From the Blue Ridge Institute for Medical Research in Horse Shoe, North Carolina USA

There are 94 FDA-approved small molecule protein kinase inhibitors as of 30 October as compiled by Robert Roskoski Jr.

To download an Excel file with the same information that can be used for sorting, click here. For additional information on the FDA-approved small molecule inhibitors, click here. 

Structurea, name, trade name, company, formula, molecular wt. The figures are drawn is such a fashion that the left-most portion of the drug extends toward or into the solvent, and the right side of the molecule interacts with hinge residues and hydrophobic components of target protein kinases, except for everolimus, sirolimus, and temsirolimus which bind to FKBP12 and indirectly inhibit mTOR. All drugs are effective orally, except for temsirolimus and trilaciclib, which are given intravenously, netarsudil, an eye-drop, and delgocitinib, a topical ointment.

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 D/Ab Drug

ALogPc:

cLogDd

 Rings/Rotatable bonds Yeare Known

targets

 Indicationsf FDA Label
1/9 Abemaciclib

4.94/3.76

 5/7 2017 CDK4/6 HR+, HER breast Ca For the label click here
2/6 Abrocitinib

1.25/0.79

3/6 2022 JAK1 Atopic dermatitis For the label, click here
2/6 Acalabrutinib

3.31/2.56

 5/4 2017 Bruton tyrosine kinase Mantle cell lymphoma, CLL, SLL For the label click here
2/8 Afatinib

4.39/3.76

 4/8 2013 and 2016 EGFR, ErbB2, ErbB4 NSCLC (2013), squamous NSCLC (2016)

For the label click here
1/5 Alectinib

4.77/4.89

 6/3 2015 ALK and RET ALK+ NSCLC For the label click here
3/6 Asciminib

3.46/3.86

4/6 2021 BCR-Abl Ph+ CML For the label click here
1/9 Avapritinib

2.61/2.12

 6/5 2020 PDGFR, Kit GIST with PDGFR exon 18 mutations For the label click here
2/11 Avutometinib

2.68/1.96

4/7 2025 MEK1/2 Second-line treatment of KRAS mutant low grade serous ovarian carcinoma For the label click here

2/4 Axitinib

4.64/4.15

 4/5 2012 VEGFR1/2/3, PDGFRβ RCC

For the label click here
1/7 Baricitinib

1.10/-0.19

 4/5 2018 JAK1/2 Rheumatoid arthritis For the label click here
3/6 Belumosudil

4.82/4.02

 5/7 2021 ROCK2 Graft vs. host disease For the label click here
3/7 Binimetinib

3.01/3.81

 3/6 2018 MEK1/2 BRAFV600E/K melanoma or BRAFV600E NSCLC with encorafenib For the label click here
1/8 Bosutinib

5.19/3.37

 4/9 2012 BCR-Abl, Src, Lyn, Hck CML

For the label click here
2/9 Brigatinib

5.09/2.49

 6/8 2017 ALK, ROS1, IGF-1R, Flt3, EGFR ALK+ NSCLC after crizotinib For the label click here
2/7 Cabozantinib

5.54/4.65

 4/8 2012

2016

 RET, Met, VEGFR1/2/3, Kit,TrkB, Flt3, Axl, Tie2, ROS1 Metastatic medullary thyroid cancer (2012) and advanced RCC (2016) and HCC (2019)

For the labels click here and here
4/6 Capivasertib

1.78

-0.16

 4/6 2023 AKT=PKB HER2-positive breast cancer For the label click here
1/6 Capmatinib

3.43/2.96

 5/4 2020 MET NSCLC with MET exon 14 skipping For the label click here

3/8 Ceritinib

6.36/3.38

 4/9 2014 ALK, IGF-1R, InsR, ROS1 ALK+ NSCLC as first-line treatment or after crizotinib resistance

