Drug Detail

Information about Zolinza

Generic Name	Vorinostat
IND	MK0683
Brand Name (US)	Zolinza
Manufacturer	Merck
Drug Type	HDAC inhibitor
Delivery	Oral
Approval Status	Approved for a non-GIST cancer
Indications	CTCL
Overall Strategy	GIST cell based
Strategy	Block KIT + Unblock cell death genes
Drug Category	HDAC inhibitor

Vorinostat is a HDAC inhibitor. It is approved for Cutaneous T-cell llymphoma (CTCL).
Research has shown that histone deacetylase (HDAC) inhibitors are able to cause significant regression in a Gleevec-resistant xenografts model (mouse model) and GIST cell lines. HDAC inhibitors are a new class of drugs that have shown anti-cancer activity in three major ways:

* Inducing apoptosis
* Arresting the cell cycle
* By destabilizing certain cancer-causing proteins such as bcr-abl (and possibly KIT). This may occur because HDAC inhibitors cause hsp90 to become inactive, possibly resulting in the destruction of the KIT protein.

Another way that HDAC inhibitors might accomplish their effects is by “turning on” some tumor suppressor genes that have been silenced.
HDAC inhibitors are in various stages of development.

* Istodax is FDA approved for CTCL.
* Zolinza (vorinostat) is FDA approved for cutaneous T-cell lymphoma (CTCL).
* LBH589 – Is in phase 3 trials and a combination trial with imatinib for GIST (Phase I).
* Others