| Summary: | This review considers the chiral phosphorus-containing drugs used to treat patients in the clinic, as well as the promising and experimental drugs that are in the process of being researched. Natural and synthetic representatives of phosphorus-containing drugs, such as tenofovir (hepatitis B and HIV treatment), fosfomycin (antibiotic), valinofos (antibiotic), phosphazinomycin A (antibiotic), (<i>R</i>)-phospholeucine, various antibacterial and antifungal agents, renin inhibitors, etc., have found practical applications as medicines and bioregulators and other medicines. The influence of the chirality of both carbon atoms and phosphorus atoms on the pharmacodynamics, pharmacokinetics, and toxicological properties of phosphorus drugs has been demonstrated. Therefore, the choice of enantiomers is critical since the wrong choice of a chiral drug can lead to undesirable consequences, carcinogenicity, and teratogenicity. New chiral technologies affecting drug development are discussed, such as the “chiral switch” of racemates already on the market, as well as phosphorus-containing prodrugs with a higher biological selectivity and low adverse effects.
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