Dược Lực Học :
Preclinical studies in both melanoma and colorectal cancer models demonstrate that PLX4032 reduces tumor size or slows the progression of tumors for extended periods, even after the completion of treatment. Highly selective against B-Raf(V600E) compared to a panel of over 70 other kinases, PLX4032 works specifically on cancer cells, leaving healthy cells untouched. Thus, PLX4032 has demonstrated a very favorable side effect profile, and should be able to be used safely in combination with other anticancer drugs. Pending activation of the IND by the FDA, Plexxikon intends to initiate Phase 1 dose escalation studies in cancer patients by the end of this year.
Cơ Chế Tác Dụng :
PLX4032, a targeted anticancer agent, selectively inhibits the cancer-causing BRAF(V600E) gene found in subsets of different cancers, including 70% of malignant melanomas and a significant number of colorectal and thyroid tumors. Plexxikon, the company developing PLX4032, will use a new test to detect the presence of this cancer-causing gene to identify patients most likely to respond to PLX4032, enabling a personalized form of treatment.
PLX4032 blocks one of the most common genetic mutations known to cause cancer. It is a selective inhibitor of the activated BRAF(V600E) gene found in 70% of malignant melanomas and a significant percentage of other cancers.
Chỉ Định :
For the treatment of various forms of cancer.