2023年6月1日 · IOA-289 is a novel, first-in-class inhibitor of autotaxin with a unique binding mode. IOA-289 inhibits biomarkers of fibrosis and shows efficacy in an in vivo lung fibrosis and cancer models. We demonstrate that ATX inhibition has three mechanisms relevant for …

2024年5月29日 · IOA-289 is a novel inhibitor of ATX, with anti-fibrotic, immune-enhancing and anti-tumour activity. This first-in-human trial evaluated safety and tolerability, pharmacokinetic (PK)/pharmacodynamic (PD) profile of IOA-289 in combination with GnP.

IOA-289 是一种高效和选择性的 ATX 抑制剂，在癌症模型中具有单药治疗活性。 基于作用机制，我们正在研究 IOA-289 与化学疗法、免疫疗法和正在进行的临床前研究中的新药物的组合。 可接受的安全性和 PK 特征支持 IOA-289 的临床开发，目前处于 I 期临床试验中。 伦理批准 4T1 研究得到了大学 Claude Bernard Lyon 1 伦理委员会的批准；批准号 DR2014-38 (vM)。 E0771 研究由 AAALAC 国际认证项目合同研究组织（Covance，Ann Arbor，MI，USA）的机构动物护理 …

2023年8月8日 · IOA-289 is a potent ATX inhibitor, developed to treat cancers containing fibrosis. In this study, we tested IOA-289 treatment on different gastrointestinal tract tumor cell lines, in order to evaluate its effects on viability and motility.

2023年5月1日 · The autotaxin inhibitor IOA-289 suppressed NFκB activation in PDAC cells and overcame resistance to galunisertib and gemcitabine. In immunocompetent orthotopic murine models, IOA-289 synergized with galunisertib in restoring sensitivity to gemcitabine.

2023年4月8日 · Our data show that IOA-289 is a novel ATX inhibitor with a unique chemical structure, excellent potency and an attractive safety profile. Our data support the further development of IOA-289 as a novel therapeutic approach for the treatment of cancer, particularly those with a high fibrotic and immun …

2023年8月8日 · We found that IOA-289 is able to inhibit both growth and migration of gastrointestinal tract tumor cell lines, both in 2D (crystal violet assay) and 3D in vitro models (spheroid formation and clonogenic assay in matrigel). This effect is dose-dependent, and the drug is most effective when administered in FBS-free culture medium.

12月9日，创新药公司iOnctura在欧洲肿瘤内科学会免疫肿瘤学（ESMO IO）大会上展示了其自分泌运动因子（autotaxin）抑制剂IOA-289的临床及临床前数据，IOA-289将成为首个开展肿瘤临床试验的autotaxin抑制剂。

2024年4月1日 · 近日，美国食品药品监督管理局 (FDA)授予荷兰生物制药公司iOnctura研发的一款创新药——Cambritaxestat (IOA-289)的孤儿药资格，它将加速该药物的临床开发进程，并为胰腺癌患者提供一种潜在的治疗选择。 截图源自“OneLive网站” Cambritaxestat:首款治疗癌症的自分泌运动因子抑制剂. Cambritaxestat是一种新型的口服小分子ATX (细胞外酶自分泌运动因子)抑制剂，ATX水平与人类癌症的分期和分级直接相关，该药也是首款用于癌症治疗的自分泌运动因子 …

IOA-289 is a highly potent and selective inhibitor of ATX with demonstrated monotherapy activity in cancer models. Based on the mechanism of action we are investigating combinations of IOA-289 with chemotherapy, immunotherapy and novel agents in ongoing preclinical studies.