Table 5.
Effects of avapritinib and nintedanib on growth of neoplastic cells obtained from patients with SM
| Patient number* | Diagnosis (SM variant) | Avapritinib (BLU-285) IC50 (µM) | Nintedanib (BIBF-1120) IC50 (µM) |
|---|---|---|---|
| #1a | ISM | >5 | 0.5-1 |
| #8 | ISM | 0.5-1 | 1-5 |
| #9 | SSM | 1-5 | n.a. |
| #10 | ASM | 1-5 | 0.1-0.25 |
| #13 | ASM-CMML | 1-5 | >5 |
| #14a | ASM-CMML | 1-5 | 0.25-0.5 |
| #15 | ASM-AML | 0.1-0.25 | 0.1-0.25 |
| #17 | MCL | 1-5 | >5 |
| #18 | MCL | 1-5 | n.a. |
| #20 | sMCL | 0.5-1 | n.a. |
Primary bone marrow cells were incubated with control medium and medium containing various concentrations of avapritinib or nintedanib at 37°C for 48 hours. Then, proliferation was determined by measuring uptake of 3H-thymidine and IC50 ranges were calculated from triplicates.
*
Patients (#) refer to patients’ numbers in Table 3.
Abbreviations: SM, Systemic Mastocytosis; IC50, Half Maximal Inhibitory Concentration; n.a., not available; ASM, Aggressive SM; MCL, Mast Cell Leukemia; sMCL, Secondary MCL; SSM, Smoldering SM; ISM, Indolent SM; CMML, Chronic Myelomonocytic Leukemia; AML, Acute Myeloid Leukemia.