Table 2.
AXL and MER inhibitors in preclinical and clinical development
| Drug other names; developer |
Targets | Indications | Phase |
|---|---|---|---|
| Cabozantinib XL184, Cometriq®; Exelixis/Ipsen |
VEGFR2, MET, RET, AXL | Thyroid NSCLCa, RCC, other solid tumors |
MA II/III |
| Bosutinib SKI-606; Bosulif®; Pfizer |
BCR-ABL, SRC, AXL | CML breast, GBM, other solid tumors |
MA II |
| Glesatinib MGCD265; Mirati |
MET, VEGFR2, RON, AXL | NSCLCa, bladder, breast | II |
| Merestinib LY2801653; Eli Lilly |
RON, MET, AXL, FTL-3 | NSCLC, biliary tract | II |
| Gilteritinib ASP2215; Astellas Pharma |
AXL, FLT3 | NSCLCa (+EGFRi), AML | II |
| BMS-777607 ASLAN002; BMS/Aslan |
AXL, RON, MET, TYRO3, FLT3 | Solid tumors | I/II |
|
S49076 Servier |
MET, MER, AXL, FGFR1–3 | GBM (+VEGFi) NSCLCa (+EGFRi) |
I/II |
| BGB324 R428; BerGenBio |
AXL | AML, NSCLC (+EGFRi) | I/II |
| Sitravatinib MGCD516, Mirati |
VEGFR2, PDGFRA, AXL, MER, RET, MET, | NSCLCa, other solid tumors | I |
| DDR2, TRKA | |||
| Ningetinib HEC Pharm |
VEGFR2, MET, AXL, MER, FLT3, RON | GBM, other solid tumors | I |
| BPI-9016 M Betta Pharmaceuticals |
MET, AXL | Solid tumors | I |
| TP-0903 Tolero Pharmaceuticals |
AXL | – | Preclinical |
| ONO-9330547 Ono Pharmaceutical |
AXL, MER | – | Preclinical |
| SLC-0211 SignalChem Lifesciences |
AXL | – | Preclinical |
| NPS-1034 NeoPharm |
AXL, FLT3, KIT, MET, ROS1, TIE1 | – | Preclinical |
| LDC1267 Lead Discovery Center |
MER, TYRO3, AXL | – | Preclinical |
| UNC2250 University of N. Carolina |
MER | – | Preclinical |
| UNC2025 University of N. Carolina |
MER, FLT3, AXL, TYRO3 | – | Preclinical |
| RXDX106 Ignyta |
AXL, MER, TYRO3, MET | – | Preclinical |
Sources of information on clinical trials include ClinicalTrials.Gov (https://clinicaltrials.gov/) and TrialTrove (https://citeline.com/). Targets are listed in order of potency (most potently hit first) based on available information
MA market authorisation
aPatients selected based on high expression or genetic aberrations of AXL