Table 1.

TAM-selective inhibitors currently in development

NameTarget(s)Development stage
DP3975AxlPreclinical
LDC1267Axl, Tyro3, MerTKPreclinical
NA80×1AxlPreclinical
YW327.6S2AxlPreclinical
GL21.TAxlPreclinical
NPS-1034Axl, c-MetPreclinical
UNC1062MerTKPreclinical
UNC569MerTKPreclinical
BGB324AxlPhase I clinical trial for NSCLC (NCT02922777), AML (NCT02488408), and metastatic melanoma (NCT02872259)
BMS777607c-Met, Ron, Flt-3, Tyro3, MerTK, AxlPhase I clinical trial for advanced and/or metastatic solid tumors (NCT01721148)
Glesatinib (MGCD265)Axl, c-MetPhase II clinical trial for NSCLC patients with activating mutations in MET (NCT02544633)
Sunitinib (SU11248)Flt-3, Axl, VEGFR-2, KitApproved for pancreatic neuroendocrine and gastrointestinal stromal tumor and kidney cancer.
CabozantinibVEGFR-2, c-Met, Ret, Kit, Flt-3, AxlApproved for medullary thyroid cancer

NOTE: All are small-molecule inhibitors except YW327.6S2, which is an mAb, and GL21.T, which is an RNA aptamer.

  • Abbreviation: AML, acute myeloid leukemia.