经FDA批准的小分子蛋白激酶抑制剂的特性:2026年更新
1Blue Ridge Institute for Medical Research, 221 Haywood Knolls Drive, Hendersonville, North Carolina 28791, United States.
Pharmacological research
|January 26, 2026
概括
蛋白激酶是主要的药物标,有94种FDA批准的抑制剂,包括2025年10种新的抑制剂. 本综述详细介绍了它们的物理化学特性和在癌症和炎症性疾病中的治疗应用.
科学领域:
- 药理学和药物发现
- 药用化学 医学化学
- 在瘤学瘤学.
背景情况:
- 蛋白质激酶是治疗瘤和炎症性疾病的关键点,因为它们的活性失调.
- 蛋白激酶抑制剂的开发在现代医学中显著推进了治疗策略.
研究的目的:
- 总结所有94种FDA批准的小分子蛋白激酶抑制剂的物理化学特性.
- 提供这些向药物的治疗应用和最近批准的概述.
主要方法:
- 对94种FDA批准的蛋白质激酶抑制剂的物理化学数据 (分子量,H键捐赠者/接受者,LE,LLE,PSA,可溶性) 的汇编和分析.
- 对每个药物的FDA批准状态和治疗指示进行审查,重点是2025年批准的药物.
主要成果:
- 94种小分子蛋白激酶抑制剂已获得FDA批准,其中10种在2025年获得批准,针对各种激酶 (MEK1/2,JAK,BTK,FAK,EGFR,ROS1,CSF1R,HER2).
- 这些抑制剂主要用于瘤 (约80种药物) 和炎症性疾病;大约有二十种治疗多种疾病.
- 大多数批准的抑制剂 (90) 是口服生物可用,而45 种至少有一种违反了利宾斯基的五项规则.
结论:
- 经FDA批准的蛋白激酶抑制剂的范围正在扩大,为癌症和炎症疾病提供各种治疗选择.
- 这些抑制剂的物理化学性质各不相同,尽管可能违反利宾斯基规则,但许多抑制剂显示出口服生物可用性.
- 对蛋白质激酶抑制剂的持续研究有望为新药开发和改善患者的治疗结果提供希望.
关键词:
亚美丁尼布 (PubChem CID: 16719221) 是一种药物.慢性免疫性血小板减少症.慢性自发性 ?? 疹.德法提尼布 (PubChem CID: 25117126) 的使用情况德尔戈提尼布 (PubChem CID: 50914062) 是一种药物,它可以手上的湿疹手湿疹.米达美提尼布 (PubChem CID: 9826528) 是一种药物.突变EGFR,HER2和ROS1非小细胞肺癌卵巢癌是发生在卵巢中的癌症.雷米布鲁丁尼布 (PubChem CID: 118107483) 是一种药物.里尔扎布鲁丁尼布 (PubChem CID: 73388818) 的使用情况孙沃泽提尼布 (PubChem CID: 139377809) 是一种药物.塔莱特雷克提尼布 (PubChem CID: 72202474) 的使用情况紧缩性巨细胞瘤维姆塞尔提尼布 (PubChem CID: 86267612) 是一种药物.格尔提尼布 (PubChem CID: 160283094) 是一种可以使用的药物.相关概念视频
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