1. Darolutamide is a novel selective androgen receptor antagonist consisting of two pharmacologically equipotent diastereoisomers. The absorption, distribution, metabolism and excretion properties of darolutamide in rats are reported.

2. Non- or [¹⁴C]-labelled darolutamide, its diastereoisomers and major metabolite were studied in intact and bile duct-cannulated rats (oral and intravenous administration), and rat hepatocytes.

3. Darolutamide was quickly (1 h to reach maximum plasma concentration) and completely absorbed after oral administration. Absolute bioavailability was high. Keto-darolutamide was the most abundant metabolite in rat hepatocytes and the only major one in plasma. Interconversion between diastereoisomers was observed.

4. After oral administration, radioactivity distributed widely and homogeneously. Penetration into brain was low (brain/blood ratio = 0.079). Elimination was rapid from most tissues. Excretion occurred rapidly, and routes were similar irrespective of administration routes. Complete mass balance was reached by 168 h post-dose. Most radioactivity (61–64%) was excreted in faeces, while relevant amounts (30–33%) were also excreted into urine. The main clearance routes were metabolism via oxidative reactions and glucuronidation. After intravenous administration, a relevant extent of the dose (20%) underwent extrabiliary excretion as darolutamide.

达洛鲁胺是一种新型的选择性雄激素受体拮抗剂，由两种药理学上等效的非对映异构体组成。报道了他鲁鲁胺在大鼠中的吸收，分布，代谢和排泄特性。

2.在完整和经胆管插管的大鼠（口服和静脉内给药）以及大鼠肝细胞中研究了非或[ ¹⁴ C]标记的达鲁鲁胺，其非对映异构体和主要代谢产物。

3.达洛鲁胺迅速（1 h达到最大血浆浓度）并在口服后完全吸收。绝对生物利用度高。酮-darolutamide是大鼠肝细胞中最丰富的代谢产物，也是血浆中唯一的主要代谢产物。观察到非对映异构体之间的相互转化。

4.口服后，放射性分布广泛且均匀。渗透入脑的几率很低（脑/血比= 0.079）。多数组织的清除很快。排泄迅速发生，并且无论施用途径如何，途径都相似。给药后168小时达到完全的质量平衡。大部分放射性（61–64％）通过粪便排泄，而相关量（30–33％）也通过尿液排泄。主要清除途径是通过氧化反应和葡萄糖醛酸化作用进行的代谢。静脉内给药后，一定剂量的剂量（20％）作为达洛鲁胺进行了胆汁外排泄。