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

  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},

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).

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.

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

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.

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).



Correlation between chemical structure, receptor binding, and biological activity of some novel, highly active, 16 alpha, 17 alpha-acetal-substituted glucocorticoids.

The affinity for the receptor in vitro was closely correlated to the topical glucocorticoid activity in vivo for the 12 steroids compared, which supports the contention that in vitro tests for receptor affinity are useful when screening for agonists among steroids with the present type of structures.

Glucocorticoids and cultured human skin cells: specific intracellular binding and structure‐activity relationships

  • M. Ponec
  • Biology, Chemistry
    The British journal of dermatology
  • 1982
Use of cytosol fractions of both cultured human skin fibroblasts and epidermal keratinocytes contain macromolecules that bind glucocorticoids with high affinity and the structure‐binding relationship studies revealed the relative contribution of various substituents on the steroid molecule for the binding affinity of the steroids.

Formation of covalent adducts between cortisol and 16 alpha-hydroxyestrone and protein: possible role in the pathogenesis of cortisol toxicity and systemic lupus erythematosus.

It is proposed that the formation of covalent steroid-protein adducts is a generalized phenomenon which may contribute to the pathological effects produced by elevated levels of certain endogenous steroids.


The vasoconstrictor assay for topical steroids has been modified and extended so that it may be used to screen for activity and to determine bioavailability and exceeds the FDA Bioequivalence Requirements and In Vivo Bioavailability Procedures.

Variations in the levels of cytoplasmic glucocorticoid receptors in lungs of various species at different developmental stages.

Cytoplasmic fractions obtained from lungs of several animal species at different stages of development were examined for dexamethasone receptors and lower but significant levels of the dexamETHasone binding component were found in lungs of mature rabbits but it could not be detected in lungs in adult rats, mice, hamsters or guinea pigs.

Atrophy of the skin

  • I. Sneddon
  • Medicine
    The British journal of dermatology
  • 1976
The topical application of corticosteroids has enabled the control of so many dermatoses that one should preserve a balanced view on the occasional harmful effects which occur as a result of their abuse, but one should be especially careful in prescribing strong steroids for children and adolescents.

Chlorosulfates as Reagents in the Synthesis of Carboxylic Acid Esters Under Phase-Transfer Conditions

Abstract During a search for a satisfactory synthesis of chloromethyl esters 1 of certain β-lactam antibiotics, e.g. penicillanic acid sulfone, we discovered that chloromethyl chlorosulfate1 (4) is