Hope for BET inhibition in patients with leukaemia or lymphoma
Mené sur 45 patients (33 atteints d'un lymphome, 12 d'un myélome multiple), cet essai international de phase I évalue la dose maximale tolérée et l'activité antitumorale d'un composé appelé OTX015, un inhibiteur de protéines BET
In cancer, bromodomain and extraterminal (BET) proteins are involved in regulating expression of key oncogenes and anti-apoptotic proteins, generally through transcriptional elongation, making them an important therapeutic target to modulate expression of disease-promoting genes. Studies have elucidated that inhibition of BETs can impede cell growth and abrogate survival mechanisms in cancerous cells by regulating selective gene expression programmes. In acute myeloid leukaemia, inhibition of BRD4 results in growth inhibition and apoptosis even in leukaemic cells from patients with relapsed or refractory disease.
The Lancet Haematology , commentaire, 2015