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osimertinib + selumetinib
- Development stage
- Phase 2
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Osimertinib (AZD9291) is a third-generation, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that selectively targets both EGFR-sensitizing and EGFR T790M resistance mutations, commonly used in the treatment of non-small cell lung cancer (NSCLC)[7]. Selumetinib (AZD6244, ARRY‑142886), marketed as Koselugo, is a selective inhibitor of mitogen‑activated protein kinase kinases 1 and 2 (MEK1/2), which are key components of the RAS/RAF/MEK/ERK signaling pathway. Selumetinib is approved for pediatric patients with neurofibromatosis type 1-associated plexiform neurofibromas and has been investigated in various cancers[1][3][5][6]. The combination of these two small molecules aims to overcome resistance mechanisms in EGFR-mutated cancers by dual inhibition of parallel oncogenic pathways.
- Brand names
- Tagrisso + Koselugo
- Other names
- osimertinib + selumetinib
02
Targets
EGFR T790M (Epidermal growth factor receptor T790M mutant)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)
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