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Superior Nuclear Receptor Selectivity and Therapeutic Index of Methylprednisolone Aceponate Versus Mometasone Furoate

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Superior Nuclear Receptor Selectivity and Therapeutic Index of Methylprednisolone Aceponate Versus Mometasone Furoate DOI:10.1111/j.1600-0625.2007.00597.x www.blackwellpublishing.com/EXD Original Article Superior nuclear receptor selectivity and therapeutic index of methylprednisolone aceponate versus mometasone furoate Parham Mirshahpanah1, Wolf-Dietrich Do¨ cke2, Udo Merbold2, Khusru Asadullah2, Lars Ro¨se2, Heike Scha¨ cke2 and Thomas M. Zollner1 1Research Business Area Dermatology, Berlex Biosciences, Richmond, CA, USA; 2Corporate Research Area Inflammation, Bayer Schering Pharma, Berlin, Germany Correspondence: Thomas M. Zollner, TRG Inflammation, Bayer Schering Pharma, Berlin, Germany, Tel.: +1 510 669 4272, e-mail: [email protected] Accepted for publication 18 June 2007 Abstract: Although introduced more than 50 years ago, topical a relevant rodent model in vivo. We demonstrate that glucocorticoids are still the first line therapy for many methylprednisolone aceponate displays higher specificity in inflammatory skin disorders such as atopic eczema, contact nuclear receptor binding compared with mometasone furoate. dermatitis and many others. Recently, significant improvements Methylprednisolone aceponate was also markedly superior in have been made to optimize the ratio of desired to unwanted terms of minimizing induction of skin atrophy or telangiectasias effects. While with early compounds such as triamcinolone, when compared with mometasone furoate. Based on these topical side effects such as skin atrophy and telangiectasias can be observations, methylprednisolone aceponate is expected to have a observed rather frequently, newer drugs such as methyl- greater therapeutic index as compared with mometasone furoate, prednisolone aceponate or mometasone furoate have a at least in the test systems used here. The degree to which this significantly improved therapeutic index. The present study observation may translate into a clinical setting requires compared these two modern topical glucocorticoids, which confirmation. possess the highest therapeutic index currently found, in terms of Key words: glucocorticosteroid – skin atrophy – skin nuclear receptor selectivity in vitro and induction of the most inflammation – telangiectasia – therapeutic index important local side effects (skin atrophy and telangiectasias) in Please cite this paper as: Superior nuclear receptor selectivity and therapeutic index of methylprednisolone aceponate versus mometasone furoate. Experimental Dermatology 2007; 16: 753–761. Introduction Although these superpotent GCs were highly effective for certain indications, localizations and types of disease, they Glucocorticoids (GCs) are the most widely used class of showed harmful local and systemic side effects when used anti-inflammatory drugs. In the early 1950s, hydrocorti- over prolonged periods or when improperly applied. In sone was observed to be an effective topical therapy of terms of local side effects, skin atrophy is one of the most inflammatory skin disorders. This initial success spurred important side effects in topical GC therapy (3–6). Skin the evolution of compounds with higher potency. Triam- atrophy compromises the skin’s function to maintain a cinolone acetonide was one of the first halogenated corti- permeability barrier between the organism and the external costeroids that led to the development of the superpotent environment (7). GC-induced skin atrophy is characterized GCs (1,2). by increased skin tearing, thinning and telangiectasia (8). Glucocorticoid atrophogenic potential is commonly assessed in a preclinical, in vivo rat model (2,8,9). Current Abbreviations: AR, androgen receptor; GC, glucocorticoid; studies prefer hairless animals such as hr ⁄ hr rats because of GR, glucocorticoid receptor; MR, mineralocorticoid receptor; NR, nuclear receptor; HPA, hypothalamic-pituitary-adrenal; the unreliability of haired skin responses (10). Skin thick- MF, mometasone furoate; MPA, methylprednisolone aceponate; ness is one parameter for skin atrophy, determined over TIX, therapeutic index; MPP, 6a-methylprednisolone-17- time in the living animal, using a specifically designed propionate; DEX, dexamethasone; CCS, charcoal-stripped calf gauge to measure skin fold thickness by applying a defined serum; CF, competition factor; nGSR, non-GC-selective receptor. pressure to ensure reproducibility (11). Skin breaking ª 2007 The Authors Journal compilation ª 2007 Blackwell Munksgaard, Experimental Dermatology, 16, 753–761 753 Mirshahpanah et al. strength measurement of GC-treated skin is used as an (a) O additional parameter for skin atrophy (10). O In comparison with human skin, the hairless rat skin is O CH 3 O more sensitive to atrophy following topical GC