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摘要
前列腺癌 (PC) 被称为世界上男性中最常见的癌症。雄激素剥夺疗法(ADT)是PC治疗的初始治疗方法之一,各种药物可用于PC治疗的常规激素治疗。尽管如此,PC 细胞可以通过不同的机制存活并继续生长,这导致它们对常见的治疗方法(即恩杂鲁胺)产生抗性。 olutamide (ODM-201) 是第二代雄激素受体 (AR) 抑制剂,具有新的化学结构,对 AR 具有高亲和力。 Darolutamide 不会穿过血脑屏障,因此降低了癫痫发作的可能性。 Darolutamide 还可以抑制几种对 Enzalutamide 耐药的 AR 突变变体(F877L、F877L/T878A 和 H875Y/T878A)的转录活性。在这篇综述中,我们回顾了不同研究的结果:体外、动物模型和 1、2 和 3 期临床试验(ARADES、ARAFOR 和 ARAMIS)。我们将讨论正在进行的全球 2 和 3 期临床试验(ARASENS 和 ODENZA),以证明 Darolutamide 在不同患者组中的优势。 Darolutamide 在抑制 MR49F(恩杂鲁胺抗性 PC 细胞)和 VCaP(去势抗性 PC 细胞)细胞系的生长和 AR 的转录活性方面显示出很高的潜力。与恩杂鲁胺相比,需要较少剂量的达鲁鲁胺。该药物具有显着的抗肿瘤活性,并且对动物模型中的血清睾酮水平没有影响。 Darolutamide 在不同的研究中证明了其安全性和有效性,并且几乎在所有患者中都具有良好的耐受性。
关键词: 前列腺癌,darolutamide,ODM-201,激素治疗,去势抵抗性前列腺癌,雄激素受体抑制剂,第二代雄激素受体抑制剂。
Current Molecular Medicine
Title:Darolutamide as a Second-Generation Androgen Receptor Inhibitor in the Treatment of Prostate Cancer
Volume: 21 Issue: 4
关键词: 前列腺癌,darolutamide,ODM-201,激素治疗,去势抵抗性前列腺癌,雄激素受体抑制剂,第二代雄激素受体抑制剂。
摘要:
Prostate cancer (PC) is known as the most frequent cancer among men in the world. Androgen Deprivation Therapy (ADT) is one of the initial treatment approaches in the PC therapy and various drugs can be used in routine Hormonal therapy for PC therapy. Nevertheless, PC cells can survive and continue their growth via different mechanisms which lead to their resistance to common treatments i.e., Enzalutamide. olutamide (ODM-201) is a second-generation androgen receptor (AR) inhibitor with a new chemical structure and has a high affinity to the AR. Darolutamide does not cross the blood-brain barrier and for this reason, reduces the possibility of seizures. Darolutamide can also inhibit the transcriptional activity of several AR mutant variants (F877L, F877L/T878A, and H875Y/T878A), which are Enzalutamide resistant. In this review, we reviewed the results of different studies: in vitro, animal model and phase 1, 2 and 3 clinical trials (ARADES, ARAFOR and ARAMIS). We shall discuss worldwide phase 2 and 3 clinical trials (ARASENS and ODENZA) that are in progress, in order to demonstrate the advantages of Darolutamide consumption in different groups of patients.
Darolutamide has shown high potential in inhibiting the growth of MR49F (Enzalutamide resistant PC cells) and VCaP (Castration-resistant PC cells) cell lines and transcriptional activities of AR. Fewer doses of Darolutamide are needed compared to Enzalutamide. The drug had significant anti-tumor activity and no effect on serum testosterone levels in animal models. Darolutamide demonstrates its safety and efficacy in different studies and was well tolerated nearly in all of the patients.
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Cite this article as:
Darolutamide as a Second-Generation Androgen Receptor Inhibitor in the Treatment of Prostate Cancer, Current Molecular Medicine 2021; 21 (4) . https://dx.doi.org/10.2174/1566524020666200903120344
DOI https://dx.doi.org/10.2174/1566524020666200903120344 |
Print ISSN 1566-5240 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5666 |
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