Acitretin

Abstract

Acitretin, a synthetic retinoid, is the pharmacologically active metabolite of etretinate. It is currently approved by the US Food and Drug Administration for the treatment of severe psoriasis in adults and has been established as a second-line therapy for the treatment of psoriasis resistant to the use of topical therapy. It is also an option for generalized pustular psoriasis, palmoplantar pustulosis, exfoliative erythrodermic psoriasis, and severe psoriasis in the setting of acitretin. It also has been shown to have chemo-preventative characteristics. Acitretin is limited by its teratogenicity and therefore considered inappropriate in most female patients of childbearing age. Common side effects include mucocutaneous dryness and elevated triglycerides.

Getting the “Kill” into “Shock and Kill”: Strategies to Eliminate Latent HIV

“…Acitretin, an FDA-approved retinoic acid derivative used to treat psoriasis (Ortiz et al, 2013), was recently shown to reactivate latent HIV and induce the selective apoptosis of HIV latently infected cells in vitro (Li et al, 2016). In the study by Li et al, acitretin induced HIV expression in latently infected T-cell lines and preferential death of HIV infected cells compared to uninfected samples.…”

Regulation of Alpha-Secretase ADAM10 In vitro and In vivo: Genetic, Epigenetic, and Protein-Based Mechanisms

“…Both, RAR alpha and beta are capable of inducing human ADAM10 promoter activity (Tippmann et al, 2009). Moreover, the commercially available drug acitretin which intracellularly liberates retinoic acid (Ortiz et al, 2013), shifts APP processing in AD model mice toward the alpha-secretase cleavage pathway (Tippmann et al, 2009). The neuroprotective property of RARalpha agonists has been shown in cortical cultures, an AD mouse model (Tg2576 mice) (Jarvis et al, 2010), as well as in hippocampal tissue of aged SAMP8 mice (Kitaoka et al, 2013).…”

Synthesis and Some Biological Properties of Pyrrolo[1,2‐a]indoles

“…A new analog 194 of the antipsoriatic drug Acitretin was used as a starting compound in the synthesis of pyrrolo[1,2‐ a ]indole 195 . Its cyclization under the action of trifluoroacetic acid leads to pyrrolo[1,2‐ a ]indol‐3‐one 195 (Scheme ).…”