Cilengitide is a molecule designed and synthesized at the Technical University Munich in collaboration with Merck KGaA in Darmstadt. Cilengitide binds to the activities of the αvβ3 and αvβ5 integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis. Cilengitide (EMD 121974) could increase systemic RIT efficacy of therapy in a human breast cancer tumor model having mutant p53 and expressing bcl-2. Cilengitide is currently in clinical phase III for treatment of glioblastomas and in phase II for several other tumors.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Integrin inhibitor cilengitide for the treatment of glioblastoma: a brief overview of current clinical results.
Scaringi C, et al. Anticancer Res. 2012 Oct;32(10):4213-23. PMID: 23060541.
A safety run-in and randomized phase 2 study of cilengitide combined with chemoradiation for newly diagnosed glioblastoma (NABTT 0306).
Nabors LB, et al. Cancer. 2012 Nov 15;118(22):5601-7. PMID: 22517399.
Cilengitide targeting of alpha(v)beta(3) integrin receptor synergizes with radioimmunotherapy to increase efficacy and apoptosis in breast cancer xenografts.
Burke PA, et al. Cancer Res. 2002 Aug 1;62(15):4263-72. PMID: 12154028.
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