Drug intelligence / Profile preview

decitabine + panobinostat + tamoxifen

Development stage
Preclinical
Lead developer
Astex Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination of three small molecule drugs with distinct mechanisms of action used primarily in oncology research and clinical trials: - **Decitabine** is a DNA methyltransferase inhibitor that induces hypomethylation of DNA by inhibiting DNA methylation. This leads to reactivation of silenced genes and apoptosis in cancer cells. It is approved for the treatment of myelodysplastic syndromes and acute myeloid leukemia[2][3][6]. - **Panobinostat** (LBH589) is a non-selective histone deacetylase inhibitor that alters gene expression by increasing acetylation of histone proteins. This results in cell cycle arrest and apoptosis in malignant cells. It is approved for use in multiple myeloma[1][4]. - **Tamoxifen** is a selective estrogen receptor modulator (SERM) that acts as an antagonist on estrogen receptors in breast tissue but can have agonist effects elsewhere. It blocks the proliferative action of estrogen on mammary epithelium and is widely used for hormone receptor-positive breast cancer[7]. The combination has been studied preclinically as an epigenetic therapy approach to overcome resistance mechanisms or enhance sensitivity to antiestrogen therapies such as tamoxifen—particularly relevant for certain subtypes of breast cancer including triple-negative or ER-negative disease[1][2]. However, clinical trial results combining these agents have shown limited efficacy due to toxicity concerns.

Brand names
Farydak
Other names
5-aza-2'-deoxycytidine (for decitabine)Panobinostat (for LBH589)Tam (for tamoxifen)
02

Targets

DNMT1 (DNA (cytosine-5)-methyltransferase 1)ESR2 (ERβ)HDAC (HDAC family)ESR1 (ERα)

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