Abstract
Inhibitors of alphav integrins have been developed as anti-angiogenic agents for
cancer therapy and, among them, cyclic RGD-containing pentapeptides, such as
cilengitide, are the most commonly used integrin antagonists. In this study,
cilengitide was tested in combination with the methylating agent temozolomide
(TMZ), a well-tolerated anticancer drug with favourable pharmacokinetic
properties currently used for the therapy of metastatic melanoma. To this end,
the influence of cilengitide and TMZ on malignant melanoma growth and endothelial
cell proliferation were investigated, using in vitro and in vivo models. The
results indicated that cilengitide and TMZ exerted synergistic antiproliferative
effects against melanoma and endothelial cells in vitro and induced a
statistically significant reduction of in vivo melanoma growth with respect to
treatment with the methylating agent only. In conclusion, this study proposes the
use of cilengitide in combination with TMZ for the treatment of metastatic
melanoma, thereby opening novel perspectives for the use of integrin inhibitors
to enhance the efficacy of chemotherapy.
Lingua originale | English |
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pagine (da-a) | 1039-1043 |
Numero di pagine | 5 |
Rivista | Oncology Reports |
Stato di pubblicazione | Pubblicato - 2008 |
Keywords
- chemoterapic
- integrin antagonist
- temozolomide