Preferred Label : Cisplatin/Vinblastine/Cell Penetration Enhancer Formulation INT230-6;
NCIt synonyms : Cisplatin/Vinblastine Formulation with Cell Penetration Enhancer INT230-6;
NCIt definition : A formulation composed of three agents in a fixed ratio: two chemotherapeutic agents,
the platinum compound cisplatin and the vinca alkaloid vinblastine, and a proprietary
amphiphilic excipient that acts as a penetration enhancer, with potential antineoplastic
activity. Upon intra-tumoral (IT) injection of INT230-6, the dispersion/cell penetration
enhancer excipient of INT230-6 facilitates dispersion of the two drugs throughout
the tumor tissue and enables increased cellular uptake of these agents into tumor
cells. Once inside the cell, cisplatin forms highly reactive, charged, platinum complexes
which bind to nucleophilic groups such as GC-rich sites in DNA, which results in apoptosis
and cell growth inhibition. Vinblastine kills the tumor cells through binding to tubulin
and thereby inhibits microtubule formation, resulting in disruption of the mitotic
spindle assembly and cell cycle arrest of tumor. In addition, the tumor cell killing
leads to recruitment of dendritic cells (DCs) and induces a tumor-specific T-cell-mediated
immune response that attacks both the injected tumor and distant tumor lesions. Local
administration of both cisplatin and vinblastine, without the diffusion/penetration
enhancer, results in to poor diffusion and a lack of cellular uptake of the agents;
INT230-6 increases the intracellular concentration of cisplatin and vinblastine, thereby
improving efficacy.;
Molecule name : INT 230-6; INT230-6;
NCI Metathesaurus CUI : CL523731;
Origin ID : C136428;
UMLS CUI : C4526674;
Semantic type(s)
- concept_is_in_subset
- has_target
