Jardim-Perassi Bruna Victorasso, Irrera Pietro, Abrahams Dominique, Estrella Veronica C, Ordway Bryce, Byrne Samantha R, Ojeda Andrew A, Whelan Christopher J, Kim Jongphil, Beatty Matthew S, Damgaci-Erturk Sultan, Longo Dario Livio, Gaspar Kim J, Siegers Gabrielle M, Centeno Barbara A, Lau Justin Y C, Ibrahim-Hashim Arig, Pilon-Thomas Shari A, Gillies Robert J
bioRxiv. 2023 Aug 28:2023.08.28.555194. doi: 10.1101/2023.08.28.555194.
Acidosis is an important immunosuppressive mechanism that leads to tumor growth. Therefore, we investigated the neutralization of tumor acidity to improve immunotherapy response. L-DOS47, a new targeted urease immunoconjugate designed to neutralize tumor acidity, has been well tolerated in phase I/IIa trials. L-DOS47 binds CEACAM6, a cell surface protein highly expressed in gastrointestinal cancers, allowing urease to cleave endogenous urea into two NH4+ and one CO2, thereby raising local pH. To test the synergetic effect of neutralizing tumor acidity with immunotherapy, we developed a pancreatic orthotopic murine tumor model (KPC961) expressing human CEACAM6. Our results demonstrate that combining L DOS47 with anti-PD1 significantly increases the efficacy of anti-PD1 monotherapy, reducing tumor growth for up to 4 weeks.
酸中毒是一种导致肿瘤生长的重要免疫抑制机制。因此,我们研究了中和肿瘤酸度以改善免疫治疗反应。L-DOS47是一种旨在中和肿瘤酸度的新型靶向脲酶免疫偶联物,在I/IIa期试验中耐受性良好。L-DOS47与癌胚抗原相关细胞黏附分子6(CEACAM6)结合,CEACAM6是一种在胃肠道癌症中高度表达的细胞表面蛋白,它能使脲酶将内源性尿素分解为两个NH4+和一个CO2,从而提高局部pH值。为了测试中和肿瘤酸度与免疫治疗的协同作用,我们建立了一个表达人CEACAM6的胰腺原位小鼠肿瘤模型(KPC961)。我们的结果表明,将L-DOS47与抗PD-1联合使用可显著提高抗PD-1单药治疗的疗效,使肿瘤生长减缓长达4周。