Generic Name | Brand Name | Kinase Target | Use | In vitro Transporter Interaction |
---|---|---|---|---|
Afatinib | Gilotrif | EGFT, HER2, HER4 | NSCLC | ABCB1 substrate and inhibitor |
Alectinib | Alecensa | ALK, RET | ALK-positive, metastatic NSCLC | May inhibit ABCB1 and ABCG2 |
Axitinib | Inlyta | VEGFR 1-3 | Renal Cell Cancer, advanced | ABCB1 inhibitor, but not at therapeutic levels |
Bosutinib | Bosulif | BCR-ABL, Src, Lyn, Hck | CML, resistant | |
Cabozantinib | Cometriq, Cabometyx | RET, MET, VEGFR 1-3, KIT, TRKB, FLT-3, AXL, ROS1, TYRO3, MER, and TIE2 | Metastatic medullary thyroid cancer, Renal cell cancer | MRP2 Substrate |
Ceritinib | Zykadia | ALK, IGF-1R, InsR, and ROS1 | ALK-positive, metastatic NSCLC | ABCB1 substrate |
Cobimetinib | Cotellic | MEK1 and MEK2 | Melanoma with BRAF mutations V600E or V600K | ABCB1 substrate |
Crizotinib | Xalkori | ALK, HGFR, c-Met, c-Ros, RON | Metastatic NSCLC | ABCB1 inhibitor |
Dabrafenib | Tafinlar | BRAF, CRAF, SIK1, NEK11, LIMK1 | Melanoma or NSCLC with BRAF mutation | ABCB1, ABCG2 substrate, ABCG2 inhibitor |
Dasatinib | Sprycel | BCR-ABL, Src, LCK, YES, FYN, c- KIT, EPHA2, and PDGFRβ | Philadelphia chromosome positive CML and ALL | ABCB1 substrate |
Erlotinib | Tarceva | EGFR | Metastatic NSCLC, Pancreatic Cancer | |
Gefitinib | Iressa | EGFR, IGF, PDGF | Metastitic NSCLC with EGFR mutation | ABCB1 substrate |
Ibrutinib | Imbruvica | BTK | Mantle Cell Lymphoma, CLL, SLL, Waldenström’s macroglobulinemia, marginal zone lymphoma, chronic Graft vs. host disease | May inhibit ABCB1 and ABCG2 |
Idelalisib | Zydelig | PI3Kδ | Relapsed CLL, Follicular B-cell non- Hodgkin lymphoma, SLL | ABCB1, ABCG2 substrate, ABCB1 inhibitor |
Imatinib | Gleevec | BCR-ABL, c-Kit, PDGF, SCF | Philadelphia chromosome positive CML and ALL, myelodysplastic/myeloproliferative diseases associated with PDGFR gene rearrangements, aggressive systemic mastocytosis, hypereosinophilic syndrome, chronic eosinophilic leukemia, dermatofibrosarcoma protuberans, GIST | |
Lapatinib | Tykerb | EGFR, HER2 | Breast Cancer, Her2 positive | ABCB1 and ABCG2 inhibitor |
Lenvatinib | Lenvima | VEGFR 1-3, FGFR 1-4, PDGFR, c- Kit, RET | Differentiated Thyroid Cancer, Renal Cell Cancer | ABCB1 and ABCG2 substrate, ABCB11 inhibitor |
Nilotinib | Tasigna | BCR-ABL, PDGFR, c-KIT, CSF-1R,and DDR1 | Philadelphia chromosome positive CML | ABCB1 inhibitor |
Niraparib | Zejula | PARP1 and -2 | Ovarian, fallopian tube, or primary peritoneal cancer | Weak ABCG2 inhibitor; ABCB1 and ABCG2 substrate |
Olaparib | Lynparza | PARP 1-3 | Recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer, advanced ovarian cancer | ABCG2 and ABCB1 inhibitor, ABCB1 substrate |
Osimertinib | Tagrisso | EGFR, HER 2-4, ACK1, and BLK | Metastatic, EGFR mutated, NSCLC | ABCG2 and ABCB1 substrate, ABCG2 inhibitor |
Palbociclib | Ibrance | CDK4/6 | Breast Cancer, Hormone Receptor positive, Her2 negative | Weak ABCB1 and ABCG2 inhibitors |
Pazopanib | Votrient | VEGFR 1-3, FGFR 1,3, Kit, Itk, Lck, c-Fms, PDGFRβ | Renal Cell Cancer, Soft tissue sarcoma | ABCB1 and ABCG2 substrate |
Ponatinib | Iclusig | ABL, BCR-ABL, VEGFR, PDGFR, FGFR, SRC, KIT, RET, TIE2, and FLT3 | CML, ALL | ABCB1, ABCG2, and ABCB11 inhibitor |
Regorafenib | Stivarga | RET, VEGFR 1-3, KIT, PDGFR, PDGFRβ, FGFR1-2, TIE2, DDR2, TRKA, Eph1A, RAF-1, BRAF, SAPK2, PTK5, Abl, CSF1R | Colorectal Cancer, GIST, hepatocellular carcinoma | ABCG2 inhibitor |
Ribociclib | Kisqali | CDK4/6 | Breast Cancer, Hormone Receptor positive, Her2 negative | ABCG2, ABCB11 inhibitor |
Rucaparib | Rubraca | PARP 1-3 | Ovarian Cancer, Advanced | ABCB1, ABCG2 substrate and inhibitor, ABCC4 inhibitor at ultra- therapeutic concentrations |
Ruxolitinib | Jakafi | JAK1 and 2 | myelofibrosis, polycythemia vera | |
Sorafenib | Nexavar | c-CRAF, BRAF, KIT, FLT-3, RET, RET/PTC, VEGFR 1-3, PDGFRβ | Renal Cell carinoma, hepatocellular carcinoma, refractory thyroid carcinoma | ABCB1 inhibitor |
Sunitinib | Sutent | PDGFR and β, c-Ki, FLT3, CSF- 1R, RET, VEGFR2 | GIST, renal cell carcinoma, pancreatic neuroendocrine tumors | |
Tofacitinib | Xeljanz | JAK1-3, | Rheumatoid arthritis | |
Trametinib | Mekinist | MEK1-2 | Malignant Melanoma or NSCLC with BRAF mutation | ABCB1, ABCB11 substrate |
Vandetanib | Caprelsa | EGFR, VEGFR, RET, BRK, TIE2, EPHR, Src | Medullary thyroid cancer | ABCB1 inhibitor |
Vemurafenib | Zelboraf | BRAF, CRAF, ARAF, SRMS, ACK1, MAP4K5, and FGR | Melanoma or Erheim-Chester Disease with BRAF V600 mutation | ABCB1 and ABCG2 substrate and inhibitor |
ALL, acute lymphocytic leukemia; AML, acute myeloid leukemia; CLL, chronic lymphocytic leukemia; CML, chronic myeloid leukemia; EGFR, EGR receptor; GIST, gastrointestinal stromal tumor; NSCLC, non-small cell lung cancer; SLL, small lymphocytic leukemia; VEGFR VEGF receptor.