Innovations and Patent Trends in the Development of USFDA Approved Protein Kinase Inhibitors in the Last Two Decades

Mohd Imran; Syed Mohammed Basheeruddin Asdaq; Shah Alam Khan; Dhanalekshmi Unnikrishnan Meenakshi; Abdulhakeem S Alamri; Walaa F Alsanie; Majid Alhomrani; Yahya Mohzari; Ahmed Alrashed; Mohammed AlMotairi; Eman H Alkhaldi; Abeer K Alorabi; Ahmed Subeh Alshrari; Mohammad Tauseef; Abida; Saleh I Alaqel; Ozair Alam; Md Afroz Bakht

doi:10.3390/ph14080710

Innovations and Patent Trends in the Development of USFDA Approved Protein Kinase Inhibitors in the Last Two Decades

Pharmaceuticals (Basel). 2021 Jul 22;14(8):710. doi: 10.3390/ph14080710.

Authors

Mohd Imran¹, Syed Mohammed Basheeruddin Asdaq², Shah Alam Khan³, Dhanalekshmi Unnikrishnan Meenakshi³, Abdulhakeem S Alamri^{4

5}, Walaa F Alsanie^{4

5}, Majid Alhomrani^{4

5}, Yahya Mohzari⁶, Ahmed Alrashed⁷, Mohammed AlMotairi⁸, Eman H Alkhaldi⁹, Abeer K Alorabi¹⁰, Ahmed Subeh Alshrari¹¹, Mohammad Tauseef¹², Abida¹, Saleh I Alaqel¹, Ozair Alam¹³, Md Afroz Bakht¹⁴

Affiliations

¹ Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Northern Border University, Arar 91911, Saudi Arabia.
² Department of Pharmacy Practice, College of Pharmacy, AlMaarefa University, Dariyah, Riyadh 13713, Saudi Arabia.
³ College of Pharmacy, National University of Science and Technology, Muscat 130, Oman.
⁴ Department of Clinical Laboratory Sciences, The Faculty of Applied Medical Sciences, Taif University, Taif 21944, Saudi Arabia.
⁵ Centre of Biomedical Sciences Research (CBSR), Deanship of Scientific Research, Taif University, Taif 21944, Saudi Arabia.
⁶ Clinical Pharmacy Department, King Saud Medical City, Riyadh 12746, Saudi Arabia.
⁷ Pharmaceutical Services Administration, Inpatient Department, Main Hospital, King Fahad Medical City, Riyadh 11564, Saudi Arabia.
⁸ Department of Clinical Pharmacy, King Fahad Medical City, Riyadh 11564, Saudi Arabia.
⁹ Pharmaceutical Care Services, King Saud Medical City, Riyadh 12746, Saudi Arabia.
¹⁰ Pharmaceutical Care Services, King Salman Specialist Hospital, Hail 55471, Saudi Arabia.
¹¹ Department of Biological Sciences, Faculty of Science, Northern Border University, Arar 91431, Saudi Arabia.
¹² Department of Pharmaceutical Sciences, College of Pharmacy, Chicago States University, Chicago, IL 60607, USA.
¹³ Medicinal Chemistry and Molecular Modelling Lab., Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India.
¹⁴ Department of Chemistry, College of Science and Humanities, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.

Abstract

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.

Keywords: USFDA; cancer; generic product; inflammation; patent review; protein kinase inhibitors.

Publication types

Review