Dược Lực Học :
All HDAC inhibitors induce histone H3 hyperacetylation, correlating with inhibition of proliferation, induction of cell differentiation and apoptosis.
Cơ Chế Tác Dụng :
MethylGene Inc, in collaboration with Pharmion Corp, is developing the small-molecule, isoform-selective compound MGCD-0103 in North America for the potential treatment of cancer. MGCD-0103 is currently undergoing phase II clinical trials in patients with lymphoma, leukemia, myelodysplastic syndromes and solid tumors, including pancreatic carcinoma. Taiho Pharmaceutical Co Ltd is evaluating MGCD-0103 for oncological indications in South East Asia.
MGCD0103 is a novel isotypic-selective inhibitor of the enzyme histone deacetylase (HDAC). HDAC inhibitors act by turning on tumour suppressor genes that have been inappropriately turned off. Tumour suppressor genes are a natural defense against cancer. It is therefore hypothesized that specifically inhibiting those HDACs involved in cancer with MGCD0103 may restore normal cell function and reduce or inhibit tumour growth.
Chỉ Định :
Investigated for use/treatment in cancer/tumors (unspecified), leukemia (lymphoid), leukemia (myeloid), lymphoma (non-hodgkin's), lymphoma (unspecified), myelodysplastic syndrome, pancreatic cancer, and solid tumors.