Generic Name |
Imatinib + Everolimus | |
---|---|---|
IND |
STI571 + RAD001 | |
Brand Name (US) |
Gleevec + Afinitor | |
Manufacturer |
Novartis, Novartis | |
Drug Type |
||
Delivery |
Oral | |
Approval Status |
Both are approved. This combination is not approved for GIST. It was evaluated in phase 2 trials for GIST. | |
Indications |
||
Overall Strategy |
KIT Protein Based Oncogenic Signal Path Based | |
Strategy |
Block KIT Block KIT Signal Path | |
Drug Category |
KIT/PDGFRA inhibitor mTOR inhibitor |
Imatinib is the first line treatment for GIST. In combination therapy, it is hoped that imatinib will continue to control sensitive "clones" and the addition of a second compound, such as RAD001, will provide additional anti-tumor effects.
RAD001 is an oral mTOR inhibitor.
Note: Prenen et al., have suggested that RAD001 (everolimus) alters the imatinib blood partition in favour of the erythrocyte. The result may be a reduction of imatinib plasma levels possibly making the imatinib ineffective. If this combination is tried outside of a clinical trial, then the treating physician should be familiar with the second link under links below. In addition, plasma testing for imatinib levels might be in order.