Drug intelligence / Profile preview

zeprumetostat + chidamide + cyclophosphamide + doxorubicin + vincristine + prednisone

Development stage
Phase 2
Lead developer
Hengrui Therapeutics
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Zeprumetostat + chidamide + CHOP is an investigational combination regimen being evaluated for the treatment of newly diagnosed peripheral T-cell lymphoma (PTCL). This regimen combines two epigenetic modulators—zeprumetostat, an EZH2 inhibitor, and chidamide, a subtype-selective histone deacetylase (HDAC) inhibitor—with the standard-of-care CHOP chemotherapy backbone (cyclophosphamide, doxorubicin, vincristine, and prednisone). The combination is currently being studied in a genotype-guided Phase I/II clinical trial sponsored by Ruijin Hospital, specifically targeting patients whose tumors harbor mutations in core epigenetic genes. By integrating targeted epigenetic inhibition with cytotoxic chemotherapy, the regimen aims to enhance therapeutic efficacy and overcome resistance in molecularly defined subsets of PTCL.

Other names
zeprumetostat + chidamide + CHOPZeprumetostat plus chidamide with CHOP
02

Targets

DNAEZH1EZH2 (Histone-lysine N-methyltransferase EZH2)GR (Glucocorticoid receptor)HDAC1 (Histone Deacetylase 1)HDAC10 (Histone Deacetylase 10)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)TOP2A (DNA topoisomerase II)TUBB (Tubulin (alpha and beta subunits))

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