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Vorinostat + tamoxifen
- Development stage
- Phase 2
- 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
CA2 (Carbonic Anhydrase 2)ESR1 (ERα)HDAC1 (Histone Deacetylase 1)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)HDAC6 (Histone deacetylase 6)
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