IN05 (In3Bio)(IN05 (In3Bio)) - 在研适应症：结直肠癌_专利_临床

概要

基本信息

药物类型

生物药

别名-

靶点-

作用机制-

治疗领域

肿瘤消化系统疾病

在研适应症

结直肠癌

非在研适应症-

原研机构

In3Bio Ltd.

在研机构

In3Bio Ltd.

非在研机构-

最高研发阶段早期临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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关联

100 项与 IN05 (In3Bio) 相关的临床结果

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100 项与 IN05 (In3Bio) 相关的转化医学

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100 项与 IN05 (In3Bio) 相关的专利（医药）

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1

项与 IN05 (In3Bio) 相关的文献（医药）

2017-10-01·Structure

Targeting Prolyl-tRNA Synthetase to Accelerate Drug Discovery against Malaria, Leishmaniasis, Toxoplasmosis, Cryptosporidiosis, and Coccidiosis

Article

作者: Kikuchi, Haruhisa ; Yogavel, Manickam ; Matsumoto, Makoto ; Jumani, Rajiv S ; Oshima, Yoshiteru ; Jain, Vitul ; Touquet, Bastien ; Sharma, Amit ; Tacchini-Cottier, Fabienne ; Goel, Preeti ; Hariguchi, Norimitsu ; Huston, Christopher D ; Hakimi, Mohamed-Ali ; Harlos, Karl

Developing anti-parasitic lead compounds that act on key vulnerabilities are necessary for new anti-infectives. Malaria, leishmaniasis, toxoplasmosis, cryptosporidiosis and coccidiosis together kill >500,000 humans annually. Their causative parasites Plasmodium, Leishmania, Toxoplasma, Cryptosporidium and Eimeria display high conservation in many housekeeping genes, suggesting that these parasites can be attacked by targeting invariant essential proteins. Here, we describe selective and potent inhibition of prolyl-tRNA synthetases (PRSs) from the above parasites using a series of quinazolinone-scaffold compounds. Our PRS-drug co-crystal structures reveal remarkable active site plasticity that accommodates diversely substituted compounds, an enzymatic feature that can be leveraged for refining drug-like properties of quinazolinones on a per parasite basis. A compound we termed In-5 exhibited a unique double conformation, enhanced drug-like properties, and cleared malaria in mice. It thus represents a new lead for optimization. Collectively, our data offer insights into the structure-guided optimization of quinazolinone-based compounds for drug development against multiple human eukaryotic pathogens.

100 项与 IN05 (In3Bio) 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
结直肠癌	临床1期	英国	In3Bio Ltd.	2022-03-30

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


WCLC2023 人工标引	临床1期	非小细胞肺癌 III期新辅助	9	radiotherapy 10 Gy in 5 fractions+Durvalumab+Chemotherapy	(鹽鹹膚餘築夢艱構壓襯) = Grade 3-4 AEs were reported in 3 (33.3%) patients, including leukopenia (22.2%), anemia (11.1%), and infectious pneumonia (11.1%). 襯餘鏇艱廠選壓觸廠築 (壓鏇醖築膚網夢齋廠淵 ) 更多	积极	2023-09-12
				radiotherapy 20 Gy in 10 fractions+Durvalumab+Chemotherapy