BTX-1188. • Human PBMCs were stimulated with aCD3 for IL-2 measurement or LPS-induced for measurement of inflammatory cytokines upon DMSO or compound treatment. • Vehicle or BTX-1188 were used in athymic or BALB/c nude mice xenograft models. RESULTS • BTX-1188 is a rapid, deep, and potent degrader of GSPT1 and

2022年6月2日 · Background: BTX-1188 is a first-in-class oral molecular glue that degrades GSPT1 and IKZF1/3 and is currently in phase 1 clinical trials for treatment of hematologic and solid malignancies. Targeted protein degradation of cereblon neosubstrates is clinically validated in the treatment (tx) of hematologic malignancies (Lu 2014, Zou 2020).

BTX-1188: 一种GSPT1抑制剂、IKZF1抑制剂、IKZF3抑制剂药物，由The Hebrew University of Jerusalem (The Hebrew University of Jerusalem)公司最早进行研发，目前全球最高研发状态为终止，作用机制: GSPT1抑制剂(G1 to S phase transition 1 inhibitors),IKZF1抑制剂(DNA结合蛋白IKAROS抑制剂),IKZF3抑制剂(锌指蛋白Aiolos抑制剂)，治疗领域 ...

2021年11月16日 · 使用MV-411人AML裸鼠异种移植模型评价BTX-1188的体内疗效，研究表明间歇性给药可显著减少肿瘤体积，进一步确定治疗候选患者AML的可能性。重要的是，BTX-1188在不到两周的剂量内完全消除了肿瘤，并在研究结束前保持动物无肿瘤状态。 BioTheryX研发管线

2024年2月1日 · BTX-1188 (Structure undisclosed) is an oral molecular glue targeted degradation of GSPT1 and IKZF1/3 [20]. Compared with CC-90009, BTX-1188 showed greater potency on human AML cells, with IC 50 values ranging from 0.4 to 1.5 nM. A phase 1 trial (NCT05144334) was conducted in January 2022 to evaluate its efficacy and safety in patients with ...

2022年5月26日 · About BTX-1188. Biotheryx’s lead molecular glue drug candidate BTX-1188 is a dual protein degrader which was designed to degrade GSPT1, a promising cancer target, and IKZF1/3 (also known as Ikaros/Aiolos), both clinically validated anti-inflammatory and immunomodulatory targets. Prior literature has demonstrated that degradation of GSPT1 can ...

BTX-1188 is a leading PHM molecular glue candidate with strong potential for treating AML and MDS. In vivo efficacy of BTX-1188 was evaluated using the MV-411 human AML xenograft model in athymic ...

About BTX-1188. BTX-1188 is the first orally bioavailable, rationally designed dual target protein degrader, engineered to specifically degrade validated oncology targets GSPT1 and IKZF1/3. By degrading GSPT1 and IKZF1/3, BTX-1188’s profile is expected to be differentiated from protein degraders that exclusively target GSPT1.

ptosis in response to BTX-1188 tx is further reflectedin in vivo efficacymodels where daily or intermittent dosing of BTX-1188 results in potent and sustained antitumor activity. Conclusions: These preclinical data show that BTX-1188 is a promising drug candidate for AML and other tumor types. Its immunomodulatory properties owing to IKZF1/3 ...

btx-1188 是治疗急性髓系白血病和骨髓增生异常综合征的领先的分子胶候选药物，目前正处于 i 期临床试验。值得指出的是， btx-1188 被发现可以降解 gspt1 、 ikzf 和 ck1α ，并有望在杀死肿瘤细胞的同时调节免疫系统，从而获得更好的疗效和更少的潜在副作用。