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| Macrolide | Advantages | Drawbacks |
|
| Pimecrolimus | (i) Plays an important role in the anti-inflammatory activities.
(ii) Applied for the treatment of atopic dermatitis (AD) [4, 9, 10].
(iii) Inhibits the synthesis of inflammatory cytokines in psoriasis [13, 14].
(iv) Produces a dose-dependent reduction in the severity of psoriasis [15].
(v) Significantly reduces the symptoms in oral lichen planus (OLP) [16, 17].
(vi) Applied for the treatment of rosacea [23].
(vii) Shows positive clinical results in pyoderma gangrenosum (PG) [27].
(viii) Acts more selectively on T cells and mast cells in lupus dermatosis and thus has a lower possibility of systemic immunosuppression [28, 29].
(ix) Is safe and efficient for the treatment of Behçet’s disease genital ulcers, by accelerating the healing process [31]. | (i) Tacrolimus is used more often for vitiligo [19, 20, 46].
(ii) Failure in treatment of chronic autoimmune urticaria [22].
(iii) Topical 1% is not a therapeutic option in alopecia areata (AA), especially for patients unresponsive to other treatments [24].
(iv) In PG, the pharmacologic activity is more selective than tacrolimus, and the rate of cutaneous permeation is 9 times lower than that of tacrolimus and, therefore, has a lower risk of systemic immune suppression [27]. |
|
| Tacrolimus | (i) Oral formulation offers an additional therapeutic option for management of severe and extensive AD [36].
(ii) Topical formulation is a highly effective treatment for psoriasis of the face and flexures [39] and is proposed as an alternative treatment for inflammatory skin diseases in thin skin areas, as well as, pruritus ani [42]. In addition, it is effective in PG [51–53] and in cutaneous T cell lymphomas [60].
(iii) Topical formulation (0.1%) has been used for the management of OLP and may be effective and well tolerated in the treatment of anogenital lichen sclerosus [41].
(iv) Treatment of contact dermatitis is often palliative and directed against the cutaneous inflammation itself.
(v) It has been shown to reduce the incidence of lupus dermatosis in the autoimmune-prone MRL/Mp-lpr/lpr (MRL/lpr) mouse.
(vi) Better results in AA treatment are achieved in combination with intralesional steroids [50].
(vii) It can be considered both effective and safe for treating skin dermatosis in systemic lupus erythematosus (LE) patients [56]. | (i) For severe active LE, its efficacy is considered limited at current dose settings and usage [55, 56].
(ii) There are contradictory results of tacrolimus as an inducer of skin cancer. |
|
| Sirolimus (rapamycin) | (i) A clinical trial has shown that macrolides, in a suitable formulation, can penetrate the human skin and exert beneficial effects for the treatment of psoriasis [75, 85]. | (i) Contact sensitization to rapamycin could be developed [85]. |
|
| Everolimus | (i) Potent immunosuppressive effects, antiproliferative properties, and anticancer effects have been observed.
(ii) Effective in psoriasis treatment [87]. | (i) It was ineffective in combination with prednisone or cyclosporine A in 2 patients with severe AD [88]. |
|
| Temsirolimus | (i) Potent immunosuppressive effects, antiproliferative properties, and anticancer effects. | (i) Applications for different types of dermatitis are not yet known. |
|
| CSY0073 | (i) Anti-inflammatory and immunomodulatory effects have been observed [93]. | (i) Applications for different types of dermatitis are not yet known. |
|
EM900
EM911 | (i) Anti-inflammatory and immunomodulatory characteristics observed. | (i) Applications for different types of dermatitis are not yet known. |
|
| Ridaforolimus | (i) One of the first possible applications as an antitumor agent. | (i) Applications for different types of dermatitis are not yet known. |
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