Drug intelligence / Profile preview

imatinib + vinorelbine

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Imatinib + vinorelbine is a combination of two small molecule chemotherapeutic agents used in clinical research for the treatment of metastatic breast cancer (MBC) and potentially other solid tumors. Imatinib is a tyrosine kinase inhibitor that targets BCR-ABL, ABL, platelet-derived growth factor receptor alpha (PDGFR-α), platelet-derived growth factor receptor beta (PDGFR-β), KIT (CD117), and discoidin domain receptor (DDR). It inhibits proliferation and invasiveness of tumor cells by blocking these kinases' signaling pathways[2][3][5][8]. Vinorelbine is a semi-synthetic vinca alkaloid that acts as an anti-mitotic agent by binding to tubulin and disrupting microtubule assembly during mitosis, leading to cell cycle arrest at metaphase and apoptosis in rapidly dividing cancer cells[4][6]. The combination has been studied in phase I/II trials for its feasibility, tolerability, safety profile, and efficacy in pretreated patients with MBC expressing PDGFR or KIT. Results suggest manageable toxicity with promising clinical benefit rates[2][3][5].

Other names
imatinib mesylatevinorelbine tartrate
02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)TUBB (Tubulin (alpha and beta subunits))ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)

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