Table 1.

Summary of HGF/c-Met inhibitors in clinical development

Compound NameTypeCompanyTarget(s)Phase of Development
AMG102 (76)AntibodyAmgenhuman HGFPhase I/II
MetMAb (23, 54, 77)Monovalent antibodyGenentechhuman c-MetPhase I
ARQ197 (23, 59, 60)Selective kinase inhibitor, non-ATP competitiveArQulec-MetPhase I/II
JNJ-38877605 (61)Selective kinase inhibitor, ATP competitiveJohnson and Johnsonc-MetPhase I
PF-04217903 (62)Selective kinase inhibitor, ATP competitivePfizerc-MetPhase I
SGX523 (63)Selective kinase inhibitor, ATP competitiveSGX Pharmaceuticalsc-MetDiscontinued*
PF-02341066 (23, 66)Multikinase inhibitor, ATP competitivePfizerc-Met, ALKPhase I/II
XL184 (71, 72)Broad-spectrum kinase inhibitor, ATP competitiveExelixisc-Met, VEGFR1-3, Ret, Kit, Flt-3, Tie-2PhaseI/II/III
XL880 (67, 69, 78, 79)Broad-spectrum kinase inhibitor, ATP competitiveExelixisc-Met, Ron, VEGFR1-3, PDGFR, Kit, Flt-3, Tie-2Phase I/II
MP470 (23, 73)Broad-spectrum kinase inhibitor, ATP competitiveSuperGenc-Met, Ret, Rad51, mutant forms of Kit, PDGFR, Flt-3Phase I
MGCD265 (74)Broad-spectrum kinase inhibitor, ATP competitiveMethylgenec-Met, VEGFR1-3, Tie-2, Ron, Kit, Flt-3Phase I
MK-2461 (75)Broad-spectrum kinase inhibitorMerckc-Met, KDR, FGFR1-3, and Flt 1,3,4.Phase I/II
  • NOTE: Inhibitor clinical development information current as of November 2008 from the United States National Institutes of Health registry of federally and privately supported clinical trials conducted in the United States and around the world. [Available from: http://www.clinicaltrials.gov].

    Abbreviations: HGF, hepatocyte growth factor; ALK, anaplastic lymphoma kinase; VEGFR, vascular endothelial growth factor receptor; Ret, rearranged during transfection; Flt-3, FMS-like tyrosine kinase 3; Tie-2, angiopoietin receptor 2; Ron, recepteur d'origine nantais; PDGFR, platelet-derived growth factor receptor; Rad51, E. coli RecA homolog; KDR, kinase insert domain receptor; FGFR1-3, fibroblast growth factor receptor 1–3.

  • * Clinical development of SGX523 was discontinued by the company as of May 2008 after initial Phase I trials. [Available from: http://www.biospace.com/news_story.aspx?NewsEntityId=96099].