For the label click here
3/5 Cobimetinib

3.78/2.73

 4/4 2015

MEK1/2

Melanoma with BRAF V600E/K mutations with vemurafenib

For the label click here
3/6 Crizotinib

5.04/0.95

 4/5 2011 ALK, c-Met (HGFR), ROS1, MST1R ALK+ NSCLC (2011) and ROS1+ NSCLC (2016) For the label click here

2/11 Dabrafenib

5.36/5.10

 4/6 2013 B-Raf Melanoma (V600K/E), NSCLC (V600E), and anaplastic thyroid cancers (V600E) with BRAF mutations For the label click here
2/7 Dacomitinib

5.16/3.53

 4/7 2018 EGFR/ErbB2/ErbB4 EGFR-mutated NSCLC For the label click here
3/9 Dasatinib

3.31/3.74

 4/7 2006 BCR-Abl, EGFR, Src, Lck, Yes, Fyn, Kit, EphA2, PDGFRβ Ph+ CML or ALL For the label click here
3/13 Defactinib

2.40/0.75

3/8 2025 FAK Second-line treatment of KRAS mutant low grade serous ovarian carcinoma For the label click here
1/5 Delgocitinib

1.30/0.6

4/2 2025 JAK1/2/3, TYK2 Used topically for hand eczema For the label click here
3/8 Deucravacitinib

 

4/7 2022 TYK2 Psoriasis For the label click here
1/4 Deuruxolitinib

3.47/2.48

4/4 2024 JAK2/1 Alopecia areata For the label click here
3/10 Encorafenib

3.91/2.61

 3/10 2018 B-RafV600E/K B-RafV600E/K mutant melanoma or B-RafV600E mutant NSCLC with binimetinib; mutant CRC with cetuximab For the label click here
3/8 Ensartinib

4.72/3.26

4/6 2024 ALK ALK-positive NSCLC For the label click here
3/8 Entrectinib

5.03/4.87

 6/7 2019 ROS1+ NSCLC; solid tumors with NTRK fusion proteins TRKA/B/C, ROS1, ALK For the label click here
1/7 Erdafitinib

4.18/1.25

 4/9 2019 FGFR1/2/3/4 Urothelial (bladder) carcinoma For the label click here
1/7 Erlotinib

3.41/3.20

 3/11 2004 EGFR NSCLC and pancreatic cancer For the label click here
3/14 Everolimus

6.20/7.40

 3/9 2009 FKBP12/mTOR HER2-negative breast cancer, PNET, RCC, RAML, SEGA For the label click here
3/9 Fedratinib

4.82/3.23

 3/9 2019 JAK2 Myelofibrosis For the label click here
4/15 Fostamatinib

3.09/-0.52

 4/10 2018 Syk, Spleen tyrosine kinase Second-line treatmenet of chronic immune thrombocytopenia For the label click here
1/7 Fruquintinib

2.86

2.64

4/5 2023 VEGFR2 Metastatic colorectal cancer For the label click here
1/7 Futibatinib

1.78/1.54

4/6 2022 FGFR2 Cholangiocarcinoma

Bile duct cancer with FGFR2 fusions or other rearrangements

 For the label click here

Approval withdrawn in the USA, but it is approved in dozens of countries. US FDA approval reinstated 15 July 2015.
1/8 Gefitinib

4.28/3.64

 4/8 2003-2005, 2015 EGFR NSCLC with exon 19 deletions or exon 21 substitutions For the label click here
3/10 Gilteritinib

2.70/1.69

 5/9 2018 FLT3 AML patients with FLT3 mutation5 For the label click here
1/6 Ibrutinib

4.22/3.63

 5/5 2013 Bruton tyrosine  kinase Mantle cell lymphoma,  CLL, Waldenstrom's macroglobulinemia, graft vs.host disease (2017). For the label click here
2/7 Imatinib

4.59/3.80

 5/7 2001 BCR-Abl, Kit, PDGFR Ph+ CML or ALL, aggressive systemic mastocytosis, CEL, DFSP, HES, GIST, MDS/MDP For the label click here
2/8 Infigratinib

