Table 1.
MERTK inhibitors in preclinical development
| Name | Primary Target(s)* | Other Targets | Therapeutic Modality | Malignancies Targeted |
|---|---|---|---|---|
| Mer590 | MERTK | Monoclonal antibody | NSCLC (Cummings, et al., 2014) | |
| ELB031 | MERTK, TYRO3 | Monoclonal antibody | Not reported | |
| UNC569 | MERTK | AXL, TYRO3, FLT3, MAPKAPK2, RET | Small-molecule kinase inhibitor | ALL, AML, AT/RT (Christoph, et al., 2013; Koda, et al., 2018; J. Liu, et al., 2012) |
| UNC1062 | MERTK | AXL, TYRO3, FLT3 | Small-molecule kinase inhibitor | Melanoma, NSCLC, rhabdoid tumors, AML (Koda, et al., 2018; J. Liu, et al., 2013; Schlegel, et al., 2013) |
| UNC1666 | MERTK, FLT3 | AXL, TYRO3 | Small-molecule kinase inhibitor | AML (Lee-Sherick, et al., 2015) |
| UNC2025 | MERTK, FLT3 | AXL, TYRO3, TRKA, TRKC | Small-molecule kinase inhibitor | ALL, AML, NSCLC, GBM, melanoma (Cummings, et al., 2015; DeRyckere, et al., 2017; McDaniel, et al., 2018; Sinik, et al., 2019; Sufit, et al., 2016; W. Zhang, et al., 2014) |
| UNC2250 | MERTK | AXL, TYRO3 | Small-molecule kinase inhibitor | Rhabdoid tumors, NSCLC, MCL (Shi, et al., 2018; W. Zhang, et al., 2013) |
| UNC2541 | MERTK | AXL, TYRO3, FLT3 | Small-molecule kinase inhibitor | Not reported |
| UNC3133 | MERTK, FLT3, AXL | TYRO3, FGFR1, ITK, KDR, PDGRα, TRKA, AURKA, p70S6K | Small-molecule kinase inhibitor | Not reported |
| LDC1267 | MERTK, AXL, TYRO3, MET, Aurora B | LCK, SRC | Small-molecule kinase inhibitor | Metastatic melanoma, metastatic breast cancer (Paolino, et al., 2014) |
| CT413 | MERTK, AXL, MET, RON | Small-molecule kinase inhibitor | Not reported | |
| Compound-52 | MERTK | Small-molecule kinase inhibitor | Not reported | |
| 6g | MERTK, AXL, MET, TYRO3 | Small-molecule kinase inhibitor | Not reported | |
| GSK2606414 | MERTK, AXL, PERK, C-KIT, Aurora B, BRK, MLK2, DDR2, MLCK2, IKKe, TRKC, MLK3, RET, LCK, NEK4, KHS, MLK1, TRKA, TRKB, YES, WNK2 | Small-molecule kinase inhibitor | Pancreatic cancer (Axten, et al., 2012) | |
| JNJ-28312141 | MERTK, FLT3, AXL, MCSFR, KIT, TRKA, LCK | TYRO3 | Small-molecule kinase inhibitor | Adenocarcinoma, AML (Manthey, et al., 2009) |
| BMS-777607 | MERTK, FLT3, AXL, TYRO3, RON, MET, AURB, LCK | Small-molecule kinase inhibitor | Prostate cancer, breast cancer, ovarian cancer, glioblastoma, pancreatic cancer (Dai & Siemann, 2010; Kasikara, et al., 2019; Onken, et al., 2016; Sharma, et al., 2014; C. C. Wu, Weng, Hsu, & Chang, 2019; Zeng, et al., 2014) | |
| RXDX-106 | MERTK, TYRO3, AXL, c-MET | Small-molecule kinase inhibitor | Gastric cancer (Kim, et al., 2017) | |
| SA4488 | MERTK | Small-molecule kinase inhibitor | Lung cancer (Pyo, et al., 2019) | |
| SGI-7079 | MERTK, FLT3, TRKB, RET, TRKA, YES, AXL, MET, JAK2, KDR, JNK3, ABL | TAO1, AURORA, TAK1, SYK, RSK1, CHK2, EPHA1, LCK, GSK3β, EPHB1, FYN, FGFR1 | Small-molecule kinase inhibitor | Breast Cancer (X. Wang, et al., 2013) |
| NPS-1034 | AXL, MET | MERTK, FLT3, KIT, DDR1, TYRO3 | Small-molecule kinase inhibitor | Lung Cancer (Rho, et al., 2014) |
*
Primary targets included are no less selective than 10-fold MERTK activity based on biochemical/enzymatic IC50