Acitretin in Dermatology: A Review
July 2011 | Volume 10 | Issue 7 | Original Article | 772 | Copyright © July 2011
Introduction: Acitretin is a systemic retinoid drug used in the treatment of severe psoriasis. It has also been used for a spectrum of
other difficult-to-treat dermatoses, including hyperkeratotic and inflammatory dermatoses and non-melanoma skin cancers. Here we
review the available data regarding both FDA-approved and off-label uses of acitretin, clinically relevant adverse events, precautions
Methods: A PubMed literature search was conducted utilizing the search term "acitretin," which yielded 714 hits. Results were further
limited to English language clinical trials in human subjects. Of 78 articles evaluated for relevance, 60 were included for review.
Results: Acitretin is effective as monotherapy and in multidrug therapeutic regimens for the treatment of psoriasis and other hyperkeratotic
and inflammatory disorders, as well as for malignancy chemoprevention. Its use is limited by its teratogenic potential and
other adverse effects, including mucocutaneous effects and hepatotoxicity. Potential adverse effects may be reduced or avoided by
using lower doses of acitretin or in combination with other therapies.
Limitations: The reviewed studies include many small trials and case reports of the use of acitretin for psoriasis. Studies of acitretin therapy for
the treatment of other cutaneous disorders are limited.
Conclusion: Acitretin is a beneficial treatment for psoriasis, and should be considered when not contraindicated. Particularly when
used in combination with ultraviolet (UV) phototherapy, is a safe and cost effective therapeutic strategy.
J Drugs Dermatol.2011;10(7):772-782.
Acitretin is a second-generation aromatic retinoid. It is
an active metabolite of the precursor drug, etretinate
(Tegison, Hoffmann-La Roche, Nutley, NJ), which was
widely used in the United States (U.S.) as a systemic psoriasis
therapy until 1998 when it was withdrawn from the market
and replaced by acitretin. Etretinate is 50 times more lipophilic
than acitretin and is sequestered in fatty tissues, leading to a
mean terminal half-life of 120 days.1-3 Compared to etretinate,
acitretin has a wider therapeutic index and improved pharmacokinetic
profile. It is relatively water-soluble and has a half-life
of 50 to 60 days. Etretinate and acitretin have nearly identical
therapeutic profiles, with similar levels of efficacy and toxicity.
Acitretin is effective for the treatment of psoriasis and a number
of other keratinizing disorders.4
Acitretin is approved by the U.S. Food and Drug Administration
(FDA) for the treatment of severe recalcitrant psoriasis. It is useful
as monotherapy and has increased efficacy when used in
combination with other topical and systemic therapies, as well
as with phototherapy. Acitretin has also been used off-label in
the treatment of severe keratinization disorders and other dermatoses,
but the data are limited.5,6 We reviewed the current literature including the safety and efficacy of acitretin in clinical
trials for the treatment of psoriasis and other disorders of keratinization,
inflammatory disorders and in the chemoprevention
We conducted a PubMed literature search for the term "acitretin"
which yielded 714 results. The results were further limited
to English language, clinical trials in human subjects. The 78
articles returned were evaluated for relevance and 60 were
included in this review (Figure 1). Here, we present clinical
efficacy data for acitretin as a therapy for psoriasis, other keratinization
and inflammatory disorders and the chemoprevention
of malignancy, as well as safety, tolerability, dosing and cost.
Acitretin is an orally administered therapy with variable absorption,
which increases with high-fat meals. It has a bioavailability
of approximately 60 percent, with 99 percent of the circulating