Drug intelligence / Profile preview

Osimertinib + Vinorelbine

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

Overview

Osimertinib + vinorelbine is a combination therapy used primarily for advanced non-small cell lung cancer (NSCLC). This combination appears to be particularly effective for patients with gradual resistance to osimertinib, where continuing osimertinib in combination with metronomic oral vinorelbine has shown promising results with a median progression-free survival of 6.3 months and disease control rate of 86.7%[1]. Osimertinib is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that specifically targets certain EGFR mutations (T790M, L858R, and exon 19 deletion) common in NSCLC tumors. It has 200 times higher affinity for mutated EGFR compared to wild-type EGFR, which reduces non-specific binding and limits toxicity[2]. Vinorelbine is a semi-synthetic vinca alkaloid that works by interfering with tubulin polymerization, preventing cell division in proliferating cancer cells. It can be administered either intravenously or orally as capsules[3][4]. The combination therapy shows synergistic effects, with vinorelbine combination therapy regimens demonstrating higher efficacy and comparable toxicity compared to vinorelbine monotherapy[1].

02

Targets

Epidermal growth factor receptor (mutant)TUBB (Tubulin (alpha and beta subunits))

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