Department of Pharmacy, University of Genova, Viale Benedetto XV, 3, 16132 Genova, Italy.
Int J Mol Sci. 2021 Jul 16;22(14):7641. doi: 10.3390/ijms22147641.
In the past few years, Bruton's tyrosine Kinase (Btk) has emerged as new target in medicinal chemistry. Since approval of ibrutinib in 2013 for treatment of different hematological cancers (as leukemias and lymphomas), two other irreversible Btk inhibitors have been launched on the market. In the attempt to overcome irreversible Btk inhibitor limitations, reversible compounds have been developed and are currently under evaluation. In recent years, many Btk inhibitors have been patented and reported in the literature. In this review, we summarized the (ir)reversible Btk inhibitors recently developed and studied clinical trials and preclinical investigations for malignancies, chronic inflammation conditions and SARS-CoV-2 infection, covering advances in the field of medicinal chemistry. Furthermore, the nanoformulations studied to increase ibrutinib bioavailability are reported.
在过去的几年中,布鲁顿酪氨酸激酶(Btk)已成为医学化学中的新靶标。自 2013 年伊布替尼获批用于治疗不同的血液系统癌症(如白血病和淋巴瘤)以来,另外两种不可逆的 Btk 抑制剂已上市。为了克服不可逆 Btk 抑制剂的局限性,已开发出并正在评估可逆化合物。近年来,许多 Btk 抑制剂已在文献中获得专利和报道。在这篇综述中,我们总结了最近开发的(不可)逆 Btk 抑制剂以及针对恶性肿瘤、慢性炎症疾病和 SARS-CoV-2 感染的临床研究和临床前研究,涵盖了医学化学领域的进展。此外,还报道了为提高伊布替尼生物利用度而研究的纳米制剂。