Side Effects of imatinib: A Synthesis of Findings from 17 Studies

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Original Abstract of the Article

Major Research Findings

Imatinib (STI571, Gleevec/Glivec) and other small-molecule tyrosine kinase inhibitors are highly effective in the treatment of chronic myeloid leukemia (CML), gastrointestinal stromal tumors and, for example, eosinophilia-associated chronic myeloproliferative disorders. 11 This molecularly targeted approach disrupts abnormal tyrosine kinase dependent signalling pathways, thus providing a preferred treatment option for selected neoplastic disorders with activating mutations of Abelson-, Abl-related-, Kit-, and platelet-derived growth factor receptor A and B genes. 11 Compared with conventional treatments, TKIs are delivered over longer periods of time and are more specific in their targets (i.e. molecularly targeted), thus presenting different side effect profiles. 1 Imatinib is generally well tolerated. However, toxicities including edema, skin rashes, fatigue, nausea and myelosuppression have been reported. 11 Imatinib contributes to disease stabilization in the treatment of gastrointestinal stromal tumors, and 34% of patients achieve tumor remission (partial or complete response). , 6 Imatinib is generally well tolerated in patients with gastrointestinal stromal tumors. 6 Cutaneous reactions to imatinib are common and occur in 9.5% to 69% of patients depending on the series reported. 10

Reasons for Side Effects

Imatinib is a tyrosine kinase inhibitor that suppresses cancer cell growth by inhibiting signal transduction pathways involved in cell proliferation and survival. 11 However, imatinib inhibits tyrosine kinases in normal cells as well as cancer cells, so it can cause side effects. 11 Side effects can worsen with increased imatinib blood levels. 4

Common Side Effects

Edema

One of the most common side effects of imatinib is edema of the face and legs. 1 , 6 , 12 Imatinib is known to cause periorbital edema. 12 , 9 Edema can worsen with increased imatinib blood levels. 4

Skin Rash

Imatinib can cause skin rash. 11 , 1 Rash can worsen with increased imatinib blood levels. 4

Fatigue

Imatinib can cause fatigue. 11 , 1

Nausea

Imatinib can cause nausea. 11 , 1 , 6

Myelosuppression

Imatinib can cause myelosuppression. 11 This is because imatinib inhibits tyrosine kinases in normal bone marrow cells, which suppresses bone marrow cell proliferation. 11 Myelosuppression can cause symptoms such as anemia, leukopenia, and thrombocytopenia. 11

Diarrhea

Imatinib can cause diarrhea. 1 , 6

Hypertension

Imatinib can cause hypertension. 1

Thyroid Dysfunction

Imatinib can cause thyroid dysfunction. 1

Muscle and Joint Pain

Imatinib can cause muscle and joint pain. 1

Skin and Oral Conditions

Imatinib can cause skin and oral conditions. 1

Ocular Side Effects

Imatinib can cause ocular side effects. 12 , 9 , 3 The most common side effect is periorbital edema. 12 , 9 In addition to periorbital edema, conjunctival hemorrhage and eye edema have also been reported. 3

Rare Side Effects

Imatinib can rarely cause serious side effects. 2 Serious side effects include gastrointestinal or intra-abdominal bleeding, sigmoid sinus thrombosis, and splenic infarction. 2

Side Effects Management

Edema

Edema can be reduced by lowering imatinib blood levels. 4

Skin Rash

Skin rash can be treated with medications such as steroid ointments and antihistamines. 10

Fatigue

Fatigue can be alleviated by rest and hydration. 11

Nausea

Nausea can be treated with antiemetics. 11

Myelosuppression

Myelosuppression can be treated with medications such as hematopoietic growth factors. 11

Comparison between Studies

Commonalities between Studies

Many studies have shown that imatinib can cause side effects such as edema, skin rash, fatigue, nausea, and myelosuppression. 11 , 1 , 6 , 10

Differences between Studies

The frequency and severity of side effects caused by imatinib vary from study to study. 10 This may be due to differences in the patient populations studied and the research methods used. 10

Cautions Regarding Real-Life Applications

Imatinib is an effective anti-cancer drug, but it can cause side effects. 11 If you are taking imatinib, it is important to talk to your doctor and understand the risks and benefits of side effects. 11

