THERAPEUTICAL NOTES   

Giornale Italiano di Dermatologia e Venereologia 2003 February;138(1):49-56

Copyright © 2003 EDIZIONI MINERVA MEDICA

language: Italian

Adapalene. Pharmacological and therapeutic features

Cassano N. ¹, Alessandrini G. ², Carrieri G. ³, Fai D. ⁴, Gabbellone M. ⁵, Gravante M. ⁶, Ligori P. ⁷, Mancino A. ⁸, Manco S. ⁹, Martina G. ¹⁰, Natalizi A. ¹¹, Sodo M. R. ¹², Stasi R. ¹³, Vena G. A. ¹⁴

¹ Istituto Dermopatico dell’Immacolata, I.D.I., I.R.C.C.S. Roma, 2 Taviano (LE), 3 Castellana Grotte (BA), 4 Parabita (LE), 5 Tricase (LE), 6 Poggiardo (LE), 7 Gallipoli (LE), 8 Nardò (LE), 9 Maglie (LE), 10 Nardò (LE), 11 Galatina (LE) 12 Galatina (LE), 13 Lecce, 14 Dipartimento di Clinica Medica Immunologia e Malattie Infettive, Unità di Dermatologia Università degli Studi di Bari, Bari

Several data indicate the particular pharmacological profile of adapalene, a synthetic arotinoid molecule which exerts a potent retinoid activity with a selective binding to RAR-b and -g receptors. Pharmacokinetic aspects of adapalene 0.1% gel are primarily related to the chemical structure, which is lipophilic and characterised by a notable stability and a high melting point, and also to the peculiar formulation containing microcrystals with 3 to 10 mm-diameter, which are selectively delivered into the pilosebaceous units. The mechanism of action of adapalene includes relevant effects on cellular differentiation and proliferation along with remarkable antiinflammatory effects. All these aspects represent the rational bases for the efficacy and tolerability of adapalene in the treatment of mild to moderate acne vulgaris. Controlled randomized trials have highlighted the clinical differences existing between adapalene 0.1% gel, tretinoin 0.025% gel and tretinoin 0.05% cream. In fact, most of these trials have showed that adapalene is at least as effective as tretinoin, possibly acting more rapidly, and is superior with respect to tolerability and patient’s preference. The rapid onset of action of adapalene can result also in a faster recovery of quality of life, whereas the good tolerability guarantees a better compliance to treatment. Moreover, the irritation potential of adapalene is very low, even if it is applied immediately after washing or used in combination with other anti-acne topical agents. The most important pharmacological and therapeutical aspects of adapalene are examined.