细胞色素P450酶系药物研发：肝脏药物代谢调控与临床应用研究进展

doi:10.19586/j.2095-2341.2025.0126

生物技术进展 ›› 2026, Vol. 16 ›› Issue (2): 309-317.DOI: 10.19586/j.2095-2341.2025.0126

• 进展评述 • 上一篇

细胞色素P450酶系药物研发：肝脏药物代谢调控与临床应用研究进展

王育萌(), 赵鹏翔(), 张旭娟, 党政, 李函, 刘子怡, 王佳腾, 于思雪, 马雪梅()

北京工业大学化学与生命科学学院，北京 100124

收稿日期:2025-09-23 接受日期:2025-12-17 出版日期:2026-03-25 发布日期:2026-04-27
通讯作者: 赵鹏翔,马雪梅
作者简介:王育萌E-mail: wangyumeng@bjut.edu.cn
基金资助:
军民融合重点项目(BHJ17L01)

Cytochrome P450 Enzyme System in Drug Development: Advances in Research on Regulation of Hepatic Drug Metabolism and Clinical Applications

Yumeng WANG(), Pengxiang ZHAO(), Xujuan ZHANG, Zheng DANG, Han LI, Ziyi LIU, Jiateng WANG, Sixue YU, Xuemei MA()

School of Chemistry and Life Sciences，Beijing University of Technology，Beijing 100124，China

Received:2025-09-23 Accepted:2025-12-17 Online:2026-03-25 Published:2026-04-27
Contact: Pengxiang ZHAO,Xuemei MA

摘要/Abstract

摘要：

肝脏是人体代谢和解毒的核心器官，其功能维持依赖于复杂的酶系统网络，其中细胞色素P450（cytochrome P450，CYP450）酶系通过催化药物Ⅰ相代谢参与外源性物质的解毒或毒性转化，其活性调控对药物疗效及用药安全具有重要影响。CYP450在肝脏疾病、心血管、肿瘤等多种疾病的发生发展中具有重要的治疗和病理生理学意义，深入研究CYP450的功能及其在疾病中的变化，可为开发新的治疗策略提供重要依据。重点阐述了CYP450抑制剂和诱导剂在临床中的应用，总结了靶向调控CYP450对优化药物代谢提升疗效、降低不良反应及推动个体化用药的重要意义，以期为肝脏疾病精准治疗及拓展应用提供新方向。

关键词: 细胞色素P450酶系, 肝脏药物代谢, 疾病治疗, 靶向调控

Abstract:

The liver， as the central organ of human metabolism and detoxification， maintains its functional integrity through a complex network of enzyme systems. Within this network， the cytochrome P450 （CYP450） enzyme system assumes a pivotal role by catalyzing phase Ⅰ drug metabolism， thereby mediating the detoxification or toxic biotransformation of exogenous compounds. Modulation of CYP450 activity exerts a profound impact on drug efficacy and drug safety. This enzyme system also plays critical therapeutic and pathophysiological roles in the development and progression of diverse diseases， including liver disorders， cardiovascular diseases， and cancer. In-depth investigations into CYP450 functions and their disease-associated alterations provide a fundamental basis for developing novel therapeutic strategies. The article centered on elucidating the clinical applications of CYP450 inhibitors and inducers， while summarizing the critical significance of targeted CYP450 regulation in optimizing drug metabolism， enhancing therapeutic efficacy， reducing adverse reactions， and promoting personalized medicine， aiming to offer new avenues for precision treatment of liver diseases and expand their applications.

Key words: cytochrome P450, hepatic drug metabolism, disease treatment, targeted regulation

中图分类号:

Q593

王育萌, 赵鹏翔, 张旭娟, 党政, 李函, 刘子怡, 王佳腾, 于思雪, 马雪梅. 细胞色素P450酶系药物研发：肝脏药物代谢调控与临床应用研究进展[J]. 生物技术进展, 2026, 16(2): 309-317.

Yumeng WANG, Pengxiang ZHAO, Xujuan ZHANG, Zheng DANG, Han LI, Ziyi LIU, Jiateng WANG, Sixue YU, Xuemei MA. Cytochrome P450 Enzyme System in Drug Development: Advances in Research on Regulation of Hepatic Drug Metabolism and Clinical Applications[J]. Current Biotechnology, 2026, 16(2): 309-317.

图/表 5

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药物类型	药物名称	主要代谢酶	临床应用/风险提示	参考文献
精神类药物	奥氮平	CYP1A2、CYP2D6	测定患者白细胞中CYP1A2 mRNA 水平，以评估奥氮平药效	[15]
精神类药物	利培酮	CYP2D6	CYP2D6多态性显著影响利培酮的血浆浓度，导致不良反应	[16]
心血管药	辛伐他汀	CYP3A4、CYP2A6	避免CYP3A4的强抑制剂和他汀类药物共同给药导致的横纹肌溶解症	[17]
心血管药	氯吡格雷	CYP2C19	CYP2C19功能丧失会导致氯吡格雷激活受阻、血小板聚集减少较小以及治疗失败高风险	[18]
抗疟疾药	青蒿素	CYP2B6	青蒿甲醇提取物对CYP2B6在体外具有不可逆的抑制作用	[19]
抗凝药	华法林	CYP2C9	携带CYP2C9变异基因的患者需降低华法林剂量，防止出血风险显著增加；可通过基因检测预测最佳起始剂量	[20]
抗炎药	布洛芬	CYP2C9	代谢受CYP2C9多态性影响，可能增加胃肠道出血风险	[21]
抗炎药	双氯芬酸	CYP2C9	代谢受CYP2C9多态性影响，可能增加胃肠道出血风险	[21]
止痛解热药	对乙酰氨基酚	CYP2E1	降低CYP2E1活性可以减少对乙酰氨基酚代谢过程中有毒中间代谢物的产生	[22]
抗菌药	利福平	CYP3A4	可引起环孢菌素等免疫抑制药物治疗患者出现急性移植排斥反应	[23]
抗肿瘤药	紫杉醇	CYP3A4、CYP2C8	紫杉醇代谢的个体差异会导致毒性增加，需要药物检测合计个性化剂量以提高总体疗效	[24-25]
抗肿瘤药	他莫昔芬	CYP2D6	饮食标志物茄碱可作为体内表型标志物快速识别CYP2D6功能低下者，适用于基因检测结果未出或已用CYP2D6药物干扰情况	[26]

