Finasteride is a selective type II 5α-reductase inhibitor with an IC₅₀ value of 4.2nM [1]. Finasteride lowers dihydrotestosterone (DHT) levels and is used to treat male pattern hair loss (androgenetic alopecia)[2]. Additionally, Finasteride can be used to treat female pattern hair loss in patients who have failed local minoxidil treatment [3]. Finasteride has been shown to significantly reduce prostate volume and improve urinary symptoms [4].
In vitro, treatment of human dermal papilla cells (DPCs) with Finasteride (10–100μM) for 5 days significantly increased cell aggregation behavior, upregulated the expression of stem cell transcription factors Nanog and Sox-2, and activated the protein kinase B (AKT), β-catenin, and integrin β-1 signaling pathways, thereby enhancing stem cell properties[5]. Treatment of human prostate cell lines RWPE-1, LNCaP, PC3, and DU145 with Finasteride (10μM and 50μM) for 72 hours significantly downregulated the activities of MMP2 and MMP9, while upregulating the expression of TIMP-2. Moreover, 50μM Finasteride significantly inhibited the invasive potential of all cell lines and also significantly inhibited the migration of RWPE-1 and LNCaP cells [6].
In vivo, Ldlr−/− mice treated orally with Finasteride (1000mg/kg) for 12 weeks showed significant reductions in total cholesterol and triglyceride levels, decreased atherosclerotic plaque area in the aortic arch and root, and reduced macrophage content and necrotic core area in the plaques [7]. In a protein-overload nephropathy chronic kidney disease (CKD) mouse model fed a high-fat diet (HFD), treatment with Finasteride (1.5mg/30g) via gavage for 2 weeks significantly lowered plasma trimethylamine N-oxide (TMAO) levels, improved renal injury, and regulated the composition and distribution of gut microbiota[8].
References:
[1] Flores E, Bratoeff E, Cabeza M, et al. Steroid 5alpha-reductase inhibitors. Mini Rev Med Chem. 2003 May;3(3):225-37.
[2] Piraccini BM, Blume-Peytavi U, Scarci F, et al. Topical Finasteride Study Group. Efficacy and safety of topical finasteride spray solution for male androgenetic alopecia: a phase III, randomized, controlled clinical trial. J Eur Acad Dermatol Venereol. 2022 Feb;36(2):286-294.
[3] Stout SM, Stumpf JL. Finasteride treatment of hair loss in women. Ann Pharmacother. 2010 Jun;44(6):1090-7.
[4] Tacklind J, Fink HA, Macdonald R, et al. Finasteride for benign prostatic hyperplasia. Cochrane Database Syst Rev. 2010 Oct 6;2010(10):CD006015.
[5] Rattanachitthawat N, Pinkhien T, Opanasopit P, et al. Finasteride Enhances Stem Cell Signals of Human Dermal Papilla Cells. In Vivo. 2019 Jul-Aug;33(4):1209-1220.
[6] Moroz A, Delella FK, Almeida R, et al. Felisbino SL. Finasteride inhibits human prostate cancer cell invasion through MMP2 and MMP9 downregulation. PLoS One. 2013 Dec 30;8(12):e84757.
[7] McQueen P, Molina D, Pinos I, et al. Finasteride delays atherosclerosis progression in mice and is associated with a reduction in plasma cholesterol in men. J Lipid Res. 2024 Mar;65(3):100507.
[8] Wang Z, You L, Ren Y, et al. Finasteride Alleviates High Fat Associated Protein-Overload Nephropathy by Inhibiting Trimethylamine N-Oxide Synthesis and Regulating Gut Microbiota. Front Physiol. 2022 Aug 15;13:900961.
Finasteride是一种选择性II型5α还原酶抑制剂，其IC₅₀值为4.2nM[1]，Finasteride能够降低双氢睾酮（DHT）水平，用于治疗男性型脱发（雄激素性脱发）[2]。此外，Finasteride可用于治疗局部米诺地尔治疗失败的患者的女性型脱发[3]。Finasteride被证实可以显著缩小前列腺体积、改善排尿症状[4]。
在体外，Finasteride（10–100μM）处理人毛乳头细胞（DPCs）5天，显著增加细胞聚集行为，同时上调干细胞转录因子Nanog和Sox-2的表达，激活蛋白激酶B（AKT）、β-catenin和整合素β-1信号通路，增强干细胞特性[5]。Finasteride（10μM和50μM）处理人前列腺细胞系RWPE-1、LNCaP、PC3和DU145 72小时，显著下调MMP2和MMP9的活性，同时上调TIMP-2的表达。此外，50μM Finasteride显著抑制所有细胞系的侵袭能力，且对RWPE-1和LNCaP细胞的迁移能力也有显著抑制作用[6]。
在体内，Finasteride（1000mg/kg）口服处理的Ldlr−/−小鼠在12周后，Finasteride显著降低了总胆固醇和甘油三酯水平，减少了主动脉弓和主动脉根部的动脉粥样硬化斑块面积，并减少了斑块中的巨噬细胞含量和坏死核心面积[7]。Finasteride（1.5mg/30g）灌胃处理高脂饮食（HFD）喂养的蛋白超负荷肾病（CKD）模型小鼠2周，Finasteride显著降低了血浆中三甲胺N-氧化物（TMAO）水平，改善了肾脏损伤，并调节了肠道菌群的组成和分布[8]。