Drug intelligence / Profile preview

purinostat mesylate + fulvestrant

Development stage
Phase 2
Lead developer
State Key Laboratory of Biotherapy
Modality
Small Molecules
Administration
Injectable
01

Overview

**Purinostat mesylate + fulvestrant** is a combination therapy under clinical investigation for advanced solid tumors. Purinostat mesylate is a highly selective and active inhibitor of histone deacetylases (HDAC) class I and IIb, showing preclinical efficacy against leukemia stem cells and enhancing anti-cancer effects through epigenetic modulation. Fulvestrant is a selective estrogen receptor degrader (SERD) used in hormone receptor-positive (HR+) advanced breast cancer to block estrogen signaling by promoting estrogen receptor degradation. The combination aims to target both epigenetic regulation and hormone receptor signaling, potentially overcoming endocrine resistance in solid tumors, particularly HR+ breast cancer.

Other names
PM + fulvestrant
02

Targets

ESR1 (ERα)HDAC1 (Histone Deacetylase 1)HDAC10 (Histone Deacetylase 10)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)HDAC6 (Histone deacetylase 6)HDAC8 (Histone Deacetylase 8)

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