2022年4月11日 · We evaluated the preclinical efficacy of NTX-301 monotherapy by establishing four different mouse models encompassing both systemic and subcutaneous xenografts.

2022年6月2日 · Preclinical data suggest a correlation between NTX-301 activity in leukemia xenograft models and decreased levels of DNMT1. NTX-301 offers an improvement over traditional DNA methyltransferase inhibitors (azacitidine, decitabine) by virtue of a higher incorporation rate into DNA at lower levels of cytotoxicity.

2024年3月15日 · NTX-301 treatment decreased levels of UFA and increased oxidized lipids, and this was blunted by deferoxamine, indicating cell death via ferroptosis. NTX-301-induced ferroptosis was rescued by oleic acid. In vivo, monotherapy with NTX-301 significantly inhibited ovarian cancer and patient-derived xenograft growth (P < 0.05). Decreased SCD ...

最近的一项研究表明，一种新型 4'-硫代修饰的类似物 5-aza-4'-thio-2'-deoxycytidine（以下称为 NTX-301）的药理学改进，包括增强的化学稳定性和掺入 DNA 以及提高临床前疗效。

NTX-301 is a highly potent and orally bioavailable HMA, in early clinical development. Experimental Design: The antitumor effects of NTX-301 were studied in ovarian cancer models by using cell viability, stemness and ferroptosis assays, RNA sequencing, lipidomic analyses, and stimulated Raman spectroscopy.

2023年11月2日 · We here investigate the therapeutic efficacy of NTX-301 (5-aza-thio 2'-deoxycytidine) (PinotBio, Inc.), a novel HMA in venetoclax-resistant and TP53-mutant AML. NTX-301 greatly reduced the levels of DNMT1 and decreased viability in various AML cells, markedly more effective than 5-azacytide (5-Aza).

临床前数据表明白血病异种移植模型中的 ntx-301 活性与 dnmt1 水平降低之间存在相关性。 NTX-301 提供了优于传统 DNA 甲基转移酶抑制剂（阿扎胞苷、地西他滨）的改进，因为它具有更高的 DNA 掺入率和更低的细胞毒性水平。

2024年1月19日 · ntx-301是一种新型的口服生物可利用去甲基化药物，正处在临床开发初期。 本研究旨在全面评估NTX-301在卵巢癌模型中的抗肿瘤效果和作用机制。 方法：通过细胞活力测试、干细胞特性分析、铁凋亡检测、RNA测序、脂质组学分析和拉曼光谱等方法，全方位研究了NTX ...

Preclinical data suggest a correlation between NTX-301 activity in leukemia xenograft models and decreased levels of DNMT1. NTX-301 offers an improvement over traditional DNA methyltransferase inhibitors (azacitidine, decita-bine) by virtue of a higher incorporation rate into DNA at lower levels of cytotoxicity.

2022年4月11日 · NTX-301 conferred benefits in combination with VCX. GSEA plots showing significant enrichment of genes regulating sensitivity or resistance to VCX among transcriptome changes induced by 48 h of treatment with NTX-301 or DAC in MV4-11 cells.