Drug updated on 4/17/2024
| Dosage Form | Tablet (oral; 100 mg, 400 mg) |
| Drug Class | Kinase inhibitors |
| Ongoing and Completed Studies | ClinicalTrials.gov |
Indication
- 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.
Summary
- 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 Title | Year | Source |
|---|---|---|
| Gleevec (imatinib mesylate) Prescribing Information. | 2024 | Novartis Pharmaceuticals Corporation East Hanover, NJ |
Systematic Reviews / Meta-Analyses
Clinical Practice Guidelines
| Document Title | Year | Source |
|---|---|---|
| Acute lymphoblastic leukemia, version 2.2021, NCCN clinical practice guidelines in oncology. | 2021 | Journal of the National Comprehensive Network of Cancer |
| Chronic myeloid leukemia, version 2.2021, NCCN clinical practice guidelines in oncology. | 2020 | Journal of the National Comprehensive Cancer Network |
| Gastrointestinal stromal tumours (GISTs): French intergroup clinical practice guidelines for diagnosis, treatments and follow-up (SNFGE, FFCD, GERCOR, UNICANCER, SFCD, SFED, SFRO). | 2019 | Digestive and Liver Disease |