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Table 1 The therapeutic protein kinase inhibiors in acute leukemia

From: Protein kinase inhibitors for acute leukemia

Targets Inhibitors Comments Main side effects Phase
FLT3 Quizartinib An anti-FLT3 TKI, was investigated in ALL or AML Nausea, anemia, vomiting, etc I-II-III [70]
Midostaurin It is an oral multi-targeted kinase inhibitor to inihibit leukemia cells including ALL and FLT3-positive AML Diarhhoea, nausea, headache, etc. I-II-III [71]
Sunitinib Sunitinib inhibits leukemia cells survival and angiogenesis Cardiotoxic, dyspnea, etc. II [72]
Lestaurtinib Lestaurtinib might inhibit the activity of FLT3 kinase and it is more appropriate during intensive chemotherapy Gastrointestinal reaction, etc. I-II-III [73]
Tandutinib It inhibits the FLT3 ITD-positive rather than the ITD-negative patients with AML. Bone pain, nausea, etc. I-II-III
Gilteritinib Gilteritinib is a kind of favourable safety agent and is being on trial at 120 mg/day Diarrhea, etc. I-II -III
Crenolanib Crenolanib is a potential selective inhibitor of FLT3-ITDs and PDGFRα/β Vomiting, headache, etc II
Bortezomib It is associated with apoptotic and autophagic cell death of AML Gastro-intestinal, asthenia, etc I-II-III [74]
BTK Ibrutinib Although ibrutinib has its own unique toxicity, it usually causes fewer infections Pneumonia, sinusitis, headache upper respiratory tract infection, etc. II
Acalabrutinib It has received accelerated approval for the treatment of cell lymphoma Headache, diarrhea, weight gain skin rash, severe diarrhea, etc. I-II
JAK-STAT Ruxolitinib The JAK1/JAK2 inhibitor, is more effective against JAK-STAT pathway Nausea, anemia, vomiting, ect. III
Pacritinib (SB1518) It is potent inhibitor FLT3-ITDs, JAK2, JAK2V617F in phase III development Anemia, ect. I-II-III [75]
Everolimus Everolimus is combined with MK-2206, particularly important in the setting of resistance to therapeutic drugs Cardiac failure, respiratory failure septic shock, etc. I-II [76]
Temsirolimus Temsirolimus combines with etoposide, cyclophosphamide and dexamethasone for relapsed pediatric ALL in adults Nausea, etc. I-II [77]
mTOR Sirolimus Sirolimus is an mTOR inhibitor, but it has a similar suppressive effect on the immune system Abdominal pain, nausea, etc. II [78]
AZD8055 AZD8055 inhibits the phosphorylation of mTORC1 with p70S6K and 4E–BP1 and downstream proteins Anorexia, etc. I
Ciclopirox Ciclopirox enhances the effect of the preclinical antileukemia while irritation Itching, blistering, swelling, etc. I
MEK Pimasertib It is a novel, selective, orally bioavailable MEK1/2 Bleeding risk, etc. II
GSK690693 It inhibits apoptosis in sensitive ALL cell lines Not clearly I
AKT MK-2206 An orally inhibitor of the PI3K/Akt pathway which can inhibit tumor cell proliferation Fatigue, vomiting, anorexia, etc I-II
T315I The mutation of T315I occurs to patients even when second- and third-genneration on trails Nausea, swelling, rash, etc. II-III
Gefitinib A third-line agent and also is an EGFR inhibitor Diarrhoea, vomiting, anorexia, etc. II [79]
Ponatinib It is a multi-targeted tyrosine-kinase inhibitor often with hypertension Hypertension, rash, abdominal pain, fatigue, etc. I-II
Bcr-Abl Dasatinib It also inhibits the Src kinase family Anemia, diarrhea, swelling, rash, etc II
ABL001 ABL001 is taken orally and the high does of it can be given safely to patients Not clearly I
BEZ235 BEZ-235 is a PI3K inhibitor. It also inhibits mTOR. It is being investigated as a possible leukemia treatment. Anemia, vomiting, etc I-II
PI3K Idelalisib Idelalisib is effective in leukemia patients who have p53 mutation Fever, fatigue, nausea, cough abdominal, pain, rash, chills, etc. on trial
PKI-587 Gedatolisib is an agent targeting the PI3K/mTOR pathway Nausea, etc. I
PLK1 Volasertib It has been reported the volasertib inhibits PLK1 in both cancer and normal cells Anaema, throm bocytopenia, nausea febrile neutropenia, etc. I-II