Limitations of Current Research

The molecular mechanisms of imatinib side effects are not yet fully understood. 11

Future Research Directions

It is necessary to elucidate the molecular mechanisms of imatinib side effects and develop new treatments to reduce side effects. 11

Conclusion

Imatinib is a tyrosine kinase inhibitor that is effective in treating CML, GIST, and eosinophilia-associated chronic myeloproliferative disorders. 11 Imatinib is generally well tolerated, but it can cause side effects such as edema, skin rash, fatigue, nausea, and myelosuppression. 11 If you are taking imatinib, it is important to talk to your doctor and understand the risks and benefits of side effects. 11

Literature analysis of 17 papers
Positive Content
15
Neutral Content
0
Negative Content
2
Article Type
0
0
1
4
17
1.

Systematic review of the side effects associated with tyrosine kinase inhibitors used in the treatment of gastrointestinal stromal tumours on behalf of the EORTC Quality of Life Group.

Author: SodergrenSamantha C, WhiteAlice, EfficaceFabio, SprangersMirjam, FitzsimmonsDeborah, BottomleyAndrew, JohnsonColin D

GIST treatment
Targeted therapy
Fatigue
Gastrointestinal effects
Haematological disorders
Oedema

Tyrosine kinase inhibitors (TKIs) have revolutionized the treatment of advanced gastrointestinal stromal tumors (GISTs), but they can have side effects. This review summarizes the safety profiles of imatinib and sunitinib, highlighting common side effects such as gastrointestinal complaints, edema, fatigue, and hematological disorders.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.
Systematic ReviewA review that systematically collects, evaluates, and integrates relevant research to answer a specific research question.

Language : English

2.

Sigmoid Sinus Thrombosis Followed by Splenic Infarction Due to Imatinib Therapy in a Patient with Gastrointestinal Stromal Tumor; Hematological Side Effects of Imatinib.

Author: YilmazHatice, DemirağGüzin, YılmazAli

GIST treatment
Sigmoid sinus thrombosis
Splenic infarction

This report describes a patient with GIST who developed sigmoid sinus thrombosis and splenic infarction during imatinib treatment. This highlights the importance of neurological and gastrointestinal evaluation in patients on imatinib therapy.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

4.

[Imatinib plasma levels in the management of cutaneous side effects induced by imatinib (Glivec®): 2 case reports].

Author: TrabelsiSameh, GaïesEmna, SraïriSamia, SahnounRim, DaghfousRiadh, LakhalMohamed, El AïdliSihem, KlouzAnis

Cancer treatment
Cutaneous toxicity
Hematologic toxicity
Neurologic toxicity

This case report highlights the importance of drug monitoring for imatinib, an antineoplastic drug, to prevent and manage cutaneous side effects.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.
English AbstractA summary of a research paper/publication written in English for a wider audience.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : French

6.

Activity and side effects of imatinib in patients with gastrointestinal stromal tumors: data from a German multicenter trial.

Author: SchlemmerMarcus, BauerS, SchütteR, HartmannJ T, BokemeyerC, HosiusC, ReichardtP

GIST treatment
Diarrhea
Eyelid edema
Fatigue
Muscle cramps
Nausea
Peripheral edema

Gastrointestinal stromal tumors (GIST) are mesenchymal tumors that were previously classified as leiomyosarcomas or leiomyomas. Imatinib is a drug that has shown efficacy in the treatment of GIST. This multicenter phase II trial assessed the efficacy, safety, and tolerability of imatinib in patients with unresectable or metastatic GIST. The trial found that 34% of patients attained a tumor remission and 70% were free of progression within the first year of treatment.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Multicenter StudyResearch conducted in collaboration with multiple research institutions. It aims to collect a wide range of data and obtain more generalizable results.

Language : English

7.

[Complete response achieved in a case of gastric gastrointestinal stromal tumor by administration of imatinib mesilate with concurrent relatively high-dose steroid therapy to control side effects].

