Drug intelligence / Profile preview

third-generation EGFR-TKI + intrathecal pemetrexed

Development stage
Unknown
Lead developer
Fujian Medical University Cancer Hospital
Modality
Small Molecules
Administration
Oral, Intrathecal
01

Overview

This combination therapeutic regimen is being evaluated by Fujian Cancer Hospital for the treatment of non-small cell lung cancer (NSCLC) patients who have developed leptomeningeal metastasis (LM) following progression on standard doses of third-generation EGFR tyrosine kinase inhibitors (TKIs). The regimen consists of a double dose of a third-generation EGFR-TKI (such as osimertinib, almonertinib, or furmonertinib) administered orally to enhance cerebrospinal fluid (CSF) penetration, combined with pemetrexed administered via intrathecal injection. This dual approach aims to overcome the blood-brain barrier limitations of systemic therapy by providing direct cytotoxic anti-folate activity within the leptomeninges while maintaining potent inhibition of mutated EGFR signaling.

Other names
Double Dose of Third-generation EGFR-TKI Plus Intrathecal PemetrexedDouble-dose 3rd-gen EGFR-TKI + Intrathecal PemetrexedThird-generation EGFR-TKI-Fujian Cancer Hospital-leptomeningeal metastasis
02

Targets

DHFR (Dihydrofolate reductase)GART (GAR transformylase)TS (Thymidylate synthase)

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