Small- molecule kinase inhibitors have the potential for broad efficacy, convenience and tissue penetrance, and thus often offer important advantages over biologics
| No. | Brand | Drug | Target Kinase | Marketed by | First Approved | Cancer Indication |
| 14. | Filgotinib | Jyseleca | JAK 1 | Galapagos NV | 2020 | Filgotinib is a selective inhibitor of JAK1 and was approved in both the European Union and Japan in September 2020, for the treatment of moderate to severe active rheumatoid arthritis in adults who have responded inadequately to, or who are intolerant to one or more disease‑modifying anti‑rheumatic drugs (DMARDs). |
| 13. | Delgocitinib | Corectim® | JAK 1/2/3 | Japan Tobacco Inc. / Torii Pharmaceutical | 2020 | Delgocitinib is a JAK inhibitor approved in Japan for the treatment of atopic dermatitis in patients 16 years of age or older. |
| 12. | Peficitinib | Smyraf ® | JAK | Astellas | 2019 | Peficitinib was approved Japan the treatment of rheumatoid arthritis. |
| 11. | Upadacitinib | Rinvoq® | JAK1 | Abbvie | 2019 | On August 2019, FDA approved fedratinib to treat adults with moderately to severely active rheumatoid arthritis. |
| 10. | Fostamatinib | Tavalisse® | SYK | Rigel Pharmaceuticals | 2018 | Indicated for the treatment of chronic immune thrombocytopenia (ITP) in adult patients who have had an insufficient response to a previous treatment. |
| 9. | Baricitinib | Olumiant | JAK 1/2 | Eli Lilly | 2017 | Indicated for the treatment of moderate to severe active rheumatoid arthritis in adult patients who have responded inadequately to, or who are intolerant to one or more disease-modifying anti-rheumatic drugs as monotherapy or in combination with methotrexate. |
| 8. | Netarsudil | Rhopressa | Aerie Pharmaceutical | 2017 | On December 18, 2017, the FDA approved netarsudil to treat glaucoma or ocular hypertension | |
| 7. | Nintedanib | Ofev | FLT 1/3/4 / FGFR1/2/3 | Boehringer Ingelheim | 2014 | Nintedanib is indicated for the treatment of idiopathic pulmonary fibrosis (IPF). |
| 6. | Ripasudil | Glanatec | ROCK 1/2 | Kowa Company, Ltd. | 2014 | Ripasudil is a prescription medicine used for the treatment of pressure in the eyes (ocular hypertension) and glaucoma. |
| 5. | Tofacitinib | Xeljanz | JAK1/2/3 / TYK2 | Pfizer | 2012 | For the treatment of moderate to severe rheumatoid arthritis which is resistant or intolerant to methotrexate therapy. |
| 4 | Everolimus | Zortress | mTOR | Novartis | 2009 | Everolimus is a Rapamycin derivative and is a medication used as an immunosuppressant to prevent rejection of organ transplants specially in Kidney Transplantation and in the treatment of renal cell cancer and other tumours. |
| 3 | Temsirolimus | Torisel | mTOR | PF Prism CV (Pfizer Subisidary) | 2007 | Temsirolimus is a is a derivative and prodrug of sirolimus (Rapamycin) developed for the kidney transplantation, is an intravenous drug for the treatment of renal cell carcinoma, originally developed by Wyeth Pharmaceuticals and approved by the U.S. FDA in May 2007, and was also approved by the European Medicines Agency in November 2007. |
| 2 | Sirolimus | Rapamycin | mTOR | 1999 | Sirolimus is a macrolide compound that is used to coat coronary stents, prevent organ transplant rejection and treat a rare lung disease called lymphangioleiomyomatosis. | |
| 1 | Fasudil | ROCK1/2 | Asahi Kasei Pharma Corp | 1995 | Fasudil is a potent inhibitor of the Rho-kinases ROCK1 and ROCK2. Fasudil is a potent Rho-kinase inhibitor and vasodilator. Since it was discovered, it has been used for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage, It has been approved for use in Japan and China since 1995, but has not been approved by the United States Food and Drug Administration or by the European Medicines Agency. |
