rly-2608是已知的第一个 变构泛突变体 (h1047x, e542x和e545x)，以及旨在克服这些限制的异构体选择性pi3kα抑制剂。rly-2608目前正在进行临床试验，旨在治疗带有pik3ca (pi3kα)突变的晚期实体肿瘤患者。

2024年5月29日 · RLY-2608, a novel, oral allosteric PI3Kα inhibitor, is designed to overcome these limitations via mutant- and isoform-selective PI3Kα inhibition for greater target coverage, improved tolerability, and anti-tumor activity.

RLY-2608 inhibited tumor growth in PIK3CA-mutant xenograft models with minimal impact on insulin, a marker of dysregulated glucose homeostasis. RLY-2608 elicited objective tumor responses in two patients diagnosed with advanced hormone receptor-positive breast cancer with kinase or helical domain PIK3CA mutations, with no observed WT PI3Kα ...

RLY-2608 is a novel, allosteric, pan-mutant and isoform selective, oral PI3Kα inhibitor. The selectivity of RLY-2608 for mutant PI3Kα provides the opportunity for greater target coverage, leading to the potential of improved efficacy and chronic tolerability. The trial will evaluate RLY-2608 in patients with PI3Kα-driven Vascular ...

RLY-2608 is a first-in-class PI3Kα inhibitor that demonstrates mutant-selective efficacy in the clinic. These features have the potential to improve outcomes in patients with PIK3CA-mutant tumors, in monotherapy, and in combination with other targeted therapies.

RLY-2608 is known as the first pan-allosteric variant (H1047X, E542X, and E545X), and as an allosteric selective PI3Kα inhibitor designed to overcome these limitations. RLY-2608 is currently under clinical trial, aiming to treat patients with advanced …

2023年3月9日 · Pazolli M, Discovery and characterization of RLY-2608, the first allosteric, mutant, and isoform-selective inhibitor of PI3Kα. Oral presentation at: AACR-NCI-EORTC Virtual International Conference on Molecular Targets Conference; October 7-10, 2021; Virtual. 1. This model also carries a second mutation at K567R; 2. HSC2 model. NCT05216432.

2023年4月28日 · AI制药公司Relay近日在AACR 2023会议上披露了PI3Kα抑制剂RLY-2608初步临床有效性数据的信号，看完官网上披露的PPT数据后，基本判定这款药没有继续开发下去的必要了。 24例可评估患者，仅出现1例PR，还是unconfirmed的，剔除那些早期爬坡的低剂量可评估患者（低于400mg BID），为16例可评估患者，1/16=6.25%的ORR依旧是不够看的。 对标药物alpelisib的3期临床试验SOLAR-1的ORR为35.7%（患者的基线有可测量的病灶）。 那么随着 …

2023年4月20日 · 近日，AI 制药明星公司 （NASDAQ: RLAY）公布了在研管线 RLY-2608 的早期临床数据，试验结果显示，RLY-2608 在多个预测有效剂量下选择性靶向目标靶点，具有良好的初始安全性和耐受性。 RLY-2608 相关的临床数据已发布在美国癌症研究协会（AACR）2023 年年会上。 据悉，这是 首个 已知的变构、泛突变体（H1047X、E542X 和 E545X）和亚型选择性 PI3Kα 抑制剂。 PI3Kα 是与癌症相关的细胞生长、增殖和存活等多种细胞功能有关联的信号通路中 …

RLY-2608 achieves maximum efficacy in both kinase and helical domain PIK3CA mutant in vivo xenograft models with significantly reduced elevation of insulin levels compared to orthosteric inhibitors