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eribulin + pemetrexed
- Development stage
- Unknown
- Lead developer
- Eisai
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Eribulin + pemetrexed is an investigational combination of two chemotherapeutic agents used in clinical trials for the treatment of advanced or metastatic nonsquamous non-small cell lung cancer (NSCLC) after failure of prior platinum-based chemotherapy. Eribulin is a microtubule dynamics inhibitor, structurally related to halichondrin B, that inhibits the growth phase of microtubules and sequesters tubulin into nonproductive aggregates, leading to G2/M cell cycle arrest and apoptosis. Pemetrexed is an antifolate antineoplastic agent that disrupts folate-dependent metabolic processes essential for cell replication by inhibiting multiple enzymes involved in purine and pyrimidine synthesis. The combination was evaluated in a phase Ib/II study; while it was generally safe and well tolerated at reduced dosing intensity compared to monotherapy regimens, it did not demonstrate therapeutic advantage over pemetrexed alone as second-line therapy for NSCLC[1][4][5].
- Brand names
- Halaven (eribulin)Alimta (pemetrexed)
- Other names
- eribulin mesylate + pemetrexed
02
Targets
GART (GAR transformylase)TUBB (Tubulin (alpha and beta subunits))DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)
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