkable functional versatility of the amide bond. In antiviral agents like nirmatrelvir (Paxlovid®), amides form the structural backbone of peptidomimetics, enabling high-affinity binding to a viral protease. In precision oncology, as seen with adagrasib (Krazati®), the amide acts as a critical, metabolically stable linker that positions a covalent warhead for selective inhibition of a mutant kinase. This analysis underscores that amide’s unique combination of planarity, resonance stabilization, and capacity for robust hydrogen bonding continues to make it an essential element in the medicinal chemist’s toolkit, underpinning the development of next-generation therapeutics across oncology, infectious diseases, and neurology. To provide a practical framework for drug discovery, the synthetic routes for each drug are detailed, with particular emphasis placed on the key amide-forming strategies employed.
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BibTeX
@article{tiz2026fdaapproved,
title = {{FDA-Approved Drugs Containing Amide Functionality in the Last Five Years (2021–2025): Pharmaceutical Use, Trends and Synthetic Approaches}},
author = {Davide Benedetto Tiz},
journal = {Medicines},
year = {2026},
month = jul,
doi = {10.3390/medicines13030022},
url = {https://doi.org/10.3390/medicines13030022},
note = {CC BY},
}
RIS
TY - JOUR
TI - FDA-Approved Drugs Containing Amide Functionality in the Last Five Years (2021–2025): Pharmaceutical Use, Trends and Synthetic Approaches
AU - Davide Benedetto Tiz
PY - 2026
DA - 2026/07/07
JO - Medicines
DO - 10.3390/medicines13030022
UR - https://doi.org/10.3390/medicines13030022
AB - The amide functional group remains a cornerstone of medicinal chemistry, serving as an indispensable scaffold in the design of modern therapeutics. This review presents an analysis of FDA-approved drugs (small molecules and peptides with MW < 1300 Da) containing amide functionality between 2021 and 2025, highlighting its continued and evolving role in addressing contemporary medical challenges. An analysis of these novel therapeutics reveals the remarkable functional versatility of the amide bond. In antiviral agents like nirmatrelvir (Paxlovid®), amides form the structural backbone of peptidomimetics, enabling high-affinity binding to a viral protease. In precision oncology, as seen with adagrasib (Krazati®), the amide acts as a critical, metabolically stable linker that positions a covalent warhead for selective inhibition of a mutant kinase. This analysis underscores that amide’s unique combination of planarity, resonance stabilization, and capacity for robust hydrogen bonding continues to make it an essential element in the medicinal chemist’s toolkit, underpinning the development of next-generation therapeutics across oncology, infectious diseases, and neurology. To provide a practical framework for drug discovery, the synthetic routes for each drug are detailed, with particular emphasis placed on the key amide-forming strategies employed.
SN - 2305-6320
ER -