Inhibitors Approved for Clinical Use

It has been estimated that approximately 30% of current R&D spend in pharmaceutical companies is focused on the development of kinase inhibitors. Protein kinases have become one of the pharmaceutical industry’s most important class of drug target.

To date, 121 drugs targeting protein kinases have been clinically approved (see table below or as a PDF to view structures at a higher resolution). They include Gleevec, an inhibitor of the Bcr-Abl tyrosine kinase, which has transformed chronic myelogenous leukaemia from a disease that was rapidly fatal into a manageable condition.

Abemaciclib
Advanced (metastatic) breast cancer
2017 FDA
Abrocitinib
Atopic dermatitis
2022 FDA
Acalabrutinib
Mantle cell lymphoma, CLL
2017 FDA 2018 EMA
Afatinib
NSCLC with EGFR mutations
2013 FDA 2013 EMA
Alectinib
NSCLC with ALK translocations
2014 Japan 2015 FDA 2017 EMA
Almonertinib
Advanced mutation +ve NSCLC
2020 China
Alpelisib
Breast cancer, HR+ve, HER2-ve
2019 FDA
Amivantamab
NSCLC
2021 FDA
Apatinib
Gastric cancer, NSCLC
2014 China 2018FDA
Asciminib
Chronic myelogenous leukemia
2021 FDA
Avapritinib
PDGFR exon 18 mutation (incl D842V)+ve
2020 FDA
Axitinib
Renal Cell Carcinoma
2012 FDA, EMA, MHRA, TGA
Baricitinib
Rheumatoid arthritis
2017 EMA, 2018 FDA
Binimetinib
BRAF mutant melanoma
2018 FDA 2018 EMA
Bosutinib
Chronic Myelogenous Leukemia
2012 FDA, 2013 EMA
Brigatinib
ALK-rearranged metastatic NSCLC
2017 FDA 2018 EMA
Cabozantinib
Medullary Thyroid Cancer
2012 FDA
Capivasertib
HR+ and PI3K mutation breast cancer
2023 FDA
Capmatinib
MET mutation+ve NSCLC
2020 FDA
Catequentinib
NSCLC
2018 China
Ceritinib
NSCLC with ALK translocations
2014 FDA 2015 EMA
Cetuximab
EGFR colorectal cancer
2004 FDA 2004 EMA
Cobimetinib
Melanoma, breast cancer
2015 FDA 2015 EMA
Copanlisib
Follicular lymphoma
2017 FDA
Crizotinib
NSCLC with Alkmutation
2011 FDA
Dabrafenib
Skin cancer
2013 FDA
Dacomitinib
NSCLC with EGFR mutations
2018 FDA 2019 EMA
Dasatinib
Chronic Myelogenous Leukemia, ALL
2006 FDA, EMA
Defactinib
Solid tumours
2022 FDA
Delgocitinib
Atopic dermatitis
2020 Japan
Deucravacitinib
Psoriasis
2022 FDA
Duvelisib
CLL, SLL, FL
2018 FDA
Encorafenib
BRAF mutant melanoma
2018 FDA 2018 EMA
Entrectinib
ROS1+ve NSCLC, solid tumors NTRK+ve
2019 FDA
Erdafitinib
Advanced metastatic urothelial carcinoma
2019 FDA
Erlotinib
Pancreatic Cancer
2004 NSCLC
Everolimus
Renel Cell Carcinoma
2009 FDA
Fasudil
Cerebral Vasospasm PAH
1995 Japan, China
Fedratinib
myelofibrosis
2019 FDA 2021EMA
Filgotinib
Rheumatoid arthritis
2020 EMA 2020 Japan
Flumatinib
Chronic myelogenous leukemia
2019 China
Fostamatinib
Autoimmune thrombocyto-penia
2018 FDA 2020 EMA
Fostamatinib
Chronic immune thrombocytopenia
2018 FDA
Fruquintinib
Metastatic colorectal cancer
2018 China
Furmonertinib
NSCLC
2021 China
Futibatinib
Cholangiocarcinoma
2022 FDA
Gefitinib
NSCLC
2002 Japan, 2003 FDA
Gilteritinib
Acute myeloid leukemia FLT3 mutant
2018 FDA 2019 EMA 2021 China
Ibrutinib
Mantle cell lymphoma
2013 FDA 2013 EMA
Icotinib
NSCLC
2012 China
Idelalisib
chronic lymphocytic leukemia
2014 FDA 2014 EMA
Imatinib
Chronic Myelogenous Leukemia
2001 FDA
Infigratinib
Cholangiocarcinoma
2021 FDA
Ivosidenib
Acute myeloid leukemia (AML) and cholangiocarcinoma
2018 FDA, 2023 EMA
Lapatinib
Breast Cancer
2007 FDA
Larotrectinib
Solid tumours with NTRK fusions
2018 FDA
Lazertinib
NSCLC
2021 S.Korea
Leniolisib
APDS PASLI disease
2019 FDA
Lenvatinib
Thyroid cancer (DTC) kidney cancer
2015 FDA 2015 EMA
Lorlatinib
ALK+ve met NSCLC
2018 FDA 2019 EMA
Margetuximab
MHER2-positive breast cancer
2020 FDA
Midostaurin
Acute myeloid leukemia (FLT3 mutation-positive)
2017 FDA 2017 EMA
Mobocertinib
NSCLC with EGFR mutations
2021 FDA
Necitumumab
NSCLC
2015 FDA 2015 EMA
Neratinib
HER2-positive breast cancer
2017 FDA 2018 EMA
Netarsudil
Glaucoma (topical)
2017 FDA
Nilotinib
Chronic Myelogenous Leukemia
2007 FDA
Nimotuzumab
cell carcinomas of the head and neck
2014 China, India
Nintedanib
Idiopathic pulmonary fibrosis
