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.