药物类型	药物名称	主要代谢酶	临床应用/风险提示	参考文献
精神类药物	奥氮平	CYP1A2、CYP2D6	测定患者白细胞中CYP1A2 mRNA 水平，以评估奥氮平药效	[15]
精神类药物	利培酮	CYP2D6	CYP2D6多态性显著影响利培酮的血浆浓度，导致不良反应	[16]
心血管药	辛伐他汀	CYP3A4、CYP2A6	避免CYP3A4的强抑制剂和他汀类药物共同给药导致的横纹肌溶解症	[17]
心血管药	氯吡格雷	CYP2C19	CYP2C19功能丧失会导致氯吡格雷激活受阻、血小板聚集减少较小以及治疗失败高风险	[18]
抗疟疾药	青蒿素	CYP2B6	青蒿甲醇提取物对CYP2B6在体外具有不可逆的抑制作用	[19]
抗凝药	华法林	CYP2C9	携带CYP2C9变异基因的患者需降低华法林剂量，防止出血风险显著增加；可通过基因检测预测最佳起始剂量	[20]
抗炎药	布洛芬	CYP2C9	代谢受CYP2C9多态性影响，可能增加胃肠道出血风险	[21]
抗炎药	双氯芬酸	CYP2C9	代谢受CYP2C9多态性影响，可能增加胃肠道出血风险	[21]
止痛解热药	对乙酰氨基酚	CYP2E1	降低CYP2E1活性可以减少对乙酰氨基酚代谢过程中有毒中间代谢物的产生	[22]
抗菌药	利福平	CYP3A4	可引起环孢菌素等免疫抑制药物治疗患者出现急性移植排斥反应	[23]
抗肿瘤药	紫杉醇	CYP3A4、CYP2C8	紫杉醇代谢的个体差异会导致毒性增加，需要药物检测合计个性化剂量以提高总体疗效	[24-25]
抗肿瘤药	他莫昔芬	CYP2D6	饮食标志物茄碱可作为体内表型标志物快速识别CYP2D6功能低下者，适用于基因检测结果未出或已用CYP2D6药物干扰情况	[26]

	名称	CYP450类型	临床效果	参考文献
抑制剂	酮康唑	CYP3A4	高选择性广谱抗真菌	[35]
	COR-500015	CYP17	调节皮质醇的产生	[36]
	氟康唑	CYP2C9	降低交感神经血管收缩	[37]
	新型异恶唑衍生物	CYP1A2	-	[38]
	类黄酮	CYP3A4	高剂量使用引发不良反应	[39]
	化合物9	CYP4Z1	有效抑制乳腺癌细胞	[40]
	黄精多糖	CYP2C9/2D6/3A4	草药共同给药时避免DDI	[41]
	光敏Ru（Ⅱ）配合物	CYP3A4	增强抗癌药物的治疗效果	[42]
	噻唑酰胺化合物B20	CYP1B1	靶向治疗克服紫杉醇耐药性	[43]
	胡椒碱	CYP2J2	抗肿瘤，降低线粒体功能障碍	[44]
	紫苏醇	CYP2A6/CYP2B6	-	[25]
诱导剂	聚乙二醇化脂质体	CYP3A	增强聚乙二醇抗肝细胞癌作用	[45]
	诃子	CYP1A2等	显著改善肝功能和组织病理学	[46]
	厄洛替尼	CYPA3	治疗晚期非小细胞肺癌	[47]
	黄芪注射液	CYP2D1	提高癌症疗效，降低耐药性	[48]

	名称	CYP450类型	临床效果	参考文献
抑制剂	酮康唑	CYP3A4	高选择性广谱抗真菌	[35]
	COR-500015	CYP17	调节皮质醇的产生	[36]
	氟康唑	CYP2C9	降低交感神经血管收缩	[37]
	新型异恶唑衍生物	CYP1A2	-	[38]
	类黄酮	CYP3A4	高剂量使用引发不良反应	[39]
	化合物9	CYP4Z1	有效抑制乳腺癌细胞	[40]
	黄精多糖	CYP2C9/2D6/3A4	草药共同给药时避免DDI	[41]
	光敏Ru（Ⅱ）配合物	CYP3A4	增强抗癌药物的治疗效果	[42]
	噻唑酰胺化合物B20	CYP1B1	靶向治疗克服紫杉醇耐药性	[43]
	胡椒碱	CYP2J2	抗肿瘤，降低线粒体功能障碍	[44]
	紫苏醇	CYP2A6/CYP2B6	-	[25]
诱导剂	聚乙二醇化脂质体	CYP3A	增强聚乙二醇抗肝细胞癌作用	[45]
	诃子	CYP1A2等	显著改善肝功能和组织病理学	[46]
	厄洛替尼	CYPA3	治疗晚期非小细胞肺癌	[47]
	黄芪注射液	CYP2D1	提高癌症疗效，降低耐药性	[48]

细胞色素P450酶系药物研发：肝脏药物代谢调控与临床应用研究进展

Cytochrome P450 Enzyme System in Drug Development: Advances in Research on Regulation of Hepatic Drug Metabolism and Clinical Applications

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