经FDA批准的小分子蛋白激酶抑制剂的特性:2025年更新
1Blue Ridge Institute for Medical Research, 221 Haywood Knolls Drive, Hendersonville, NC 28791, United States.
Pharmacological research
|April 19, 2025
概括
蛋白激酶抑制剂是癌症和炎症性疾病的关键药物标. 这项研究分析了85种FDA批准的药物,详细介绍了它们的物理化学特性和治疗应用.
科学领域:
- 生物化学 生化学
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
背景情况:
- 蛋白质激酶放松调节与许多炎症性疾病和癌症有关,使蛋白质激酶家族成为重要的治疗点.
- 美国食品和药物管理局已经批准了85种小分子蛋白激酶抑制剂,最近的批准是在2024年和2025年,突出了这些药物的不断扩大的作用.
- 这些抑制剂向各种酶家族,包括受体和非受体氨酸酶,氨酸/氨酸酶和双特异性酶,大多数用于瘤治疗.
研究的目的:
- 总结所有85种FDA批准的小分子蛋白激酶抑制剂的物理化学特性.
- 提供药物标,治疗指示和最近在蛋白质激酶抑制剂类中的批准的全面概述.
- 分析药物特征,如分子量,结潜力,联体效率,脂性效率,极地表面积和可溶性.
主要方法:
- 汇编和总结85种FDA批准的蛋白激酶抑制剂的物理化学数据.
- 基于向激酶家族的抑制剂的分类 (例如,MEK1/2,氨酸/氨酸,氨酸激酶).
- 与利宾斯基的第五规则和口服生物可用性相关的药物特性分析.
主要成果:
- 在FDA批准的85种药物中,有75种用于治疗瘤,7种用于治疗炎症.
- 最近FDA批准的药物包括deuruxolitinib,ensartinib,lazertinib,tovorafenib (2024年) 和mirdametinib (2025年),针对各种癌症和罕见疾病.
- 在这些抑制剂中,很大一部分 (85种中39种) 至少有一种违反了利宾斯基的第5规则,这表明药物设计策略多样化.
结论:
- 美国食品和药物管理局批准的蛋白激酶抑制剂的范围广泛且不断增长,对瘤学和免疫学有重大影响.
- 在批准的抑制剂中,物理化学性质的差异很大,影响它们的药理动力学和药理动力学概况.
- 本摘要为研究人员和药物开发人员在酶向疗法领域提供了有价值的数据.
关键词:
阿洛佩西亚 areata 地区.卡博赞提尼布 (PubChem CID: 25102847) 是一种药物.慢性骨髓性白血病 慢性骨髓性白血病克里佐替尼 (PubChem CID: 11626560) 是一种可以使用的药物.德鲁克索利提尼布 (PubChem CID: 72704611) 的使用情况恩萨尔提尼布 (PubChem CID: 56960363) 是一个药物.皮肤表皮生长因子受体.伊马替尼布 (PubChem CID: 5291) 的使用情况拉泽提尼布 (PubChem CID: 121269225) 是一种药物.米达美提尼布 (PubChem CID: 9826528) 是一种药物.神经纤维细胞增生症非小细胞肺癌,儿科质瘤索拉费尼布 (PubChem CID: 216239) 是一种药物.苏尼蒂尼布 (PubChem CID: 5329102) 是一种药物.托沃法尼布 (PubChem CID: 25161177) 的使用情况相关概念视频
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