Imran Mohd, Asdaq Syed Mohammed Basheeruddin, Khan Shah Alam, Unnikrishnan Meenakshi Dhanalekshmi, Alamri Abdulhakeem S, Alsanie Walaa F, Alhomrani Majid, Mohzari Yahya, Alrashed Ahmed, AlMotairi Mohammed, Alkhaldi Eman H, Alorabi Abeer K, Alshrari Ahmed Subeh, Tauseef Mohammad, Alaqel Saleh I, Alam Ozair, Bakht Md Afroz
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Northern Border University, Arar 91911, Saudi Arabia.
Department of Pharmacy Practice, College of Pharmacy, AlMaarefa University, Dariyah, Riyadh 13713, Saudi Arabia.
Pharmaceuticals (Basel). 2021 Jul 22;14(8):710. doi: 10.3390/ph14080710.
Protein kinase inhibitors (PKIs) are important therapeutic agents. As of 31 May 2021, the United States Food and Drug Administration (USFDA) has approved 70 PKIs. Most of the PKIs are employed to treat cancer and inflammatory diseases. Imatinib was the first PKI approved by USFDA in 2001. This review summarizes the compound patents and the essential polymorph patents of the PKIs approved by the USFDA from 2001 to 31 May 2021. The dates on the generic drug availability of the PKIs in the USA market have also been forecasted. It is expected that 19 and 48 PKIs will be genericized by 2025 and 2030, respectively, due to their compound patent expiry. This may reduce the financial toxicity associated with the existing PKIs. There are nearly 535 reported PKs. However, the USFDA approved PKIs target only about 10-15% of the total said PKs. As a result, there are still a large number of unexplored PKs. As the field advances during the next 20 years, one can anticipate that PKIs with many scaffolds, chemotypes, and pharmacophores will be developed.
蛋白激酶抑制剂（PKIs）是重要的治疗药物。截至2021年5月31日，美国食品药品监督管理局（USFDA）已批准70种PKIs。大多数PKIs用于治疗癌症和炎症性疾病。伊马替尼是2001年USFDA批准的首个PKI。本综述总结了2001年至2021年5月31日期间USFDA批准的PKIs的化合物专利和关键晶型专利。还预测了PKIs在美国市场的仿制药上市日期。预计由于化合物专利到期，到2025年和2030年将分别有19种和48种PKIs实现仿制药化。这可能会降低与现有PKIs相关的经济毒性。据报道有近535种蛋白激酶。然而，USFDA批准的PKIs仅针对约10%-15%的上述蛋白激酶。因此，仍有大量未被探索的蛋白激酶。随着该领域在未来20年的发展，可以预见将会开发出具有多种骨架、化学型和药效团的PKIs。