2014 FDA 2014 EMA
Olaratumab
Soft tissue sarcoma
2016 DFA 2016 EMA
Olmutinib
T790M+ve NSCLC
2016 S.Korea
Orelabrutinib
mantle cell lymphoma CLL, SLL
2020 China
Osimertinib
T790M+ve NSCLC
2015 FDA 2016 EMA
Pacritinib
Myelofibrosis
2022 FDA
Palbociclib
Advanced (metastatic) breast cancer
2015 FDA 2016 EMA
Panitumumab
EGFR colorectal cancer
2006 FDA 2007 EMA
Paxalisib
Malignant glioblastoma
2020 FDA
Pazopanib
Renal cancer
2009 FDA, 2010 EMA, MHRA, TGA
Peficitinib
Rhematoid arthritis
2021 Japan
Pemigatinib
Cholangiocarcinoma with FGFR2 fusion 
2020 FDA
Pertuzumab
HER2-positive breast cancer
2012 FDA 2013 EMA
Pexidartinib
Tenosynovial giant cell tumour
2019 FDA
Pirtobrutinib
Mantle Cell Lymphoma
2023 FDA
Ponatinib
Chronic Myelogenous Leukemia, ALL
2012 FDA
Pralsetinib
Met RET fusion +ve NSCLC MTC
2020 FDA
Pyrotinib
Breast cancer
2020 China
Quizartinib
Acute myeloid leukemia
2019 Japan, 2023 FDA
Radotinib
Chronic Myelogenous Leukemia
2012 FDA
Ramucirumab
MNSCLC colorectal cancer
2014 FDA 2014 EMA
Regorafenib
Clorectal Cancer GIST, HCC
2012 FDA
Ribociclib
Advanced (metastatic) breast cancer HR+, HER2-ve
2017 FDA 2017 EMA
Ripasudil
Glaucoma ocular hypertension
2014 Japan
Ripretinib
Advanced GIST Mastocytosis
2020 FDA
Ritlecitinib
Severe alopecia
2023 FDA
Ruxolitinib
Myelofibrosis
2011 FDA, 2012 EMA
Savolitinib
Adenocarcinoma, NSCLC
2021 China
Selpercatinib
NSCLC, MTC, thyroid cancers
2020 FDA
Selumetinib
Neurofibromatosis type 1
2020 FDA
Simotinib
Solid tumours
2018 China
Sirolimus
Kidney Transplantation
1999 FDA
Sorafenib
Renal Cancer HCC
2005 FDA, 2006 EMA
Sotorasib
KRAS non-small-cell lung cancer
2021 FDA, 2022 EMA
Sunitinib
Renal Cancer, Imatinib resistant GIST
2006 FDA
Surufatinib
Advanced pancreatic NET
2021 China
Temsirolimus
Advanced Renal Cell Carcinoma
2007 FDA, EMA
Tenalisib
PTCL, brest cancer
2019 FDA
Tepotinib
Metastatic NSCLC
2020 Japan 2021 FDA
Tirabrutinib
Chronic myelogenous leukemia
2020 Japan
Tirbanibulin
Actinic keratosis
2020 FDA
Tivozanib
Advanced RCC
2017 EMA
Tofacitinib
Rheumatoid arthritis
2012 FDA 2017 EMA
Trametinib
M-Melanoma with BRAFV600E
2013 FDA 2014 EMA
Trastuzumab
EGFR breast cancer
1998 FDA 2000 EMA
Trilaciclib
SCLC chemo myelopreservation
2021 FDA
Tucatinib
HER2-positive breast cancer
2020 FDA 2021EMA
Umbralisib
Marginal zone lymphoma
2019 FDA
Upadacitinib
Rheumatoid arthritis
2019 FDA 2019 EMA
Vandetanib
Thyroid Cancer
2011 FDA
Vemurafenib
Metastatic Melanoma BRAFV600E
2011 FDA, 2012 EMA
Volasertib
Acute myeloid leukemia
2014 FDA
Zanubrutinib
mantle cell lymphoma
2019 FDA
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The current global market for kinase therapies is about US$20 billion per annum, forecast to increase markedly. There are over 100 small-molecule kinase inhibitors active in late stages of clinical development and many more are likely to be approved in the coming years.

Transparent image to prevent safari browser adding its own map to the image Image of a human body showing the internal organs. Lists of approved drugs point to where they take effect Vandetanib Cabozantinib Sorafenib Lenvatinib Selpercatinib Lapatinib Everolimus Abemaciclib Neratinib Ribociclib Tucatinib Sorafenib Regorafenib Lenvatinib Cabozantinib Pemigatinib Ivosidenib Infigratinib Erlotinib Everolimus Sunitinib Vemurafenib Trametinib Dabrafenib Cobimetinib Binimetinib Encorafenib Erlotinib Crizotinib Afatinib Dabrafenib Ceritinib Gefitinib Alectinib Dacomitinib Osimertinib Brigatinib Trametinib Entrectinib Selpercatinib Pralsetinib Capmatinib Mobocertinib Tepotinib Sotorasib Lorlatinib Sorafenib Sunitinib Everolimus Pazopanib Axitinib Lenvatinib Cabozantinib Tivozanib Imatinib Sunitinib Regorafenib Avapritinib Ripretinib Vandetinib Regorafenib

As only about 10% of kinases have been studied in detail there is still much to understand on the roles that protein kinases play in human health and disease.

We believe that development of kinase inhibitors will remain at the forefront of medicine for the foreseeable future.