Drug intelligence / Profile preview

Gefitinib + Vinorelbine

Development stage
Discontinued
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

The combination of gefitinib and vinorelbine is a treatment regimen that has been studied for use in non-small cell lung cancer (NSCLC) and metastatic breast cancer. This combination has shown significant safety concerns, particularly regarding hematologic toxicity. A phase I study found a higher than expected incidence of grade 3 or 4 hematologic adverse events, specifically febrile neutropenia and neutropenia, leading to severe myelosuppression and an unacceptable rate of febrile neutropenia. Due to these findings, concurrent administration of gefitinib and vinorelbine, with or without cisplatin, was not supported as a valid treatment for advanced NSCLC. A case report also highlighted severe myelotoxicity, including anemia, neutropenia, and thrombocytopenia, with this combination. While some antitumor activity was observed in a study for metastatic breast cancer, that study was prematurely discontinued due to low accrual.

02

Targets

TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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