FDA Approves Merck & Co., Inc. (MRK)'s ZOLINZA(TM) For The Treatment Of Cutaneous Manifestations In Patients With Cutaneous T-Cell Lymphoma Who Have T

WHITEHOUSE STATION, N.J.--Merck & Co., Inc. announced today that the U.S. Food and Drug Administration (FDA) has approved oral ZOLINZA(TM) (vorinostat) 400 mg once daily for the treatment of cutaneous manifestations [skin lesions] in patients with cutaneous T-cell lymphoma (CTCL), a form of non-Hodgkin's lymphoma, who have progressive, persistent or recurrent disease on or following two systemic therapies. CTCL is a cancer of the T-cells, a type of white blood cell, which affects the skin.

"With today's FDA approval of ZOLINZA, there is now an effective new option in the fight against cutaneous manifestations of cutaneous T-cell lymphoma, specifically in patients who have tried and failed other cancer treatment options," said Elise Olsen, M.D., director, CTCL Clinic & Research Center at Duke University Medical Center and lead investigator of one of the studies that led to the approval.


ZOLINZA is a histone deacetylase (HDAC) inhibitor. WELL SO WHAT! WHAT THE HELL IS THAT?
DNA that is actively replicating is very stringy and not bunched up on itself such that polymerases etc can bind to it and do their job. When this occurs, the DNA has been acteylated, an acetyl group attached, so that it stays unwound and continues replicating. When there are no acetyl group attached, proteins called histones bind to the DNA and terminate transcription (replication). Zolinza helps stop the DNA from replicating (what cancer cells do and making more cancer cells) by stopping the removal of acyl groups.

Based on in vitro studies, ZOLINZA inhibits the enzymatic activity of HDAC1, HDAC2, HDAC3 and HDAC 6 at nanomolar [10 -9] concentrations (IC50<86 nM). In some cancer cells, excess amounts of the enzyme HDAC prevent the activation of genes that control normal cell activity. ZOLINZA is believed to decrease the activity of HDAC. Decreasing the activity of HDAC allows for the activation of genes that may help to slow or stop the growth of cancer cells. The exact mechanism of the anticancer effect of ZOLINZA has not been fully characterized.

MERCK (NYSE:MRK)was unchanged today at 41.86 but topped 42 dollars in early afternoon trading.