The efficacy of Idhifa was studied in a single-arm trial of 199 patients with relapsed or refractory AML who had IDH2 mutations as detected by the RealTime IDH2 Assay. The trial measured the percentage of patients with no evidence of disease and full recovery of blood counts after treatment (complete remission or CR), as well as patients with no evidence of disease and partial recovery of blood counts after treatment (complete remission with partial hematologic recovery or CRh). With a minimum of six months of treatment, 19 percent of patients experienced CR for a median months, and 4 percent of patients experienced CRh for a median months. Of the 157 patients who required transfusions of blood or platelets due to AML at the start of the study, 34 percent no longer required transfusions after treatment with Idhifa.
Developing a Plate
A TLC plate can be developed in a beaker or closed jar (see picture below). Place a small amount of solvent (= mobile phase) in the container. The solvent level has to be below the starting line of the TLC, otherwise the spots will dissolve away. The lower edge of the plate is then dipped in a solvent. The solvent (eluent) travels up the matrix by capillarity, moving the components of the samples at various rates because of their different degrees of interaction with the matrix (=stationary phase) and solubility in the developing solvent. Non-polar solvents will force non-polar compounds to the top of the plate, because the compounds dissolve well and do not interact with the polar stationary phase. Allow the solvent to travel up the plate until ~1 cm from the top. Take the plate out and mark the solvent front immediately . Do not allow the solvent to run over the edge of the plate. Next, let the solvent evaporate completely.
From the data above, we see compound 3 has suitable Rf values of and in 10% and 20% ethyl acetate, respectively. Though the Rf values convert to CV values of and , we need to look at how well separated compound 3 (our target in this case) is from compounds 2 and 4. What we see from the table above is at 10% ethyl acetate, compound 3 has a Δ CV of vs. compound 2 and Δ CV vs. compound 4. In 20% ethyl acetate however, the Δ CV values are much smaller ( and , respectively) which does limit our loading capacity, refer to the flash loading table in the link (page 27). Loading is based on the smaller of the Δ CV values. The table tells us that with a Δ CV of we should be able to load between 100 and 500 mg on a 10g silica cartridge but with a Δ CV of , we are limited to less than a 100 mg load.