P-glycoprotein, a pump located in the plasma cell membrane, extrudes severa
l clinically important drugs from the cell, and hence causes multidrug resi
stance. Reversing clinical drug resistance is possible by using agents that
inhibit the activity of P-glycoprotein. We describe the results of sequent
ial flow cytometric determinations of P-glycoprotein expression and activit
y in two patients suffering from acute lymphoblastic transformation of chro
nic myeloid leukaemia. Neither P-glycoprotein expression, nor its activity
could be detected in the initial sample of the first patient. In the second
patient, no P-glycoprotein expression was found at diagnosis. However, aft
er chemotherapy containing P-glycoprotein substrates, a significant express
ion was found in both patients and the functional flow cytometric test was
positive. In order to achieve an accurate selection of patients that might
benefit from the clinical use of P-gp inhibitors, repeated analyses are ind
icated in each patient suffering from acute leukaemia, during the course of
the illness.