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Journal Article

PMID

(26555154)

Authors

Myers SH, Brunton VG, Unciti-Broceta A

Title

AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.

Journal	Vol	Issue	Date	Pages	Journal Short Title
Journal of medicinal chemistry	59	8	2016 Apr 28	3593-608	J Med Chem

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Abstract Text

Dysregulation of the AXL receptor tyrosine kinase has been associated with many types of cancer. It has not been until recently, however, that targeting AXL has come under the spotlight because of ever accumulating evidence of its strong correlation with poor prognosis and drug resistance. The entry of the first AXL-branded inhibitor in clinical trials in 2013 marked an important milestone for the clinical validation of AXL as an anticancer target. Nevertheless, to weigh the current contribution and potential future impact of AXL inhibition in the clinic, it is fundamental to recognize that several kinase inhibitors approved or in clinical development have AXL as either a prominent secondary or even the primary target. Through this review, the chemical and biological properties of the main inhibitors targeting AXL (either intentionally or unintentionally) will be discussed, along with the prospects and challenges to translate AXL inhibitors into a bona fide therapeutic option.

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Molecular Profile	Treatment Approach
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Gene Name	Source	Synonyms	Protein Domains	Gene Description	Gene Role
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Therapy Name	Drugs	Efficacy Evidence	Clinical Trials
BMS-777607	BMS-777607	5	0
Bosutinib	Bosutinib	3	12
Glesatinib	Glesatinib	2	2

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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
BMS-777607		ASLAN002\|BMS777607\|BMS 777607	AXL Inhibitor 30 MET Inhibitor 59 RON Inhibitor 11 TYRO3 Inhibitor 7	BMS-777607 (ASLAN002) is a small molecule that inhibits MET, MST1R (RON), TYRO3, and AXL, resulting in decreased downstream pathway activation, potentially resulting in decreased tumor cell growth and metastasis (PMID: 19260711, PMID: 20515943, PMID: 24233399, PMID: 26555154).
Bosutinib	Bosulif	SKI-606\|PF-5208763	ABL Inhibitor (pan) 9 AXL Inhibitor 30 BCR-ABL Inhibitor 32 BTK inhibitor 38 SRC Inhibitor 31 TNK2 Inhibitor 7	Bosulif (bosutinib) inhibits SRC and ABL kinases and has additional activity against other kinases including AXL, TNK2, and BTK, resulting in decreased pathway activation and inhibition of tumor cell proliferation (PMID: 12543790, PMID: 19039322, PMID: 26555154). Bosulif (bosutinib) is FDA-approved for use in adult and pediatric patients 1 year of age and older with Ph+ (BCR-ABL) chronic myelogenous leukemia (FDA.gov).
Glesatinib		MGCD-265\|MGCD 265	AXL Inhibitor 30 MET Inhibitor 59 RON Inhibitor 11 VEGFR Inhibitor (Pan) 36	Glesatinib (MGCD265) inhibits several tyrosine kinases including MET (type II inhibitor), MST1R (RON), and AXL, as well as VEGFR1-3, and TIE2, which may result in decreased tumor growth (PMID: 25806189, PMID: 26555154, PMID: 32306194).

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Gene	Variant	Impact	Protein Effect	Variant Description	Associated with drug Resistance
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Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
AXL amp	lung non-small cell carcinoma	predicted - sensitive	Glesatinib	Phase I	Actionable	In a Phase I trial, a patient with non-small cell lung carcinoma harboring AXL amplification was sensitive to treatment with Glesatinib (MGCD265), demonstrating a 50% decrease in lesion size (PMID: 26555154).	26555154

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