Sulfur- and phosphorus-containing FDA approved drugs in the last five years (2020–2024): A journey among small molecules

Abstract

Sulfur and phosphorus are elements that can be found in various FDA-approved drugs, either as part of the active pharmaceutical ingredients (APIs) or as components of excipients (inactive ingredients). In this review we will explore the therapeutical use and the synthesis of the approved small molecules (<1000 Da) in the last five years. Sulfur contributes to the redox properties of drugs, the ability to form disulfide bonds, and hydrophobicity, influencing drug interactions and efficacy. Phosphorus contributes to the charge, polarity, and binding affinity of drugs, enhancing their activity in biological systems. These two elements have been increasingly incorporated into therapeutic agents, enhancing drug efficacy, selectivity, and pharmacokinetic profiles. 33 sulfur-based and 3 phosphorus-based drugs are described in this paper. The therapeutic uses and the synthesis of the S- and P- containing approved drugs will be given.