5.35/3.99

4/8 2021 FGFR2/1/3/4 Cholangiocarcinomas with FGFR2 fusions or other rearrangements For the label click here
2/9 Lapatinib

6.14/4.40

 5/11 2007 EGFR, ErbB2 Breast cancer For the label click here
2/7 Larotrectinib

2.95/2.44

 5/3 2018 NTRK Solid tumors with NTRK gene fusion proteins For the label click here
2/9 Lazertinib

4.1/3.6

5/10 2024 Mutant EGFR NSCLC with ex19 del or ex21 L848R substitutions For the label click here
3/5 Lenvatinib

4.07/2.52

 4/6 2015 VEGFRs, FGFRs, PDGFR, Kit, RET DTC For the label click here 
1/7 Lorlatinib

2.80/1.62

 3/0 2018 ALK ALK-positive NSCLC For the lable click here

1/4 Midostaurin

5.91/5.43

 8/3 2017 Flt3 Flt3 mutation + acute myeloid leukemia and mastocytosis For the label click here
4/8 Mirdametinib

2.64/3.98

2/7 2025 MEK1/2 Neurofibromatosis type 1

von Recklinghausen disease

 For the label click here
2/9 Mobocertinib

5.08/3.79

 4/13 2021 EGFR with exon 20 insertions NSCLC For the label click here
2/7 Momelotinib

2.98/2.70

4/6 2023 JAK1/2 Myelofibrosis patients with anemia For the label click here
2/8 Neratinib

5.93/3.05

 4/11 2017 ErbB2/HER2 HER2+ breast cancer For the label click here
2/5 Netarsudil

4.89/3.42

 4/8 2018 Rho kinase Glaucoma For the label click here
2/9 Nilotinib

6.36/5.35

 5/6 2007 BCR-Abl, PDGFR, DDR1 First-line and second-line treatment of Ph+ CML For the label click here
2/7 Nintedanib

3.62/2.57

 5/8 2014

FGFR1/2/3, PDGFRα/β, VEGFR1/2/3, Flt3

Idiopathic pulmonary fibrosis

 For the label click here
2/7 Osimertinib

4.51/3.01

 4/10 2015 EGFR T970M NSCLC with exon 19 deletions or exon 21 substitutions For the label click here
1/7 Pacritinib

4.96/3.11

4/4 2022 JAK2 Myelofibrosis For the label click here
2/8 Palbociclib

2.97/1.30

 5/5 2015 CDK4/6 ER+ and HER2 breast cancer as first-line (2015) and second-line therapy (2016) For the label click here
2/8 Pazopanib

3.14/3.55

 4/5 2009 VEGFR1/2/3, PDGFRα/β, FGFR1/3, Kit, Lck, Fms, Itk RCC, soft tissue sarcomas For the label click here
1/8 Pemigatinib

3.66/1.80

 5/6 2020 FGFR1/2/3 Cholangiocarcinoma with a FGFR2 fusions or other rearrangements For the label click here
2/7 Pexidartinib

5.23/4.55

 4/5 2019

CSFR1/Kit/Flt3

 Tenosynovial giant cell tumors For the label click here
3/9 Pirtobrutinib

3.43/3.51

3/7 2023 BTK Mantle cell lymphoma, chronic lymphocytic leukemia, small lymphocytic lymphoma For the label click here

1/8 Ponatinib

4.66/4.54

 5/6 2012 BCR-Abl, BCR-Abl T315I, VEGFR, PDGFR, FGFR, EphR, Src family kinases, Kit, RET, Tie2, Flt3 Ph+ CML or ALL For the label click here
3/9 Pralsetinib

4.20/3.64

5/8 2020 RET RET fusion-positive NSCLC; RET mutant medullary thyroid cancer; RET fusion-positive thyroid cancer For the label click here
2/9 Quizartinib

5.66/5.05

6/8 2023 Flt3 FLT3 tadem internal duplication positive AML For the label click here
3/8 Regorafenib