Author: TsukadaYuichiro, TauchiKatsunori, NakamuraMasato, KishimotoHirofumi, YoshifukuSeijiro, OtagiriNoriaki, SasaharaKotaro

Reduce tumor size
Treat GIST
Fever
Pruritic dermatitis
Pruritic rash
Pruritus

This case report describes a 53-year-old man with gastric gastrointestinal stromal tumor (GIST) who achieved a complete response to imatinib therapy after experiencing significant side effects.

Case ReportsIn the medical field, a report that describes in detail a unique case, an unusual medical condition, or the effect of a treatment. Provides new insights and possibilities for treatment through individual patient cases.
English AbstractA summary of a research paper/publication written in English for a wider audience.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : Japanese

9.

Ocular side effects in chronic myeloid leukemia patients treated with imatinib.

Author: BrecciaMassimo, GentiliniFabiana, CannellaLaura, LatagliataRoberto, CarmosinoIda, FrustaciAnnamaria, AlimenaGiuliana

Ocular toxicity

Imatinib mesylate, a tyrosine kinase inhibitor, is used to treat chronic myeloid leukemia (CML). This report describes the ocular complications observed in imatinib-treated Ph+ CML patients, ranging from mild periorbital edema to serious adverse events such as glaucoma.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

11.

[Hematological side effects of tyrosine kinase inhibition using imatinib].

Author: Schmitt-GraeffA, HochhausA

Leukemia treatment
Tumor treatment
Hematological side effects
Myelosuppression

Imatinib is effective in treating chronic myeloid leukemia, but it can cause side effects such as edema, skin rashes, fatigue, nausea, and myelosuppression.

English AbstractA summary of a research paper/publication written in English for a wider audience.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : German

12.

Ocular side-effects associated with imatinib mesylate (Gleevec).

Author: FraunfelderFrederick W, SolomonJonathan, DrukerBrian J, EsmaeliBita, KuylJennifer

Epiphora
Periorbital edema

This retrospective case series describes ocular side effects associated with imatinib mesylate therapy. Periorbital edema and epiphora are the two most common side effects, and they are typically managed conservatively.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

13.

[A case of heritable pulmonary arterial hypertension treated with long-term oral low-dose imatinib].

Author: GaoA L, GongJ N, LiJ F, YangY H

Improved symptoms

A patient with heritable pulmonary arterial hypertension (HPAH) due to a bone morphogenetic protein 2 (BMPR2) gene mutation showed significant improvement after receiving oral imatinib for 45 months. This case report suggests that imatinib may be a feasible treatment option for HPAH.

English AbstractA summary of a research paper/publication written in English for a wider audience.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : Chinese

14.

The small-molecule kinase inhibitor ceritinib, unlike imatinib, causes a significant disturbance of lipid membrane integrity: A combined experimental and MD study.

Author: FischerMarkus, LuckMeike, WerleMax, VogelAlexander, BashawatMohammad, LudwigKai, ScheidtHolger A, MüllerPeter

Cancer treatment
Apoptosis
Cell lysis

This study investigated the interaction of ceritinib and imatinib, protein kinase inhibitors, with lipid membranes. Ceritinib was found to interact more strongly with membranes, potentially impacting its safety and efficacy.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

15.

The Progress of Small Molecule Targeting BCR-ABL in the Treatment of Chronic Myeloid Leukemia.

Author: ZhangYuan, WuXin, SunXueyan, YangJun, LiuChang, TangGuotao, LeiXiaoyong, HuangHonglin, PengJunmei Peng

New drug candidates
Targeted CML therapy

This review summarizes the current state of small-molecule drugs for treating chronic myelogenous leukemia (CML), including tyrosine kinase inhibitors (TKIs) and BCR-ABL protein degraders. These advancements provide new therapeutic options for CML.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

17.

Revisiting six established practices in the treatment of chronic myeloid leukaemia.

Author: KantarjianHagop M, WelchMary Alma, JabbourElias

Improved CML treatment
Improved compliance
Reduced toxicity
CML
TKI resistance

This viewpoint suggests that lower than approved doses of tyrosine kinase inhibitors (TKIs) may be equally effective in treating chronic myeloid leukemia (CML), while reducing toxicity, improving compliance, and lowering costs. The article also discusses considerations for TKI dose reduction in response to side effects and the potential benefits of generic TKIs.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

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