Bicalutamide is a non-steroidal antiandrogen that selectively and competitively blocks androgen binding to the androgen receptor (AR), exerting anti-androgenic effects in peripheral tissues[1-2]. Bicalutamide is used for the treatment of advanced prostate cancer[3].
In vitro, after VCaP cells were treated for 7 days with increasing concentrations of Bicalutamide (10-10-10-5mol/L), Bicalutamide dose-dependently promoted cell proliferation and partially antagonized the effect of the synthetic androgen R1881[4]. Treatment of mature dendritic cells (mDCs) with 20μM Bicalutamide for 24h induced a modest but significant up-regulation of CD86 and HLA-DR, down-regulated CD11c, and markedly reduced both transforming growth factor-β (TGF-β) and interleukin-10 (IL-10) protein levels[5].
In vivo, in male BALB/c mice, daily intraperitoneal injection of 0.02mg Bicalutamide in 0.5ml saline for 7 consecutive days significantly reduced eosinophil infiltration in the nasal mucosa, markedly lowered serum levels of IgE, IL-4, and IL-6, and substantially decreased the surface expression of histamine receptors on mast cells, while also markedly suppressing p-protein kinase B (p-PKB) and mTOR protein levels in these cells[6]. In knock-in spinal and bulbar muscular atrophy (SBMA) (KI AR113Q) mice given twice-weekly subcutaneous Bicalutamide (2mg/kg in 50µL corn oil), the drug reversed muscle AR insoluble aggregate formation, restored autophagic flux, and suppressed apoptosis, yielding partial recovery of muscle morphology and function, improved motor performance, and prolonged survival[7].
References:
[1] Carvalho RM, Santos LDN, Ramos PM, et al. Bicalutamide and the new perspectives for female pattern hair loss treatment: What dermatologists should know. J Cosmet Dermatol. 2022;21(10):4171-4175.
[2] Aulakh S, Mysore V. Bicalutamide: A review. J Cutan Aesthet Surg. 2025;18(2):78-85.
[3] Kolvenbag GJ, Blackledge GR. Worldwide activity and safety of bicalutamide: a summary review. Urology. 1996;47(1A Suppl):70-84.
[4] Clegg NJ, Wongvipat J, Joseph JD, et al. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012;72(6):1494-1503.
[5] Nourbakhsh NS, Naeimi S, Moghanibashi M, et al. Bicalutamide reveals immunomodulatory effects in prostate cancer by regulating immunogenic dendritic cell maturation. Tissue Cell. 2024;91:102530.
[6] Zhang Y, Zhang Q, Wu X, et al. Bicalutamide, an androgen receptor antagonist, effectively alleviate allergic rhinitis via suppression of PI3K-PKB activity. Eur Arch Otorhinolaryngol. 2023;280(2):703-711.
[7] Galbiati M, Meroni M, Boido M, et al. Bicalutamide and Trehalose Ameliorate Spinal and Bulbar Muscular Atrophy Pathology in Mice. Neurotherapeutics. 2023;20(2):524-545.
Bicalutamide是一种非甾体抗雄激素药物，可通过选择性和竞争性地阻断雄激素与雄激素受体（AR）的结合，在外周组织中发挥抗雄激素作用[1-2]。Bicalutamide用于治疗晚期前列腺癌[3]。
在体外，将VCaP细胞用递增浓度的Bicalutamide（10-10-10-5mol/L）处理7天后，Bicalutamide呈剂量依赖性促进细胞增殖，并可部分拮抗合成雄激素R1881的作用[4]。用20μM的Bicalutamide处理成熟树突状细胞（mDCs）24小时，可温和但显著地上调CD86和HLA-DR表达，下调CD11c，并显著降低转化生长因子-β（TGF-β）和白细胞介素-10（IL-10）蛋白水平[5]。
在体内，对雄性BALB/c小鼠每日腹腔注射0.02mg的Bicalutamide（溶于0.5ml生理盐水），连续7天，可显著减少鼻黏膜嗜酸性粒细胞浸润，显著降低血清IgE、IL-4和IL-6的水平，并显著抑制肥大细胞表面组胺受体的表达，同时显著下调肥大细胞内p-蛋白激酶B（p-PKB）和mTOR蛋白水平[6]。在敲入脊髓延髓肌萎缩症（SBMA）KI AR113Q小鼠中，每周两次皮下注射Bicalutamide（2mg/kg，溶于50µL玉米油），可逆转肌肉内AR不溶性聚集体形成、恢复自噬通量、抑制凋亡，从而部分恢复肌肉形态与功能，改善运动表现并延长生存期[7]。