PRN-371(PRN-371) - 药物靶点：JAK3_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

JAK3

作用机制

JAK3抑制剂(酪氨酸蛋白激酶JAK3抑制剂)

治疗领域

肿瘤免疫系统疾病血液及淋巴系统疾病

在研适应症-

非在研适应症

NK细胞淋巴瘤T细胞淋巴瘤

原研机构

Principia Biopharma, Inc.

在研机构-

非在研机构

National Cancer Centre of Singapore Pte Ltd.

Principia Biopharma, Inc.

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C20H21N5O2

InChIKeyRGYYZLGXRYSDRO-UHFFFAOYSA-N

CAS号1610974-55-4

关联

100 项与 PRN-371 相关的临床结果

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100 项与 PRN-371 相关的转化医学

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100 项与 PRN-371 相关的专利（医药）

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1

项与 PRN-371 相关的文献（医药）

2018-05-01·Leukemia1区 · 医学

Oncogenic activation of JAK3-STAT signaling confers clinical sensitivity to PRN371, a novel selective and potent JAK3 inhibitor, in natural killer/T-cell lymphoma

1区 · 医学

Article

作者: Teh, B T ; Song, T L L ; Hill, R J ; Yeoh, K W ; Chia, B K H ; Tan, J ; Bradshaw, J M ; Rajasegaran, V ; Pang, W L ; Lim, J Q ; Xia, X J ; Huang, D ; Ng, C C Y ; Nairismägi, M -L ; Kang, T B ; Bisconte, A ; Tang, Q Q ; Ong, C K ; Wijaya, G C ; Yao, X S ; Laurensia, Y ; Lim, S T ; Tang, T ; Li, Z M ; Gerritsen, M E

Aberrant activation of the JAK3-STAT signaling pathway is a characteristic feature of many hematological malignancies. In particular, hyperactivity of this cascade has been observed in natural killer/T-cell lymphoma (NKTL) cases. Although the first-in-class JAK3 inhibitor tofacitinib blocks JAK3 activity in NKTL both in vitro and in vivo, its clinical utilization in cancer therapy has been limited by the pan-JAK inhibition activity. To improve the therapeutic efficacy of JAK3 inhibition in NKTL, we have developed a highly selective and durable JAK3 inhibitor PRN371 that potently inhibits JAK3 activity over the other JAK family members JAK1, JAK2, and TYK2. PRN371 effectively suppresses NKTL cell proliferation and induces apoptosis through abrogation of the JAK3-STAT signaling. Moreover, the activity of PRN371 has a more durable inhibition on JAK3 compared to tofacitinib in vitro, leading to significant tumor growth inhibition in a NKTL xenograft model harboring JAK3 activating mutation. These findings provide a novel therapeutic approach for the treatment of NKTL.

100 项与 PRN-371 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
NK细胞淋巴瘤	临床前	美国	Principia Biopharma, Inc.	2018-04-30
NK细胞淋巴瘤	临床前	美国	National Cancer Centre of Singapore Pte Ltd.	2018-04-30
T细胞淋巴瘤	临床前	美国	Principia Biopharma, Inc.	2018-04-30
T细胞淋巴瘤	临床前	美国	National Cancer Centre of Singapore Pte Ltd.	2018-04-30