Vorolanib (CM-082)

Mechanism of action

From the NCI Drug Dictionary: An orally available small molecule dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth factor receptors (PDGFRs) with antiangiogenic and antineoplastic activities. Vorolanib inhibits all isoforms of VEGFR and PDGFR, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. Both VEGFRs and PDGFRs are receptor tyrosine kinases that may be upregulated in various tumor cell types. VEGFR/PDGFR dual kinase inhibitor X-82 has been shown to reduce tissue toxicity by 95 percent compared with first-generation kinase inhibitors.

Preliminary data

Renal cell carcinoma

1. Sherman SI, Wirth LJ, Droz JP, Hofmann M, Bastholt L, Martins RG, Licitra L, Eschenberg MJ, Sun YN, Juan T, Stepan DE, Schlumberger MJ; Motesanib Thyroid Cancer Study Group. Motesanib diphosphate in progressive differentiated thyroid cancer. N Engl J Med. 2008 Jul 3;359(1):31-42. link to original article PubMed

Also known as

• Code names: CM-082, X-82