application. HO Anatomical differences between the rodent and human CH H skin, such as increased dermal layers in human skin, may 3 O influence pharmacokinetics (2,12). Using this model has H H helped gauge the evolution of GCs. Recently, the therapeutic index (TIX) has been estab- O lished as a standard for topical GCs by measuring both the CH 3 desired anti-inflammatory effects and the unwanted side effects (13). The concept of the benefit to risk ratio evalua- β tion with topical GCs is based on in vitro and in vivo data IUPAC name: 21-Acetoxy-11 -hydroxy- 6 α-methyl-17-propionyloxy-1,4- with regards to efficacy and safety (14–16). The TIX value pregnadiene-3,20-dione is indicated as a ratio of desired to adverse effects, thus a ratio approximating 1 signifies an equal relation of desired (b) O and adverse effects, whereas a ratio of 2–3 indicates a GC Cl H C O 3 with increased benefit to risk ratio. With increasing know- HO O ledge of the mechanism of action of GCs and pharmacoki- CH H O 3 netics of the skin, GC development turned towards CH compounds with a better TIX, leading to compounds such 3 as prednicarbate, methylprednisolone aceponate (MPA) Cl H and mometasone furoate (MF) with the highest TIX of 2.0; O here we focus on the latter two compounds. Methylprednisolone aceponate (Fig. 1a) and MF (Fig. 1b) IUPAC name: 9,21-Dichloro-17-(2-furoyloxy)- are both applied once daily as 0.1% topical cream, oint- 11 β-hydroxy-16 α-methylpregna-1,4-diene- ment, or lotion formulations for the treatment of patients 3,20-dione with inflammatory GC-responsive dermatoses (17,18). Figure 1. Chemical structures of (a) methylprednisolone aceponate Compared with previous generations of GCs, MPA and MF and (b) mometasone furoate. exhibit marked improvement with regards to lipophilicity, local and systemic side effect profile and TIX score. Lipo- of inflammation (20). In contrast, MF’s potent anti-inflam- philicity has increased as a function of esterification, one- matory activity can be partly attributed to the chlorine fold in MF and twofold in MPA (19). Both compounds moiety present at the C-21 position, which inhibits esterase present an increased TIX value as a function of decreased activity leading to high compound retention at the applica- side effect profiles coupled with potent anti-inflammatory tion site (17,21). activity. Major systemic side effects, such as hypothalamic- As the MPA metabolite (MPP) passes through the skin pituitary-adrenal (HPA) axis suppression and decreased and enters the blood, glucuronic acid rapidly inactivates serum cortisol levels, have also been minimized (19). How- MPP by conjugation followed by excretion mainly through ever, the fundamental structural differences between MPA urine, which explains the low systemic activity of MPA (22). and MF offer the opportunity for further differentiation. Although MF does not cause marked systemic side effects, Highly lipophilic agents, such as MPA and MF, generally only 0.00076% of the total administered dose is excreted in do not attain high serum concentrations, thus reducing the urine as the metabolite, 6b-hydroxy mometasone (23). Fur- potential for systemic side effects (20). MPA shows a thermore, Sahasranaman et al. (24) reported that orally marked improvement in lipophilicity because of its twofold inhaled and intravenously administered MF might produce esterification compared with the onefold esterification in higher systemic exposure than originally anticipated because MF. Consequently, MPA shows increased penetration into of the presence of active metabolites generated from distinct the skin and exhibits high local anti-inflammatory activity. extrahepatic metabolism, which may be partly responsible Once in the skin, esterases hydrolyse MPA forming for MF’s systemic side effects (24). 6a-methylprednisolone-17-propionate (MPP), a more Indeed, MPA and MF are appreciably better topical GCs potent corticoid than MPA. Bioactivation of MPA is accel- than many predecessors; however, MPA seems to display erated in inflamed skin relative to normal skin because of an even better local side effect profile than MF, one of the higher levels of esterases found in inflamed skin, leading to most important parameters being skin atrophy. Kecskes a further increase in active MPP concentration at the site et al. (19) reported that MPA causes significantly less ª 2007 The Authors 754 Journal compilation ª 2007 Blackwell Munksgaard, Experimental Dermatology, 16, 753–761 Therapeutic index of topical GCs atrophy and significantly less severe telangiectasias than oestrogen-sensitive promoter reporter gene construct (pvit- MF. This article provides additional data supporting this tk-luciferase); oestradiol and fulvestrant were used as agon- claim by examining skin atrophy, breaking strength and ist and antagonist reference compounds respectively. Pro- telangiectasias as a result of MPA and MF administration gestenic activity
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