Protein Kinase Inhibitors
From the Blue Ridge Institute for Medical Research in Horse Shoe, North Carolina USA
There are 93 FDA-approved small molecule protein kinase inhibitors as of 08 August 2026 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.
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, and netarsudil, an eye-drop.
Click on the images to view a larger version.
Structurea, name, trade name, company, formula, molecular wt
D/Ab
Drug
ALogPc: cLogDd
Rings/
Rotatable bonds
Yeare
Known Targets
Indicationsf
FDA Label
1/9
2.61/2.12
6/5
2020
PDGFR
GIST with PDGFR exon 18 mutations; systemic mastocytosis
2/11
Avutometinib
2.68/1.96
4/7
2025
MEK1/2
Second-line treatment of KRAS mutant low grade serous ovarian carcinoma
3/7
Binimetinib
3.01/3.81
3/6
2018
MEK1/2
BRAF V600E/K mutant melanoma or BRAFV600E mutant NSCLC in combination with encorafenib
2/7
5.54/4.65
4/8
2016
RET, Met, VEGFR1/2/3, Kit,TrkB,
Flt3, Axl, Tie2, ROS1
RCC; HCC; differentiated thyroid cancer; pancreatic and extrapancreatic neuroendocrine tumors
3/8
6.36/3.38
4/9
2014
ALK, IGF-1R, InsR, ROS1
ALK+ NSCLC as first-line treatment or after crizotinib resistance
3/5
3.78/2.73
4/4
2015
MEK1/2
Melanoma with BRAF V600E/K mutations; histiocytic neoplasms
3/6
5.04/0.95
4/5
2011
ALK, c-Met (HGFR), ROS1, MST1R
2/11
5.36/5.10
4/6
2013
B-Raf
BRAF mutation-positive (i) melanoma (V600E/K), (ii), NSCLC (V600E), (iii) anaplastic thyroid cancer (V600E), (iv) solid tumors (V600E), and (v) low grade glioma
3/9
3.31/3.74
4/7
2006
BCR-Abl, EGFR, Src, Lck, Yes, Fyn, Kit, EphA2, PDGFRβ
Ph+ CML or ALL
3/13
Defactinib
2.40/0.75
3/8
2025
FAK
Second-line treatment of KRAS mutant low grade serous ovarian carcinoma
3/10
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
3/8
5.03/4.87
6/7
2019
ROS1+ NSCLC; solid tumors with NTRK fusion proteins
4/14
3.09/-0.52
4/10
2018
Syk, Spleen tyrosine kinase
Second-line treatmenet of chronic immune thrombocytopenia
1/7
Futibatinib
1.78/1.77
4/6
2022
FGFR2
Cholangiocarcinomas with FGFR2 fusions or other rearrangements
Approval withdrawn in the USA, but it is approved in dozens of countries. US FDA approval reinstated 15 July 2015.
1/8
4.28/3.64
4/8
2003-2005, 2015
EGFR
NSCLC
1/6
4.22/3.63
5/5
2013
Bruton tyrosine kinase
CLL; Waldenström macroglobulinemia; small lymphocytic lymphoma; graft vs. host disease
2/7
4.59/3.80
5/7
2001
BCR-Abl, Kit, PDGFR
Ph+ CML or ALL, aggressive systemic mastocytosis, CEL, DFSP, HES, GIST, MDS/MDP
2/9
6.36/5.35
5/6
2007
BCR-Abl, PDGFR, DDR1
First-line and second-line treatment of Ph+ CML
2/7
3.62/2.57
5/8
2014
FGFR1/2/3, PDGFRα/β, VEGFR1/2/3, Flt3
Idiopathic pulmonary fibrosis; interstitial lung disease
2/7
4.51/3.01
4/10
2015
EGFR T970M
NSCLC with an EGFR (i) exon 19 deletion, (ii) exon 21 substitution, or (iii) a T790M mutation
2/8
2.97/1.30
5/5
2015
CDK4/6
2/8
3.14/3.55
4/5
2009
VEGFR1/2/3, PDGFRα/β, FGFR1/3, Kit, Lck, Fms, Itk
RCC, soft tissue sarcomas
1/8
3.66/1.80
5/6
2020
FGFR2
Cholangiocarcinomas with FGFR2 gene fusions or other rearrangements; myeloid neoplasms with FGFR1 rearrangement
3/9
Pirtobrutinib
3.43/3.35
3/7
2023
BTK
Mantle cell lymphoma, chronic lymphocytic leukemia, and small lymphocytic lymphoma
1/8
4.66/4.54
5/6
2012
BCR-Abl, BCR-Abl T315I, VEGFR, PDGFR, FGFR, EphR, Src family kinases, Kit, RET, Tie2, Flt3
3/8
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
Colorectal cancer; HCC; GIST
2/8
Remibrutinib
3.0/3.29
4/9
2025
BTK
Chronic spontaneous uricaria in adults who remain symptomatic despite H1 antihistamine treatment
2/6
Repotrectinib
2.55/2.17
3/5
2023
ROS1/TRKA
1/4
3.47/2.48
4/4
2011
JAK1/2
Myelofibrosis; polycythemia vera; graft vs. host disease; atopic dermatitis and vitiligo (applied topically)
1/9
3.28/3.11
8/5
2020
RET
RET gene fusion (i) NSCLC, (ii) thyroid cancer, (iii) solid tumors; RET mutant medullary thyroid cancer
3/7
5.55/4.34
3/5
2005
B/C-Raf, B-Raf (V600E), Kit, Flt3, RET, VEGFR1/2/3, PDGFRβ
Hepatocellular carcinoma, RCC, DTC
1/5
1.54/1.19
3/3
2012
JAK1/3
Rheumatoid arthritis; psoriatic arthritis; ulcerative colitis; ankylosing spondylitis; juvenile idiopathic arthritis
2/7
2.72/2.29
6/3
2021
CDK4/6
Myelosuppression prior to treatment of small cell lung cancer with cytotoxic therapy
2/8
5.09/5.25
6/6
2020
ErbB2/HER2
2/6
2.91/0.85
4/3
2019
JAK1
Rheumatoid arthritis; psoriatic arthritis; atopic dermatitis; ulcerative colitis
1/7
Vandetanib
4.43/2.14
4/6
2011
EGFRs, VEGFRs, RET, Brk, Tie2,
EphRs, Src family kinases
Medullary thyroid cancer
2/7
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
2/5
4.22/3.42
5/6
2019
Bruton tyrosine kinase
Mantle cell lymphoma; marginal zone lymphoma; follicular lymphoma; chronic lymphocytic leukemia; small lymphocytic lymphoma; Waldenström macroglobulinemia
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, 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.
For reviews of the first 80 US FDA-approved drugs, see the following:
Properties of FDA-approved small molecule protein kinase inhibitors: A 2024 update. Pharmacol. Res. (2024) 200, 107059.
See Excel files to download below:
Same information on the 93 FDA-approved drugs for sorting
Additional information on the 93 FDA-approved small molecule inhibitors
The advantage of the spreadsheet format is that one can sort by molecular weight, year approved, number of hydrogen-bond donors, etc.
List of all protein kinase inhibitors in clinical trials.
To report updates or errors, please email
Posted 9 December 2012. Updated 11 August 2026.