Imatinib mesylate


Imatinib mesylate

Drug updated on 4/17/2024

Dosage FormTablet (oral; 100 mg, 400 mg)
Drug ClassKinase inhibitors
Ongoing and
Completed Studies


  • Indicated for the treatment of newly diagnosed adult and pediatric patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase.
  • Indicated for the treatment of patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in blast crisis (BC), accelerated phase (AP), or in chronic phase (CP) after failure of interferon-alpha therapy.
  • Indicated for the treatment of adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL).
  • Indicated for the treatment of pediatric patients with newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in combination with chemotherapy.
  • Indicated for the treatment of adult patients with myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with platelet-derived growth factor receptor (PDGFR) gene re-arrangements.
  • Indicated for the treatment of adult patients with aggressive systemic mastocytosis (ASM) without the D816V c-Kit mutation or with c-Kit mutational status unknown.
  • Indicated for the treatment of adult patients with hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL) who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or fluorescence in situ hybridization [FISH] demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unknown.
  • Indicated for the treatment of adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans (DFSP).
  • Indicated for the treatment of patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST).
  • Indicated for the treatment of adjuvant treatment of adult patients following resection of Kit (CD117) positive GIST.

Latest News

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  • Imatinib mesylate (Gleevec) is indicated for the treatment of various conditions, including Philadelphia chromosome-positive chronic myeloid leukemia, acute lymphoblastic leukemia, myelodysplastic/myeloproliferative diseases associated with PDGFR gene rearrangements, aggressive systemic mastocytosis without D816V c-Kit mutation or unknown status, hypereosinophilic syndrome and/or chronic eosinophilic leukemia with FIP1L1-PDGFRα fusion kinase presence or unknown status. Additionally, it is used in unresectable dermatofibrosarcoma protuberans and Kit-positive gastrointestinal stromal tumors.
  • Ten studies were reviewed to gather information about Gleevec, providing a comparative analysis on safety and effectiveness across different conditions.
  • The drug has been associated with both mild (64.7%) and severe (28.6%) hepatotoxicity in CML patients, but its impact on thyroid functions appears minimal, which suggests better safety in this aspect compared to other treatments.
  • In pediatric populations suffering from CML, Imatinib causes significant short-term adverse effects on height growth, regardless of their pubertal status, raising concerns for its use when compared to available data on other drugs.
  • For Caucasian populations specifically, who have MDR1 G2677T/A and C3435T polymorphisms predicting resistance against Imatinib, genetic testing may be required for optimizing therapy effectiveness, indicating a nuanced need within this subgroup population.
  • In comparison with second- and third-generation TKIs while treating Philadelphia chromosome-positive chronic phase CML patients, although these newer generation TKIs outperform Imatinib in clinical responses, they exhibit a higher incidence of severe adverse events. This suggests that despite lower efficacy, Imatinib could be considered a safer option, especially among patients with comorbidities.

Product Monograph / Prescribing Information

Document TitleYearSource
Gleevec (imatinib mesylate) Prescribing Information.2024Novartis Pharmaceuticals Corporation East Hanover, NJ

Systematic Reviews / Meta-Analyses

Document TitleYearSource
The prevalence of hepatic and thyroid toxicity associated with imatinib treatment of chronic myeloid leukaemia: a systematic review. 2024International Journal of Clinical Pharmacy
Effect of imatinib mesylate on growth in pediatric chronic myeloid leukemia: a systematic review and meta-analysis.2023Journal of Pediatric Hematology/Oncology
Tyrosine kinase inhibitors versus radiation therapy in unresectable dermatofibrosarcoma protuberans (DFSP): a narrative systematic review. 2023American Journal of Surgery
MDR1 gene polymorphisms and imatinib response in chronic myeloid leukemia: a meta-analysis. 2022Journal of Oncology Pharmacy Practice
Prevalence of anemia among chronic myeloid leukemia patients treated with imatinib: a evidence-based meta-analysis. 2022Current Reviews in Clinical and Experimental Pharmacology
Use of tyrosine kinase inhibitors for paediatric Philadelphia chromosome-positive acute lymphoblastic leukaemia: a systematic review and meta-analysis. 2021BMJ Open
Treatment of lymphocyte-variant hypereosinophilic syndrome (L-HES): what to consider after confirming the elusive diagnosis.2021British Journal of Haematology
Efficacy and safety of imatinib mesylate in systemic sclerosis. A systematic review and meta-analysis.2020Expert Review of Clinical Immunology
First-line imatinib vs second- and third-generation TKIs for chronic-phase CML: a systematic review and meta-analysis.2020Blood Advances
Association of oral mucosa hyperpigmentation with imatinib mesylate use: a cross-sectional study and a systematic literature review.2019Clinical Oral Investigation

Clinical Practice Guidelines