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eribulin + tucidinostat
- Development stage
- Phase 2
- Lead developer
- Eisai
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Eribulin + tucidinostat is an investigational combination therapy consisting of two small molecule drugs with distinct mechanisms of action, being studied primarily for advanced or metastatic breast cancer. Eribulin is a synthetic analog of halichondrin B and acts as a microtubule dynamics inhibitor, leading to G2/M cell cycle arrest and apoptosis in cancer cells. Tucidinostat (also known as chidamide) is an orally available benzamide-type histone deacetylase (HDAC) inhibitor that selectively targets class I HDACs (HDAC1, HDAC2, HDAC3) and class IIb HDAC10. By inhibiting these enzymes, tucidinostat increases acetylation of histones and non-histone proteins, resulting in chromatin relaxation, altered gene expression, cell cycle arrest, apoptosis induction in tumor cells, and potential immunomodulatory effects. The combination aims to leverage the cytotoxic effects of eribulin with the epigenetic modulation provided by tucidinostat to enhance antitumor efficacy[2][4][6][8][10].
- Brand names
- Halaven (eribulin)Epidaza (tucidinostat)Hiyasta (tucidinostat)
- Other names
- eribulin mesylatechidamide
02
Targets
HDAC1 (Histone Deacetylase 1)HDAC10 (Histone Deacetylase 10)HDAC11 (Histone Deacetylase 11)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)HDAC8 (Histone Deacetylase 8)Beta-tubulin / microtubule plus endsTUBB (Tubulin (alpha and beta subunits))
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