Approved and investigational kinase inhibitors, with target genes and mechanism of action.
| Drug ↑ | Synonyms | Target kinase gene(s) | Group ↕ | Approval ↕ | Indication | Inhibitor type |
|---|---|---|---|---|---|---|
| Abemaciclib | Verzenio | CDK4, CDK6 | CMGC | FDA Approved | Breast cancer | ATP-competitive inhibitor |
| Abrocitinib | Cibinqo | JAK1 | TK | FDA Approved | Atopic dermatitis | Type I inhibitor |
| Acalabrutinib | Calquence | BTK | TK | FDA Approved | CLL, MCL | Covalent irreversible |
| Adagrasib | Krazati | KRAS G12C (GTPase, non-kinase but co-targets downstream kinase signaling) | N/A - GTPase | FDA Approved | NSCLC, CRC (KRAS G12C) | Covalent inhibitor |
| Afatinib | Gilotrif | EGFR, ERBB2, ERBB4 | TK | FDA Approved | NSCLC | Covalent irreversible |
| Alectinib | Alecensa | ALK, RET | TK | FDA Approved | NSCLC | Type I inhibitor |
| Alpelisib | Piqray | PI3K alpha (PIK3CA) | PIKK-related lipid kinase | FDA Approved | Breast cancer (PIK3CA-mutant) | ATP-competitive inhibitor |
| Asciminib | Scemblix | ABL1 (STAMP inhibitor) | TK | FDA Approved | CML | Allosteric inhibitor |
| Avapritinib | Ayvakit | KIT, PDGFRA (D842V) | TK | FDA Approved | GIST | Type I inhibitor |
| Axitinib | Inlyta | VEGFR1-3 | TK | FDA Approved | RCC | Type II inhibitor |
| Baricitinib | Olumiant | JAK1, JAK2 | TK | FDA Approved | Rheumatoid arthritis, alopecia areata | Type I inhibitor |
| Belumosudil | Rezurock | ROCK2 (RHOA-associated kinase) | AGC | FDA Approved | Chronic GVHD | ATP-competitive inhibitor |
| Binimetinib | Mektovi | MEK1/2 (MAP2K1/2) | STE | FDA Approved | Melanoma | Allosteric inhibitor |
| Bosutinib | Bosulif | ABL1, SRC | TK | FDA Approved | CML | Type I inhibitor |
| Brigatinib | Alunbrig | ALK, ROS1, EGFR | TK | FDA Approved | NSCLC | Type I inhibitor |
| Cabozantinib | Cabometyx, Cometriq | MET, VEGFR2, RET, KIT, AXL | TK | FDA Approved | RCC, HCC, thyroid cancer | Type II inhibitor |
| Capmatinib | Tabrecta | MET | TK | FDA Approved | NSCLC (METex14) | Type Ib inhibitor |
| Ceritinib | Zykadia | ALK | TK | FDA Approved | NSCLC | Type I inhibitor |
| Cobimetinib | Cotellic | MEK1/2 (MAP2K1/2) | STE | FDA Approved | Melanoma | Allosteric inhibitor |
| Copanlisib | Aliqopa | PI3K alpha/delta | PIKK-related lipid kinase | FDA Approved | Follicular lymphoma | ATP-competitive inhibitor |
| Crizotinib | Xalkori | ALK, ROS1, MET | TK | FDA Approved | NSCLC | Type I inhibitor |
| Dabrafenib | Tafinlar | BRAF (V600E/K) | TKL | FDA Approved | Melanoma, NSCLC | Type I inhibitor |
| Dacomitinib | Vizimpro | EGFR, ERBB2, ERBB4 | TK | FDA Approved | NSCLC | Covalent irreversible |
| Dasatinib | Sprycel | ABL1, SRC, KIT, PDGFRB | TK | FDA Approved | CML, ALL | Type I inhibitor |
| Deucravacitinib | Sotyktu | TYK2 (allosteric, pseudokinase domain) | TK | FDA Approved | Psoriasis | Allosteric inhibitor |
| Duvelisib | Copiktra | PI3K delta/gamma | PIKK-related lipid kinase | FDA Approved | CLL, follicular lymphoma | ATP-competitive inhibitor |
| Encorafenib | Braftovi | BRAF (V600E) | TKL | FDA Approved | Melanoma, CRC | Type I inhibitor |
