Soft drugs—10. Blanching activity and receptor binding affinity of a new type of glucocorticoid: Loteprednol etabonate

@article{Druzgala1991SoftDB,
  title={Soft drugs—10. Blanching activity and receptor binding affinity of a new type of glucocorticoid: Loteprednol etabonate},
  author={Pascal Druzgala and Guenther Hochhaus and NICHOLAS S. Bodor},
  journal={The Journal of Steroid Biochemistry and Molecular Biology},
  year={1991},
  volume={38},
  pages={149-154}
}
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82 Citations
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3
Background Citations
20
Methods Citations
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82 Citations

Pharmacokinetic characterization and tissue distribution of the new glucocorticoid soft drug loteprednol etabonate in rats and dogs.

Levels of intact drug and metabolites were highest in liver and kidney, whereas significantly lower levels were found in other investigated organs (lung, brain, heart).

Structural studies of loteprednol etabonate and other analogs of prednisolone using NMR techniques

Budesonide and Ciclesonide: Effect of Tissue Binding on Pulmonary Receptor Binding

The PK/PD model predicted lower receptor occupancy in the lung and the systemic tissues when a drug with pronounced binding was inhaled, including des-CIC, which was predicted to be lower than BUD.

Glucocorticoid receptor binding: A biphasic dependence on molecular size as revealed by the bilinear LinBiExp model

17β-carboxamide steroids--in vitro prediction of human skin permeability and retention using PAMPA technique.

Novel steroid spiro enones: condensation of prednisolone derivatives with diethyl oxalate☆

Soft Drugs 19. Pharmacokinetics, Metabolism and Excretion of a Novel Soft Corticosteroid, Loteprednol Etabonate, in Rats

The results indicate that LE absorbed systemically, after topical administration, can be rapidly transformed to the inactive metabolites, and eliminated from the body mainly through the bile and urine.

Pharmacokinetics and delta1-cortienic acid excretion after intravenous administration of prednisolone and loteprednol etabonate in rats.

Detailed pharmacokinetic studies in rats were performed to compare the PK of prednisolone (PRN) and loteprednol etabonate (LE) as well as their common inactive metabolite delta1-cortienic acid (delta1-CA), and to investigate the excretion of delta 1-CA after PRN and LE administration.

An HPLC method to evaluate purity of a steroidal drug, loteprednol etabonate.

Development of simultaneous quantification method of loteprednol etabonate (LE) and its acidic metabolites, and analysis of LE metabolism in rat

Loteprednol etabonate is a soft corticosteroid with two labile ester bonds at 17α- and 17β-positions that disappears upon hydrolysis of either ester bond, producing the inactive metabolite, Δ1-cortienic acid (Δ1-CA).
...

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