Rapid deprotection and purification of ceftaroline free base from its phosphoramidate prodrug.

ABSTRACT: Contemporary pharmaceutical design often incorporates functional groups to improve the pharmacokinetic/pharmacodynamic profile of a desired active chemical entity. These compounds are known as prodrugs. While prodrug enhancements may improve a medication's clinical utility, they often limit the ability for in vitro testing of the active drug. Published protocols suggest that commercially available phosphatase enzymes can provide a straightforward and cost-effective way to access the active components of phosphoramidate prodrugs. Here, we demonstrate that commercial phosphatases lack reproducibility in generating the active antibiotic ceftaroline from its prodrug ceftaroline fosamil (Teflaro^®). We propose that previously reported successes with phosphatase-mediated convers

SUBMITTER: Roy S 

PROVIDER: S-EPMC12444786 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature