Reported Approved for Reported Approved for Reported Approved for Name Structure Company Name Structure Company Name Structure Company target clinical use target clinical use target clinical use

1995 cerebral ARRAY Fasudil (Eril) ROCK1/2 Asahi Kasei Trametinib MEK1/2 GSK 2013 skin cancer Binimetinib MEK RAF 2018 melanoma vasospasm PAH Novartis

Sirolimus 1999 kidney 2013 NSCLC with Infinity mTOR Wyeth Pfizer Afatinib HER2 EGFR BI Duvelisib PI3K δ/ γ 2018 CLL SLL (Rapamune) transplantation EGFR mutations Verastem

2001 chronic Bruton's Bcr-Abl c- Janssen 2013 mantle cell 2018 NSCLC with Imatinib Novartis myelogenous Ibrutinib Tyrosine Dacomitinib EGFR Pfizer KIT PDGFR Pharmacyclic lymphoma, CLL EGFR mutations leukemia Kinase

2014 glaucoma 2018 acute Gefitinib EGFR AZ 2003 NSCLC Ripasudil ROCK Kowa Gilteritinib FLT3 AXL Astellas ocular hypertension myeloid leukemia

Genetech 2004 NSCLC 2014 NSCLC with 2018 cancer with Erlotinib EGFR Ceritinib ALK Novartis Larotrectinib NTRK LOXO Bayer Roche pancreatic cancer ALK translocations NTRK fusions

Multiple Gilead, 2014 chronic Tyrosine 2005 renal cancer Sorafenib Onyx Bayer Idelalisib PI3K δ Calistoga, lymphocytic Catequentinib VEGFRs Advenchen 2018 NSCLC kinases HCC ICOS leukemia, FL targeted Multiple 2006 renal cancer, VEGFR Tyrosine- 2014 idiopathic Sunitinib Sugen Pfizer Imatinib resistant Nintedanib PDGFR BI Lorlatinib ALK ROS Pfizer 2018 NSCLC kinases pulmonary fibrosis GIST FGFR targeted Multiple 2006 chronic Tyrosine- 2014 NSCLC with 2018 autoimmune Dasatinib BMS myelogenous Alectinib ALK Roche, Chugai Fostamatinib SYK Rigel kinases ALK translocations thrombocyto-penia leukemia , ALL targeted

2015 advanced EGFR 2019 urothelial Lapatinib GSK 2007 breast cancer Palbociclib CDK4/6 Pfizer (metastatic) breast Erdafitinib FGFR Astex Janssen ERBB2 cancer cancer

2007 chronic 2015 thyroid cancer Nilotinib Bcr-Abl Novartis myelogenous Lenvatinib VEGFRs Eisai (DTC), kidney Alpelisib PI3Kα Novartis 2019 breast cancer leukemia cancer

2007 advanced Temsirolimus mTOR Wyeth Pfizer renal cell Cobimetinib MEK Roche, Exelixis 2015 melanoma Pexidartinib CSF1R c-KIT Plexxikon 2019 TGCT carcinoma

2009 renal cell 2015 NSCLC with TRK ROS Everolimus mTOR Novartis Osimertinib EGFR AZ Entrectinib Ignyta Roche 2019 NSCLC carcinoma EGFR mutation ALK

VEGFR2 2016 NSCLC with 2019 rheumatoid Pazopanib PDGFR c- GSK 2009 renal cancer Olmutinib EGFR BI Upadacitinib JAK AbbVie EGFR mutation arthritis KIT 2017 advanced 2011 NSCLC with Crizotinib ALK MET Pfizer Ribociclib CDK4/6 Novartis (metastatic) breast Fedratinib JAK Celgene 2019 myelofibrosis Alk mutation cancer

Multiple Tyrosine 2011 thyroid 2017 NSCLC with TG 2019 marginal Vandetanib AZ Brigatinib ALK EGFR Ariad Umbralisib PI3Kδ kinases cancer EGFR mutation Therapeutic zone lymphoma targeted

2017 acute myeloid Bruton's Incyte 2019 mantle cell Ruxolitinib JAKs 2011 myelofibrosis Midostaurin FLT3 KIT Novartis leukemia Zanubrutinib Tyrosine Beigene Novartis lymphoma mastocytosis Kinase

2011 metastatic Roche 2017 breast cancer 2019 APDS PASLI Vemurafenib BRAF melanoma Neratinib EGFR Wyeth Pfizer Leniolisib PI3Kδ Novartis Plexxikon HER2 disease BRAFV600E

VEGFRs 2012 renal cell 2017 rheumatoid Axitinib PDGFRB c- Pfizer Baricitinib JAKs Incyte Eli Lilly Avapritinib PDGFR KIT Blueprint 2020 GIST carcinoma arthritis KIT

VEGFR2 2017 advanced 2012 colorectal ARRAY Onco- 2020 HER2 breast Regorafenib TIE2 others Bayer Abemaciclib CDK4/6 Eli Lilly (metastatic) breast Tucatinib HER2 cancer GIST, HCC thyreon cancer PTKs cancer

2020 2012 rheumatoid 2017 follicular cholangiocarcinom Tofacitinib JAKs Pfizer Copanlisib PI3K mTOR Bayer Pemigatinib FGFR2 Incyte arthritis lymphoma a with FGFR2 fusion

VEGFR2 2012 medullary 2017 glaucoma 2020 mNSCLC with Cabozantinib Exelixis Netarsudil ROCK Aerie Tabrecta MET Novartis PDGFR KIT thyroid cancer (topical) ex14 mutation

2012 chronic 2020 NSCLC MTC, Ponatinib SRC Abl Ariad myelogenous Tivozanib VEGFR EUSA Pharma 2017 RCC Selpercatinib RET Eli Lilly thyroid cancers leukemia, ALL

2012 chronic Bruton's AZ Acerta 2017 mantle cell 2020 GIST Bosutinib Bcr-Abl SRC Pfizer myelogenous Acalabrutinib Tyrosine Ripretinib KIT Deciphera Pharma lymphoma, CLL Mastocytosis leukemia Kinase

2012 chronic Jiangsu Bcr-Abl Kazia Radotinib Daewoong myelogenous Simotinib EGFR Simcere 2018 NSCLC Paxalisib PI3K mTOR 2020 Glioblastoma PDGFR Therapeutics leukemia Pharm.

ARRAY Dabrafenib BRAF GSK 2013 skin cancer Encorafenib MEK RAF 2018 melanoma Novartis