Table 3 Properties of approved small-molecule inhibitors of serine/theonine kinases
From: Small molecules in targeted cancer therapy: advances, challenges, and future perspectives
Chemical structure | Name | Targets | Approved indications (year) | Corporation |
|---|---|---|---|---|
| Vemurafenib (Zelboraf) | BRAF | Melanoma (2011) | Roche/Genentech |
| Dabrafenib (Tafinlar) | BRAF/CRAF | Melanoma (2013) NSCLC (2017) ATC (2018) | Novartis/GlaxoSmithkline |
| Encorafenib (Braftovi) | BRAF | Melanoma (2018) | Array |
| Trametinib (Mekinist) | MEK1/2 | Melanoma (2013) NSCLC (2017) ATC (2018) | Novartis/GlaxoSmithkline |
| Cobimetinib (Cotellic) | MEK1/2 | Melanoma (2015) | Roche/Genentech/ Exelixis |
| Binimetinib (Balimek) | MEK1/2 | Melanoma (2018) | Array |
| Selumetinib (Koselugo) | MEK1/2 | Neurofibromatosis type 1 (2020) Plexiform neurofibromas (2020) | AstraZeneca/Merck |
| Palbociclib (Aiboxin) | CDK4/6 | Breast cancer (2015) | Pfizer |
| Ribociclib (Kisqali) | CDK4/6 | Breast cancer (2017) | Novartis |
| Abemaciclib (Verzenio) | CDK4/6 | Breast cancer (2017) | Lilly |
| Idelalisib (Zydelig) | PI3Kδ | CLL (2014) Follicular lymphoma (2014) | Gilead |
| Copanlisib (Aliqopa) | Pan-PI3K | Follicular lymphoma (2017) | Bayer |
| Duvelisib (Copiktra) | PI3Kγ/δ | CLL (2018) SLL (2018) Follicular lymphoma (2018) | Verastem |
| Alpelisib (Piqray) | PI3Kα | Breast cancer (2019) | Novartis |
| Temsirolimus (Torisel) | mTOR | RCC (2007) | Pfizer |
| Everolimus (Afinitor) | mTOR | RCC (2009) Pancreatic cancer (2011) Breast cancer (2012) | Novartis |
| Sirolimus (Rapamune) | mTOR | LAM (2015) | Pfizer |
