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docetaxel + vorinostat
- Development stage
- Unknown
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Docetaxel + vorinostat is a combination therapy that pairs docetaxel, a taxane chemotherapy agent, with vorinostat, a histone deacetylase inhibitor (HDACi). This combination has been studied for its potential synergistic effects in treating various cancers. Docetaxel works by binding to and inhibiting the depolymerization of the α-tubulin subunit of microtubules, inducing cell cycle arrest and apoptosis. Vorinostat enhances docetaxel's effects by inhibiting histone deacetylase, which leads to relaxation of chromatin structure and increased sensitivity to DNA-targeting drugs. The combination has shown synergistic anti-proliferative effects in castration-resistant prostate cancer (CRPC) cells by suppressing androgen receptor (AR) signaling, including full-length AR and AR splice variants. The combination also accelerates the acetylation and bundling of tubulin, which inhibits the nuclear accumulation of AR. Additionally, this combination has been investigated for breast cancer treatment, where vorinostat enhances docetaxel-induced G2/M arrest in breast cancer cells.
- Brand names
- ZolinzaTaxotere
- Other names
- DTX + VRS
02
Targets
HDAC (HDAC family)TUBB (Tubulin (alpha and beta subunits))
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