Drug Detail

Information about Flavopiridol, alvocidib

Generic Name	Flavopiridol, alvocidib
IND	HMR 1275, L86-8275
Brand Name (US)
Manufacturer	Aventis
Drug Type
Delivery	Intravenous
Approval Status	Phase 2
Indications
Overall Strategy	GIST cell based
Strategy	Freeze the cell division cycle Block KIT
Drug Category	Transcription inhibitor

Flavopiridol is widely known as an inhibitor of cyclin- dependent kinase (CDK2 and CDK1), its effects may be mediated more by inhibition of transcription than anything else (Cell Cycle review, December 2004).
In 2006, a team of researchers from Memorial Sloan-Kettering Cancer Center reported that flavopiridol reduces the amount of KIT protein (inhibits transcription) and caused cell death in GIST tumor cells.
The way flavopiridol works against KIT is different than Gleevec. Flavopiridol reduces the total amount of KIT protein, where Gleevec inhibits the activation (phosyphorylation) of the KIT protein present without lowering the amount of KIT protein. One of the mechanisms of Gleevec-resistance is overexpression of KIT or PDGFRA (too much KIT or PDGFRA protein).