N-(2-hydroxyphenyl)-2-propylpentanamide (HO-AAVPA) is a novel valproic acid derivative that has shown anti-proliferative activity against epitheloid cervix carcinoma (HeLa), rhabdomyosarcoma (A204), and several breast cancer cell lines. The aim of this research was to evaluate the pharmacokinetic profile and tissue distribution of HO-AAVPA in Wistar rats, as well as its human serum albumin binding potential by experimental and in silico methods. A single dose of HO-AAVPA was given to male rats by intravenous, intragastric or intraperitoneal routes at doses of 25, 100, and 100 mg/kg, respectively. Then, blood samples were drawn at predetermined intervals of time, and the HO-AAVPA concentration in the plasma was quantified with a validated HPLC method. The elimination half-life (t_1/2) was approximately 222 min, and the systemic clearance (CL) and apparent volume of distribution (Vd) were 2.20 mL/min/kg and 0.70 L/kg, respectively. The absolute oral bioavailability of HO-AAVPA was 33.8%, and the binding rate of HO-AAVPA with rat plasma proteins was between 66.2% and 83.0%. Additionally, in silico, UV and Raman spectroscopy data showed weak interactions between the test compound and human serum albumin. Thus, the results that were obtained demonstrated that despite its low oral bioavailability, the potential anticancer agent HO-AAVPA exhibits acceptable pharmacokinetic properties that would allow it to reach its site of action and exert its pharmacological effect in Wistar Rats, and it has a convenient profile for future assays to evaluate its human applications.

N-（2-羟苯基）-2-丙基戊酰胺（HO-AAVPA）是一种新型丙戊酸衍生物，已显示出对上皮子宫颈癌（HeLa），横纹肌肉瘤（A204）和几种乳腺癌细胞系的抗增殖活性。这项研究的目的是通过实验和计算机模拟方法评估HO-AAVPA在Wistar大鼠中的药代动力学特征和组织分布，以及其与人血清白蛋白的结合潜力。通过静脉内，胃内或腹膜内途径分别给雄性大鼠单剂量HO-AAVPA，剂量分别为25、100和100 mg / kg。然后，以预定的时间间隔抽取血样，并使用经过验证的HPLC方法对血浆中的HO-AAVPA浓度进行定量。消除半衰期（t _1/2）约为222分钟，全身清除率（CL）和表观分布体积（Vd）分别为2.20 mL / min / kg和0.70 L / kg。HO-AAVPA的绝对口服生物利用度为33.8％，HO-AAVPA与大鼠血浆蛋白的结合率为66.2％至83.0％。另外，计算机，紫外和拉曼光谱数据表明受试化合物与人血清白蛋白之间的相互作用较弱。因此，获得的结果表明，尽管口服生物利用度低，潜在的抗癌药HO-AAVPA仍显示出可接受的药代动力学特性，使其能够在Wistar大鼠中发挥作用并发挥药理作用，并且具有便利性。以便将来用于评估其人类应用的检测方法。