title: Pharmacological and pharmacokinetic properties of lanthipeptides undergoing clinical studies.
abstract: The intrinsic qualities of lanthipeptides for their use as therapeutic drugs present several challenges because of their properties, which include stability, solubility and bioavailability, which, under physiological conditions, are very low. Researches have encouraged clinical evaluation of a few compounds, such as mutacin 1140, microbisporicin, actagardine and duramycin, with pharmacokinetic profiles showing rapid distribution and elimination rates, good bioavailability and fecal excretion, as well as high protein binding. Local and parenteral administration are currently suitable to minimize environmental influences on lanthipeptides and ensure efficient activity. Nevertheless, valuable improvements on pharmacodynamic and pharmacokinetic properties may also permit systemic applications via enteral routes. Understanding how rational modifications influence the desired pharmacological and pharmacokinetic properties of these biomolecules would help to answer some specific questions about their susceptibility to environmental changes, mechanism of action and how to engineer other peptides of the same group to improve their clinical relevance.
authors.affiliation: Chair of Bioprocess Engineering, Department of Biotechnology, Technische Universität Berlin, Ackerstraße 76, ACK24, 13355, Berlin, Germany. elvis.ongey2@gmail.com.|Department of Biotechnology, Technische Universität Berlin, Ackerstraße 76, ACK24, 13355, Berlin, Germany. elvis.ongey2@gmail.com.
authors.forename: Elvis Legala
authors.initials: EL
authors.lastname: Ongey
authors.affiliation: Chair of Bioprocess Engineering, Department of Biotechnology, Technische Universität Berlin, Ackerstraße 76, ACK24, 13355, Berlin, Germany.
authors.forename: Hüseyin
authors.initials: H
authors.lastname: Yassi
authors.affiliation: Department Ecological Impact Research and Ecotoxicology, Institute of Ecology, Berlin Institute of Technology (BIT), 10538, Berlin, Germany.
authors.forename: Stephan
authors.initials: S
authors.lastname: Pflugmacher
authors.affiliation: Chair of Bioprocess Engineering, Department of Biotechnology, Technische Universität Berlin, Ackerstraße 76, ACK24, 13355, Berlin, Germany.
authors.forename: Peter
authors.initials: P
authors.lastname: Neubauer
mesh_terms: D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics* / Q000494:pharmacology*; D001430:Bacteriocins / Q000493:pharmacokinetics* / Q000494:pharmacology*; D001682:Biological Availability; D004355:Drug Stability; D006801:Humans; D010455:Peptides / Q000493:pharmacokinetics* / Q000494:pharmacology*; D011485:Protein Binding; D012995:Solubility
chemical_list: D000900:Anti-Bacterial Agents; D001430:Bacteriocins; D010455:Peptides; C528150:microbisporicin; C112560:mutacin 1140; C040522:duramycin; C012993:gardimycin
keywords: Antimicrobials; Infectious diseases; Lanthipeptides; Microbisporicin; Pharmacological effects; Therapeutic effects