Melillo Nicola, Dickinson Jake, Tan Lu, Mistry Hitesh B, Huber Heinrich J
Seda Pharmaceutical Developments Services Unit D Cheadle Royal Business Park, Stockport, United Kingdom.
Division Drug Discovery Sciences, Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria.
Front Pharmacol. 2023 Oct 13;14:1272058. doi: 10.3389/fphar.2023.1272058. eCollection 2023.
The effect of combination therapies in many cancers has often been shown to be superior to that of monotherapies. This success is commonly attributed to drug synergies. Combinations of two (or more) drugs in xenograft tumor growth inhibition (TGI) studies are typically designed at fixed doses for each compound. The available methods for assessing synergy in such study designs are based on combination indices (CI) and model-based analyses. The former methods are suitable for screening exercises but are difficult to verify in in vivo studies, while the latter incorporate drug synergy in semi-mechanistic frameworks describing disease progression and drug action but are unsuitable for screening. In the current study, we proposed the empirical radius additivity (Rad-add) score, a novel CI for synergy detection in fixed-dose xenograft TGI combination studies. The Rad-add score approximates model-based analysis performed using the semi-mechanistic constant-radius growth TGI model. The Rad-add score was compared with response additivity, defined as the addition of the two response values, and the bliss independence model in combination studies derived from the Novartis PDX dataset. The results showed that the bliss independence and response additivity models predicted synergistic interactions with high and low probabilities, respectively. The Rad-add score predicted synergistic probabilities that appeared to be between those predicted with response additivity and the Bliss model. We believe that the Rad-add score is particularly suitable for assessing synergy in the context of xenograft combination TGI studies, as it combines the advantages of CI approaches suitable for screening exercises with those of semi-mechanistic TGI models based on a mechanistic understanding of tumor growth.
在许多癌症中,联合疗法的效果往往优于单一疗法。这种成功通常归因于药物协同作用。在异种移植肿瘤生长抑制(TGI)研究中,两种(或更多)药物的组合通常针对每种化合物以固定剂量设计。在此类研究设计中评估协同作用的现有方法基于联合指数(CI)和基于模型的分析。前一种方法适用于筛选,但在体内研究中难以验证,而后一种方法在描述疾病进展和药物作用的半机制框架中纳入了药物协同作用,但不适用于筛选。在本研究中,我们提出了经验半径相加(Rad-add)评分,这是一种用于固定剂量异种移植TGI联合研究中协同作用检测的新型CI。Rad-add评分近似于使用半机制恒定半径生长TGI模型进行的基于模型的分析。将Rad-add评分与反应相加性(定义为两个反应值的相加)以及源自诺华PDX数据集的联合研究中的布利斯独立性模型进行了比较。结果表明,布利斯独立性模型和反应相加性模型分别以高概率和低概率预测协同相互作用。Rad-add评分预测的协同概率似乎介于反应相加性模型和布利斯模型预测的概率之间。我们认为,Rad-add评分特别适合在异种移植联合TGI研究的背景下评估协同作用,因为它结合了适用于筛选的CI方法的优点和基于对肿瘤生长的机制理解的半机制TGI模型的优点。