How Does CUDC-101 Work?
Posted: Mon Feb 08, 2010 8:36 amCUDC-101 is a molecule that can target 3 different and novel cancer pathways at once. This allows patients to take a single doses instead of having to take multiple agents at once or at various times. The intent of this design is for network disruption.
What does CUDC-101 Target? (EGFR, HDAC, HER2)
EGFR (Epidermal growth factor receptor)
Mutations that lead to EGFR overexpression (known as upregulation) or overactivity have been associated with a number of cancers, including lung cancer, anal cancers and glioblastoma multiforme. In this latter case a more or less specific mutation of EGFR, called EGFRvIII is often observed. Mutations, amplifications or misregulations of EGFR or family members are implicated in about 30% of all epithelial cancers.
HDAC (HDAC1, HDAC2, HDAC3, HDAC6)
Histone Deacetylase
HER2 (Human Epidermal growth factor Receptor 2)
Overexpression can occur in other cancers such as breast cancer, ovarian cancer, stomach cancer, and biologically aggressive forms of uterine cancer, such as uterine serous endometrial carcinoma.
- Efficacy dose ranges are above 150mg/m2
- About double the half life in tumors when compared to plasma
What does CUDC-101 Target? (EGFR, HDAC, HER2)
EGFR (Epidermal growth factor receptor)
Mutations that lead to EGFR overexpression (known as upregulation) or overactivity have been associated with a number of cancers, including lung cancer, anal cancers and glioblastoma multiforme. In this latter case a more or less specific mutation of EGFR, called EGFRvIII is often observed. Mutations, amplifications or misregulations of EGFR or family members are implicated in about 30% of all epithelial cancers.
HDAC (HDAC1, HDAC2, HDAC3, HDAC6)
Histone Deacetylase
- CLASS 1 (Nucleus), inhibits important pieces that modulate DNA and expression of various proteins.
- HDAC1
Together with metastasis-associated protein-2, it deacetylates p53 and modulates its effect on cell growth and apoptosis.
HDAC2
Plays an important role in transcriptional regulation, cell cycle progression and developmental events.
HDAC3
This protein can also down-regulate p53 function and thus modulate cell growth and apoptosis. This gene is regarded as a potential tumor suppressor gene.
CLASS 2 (Cytoplasm)
- HDAC6 ie HSP90
HER2 (Human Epidermal growth factor Receptor 2)
Overexpression can occur in other cancers such as breast cancer, ovarian cancer, stomach cancer, and biologically aggressive forms of uterine cancer, such as uterine serous endometrial carcinoma.