Mepacrine in Recalcitrant Cutaneous Lupus Erythematosus: Old-fashioned or Still Useful?

Abstract

Treatment of recalcitrant cutaneous lupus erythematosus (CLE) is challenging. In situations where conventional treatment approaches fail mepacrine - an antimalarial/antiinflammatory drug that has fallen into oblivion in the last decades - might still be a promising option. We retrospectively analysed medical records of 10 patients with refractory CLE that were treated with mepacrine (100-200 mg/day) as mono- or combination therapy for various time intervals between 2001 and 2013 at the University Hospital Würzburg. Mepacrine was generally well tolerated. Side effects were mild and usually resolved after reduction or cessation. Over 50% of the patients experienced amelioration of their symptoms despite a previously recalcitrant clinical course. Altogether, our data demonstrate that mepacrine still remains a useful and effective therapeutic option for other-wise treatment-resistant CLE.

Development of a synthetic route towards N4,N9-disubstituted 4,9-diaminoacridines: On the way to multi-stage antimalarials

“…Mepacrine's role as a first-line antimalarial was ephemeral, as it was soon superseded by chloroquine, a much safer, cheaper and effective antimalarial. Still, it has been rapidly repurposed for other conditions, finding applications as anti-helminthic [5], anti-rheumatic [6], anti-lupus [7], anti-cancer [8], anti-inflammatory [9], and female-sterilizing [10] agent. Its potential to treat Creutzfeld-Jakob disease was also investigated [11].…”

Antimalarial drug toxicities in patients with cutaneous lupus and dermatomyositis: A retrospective cohort study

“…This drug has synergistic efficacy when given as part of an antimalarial combination and has demonstrated therapeutic promise for recalcitrant disease. 3,4 Emerging evidence suggests that this effect may be because quinacrine has a distinct mechanism compared to its counterparts involving the downregulation of TLR-3, -4 and -8 responses. 5,6 Quinacrine has been compounded since the early 1990’s when production was discontinued by Sanofi-Winthrop.…”

Quinacrine Suppresses Tumor Necrosis Factor-α and IFN-α in Dermatomyositis and Cutaneous Lupus Erythematosus

“…Although approximately 50% of CLE patients respond to HCQ, potentially two thirds of the remaining patients respond when QC therapy is added (Chang et al, 2011). However, QC is now available only as a compounded medication, making understanding potential distinguishing features of its mechanism of action imperative, particularly because there is risk of losing access to this medication (Benoit and Goebeler, 2015). African Americans frequently have generalized discoid lupus erythematosus, a form of CLE that is more refractory to therapy (Bonilla-Martinez et al, 2008; Moghadam-Kia et al, 2009).…”