Drug updated on 12/11/2024
| 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-PDGFR 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-PDGFR 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
Summary
- This summary is based on the review of five systematic review(s)/meta-analysis(es). [1-5]
- Gastrointestinal Stromal Tumors (GIST): In three out of four studies reviewed, low-dose imatinib (400 mg/day) demonstrated clinically meaningful responses, with no significant difference in response outcomes compared to higher doses (600-800 mg/day).
- Chronic Myeloid Leukemia (CML) and GIST with Genetic Polymorphisms: The genotype ATP binding cassette subfamily G member 2 (ABCG2) c.421C>A is associated with increased imatinib plasma trough levels, suggesting potential implications for efficacy, while ATP binding cassette subfamily B member 1 (ABCB1) polymorphisms showed no significant association with imatinib plasma levels.
- Philadelphia Chromosome Positive Myelodysplastic Syndrome (Ph+ MDS): A 38-year-old female patient achieved bone marrow remission with no recurrence following a combination of imatinib mesylate and chemotherapy, followed by allogeneic hematopoietic stem cell transplantation.
- In patients with advanced GIST, high-dose imatinib was associated with a higher incidence of grade ≥ 3 adverse events (AEs), particularly in blood and lymphatic system disorders, gastrointestinal disorders, and general disorders, compared to low-dose imatinib.
- Generic imatinib exhibited a safety profile comparable to branded imatinib, though some studies noted inconsistent findings regarding toxicity.
- Patients with advanced metastatic or nonresectable GIST benefit from low-dose imatinib due to fewer severe adverse events. Homozygous carriers of the ABCG2 c.421 A allele among GIST and CML patients show higher imatinib plasma levels, potentially affecting efficacy and safety. A 38-year-old Ph+ MDS patient demonstrated remission with combination therapy and stem cell transplant. Generic imatinib generally shows effectiveness and safety in CML patients, though long-term assessments are suggested. Prolonged imatinib use in leukemia patients is linked to oral hyperpigmentation, which is heightened with concurrent hydroxyurea use.
Product Monograph / Prescribing Information
| Document Title | Year | Source |
|---|---|---|
| Gleevec (imatinib mesylate) Prescribing Information. | 2024 | Novartis Pharmaceuticals Corporation, East Hanover, NJ |
Systematic Reviews / Meta-Analyses
| Document Title | Year | Source |
|---|---|---|
| Safety outcomes of low versus high dose imatinib mesylate in patients with advanced, metastatic, or nonresectable gastrointestinal stromal tumors: A systematic review | 2024 | Gastrointestinal Tract (Hong Kong, China) |
| Impact of ABCG2 and ABCB1 Polymorphisms on Imatinib Plasmatic Exposure: An Original Work and Meta-Analysis | 2023 | International Journal Of Molecular Sciences |
| TKIs combined with chemotherapy followed by allo-HSCT in Philadelphia chromosome-positive myelodysplastic syndrome: A case report and literature review | 2022 | Medicine |
| Current evidence on the efficacy and safety of generic imatinib in CML and the impact of generics on health care costs | 2021 | Blood Advances |
| Association of oral mucosa hyperpigmentation with imatinib mesylate use: a cross-sectional study and a systematic literature review | 2019 | Clinical Oral Investigations |
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 |