| Entrectinib | Rozlytrek | NTRK1-3, ROS1, ALK | TK | FDA Approved | NTRK fusion cancers, NSCLC | Type I inhibitor |
| Enzastaurin | LY317615 | PKC-beta (PRKCB) | AGC | Investigational | Lymphoma | ATP-competitive inhibitor |
| Erdafitinib | Balversa | FGFR1-4 | TK | FDA Approved | Urothelial carcinoma | Type I inhibitor |
| Erlotinib | Tarceva | EGFR | TK | FDA Approved | NSCLC, pancreatic cancer | Type I inhibitor, reversible |
| Everolimus | Afinitor | mTOR (MTOR) | PIKK | FDA Approved | RCC, breast cancer, TSC | Allosteric inhibitor |
| Fasudil | Eril | ROCK1/2 | AGC | Approved (Japan) | Cerebral vasospasm | ATP-competitive inhibitor |
| Fedratinib | Inrebic | JAK2 | TK | FDA Approved | Myelofibrosis | Type I inhibitor |
| Fostamatinib | Tavalisse | SYK | TK | FDA Approved | Chronic ITP | Type I inhibitor (prodrug of R406) |
| Futibatinib | Lytgobi | FGFR1-4 | TK | FDA Approved | Cholangiocarcinoma | Covalent irreversible |
| Gefitinib | Iressa | EGFR | TK | FDA Approved | NSCLC | Type I inhibitor, reversible |
| Gilteritinib | Xospata | FLT3, AXL | TK | FDA Approved | AML (FLT3-mutant) | Type I inhibitor |
| Ibrutinib | Imbruvica | BTK | TK | FDA Approved | CLL, MCL, WM | Covalent irreversible |
| Idelalisib | Zydelig | PI3K delta (PIK3CD) | PIKK-related lipid kinase | FDA Approved | CLL, follicular lymphoma | ATP-competitive inhibitor |
| Imatinib | Gleevec, STI-571 | ABL1, KIT, PDGFRA, PDGFRB | TK | FDA Approved | CML, GIST | Type II inhibitor |
| Infigratinib | Truseltiq | FGFR1-3 | TK | FDA Approved | Cholangiocarcinoma | Type I inhibitor |
| Lapatinib | Tykerb | EGFR, ERBB2 | TK | FDA Approved | Breast cancer | Type I inhibitor |
| Larotrectinib | Vitrakvi | NTRK1-3 | TK | FDA Approved | NTRK fusion cancers | Type I inhibitor |
| Lenvatinib | Lenvima | VEGFR1-3, FGFR1-4, PDGFRA, KIT, RET | TK | FDA Approved | Thyroid cancer, HCC, RCC | Type I inhibitor |
| Lorlatinib | Lorbrena | ALK, ROS1 | TK | FDA Approved | NSCLC | Type I macrocyclic inhibitor |
| Midostaurin | Rydapt | FLT3, KIT, PDGFR, PKC | TK/AGC | FDA Approved | AML, systemic mastocytosis | Multi-kinase inhibitor |
| Momelotinib | Ojjaara | JAK1, JAK2, ACVR1 | TK | FDA Approved | Myelofibrosis with anemia | Type I inhibitor |
| Neratinib | Nerlynx | ERBB2, EGFR, ERBB4 | TK | FDA Approved | Breast cancer | Covalent irreversible |
| Netarsudil | Rhopressa | ROCK1/2 | AGC | FDA Approved | Glaucoma | ATP-competitive inhibitor |
| Nilotinib | Tasigna | ABL1, KIT, PDGFRB | TK | FDA Approved | CML | Type II inhibitor |
| Nintedanib | Ofev, Vargatef | VEGFR1-3, FGFR1-3, PDGFRA/B, FLT3, SRC | TK | FDA Approved | IPF, NSCLC | Type I triple angiokinase inhibitor |
| Osimertinib | Tagrisso | EGFR (T790M, C797S) | TK | FDA Approved | NSCLC | Covalent irreversible |
| Pacritinib | Vonjo | JAK2, FLT3, IRAK1 | TK | FDA Approved | Myelofibrosis | Type I inhibitor |
| Palbociclib | Ibrance | CDK4, CDK6 | CMGC | FDA Approved | Breast cancer | ATP-competitive inhibitor |
| Pazopanib | Votrient | VEGFR1-3, PDGFRA/B, KIT | TK | FDA Approved | RCC, soft tissue sarcoma | Type II inhibitor |
| Pemigatinib | Pemazyre | FGFR1-3 | TK | FDA Approved | Cholangiocarcinoma | Type I inhibitor |
