Drug intelligence / Profile preview

Vorinostat + tamoxifen

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Vorinostat + tamoxifen is a combination therapy investigated primarily for hormone receptor-positive, endocrine therapy-resistant breast cancer. Vorinostat is a histone deacetylase inhibitor (HDACi) that targets HDAC1, HDAC2, HDAC3 (Class I), and HDAC6 (Class II), leading to increased acetylation of histones and modulation of gene expression. This can reverse hormone resistance in breast cancer cells[1][5]. Tamoxifen is a selective estrogen receptor modulator that competitively inhibits estrogen binding to its receptor, thereby inhibiting growth and promoting apoptosis in estrogen receptor-positive tumors[6]. The combination has shown activity in reversing hormone resistance with tumor shrinkage observed in some patients who had progressed on prior hormonal therapies[1][2]. Clinical trials have demonstrated the regimen is generally well tolerated with manageable toxicity profiles[1][4].

Other names
vorinostat + tamoxifen
02

Targets

HDAC6 (Histone deacetylase 6)ESR1 (ERα)HDAC1 (Histone Deacetylase 1)CA2 (Carbonic Anhydrase 2)

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