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Table 2 Summary of the basic profile of type II AXL inhibitors and the related ongoing clinical trials

From: AXL receptor tyrosine kinase as a promising anti-cancer approach: functions, molecular mechanisms and clinical applications

Drug Developer Target(s)a IC50 for AXL Clinical Trial No.b Phase of approval Indications Monotherapy/Combinations Adverse events Status
Cabozantinib (Cabometyx, XL184, BMS-907351, marketed as Cometriq) Exelixis/Ipsen company VEGFR2, MET, RET, KIT, AXL, FLT1/3/4 IC50 (in vitro) = 7 nM IC50 (in cells) = 42 nM NCT01908426 III Advanced HCC Monotherapy Fatigue, diarrhea, hypertension, palmar-plantar erythrodysesthesia syndrome Completed
NCT01865747 III Advanced or metastatic RCC Cabozantinib or Everolimus Completed
NCT01716715 II Persistent or recurrent epithelial ovarian, fallopian tube, or primary peritoneal carcinoma Cabozantinib vs. Paclitaxel Completed
     NCT00596648 Ib/II NSCLC ± Erlotinib   Completed
BMS-777607 (ASLAN002) Bristol-Myers Squibb/Aslan Pharmaceuticals AXL, RON, MET, Tyro3 IC50 (in vitro) = 1.1 nM NCT00605618 I/II Advanced solid tumors Monotherapy Not reported Completed
  NCT01721148 I Advanced solid tumors Monotherapy   Completed
LY2801653 (Merestinib) Eli Lilly and Company; Dana-Farber Cancer Institute TEK, MET, AXL, RON IC50 (in vitro) = 11 nM IC50 (in cells) = 2 nM NCT02711553 II Advanced or metastatic biliary tract cancer Ramucirumab or merestinib or placebo, + cisplatin and gemcitabine Not reported Active, not recruiting
  NCT02920996 II NSCLC Monotherapy   Recruiting
  NCT03027284 I Advanced and/or metastatic cancer ± Other anti-cancer agents   Active, not recruiting
Foretinib (XL880, EXEL-2880, GSK1363089) GSK MET, VEGFR2, TIE-2, VEGFR3, RON, AXL IC50 (in vitro) = 11 nM IC50 (in cells) < 100 nM NCT01147484 II Recurrent breast cancer Monotherapy Fatigue, hypertension, gastrointestinal toxicities, nonfatal pulmonary emboli Completed
NCT00726323 II RCC Monotherapy Completed
NCT00920192 I HCC Monotherapy Completed
MGCD516 (Sitravatinib) Mirati Therapeutics Inc. DDR2, EPHA3, AXL, MER, VEGFR3 IC50 (in vitro) = 1.5 nM IC50 (in cells) = 250–800 nM NCT03680521 II Clear cell RCC + Nivolumab Not reported Recruiting
  NCT02219711 I/Ib Advanced solid tumors Monotherapy   Recruiting
MGCD265 (Glesatinib) Mirati Therapeutics MET, RON, VEGFR1/2/3, AXLc Not reported NCT02544633 II NSCLC with genetic alterations in MET Monotherapy Diarrhea, rash, fatigue Completed
NCT00697632 I Advanced malignancies Monotherapy   Completed
NCT00975767 I NSCLC + Erlotinib/docetaxel   Terminated
RXDX-106 (CEP-40783) Ignyta, Inc. AXL, MET, Tyro3, MER IC50 (in vitro) = 7 nM NCT03454243 I Advanced or metastatic solid tumors Monotherapy Not reported Terminated
Rebastinib (DCC-2036) Deciphera Pharmaceuticals LLC ABL, FLT3, VEGFR2, TIE-2, Lyn, SRC, FGR, AXL IC50 (in vitro) = 42 nM NCT03717415 I/II Locally advanced or metastatic solid tumor + Carboplatin Dry mouth, constipation, fatigue, muscular weakness, headache, nausea, blurred vision Recruiting
NCT00827138 I CML Monotherapy   Completed
NPS-1034 NeoPharm AXL, MET IC50 (in vitro) = 10.3 nM IC50 (in cells) < 0.5 μM Preclinical
LDC1267 Lead Discovery Centre MER, Tyro3, AXL IC50 (in vitro) = 29 nM IC50 (in vivo) = ~ 15 μM Preclinical
  1. Abbreviations: NSCLC non-small cell lung cancer, RCC renal cell carcinoma, CML chronic myelogenous leukemia, HCC hepatocellular carcinoma
  2. aIn the order of inhibition potency
  3. bAll the relevant information of clinical trials can be found on the public clinical trial registry website (clinicaltrials.gov). Here is a partial list of all the relevant clinical trials
  4. cData for AXL not reported