MDV3100 is a small molecule compound developed to treat hormone-refractory prostate cancer. MDV3100, which was rationally designed based on a breakthrough discovery, directly addresses a key mechanism that leads to prostate cancer cell death. MDV3100 may block both hormone-refractory and hormone-sensitive prostate cancer better than currently available therapies.
Investigated for use/treatment in prostate cancer.
Mechanism of action
MDV3100 is the lead development candidate from a library of approximately 170 small molecules licensed by Medivation. These molecules were rationally designed to treat hormone-refractory prostate cancer by inhibiting the androgen receptor (AR) in a different manner from currently approved AR antagonist drugs, which are ineffective in treating prostate cancers that have become hormone-refractory.
Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins. Transcription activation is down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3.