5.69/4.49

 3/5 2012 VEGFR1/2/3, BCR-Abl, B-Raf, B-Raf(V600E), Kit, PDGFRα/β, RET, FGFR1/2, Tie2, 
Eph2A		 CRC, GIST, HCC For the label click here
2/8 Remibrutinib

3.0/ 3.29

4/9 2025 BTK Chronic spontaneous uricaria in adults who remain symptomatic despite H1 antihistamine treatment For the label click here
2/6 Repotrectinib

2.55

2.17

3/0 2023 ROS1/TRKA ROS1-positive NSCLC For the label click here
2/7 Ribociclib

2.80/0.91

 5/5 2017 CDK4/6 HR+-EGFR metastatic breast cancer with an aromatase inhibitor For the label click here
1/11 Rilzabrutinib

4.42/3.44

 7/8 2025 BTK Chronic immune thrombocytopenia For the label click here
3/5 Ripretinib

5.67/4.48

 5/4 2020 Kit/PDGFRa Gastrointestinal stromal tumors For the label click here
2/4 Ritlecitinib

 

3/3 2023 JAK3 Alopecia areata For the label click here
1/4 Ruxolitinib

3.47/2.48

 4/4 2011 JAK1/2 Myelofibrosis, PV, graft vs. host disease, and atopic dermatitis (September 2021) For the label click here and here
1/9 Selpercatinib

3.28/3.11

 8/5 2020 RET RET lung & thyroid cancers For the label click here
3/6 Selumetinib

3.53/4.27

 6/3 2020 MEK1/2 Neurofibromatosis type 1

von Recklinghausen disease

 For the label click here
3/13 Sirolimus

6.18/7.45

 3/6 1999 FKBP12/mTOR Renal transplant, lymphangioleiomyomatosis For the label click here
3/7 Sorafenib

5.55/4.34

 3/5 2005 B/C-Raf, B-Raf (V600E), Kit, Flt3, RET, VEGFR1/2/3, PDGFRβ Hepatocellular carcinoma, RCC, DTC For the label click here
3/4 Sunitinib

3.33/1.28

 3/7 2006 PDGFRα/β, VEGFR1/2/3, Kit, Flt3, CSF-1R, RET RCC, GIST, PNET For the label click here
4/9 Sunvozertinib

4.472.84

4/10 2025 EGFR/HER2 Exon 20 mutant EGFR NSCLC For the label click here
2/6 Taletrectinib

4.43/1.9

4/7 2025 ROS1, TRK1/2/3 Rearranged mutant ROS1 NSCLC For the label click here
4/16 Temsirolimus

4.39/?

 3/11 2007 FKBP12/mTOR Advanced RCC For the label click here
7/7 Tepotinib

4.01/2.26

5/7 2021 Met Met mutation-positive NSCLC For the label click here
2/6 Tivozanib

5.64/4.16

4/6 2021 VEGFR2 Third-line treatment of RCC For the label click here
1/5 Tofacitinib

1.54/1.19

 3/3 2012 JAK1/3 Rheumatoid arthritis, psoriatic arthritis, ulcerative colitis For the label click here
3/11 Tovorafenib

3.98/2.99

3/5 2024 B/C-Raf Pediatric low grade gliomas For the label click here

2/6 Trametinib

3.94/3.18

 4/5 2013 MEK1/2
BRAFV600E/K mutant melanoma; BRAFV600E mutant NSCLC		 For the label click here
2/7 Trilaciclib

2.72/2.29

 6/3 2021 CDK4/6

 

Chemotherapy-induced myelosuppression when administered prior to a platinum/etoposide-containing regimen or topotecan-containing regimen for extensive-stage small cell lung cancer

 

 For the label click here
2/8 Tucatinib

5.09/5.25

 6/6 2020 ErbB2/HER2 HER2 + breast cancer For the label click here
2/6 Upadacitinib