| Pexidartinib | Turalio | CSF1R, KIT, FLT3 | TK | FDA Approved | Tenosynovial giant cell tumor | Type II inhibitor |
| Pirtobrutinib | Jaypirca | BTK | TK | FDA Approved | MCL, CLL | Non-covalent reversible |
| Ponatinib | Iclusig | ABL1 (incl. T315I), FGFR1-3, VEGFR2, SRC | TK | FDA Approved | CML, ALL | Type II inhibitor |
| Pralsetinib | Gavreto | RET | TK | FDA Approved | RET-altered cancers | Type I inhibitor |
| Quizartinib | Vanflyta | FLT3 | TK | FDA Approved | AML (FLT3-ITD) | Type II inhibitor |
| Regorafenib | Stivarga | VEGFR1-3, KIT, RET, RAF1, BRAF | TKL/TK | FDA Approved | CRC, GIST, HCC | Type II multi-kinase inhibitor |
| Ribociclib | Kisqali | CDK4, CDK6 | CMGC | FDA Approved | Breast cancer | ATP-competitive inhibitor |
| Ripretinib | Qinlock | KIT, PDGFRA | TK | FDA Approved | GIST | Switch-control inhibitor |
| Ritlecitinib | Litfulo | JAK3, TEC family kinases | TK | FDA Approved | Alopecia areata | Covalent irreversible |
| Ruxolitinib | Jakafi | JAK1, JAK2 | TK | FDA Approved | Myelofibrosis, PV, GVHD | Type I inhibitor |
| Selpercatinib | Retevmo | RET | TK | FDA Approved | RET-altered cancers | Type I inhibitor |
| Selumetinib | Koselugo | MEK1/2 (MAP2K1/2) | STE | FDA Approved | Neurofibromatosis type 1 | Allosteric inhibitor |
| Sirolimus | Rapamune, Rapamycin | mTOR (MTOR) | PIKK | FDA Approved | Immunosuppression, LAM | Allosteric inhibitor |
| Sorafenib | Nexavar | VEGFR2/3, PDGFRB, KIT, RAF1, BRAF | TKL/TK | FDA Approved | HCC, RCC, thyroid cancer | Type II multi-kinase inhibitor |
| Sotorasib | Lumakras | KRAS G12C (GTPase, non-kinase but co-targets downstream kinase signaling) | N/A - GTPase | FDA Approved | NSCLC (KRAS G12C) | Covalent inhibitor |
| Sotrastaurin | AEB071 | PKC (PRKCA, PRKCB, PRKCQ) | AGC | Investigational | Transplant rejection, psoriasis | ATP-competitive inhibitor |
| Sunitinib | Sutent | VEGFR1-3, PDGFRA/B, KIT, FLT3, RET | TK | FDA Approved | RCC, GIST, pNET | Type I multi-kinase inhibitor |
| Temsirolimus | Torisel | mTOR (MTOR) | PIKK | FDA Approved | RCC | Allosteric inhibitor |
| Tepotinib | Tepmetko | MET | TK | FDA Approved | NSCLC (METex14) | Type Ib inhibitor |
| Tofacitinib | Xeljanz | JAK1, JAK2, JAK3 | TK | FDA Approved | Rheumatoid arthritis, UC | Type I inhibitor |
| Trametinib | Mekinist | MEK1/2 (MAP2K1/2) | STE | FDA Approved | Melanoma, NSCLC | Allosteric inhibitor |
| Trilaciclib | Cosela | CDK4, CDK6 | CMGC | FDA Approved | Chemo-induced myelosuppression prevention | ATP-competitive inhibitor |
| Tucatinib | Tukysa | ERBB2 | TK | FDA Approved | Breast cancer | Type I inhibitor |
| Umbralisib | Ukoniq | PI3K delta, CK1 | PIKK-related lipid kinase / CMGC | Withdrawn (2022) | Marginal zone lymphoma | ATP-competitive inhibitor |
| Upadacitinib | Rinvoq | JAK1 | TK | FDA Approved | Rheumatoid arthritis, UC, atopic dermatitis | Type I inhibitor |
| Vandetanib | Caprelsa | RET, EGFR, VEGFR2 | TK | FDA Approved | Medullary thyroid cancer | Type I inhibitor |
| Vemurafenib | Zelboraf | BRAF (V600E) | TKL | FDA Approved | Melanoma | Type I inhibitor |
| Zanubrutinib | Brukinsa | BTK | TK | FDA Approved | MCL, CLL | Covalent irreversible |