Clinical Pharmacology, Global Product Development, Pfizer, San Diego, California, USA.
San Diego Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, California, USA.
Clin Transl Sci. 2023 Jun;16(6):922-936. doi: 10.1111/cts.13507. Epub 2023 Apr 23.
It is well-recognized that therapeutic proteins (TPs) with pro-inflammatory activities elevate the pro-inflammatory cytokines and result in cytokine-drug interactions. In the current review, several pro-inflammatory cytokines, including IL-2, IL-6, IFN-γ, and TNF-α, as well as an anti-inflammatory cytokine IL-10, were summarized for their respective effect on major cytochrome P450 enzymes and efflux transporter PgP. Pro-inflammatory cytokines are generally associated with suppression of CYP enzymes across assay systems but have varied effect on Pgp expression levels and activities depending on the individual cytokines and assay systems, whereas IL-10 had no significant impact on CYP enzymes and P-gp. A cocktail drug-drug interaction (DDI) study design could be an ideal approach for simultaneously assess the impact of TPs with pro-inflammatory activities on multiple CYP enzymes. Clinical DDI studies using the cocktail approach have been conducted for several TPs with pro-inflammatory activities and for those TPs with pro-inflammatory activities which had no clinical DDI study conducted, languages for potential DDI risk due to cytokine-drug interaction were included in the label. Up to date drug cocktails, including clinically validated and unvalidated for DDI assessment, were summarized in this review. Most clinically validated cocktails focused either on CYP enzymes or transporters. Additional effort was needed to validate a cocktail to include both the major CYP enzymes and key transporters. In silico methods for assessment of the DDI for TPs with pro-inflammatory activities were also discussed.
众所周知,具有促炎活性的治疗性蛋白(TPs)会升高促炎细胞因子,从而导致细胞因子-药物相互作用。在本综述中,总结了几种促炎细胞因子,包括 IL-2、IL-6、IFN-γ 和 TNF-α,以及抗炎细胞因子 IL-10,分别讨论了它们对主要细胞色素 P450 酶和外排转运蛋白 PgP 的各自影响。促炎细胞因子通常与 CYP 酶在整个检测系统中的抑制有关,但对 Pgp 表达水平和活性的影响因个体细胞因子和检测系统而异,而 IL-10 对 CYP 酶和 P-gp 没有显著影响。鸡尾酒药物相互作用(DDI)研究设计可能是同时评估具有促炎活性的 TP 对多种 CYP 酶影响的理想方法。已经对几种具有促炎活性的 TP 进行了使用鸡尾酒方法的临床 DDI 研究,对于那些没有进行临床 DDI 研究的具有促炎活性的 TP,由于细胞因子-药物相互作用而具有潜在 DDI 风险的语言被包含在标签中。本文综述了截至目前的药物鸡尾酒,包括已用于 DDI 评估的临床验证和未验证的药物鸡尾酒。大多数经临床验证的鸡尾酒主要集中在 CYP 酶或转运体上。需要进一步努力验证一种鸡尾酒,以包括主要的 CYP 酶和关键的转运体。还讨论了用于评估具有促炎活性的 TP 的 DDI 的计算方法。