The use of quinacrine (Atabrine) in rheumatic diseases: A reexamination
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Cited by (132)
New insights into self-structure induction in poly (rA) by Quinacrine through non-classical intercalation: Spectroscopic and theoretical perspectives
2023, International Journal of Biological MacromoleculesAssessment of proarrhythmogenic risk for chloroquine and hydroxychloroquine using the CiPA concept
2021, European Journal of PharmacologyCitation Excerpt :Chloroquine was synthesized in 1934 by Johann (Hans) Andersag at Bayer A.G. by replacing the acridine with a quinoline ring in quinacrine (Atabrine) and was used under the name Resochin; in 1945 it was rediscovered by E.K. Marshall and received its current name (Krafts et al., 2012), remaining for decades a first-line antimalarial therapy. The mechanisms of action of quinoline antimalarials in autoimmune diseases are complex (Chew et al., 2020; Haładyj et al., 2018; Wallace, 1989). The antiviral activity of chloroquine and hydroxychloroquine is deemed to result from accumulation of the protonated charged form in the acidic environment of endosomes, lysosomes and Golgi vesicles, leading to increased internal endosomal pH, thus preventing their use by viral particles as entry gateways (Ducharme and Farinotti, 1996).
Hydroxychloroquine: Pharmacological, physicochemical aspects and activity enhancement through experimental formulations
2021, Journal of Drug Delivery Science and TechnologyFirst-in-Human Phase 1b Trial of Quinacrine Plus Capecitabine in Patients With Refractory Metastatic Colorectal Cancer
2021, Clinical Colorectal CancerCitation Excerpt :Acridine is a compound first isolated from coal tar, and its analogs, such as CP-31398, have been shown to restore p53 functioning.10 Quinacrine is an acridine derivative that was developed over 90 years ago as an antimalarial drug and has since been used to treat many rheumatic and infectious diseases.11 We found that quinacrine induces p53 pathway-dependent transcription in p53-deficient cells, leading to apoptosis in tumor xenografts.12
Repurposing quinacrine for treatment-refractory cancer
2021, Seminars in Cancer BiologyConnective Tissue Disease: Current Concepts
2019, Dermatologic ClinicsCitation Excerpt :Quinacrine has the advantage of not being associated with retinal toxicity, unlike HCQ and CQ. Studies have also suggested quinacrine may be a stronger antiinflammatory agent than HCQ or CQ, and recently it was shown to more effectively suppress both tumor necrosis factor-α and IFN-α in peripheral blood mononuclear cells from patients with DM and CLE.32,33 Importantly, multiple studies have been performed recently that can potentially be translated into safer and more effective use of antimalarials for CLE in everyday clinical practice.
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From the Division of Rheumatology, Department of Medicine, Cedars-Sinai Medical Center, UCLA School of Medicine, Los Angeles.