Drug Detail

Information about Gleevec

Generic Name
Imatinib + Panobinostat
STI571 + LBH589
Brand Name (US)
Novartis + Novartis
Drug Type
Tyrosine Kinase Inhibitor
Approval Status
Gleevec is approved for GIST. This combination is in a phase 1/2 trial for GIST.
Overall Strategy
KIT Protein + GIST cell based
Block KIT + Unblock cell death genes + Destroy KIT
Drug Category
HDAC inhibitor + KIT/PDGFRA inhibitor

Work presented at the Life Fest meeting in Dallas, showed that a histone deacetylase (HDAC) inhibitor was able to cause significant regression in a Gleevec-resistant xenografts model (mouse model). HDAC inhibitors are a new class of drugs that have shown anti-cancer activity in several 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. Panobinostat is the only HDAC inhibitor that is in a GIST-specific trial (in a combination with imatinib).

Deibec-Rychter et al, have shown that HDAC inhibitors are able to cause significant regression in a Gleevec-resistant xenograft model. Bauer et al have shown that LBH589 has antiproliferative and proapoptotic effects in IM-sensitive and IM-resistant KIT+ GIST. In this study, the antiproliferative effects of LBH589 were 22-38x stronger that SAHA (vorinostat/Zolinza).



See panobinostat drug link

Trials of this drug


LBH589 Plus Imatinib

Trial results

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