Soft drug loteprednol etabonate

G. Hochhaus, L.-S. Chen, A. Ratka, P. Druzgala, J. Howes, N. Bodor, and H. De-rendorf, Pharmacokinetic characterization and tissue distribution of the new glucocorticoid soft drug loteprednol etabonate in rats and dogs, J. Pharm. Sci. 81 1210 (1992). 

Synthesis of the soft drug , loteprednol etabonate, was achieved by starting with a known inactive metabolite of a known active dmg. The inactive metabolite was then modified to an active form which, after having achieved its therapeutic role, was subsequently metabolized to an inactive species. 

N. Bodor, T. Loftsson, W. M. Wu, Metabolism, Distribution, and Transdermal Permeation of a Soft Corticosteroid, Loteprednol Etabonate , Pharm. Res. 1992, 9, 1275-1278 N. Bodor, W. M. Wu, T. Murakami, S. Engel, Soft Drugs 19. Pharmacokinetics, Metabolism and Excretion of a Novel Soft Corticosteroid, Loteprednol Etabonate, in Rats , Pharm. Res. 1995, 72, 875-879. 

Sample preparation Vortex 100 irL blood with 200 LL MeCN DMSO 95 5, cool at 0° for several min, centrifuge at 3000 rpm for 10 min, inject an aliquot of the supernatant. (A similar procedure can also be used for bile and urine, see Bodor,N. Wu,W.-M. Murakami,T. Engel,S. Soft drugs 19. Pharmacokinetics, metabolism and excretion of a novel soft corticosteroid, loteprednol etabonate, in rats. Pharm.Res. 1995,12, 875-879.)... 

Recent results suggest a promising application of soft drugs in the field of topical corticosteroids (e.g., loteprednol etabonate [142]) and calcium antagonists (e.g., clevipidine [143]). 

Proving effective reversed targeting, which results from the soft nature of this steroid, systemic levels or effects cannot be detected even after chronic ocular administration [57], Plasma levels of loteprednol etabonate and its primary metabolite (PJ-91) were less than the 1 ng/L detection limit in 10 healthy volunteers who received the drug in both eyes eight times daily for 2 days and four times daily for a further 41 days [57], In addition to its already approved uses, loteprednol etabonate is also being developed for the treatment of colitis, atopic dermatitis, and asthma based on promising results from animal studies [47, 48],... 

P. Druzgala, G. Hochhaus, and N. Bodor, Soft drugs. 10. Blanching activity and receptor binding affinity of a new type of glucocorticoid loteprednol etabonate, J. Steroid Biochem. 38 149 (1991). 

T. Loftsson and N. Bodor, The pharmacokinetics and transdermal delivery of loteprednol etabonate and related soft steroids, Adv. Drug Del. Rev. 14 293 (1994). 

Bodor, N. Murakami, T. Wu, W.M. Soft drugs 18. Oral and rectal delivery of loteprednol etabonate, a novel soft corticosteroid, in rats—for safer treatment of gastrointestinal inflammation. Pharm. Res. 1995, 12 (6), 869-874. 

Currently, it is the only corticosteroid approved by the FDA for use in all inflammatory and allergy-related ophthalmic disorders, including inflammation after cataract surgery, uveitis, allergic conjunctivitis, and giant papillary conjunctivitis. Loteprednol etabonate resulted from a classic inactive metabolite-based soft drug approach (103-114). 

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