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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
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Molecular Cancer

ISSN: 1476-4598