Review Article

Tumor Lymphangiogenesis as a Potential Therapeutic Target

Table 5

Clinical trials of tyrosine kinase inhibitors on the VEGF pathway.

DrugsClinical trialsTargetReferences

PTK787/ZK 222584 (chloroanilino-pyridylmethyl phthalazine succinate)Phase III for colorectal cancer Phase I, II for advanced hepatocellular carcinoma patients (in combination with intravenous doxorubicin)Target VEGFR-3, -2, -1, PDGFR-beta (need new strategies for trials to specifically monitor effects on metastasis)[210, 211]
CEP-7055 (N, N-dimethyl glycine ester)Phase I as an oral-administered therapy for various malignanciesTarget VEGFR-3, -2, -1[212]
BAY 43-9006 (Bi-aryl urea)Phase III for renal cell carcinoma
Phase II for multiple tumor types (e.g., prostate, ovarian, pancreatic, breast, and lung cancers…)
Target VEGFR-3, -2 tyrosine kinase, PDGFR-beta, FGFR-1[213]
JNJ-26483327Phase I for patients with advanced solid tumorsMultitargeted tyrosine kinase inhibitor, inhibiting kinase of (EGFR)-1, -2, -4; VEGFR-3, Src family (Lyn, Fyn, Yes)[214]
SU-014813Phase I for patients with advance solid tumorsOral multitargeted tyrosine kinase inhibitor[215]

(modified from the table in paper “Focus on lymphangiogenesis in tumor metastasis”- Cancer cell, Achen et al., 2005 [206]).