2.91/0.85

 4/3 2019 JAK1 Rheumatoid arthritis, psoriatic arthritis, atopic dermatitis For the label click here
1/7 Vandetanib

5.00/2.81

 4/6 2011 EGFRs, VEGFRs, RET, Brk, Tie2, EphRs, Src family kinases Medullary thyroid cancer For the label click here
2/7 Vemurafenib

5.54/4.61

 4/7 2011 A/B/C-Raf, B-Raf (V600E), SRMS, ACK1, MAP4K5, FGR Melanoma with BRAFV600E mutation and Erdheim-Chester disease

For the label click here
1/6 Vimseltinib

3.56/2.20

4/6 2025 CSF1R Tenosynovial giant cell tumors For the label click here
2/5 Zanubrutinib

4.22/3.42

 5/6 2019 Bruton tyrosine kinase Mantle cell lymphoma For the label click here
2/9 Zongertinib

4.42/3.8

6/7 2025 ErbB2/HER2 Mutant HER2 NSCLC For the label click here

aStructures drawn with Accelrys Draw 4.1, Accelrys, Inc. San Diego, CA 92121. 

bD, number of hydrogen bond donors; A, number of hydrogen bond acceptors.

cAtom-based calculated log of the partition coefficient; dCalculated log of the distribution coefficient at pH 7.4. Values for ALogP and cLogD from https://www.ebi.ac.uk/chembl/.  The partition coefficient (P) is the solubility where pH is not taken into account. The distribution coefficient (D) is the ratio of a compounds solubility in n-octanol/water at pH 7.4.

eYear approved 

fALL, acute lymphoblastic leukemia, AML, acute myelogenous leukemia; CEL, chronic eosinophilic leukemia; CLL, chronic lymphocytic leukemia; CML, chronic myelogenous leukemia; CRC, colorectal cancer; DDR1, Discoidin domain receptor family, member 1; DFSP, dermatofibrosarcoma protuberans; DTC, differentiated thyroid carcinoma; GIST, gastrointestinal stromal tumor; HER2, HER2 negative; HES, hypereosinophilic syndrome, HGFR, hepatocyte growth factor recepter; MDS/MPD, myelodisplastic/myeloproliferative diseases; MST1R, macrophage-stimulating protein receptor aka RON (Recepteur d'Origine Nantais); NSCLC, non-small cell lung cancer; PNET, progressive neuroendocrine tumors of pancreatic origin; Ph+, Philadelphia chromosome positive;  PV, polycythemia vera; RAML, renal angiomyolipoma; RCC, renal cell carcinoma; SEGA, subependymal giant cell astrocytoma; SLL small lymphocytic lymphoma. See the drug label for specifics. For example, one indication for everolimus is for postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer in combination with exemestane after failure of treatment with letrozole or anastrozole. Ponatinib, Regorafenib, Ruxolitinib, Sirolimus, Sorafenib, Sunitinib, Temsirolimus

For reviews of the the first 62 US FDA-approved drugs see the following three papers by clicking on the journal title. Properties of FDA-approved small molecule protein kinase inhibitors. Pharmacol. Res (2019) 144, 19-50, Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update. Pharmacol Res. (2020) 152, 104609, and Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update, Pharmacol Res. (2022) 175, 106037; A 2023 update, Pharmacol. Res. (2023) 187 106552. A 2024 update, Pharmacol. Res. (2024) 200, 107059. A 2025 update, Pharmacol Res. (2025) 216, 107713.

To download an Excel file with the same information on the 88 FDA approved drugs that can be used for sorting, click here. For additional information on the 88 FDA-approved small molecule inhibitors, click here. The advantage of the spreadsheet format is that one can sort by molecular weight, year approved, number of hydrogen-bond donors, etc. 

For a list of all protein kinase inhibitors in clinical trials, go to https://www.icoa.fr/pkidb/

To report updates or errors, please e-mail webmaster@brimr1.org

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Posted 9 December 2012 and updated 30 October 2025

Visitors since 9 December 2012