DDInter484 DDInter1658
Dasatinib is an orally available multikinase inhibitor indicated for the treatment of Philadelphia chromosome (Ph)-positive leukemias.[A2224,L45171] Ph is a chromosomal abnormality found in patients with chronic myelogenous leukemia (CML) and acute lymphocytic leukemia (ALL), where the ABL tyrosine kinase and the breakpoint cluster region (BCR) gene transcribe the chimeric protein BCR-ABL. BCR-ABL is associated with the uncontrolled activity of the ABL tyrosine kinase and is involved in the pathogenesis of CML and 15-30% of ALL cases.[A11377,A33432] Dasatinib also inhibits a spectrum of kinases involved in cancer, including several SRC-family kinases. Unlike [imatinib], another tyrosine kinase used for the treatment of CML and Ph-positive ALL, dasatinib inhibits the active and inactive conformations of the ABL
Selpercatinib is a kinase inhibitor with enhanced specificity for RET tyrosine kinase receptors (RTKs) over other RTK classes.[A202055, A202052, L13604] Enhanced RET (Rearranged during transfection) oncogene expression is a hallmark of many cancers. Although multikinase inhibitors, including [cabozantinib], [ponatinib], [sorafenib], [sunitinib], and [vandetanib], have shown efficacy in RET-driven cancers, their lack of specificity is generally associated with substantial toxicity. Selpercatinib (LOXO-292) and pralsetinib (BLU-667) represent the first generation of specific RET RTK inhibitors for the treatment of RET-driven cancers.[A202049, A202055, A202052, L13604] Although selpercatinib is currently still under investigation in clinical trial NCT04211337, it was granted accelerated FDA approval on May 8, 2020, for specific RET-driven cancer indications. It is currently marketed under the brand name RETEVMO™ by Loxo Oncology Inc. Selpercatinib is also approved by the European Commission.
Dasatinib {u} (Compound) treats {v} (Disease) hematologic cancer
Dasatinib {u} (Compound) binds {v} (Gene) SRC
Dasatinib {u} (Compound) upregulates {v} (Gene) SATB1
Dasatinib {u} (Compound) downregulates {v} (Gene) EBNA1BP2
Dasatinib {u} (Compound) causes {v} (Side Effect) Body temperature increased
Dasatinib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Sulfamethoxazole
Dasatinib {u} may cause a minor interaction that can limit clinical effects when taken with {v} Doravirine
Dasatinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Denosumab
Dasatinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Granisetron
Dasatinib {u} may lead to a major life threatening interaction when taken with {v} Halofantrine
Dasatinib (Compound) treats hematologic cancer (Disease)
Dasatinib (Compound) binds SRC (Gene)
Dasatinib (Compound) upregulates SATB1 (Gene)
Dasatinib (Compound) downregulates EBNA1BP2 (Gene)
Dasatinib (Compound) causes Body temperature increased (Side Effect)
Dasatinib may cause a minor interaction that can limit clinical effects when taken with Sulfamethoxazole
Dasatinib may cause a minor interaction that can limit clinical effects when taken with Doravirine
Dasatinib may cause a moderate interaction that could exacerbate diseases when taken with Denosumab
Dasatinib may cause a moderate interaction that could exacerbate diseases when taken with Granisetron
Dasatinib may lead to a major life threatening interaction when taken with Halofantrine