An update of new small-molecule anticancer drugs approved from 2015 to 2020

Area of Science:

• Oncology
• Pharmacology
• Medicinal Chemistry

Background:

• Cancer incidence necessitates novel therapeutic strategies.
• Drug development has focused on targeted therapies with improved efficacy and reduced toxicity.

Purpose of the Study:

• To review the landscape of newly approved small-molecule anticancer drugs from 2015-2020.
• To categorize these drugs based on their anti-tumor target activities.
• To highlight the significance of protein tyrosine kinase (PTK) inhibitors in cancer treatment.

Main Methods:

• Comprehensive literature review of approved anticancer drugs.
• Categorization of drugs by mechanism of action (e.g., TKIs, MAPK inhibitors, CDK inhibitors).
• Summary of drug structures, approval status, applications, SAR, and synthesis routes.

Main Results:

• 56 new small-molecule anticancer drugs approved between 2015-2020.
• Drugs categorized into ten target activity groups, including TKIs (30), MAPK inhibitors (3), CDK inhibitors (3), PARP inhibitors (3), PI3K inhibitors (3), SMO receptor antagonists (2), AR antagonists (2), SSTR inhibitors (2), IDH inhibitors (2), and others (6).
• Protein tyrosine kinase (PTK) inhibitors represent the largest class (30/56) and have significantly advanced cancer treatment due to potency and lower toxicity.

Conclusions:

• The review provides a comprehensive overview of recent anticancer drug approvals.
• PTK inhibitors have emerged as a pivotal class, demonstrating a paradigm shift in cancer therapy.
• This summary serves as a valuable resource for designing future targeted anticancer agents.