Dutasteride in Androgenetic Alopecia: An Update

Arif, Tasleem; Dorjay, Konchok; Adil, Mohammad; Sami, Marwa

doi:10.2174/1574884712666170310111125

Cited by 53 publications

(45 citation statements)

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“…Although hepatic metabolism mediated by CYP3A4 and CYP3A5 is well recognized as a major elimination pathway of DUT in humans [6,7], little information has been available as to the hepatic CYPs involved in the metabolism of DUT in rats. The in vitro microsomal metabolism data presented in this study revealed that the metabolism of DUT was markedly reduced by KET, a potent inhibitor of CYP3A in rats and humans ( Figures 6B and 7B) [26,27].…”

Section: Discussionmentioning

confidence: 99%

“…DUT, a dual inhibitor of type-1 and type-2 5AR, was approved by the US Food and Drug Administration (FDA) in 2001 for the treatment of symptomatic benign prostatic hyperplasia [6]. Further, it was approved for androgenic alopecia in Korea and Japan [7]. Previous in vitro studies have shown that compared to finasteride, DUT more potently inhibited type-1 and type-2 5AR by 45-and 2.5-fold, respectively [8,9].…”

Section: Introductionmentioning

confidence: 99%

“…Among three major and two minor metabolites, 6β-hydroxydutasteride (H-DUT; Figure 1) exerts 5AR inhibition activity similar to that of DUT [6]. Only trace amounts of unchanged DUT are excreted in the urine [7]. The terminal half-life of DUT after reaching a steady state is approximately 5 weeks [6].…”

Section: Introductionmentioning

confidence: 99%

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In Vitro and In Vivo Assessment of Metabolic Drug Interaction Potential of Dutasteride with Ketoconazole

et al. 2019

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Dutasteride (DUT) is a selective, potent, competitive, and irreversible inhibitor of both type-1 and type-2 5α-reductase (5AR) commonly used in the treatment of benign prostatic hyperplasia and androgenetic alopecia. In the present study, we developed a simple and sensitive high-performance liquid chromatography with fluorescence detection (HPLC-FL) method for simultaneous determination of DUT and its major active metabolite, 6β-hydroxydutasteride (H-DUT). Next, the pharmacokinetic interactions of DUT with ketoconazole (KET), a potent CYP3A inhibitor, were comprehensively investigated. In vivo rat intravenous and oral studies revealed that the pharmacokinetics of DUT and H-DUT were significantly altered by the co-administration of KET. Furthermore, the in vitro microsomal metabolism, blood distribution, and protein-binding studies suggest that the altered pharmacokinetics of DUT could be attributed primarily to the inhibition of the DUT metabolism by KET. To the best of our knowledge, this is the first study to show the drug interaction potential of DUT with azole antifungal drugs including KET, together with a newly developed HPLC-FL method for the simultaneous quantification of DUT and H-DUT.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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In Vitro and In Vivo Assessment of Metabolic Drug Interaction Potential of Dutasteride with Ketoconazole

et al. 2019

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“…Accordingly, administration of finasteride and dutasteride for androgenic alopecia might be viewed in two very different ways. Taking into account only its therapeutic efficiency for AGA, several authors have demonstrated that dutasteride (a stronger inhibitor/ more potent antiandrogen than finasteride) produces superior results in ameliorating androgenic alopecia than finasteride, such that it should be preferred in clinical practice for AGA (11).…”

Section: Discussionmentioning

confidence: 99%

Androgenic alopecia; the risk–benefit ratio of Finasteride

Rowland¹,

Motofei²,

Păunica³

et al. 2018

JMMS

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Finasteride is currently approved and largely used as a therapeutic option for androgenetic alopecia. Apparently a safe drug and effective at the onset of its application, several concerns have since appeared over the years regarding the frequency and magnitude of finasteride adverse effects, which in some cases appear irreversible even after drug termination. This paper discusses the use of finasteride for androgenic alopecia from two distinct perspectives. On the one hand, androgenic alopecia is a condition that especially affects a person's self-image and esteem, aspects that are subjectively-constructed and thus relative and changeable.On the other hand, this condition involves a multifactorial etiology, with androgens being only partly responsible. Because androgens have important and unique physiological roles within the body, any procedure that results in androgenic suppression should be advised with caution.Furthermore, adverse effects induced by finasteride are neither fully documented nor easily treated. Finally, as alternative therapeutic approaches (such as topical finasteride) become available, the oral administration of finasteride for androgenic alopecia should, in our opinion, be reevaluated. Due to such concerns, a detailed and informed discussion should take place with patients considering therapy with finasteride for androgenic alopecia. Keywords androgenic alopecia, the risk-benefit ratio, finasteride, adverse effects, post-finasteride syndrome Highlights ✓ Finasteride administration places the subjects with androgenic alopecia into an abnormal state, characterized by a low level of DHT ✓ Finasteride adverse effects persist in some men indefinitely after treatment cessation, the corresponding medical support being non-specific, namely symptomatic

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“…While hair loss is a problem for many people, effective therapeutic agents for this condition are quite limited (1,2). Intensive efforts toward developing therapeutic chemical compounds have been made by analyzing the mechanisms underlying hair follicle development, regeneration, and induction of the telogen-to-anagen transition in mouse models (3,4).…”

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confidence: 99%

Generation of iPS-Derived Model Cells for Analyses of Hair Shaft Differentiation

et al. 2017

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Biological evaluation of hair growth/differentiation activity in vitro has been a formidable challenge, primarily due to the lack of relevant model cell systems. To solve this problem, we generated a stable model cell line in which successive differentiation via epidermal progenitors to hair components is easily inducible and traceable. Mouse induced pluripotent stem (iPS) cell-derived cells were selected to stably express a tetracycline (Tet)-inducible bone morphogenic protein-4 (BMP4) expression cassette and a luciferase reporter driven by a hair-specific keratin 31 gene (krt31) promoter (Tet-BMP4-KRT31-Luc iPS). While Tet- BMP4-KRT31-Luc iPS cells could be maintained as stable iPS cells, the cells differentiated to produce luciferase luminescence in the presence of all-trans retinoic acid (RA) and doxycycline (Dox), and addition of a hair differentiation factor significantly increased luciferase fluorescence. Thus, this cell line may provide a reliable cell-based screening system to evaluate drug candidates for hair differentiation activity.

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Dutasteride in Androgenetic Alopecia: An Update

Cited by 53 publications

References 0 publications

In Vitro and In Vivo Assessment of Metabolic Drug Interaction Potential of Dutasteride with Ketoconazole

In Vitro and In Vivo Assessment of Metabolic Drug Interaction Potential of Dutasteride with Ketoconazole

Androgenic alopecia; the risk–benefit ratio of Finasteride

Generation of iPS-Derived Model Cells for Analyses of Hair Shaft Differentiation

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