Drug intelligence / Profile preview

vorinostat + niacinamide + etoposide

Development stage
Phase 1
Lead developer
Columbia University
Modality
Small Molecules
Administration
Oral
01

Overview

This combination therapy involves the pan-histone deacetylase (HDAC) inhibitor vorinostat, the vitamin niacinamide, and the topoisomerase II inhibitor etoposide. Developed as an experimental regimen by Columbia University, it is primarily investigated for relapsed or refractory lymphoid malignancies, including Hodgkin's disease and various non-Hodgkin lymphomas. Vorinostat works by inhibiting class I and II HDACs, leading to increased histone acetylation and induction of apoptosis. Niacinamide, a form of vitamin B3, is utilized at high doses in this context to potentially inhibit sirtuins (like SIRT1) and enhance the anti-tumor activity of HDAC inhibitors. Etoposide provides a cytotoxic component by causing DNA strand breaks through the inhibition of topoisomerase II.

Other names
Vorinostat, Niacinamide, and Etoposide combination therapy
02

Targets

HDAC1 (Histone Deacetylase 1)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)HDAC6 (Histone deacetylase 6)PARP1 (Poly (adp-ribose) polymerase 1)SIRT1 (NAD-dependent protein deacetylase sirtuin-1)TOP2A (DNA topoisomerase II)

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