Side Effects of gefitinib: A Synthesis of Findings from 24 Studies

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Original Abstract of the Article

Major Research Findings

Gefitinib is an EGFR tyrosine kinase inhibitor used to treat EGFR-mutant positive lung cancer. Multiple studies have shown that gefitinib is effective in treating lung cancer. However, gefitinib can cause some side effects. For example, a study by 1 shows that gefitinib can cause inflammatory responses such as interstitial pneumonia.

A study by 23 shows that gefitinib can cause intestinal toxicity, which may be responsible for diarrhea, one of the most common side effects of gefitinib therapy.

A study by 11 reports that gefitinib can cause skin side effects.

A study by 3 reports that gefitinib can cause eyelash trichomegaly. This is thought to be due to gefitinib's effect on skin cell growth. However, this side effect often does not affect the patient's quality of life and does not require discontinuation of treatment.

A study by 4 suggests that gefitinib may also be effective in treating Cushing's disease.

Reasons for Side Effects

The side effects of gefitinib are thought to be caused by inhibiting EGFR tyrosine kinase, which affects cell growth and survival. By inhibiting EGFR, gefitinib may also affect the growth of normal cells, which may cause side effects.

Common Side Effects

Diarrhea

One of the most common side effects of gefitinib is diarrhea. This is confirmed by a study by 23 . Diarrhea is thought to occur when gefitinib affects intestinal cells, inhibiting their function. Diarrhea usually improves when gefitinib is discontinued.

Skin Side Effects

Gefitinib can cause skin side effects. This is confirmed by a study by 11 . Skin side effects include rash, dryness, and itching. Skin side effects usually improve when gefitinib is discontinued.

Interstitial Pneumonia

Gefitinib can cause inflammatory responses such as interstitial pneumonia. This is confirmed by a study by 1 . Interstitial pneumonia is a condition in which the tissue in the lungs becomes inflamed. Interstitial pneumonia can rarely cause serious symptoms, but it usually improves when gefitinib is discontinued.

Other

In addition to the above, gefitinib can also cause side effects such as nausea, vomiting, loss of appetite, fatigue, and liver dysfunction.

Countermeasures for Side Effects

Diarrhea

Treatment for diarrhea may include the use of intestinal regulators and antidiarrheal medications. Dietary and hydration therapy are also important. In severe cases, the dose of gefitinib may be reduced or temporarily discontinued.

Skin Side Effects

Treatment for skin side effects may include the use of moisturizers and steroid ointments. It is also important to use sunscreen and reduce time spent in the sun. In severe cases, the dose of gefitinib may be reduced or temporarily discontinued.

Interstitial Pneumonia

Treatment for interstitial pneumonia may include the use of steroid medications. In severe cases, gefitinib may need to be discontinued.

Comparison between Studies

Common Points

Multiple studies have confirmed that gefitinib can cause a variety of side effects. These studies show that gefitinib is effective in treating lung cancer, but it is important to consider the risk of side effects.

Points of Difference

The frequency and severity of gefitinib side effects differ across studies. This is likely due to differences in the characteristics of the study participants, the dose of gefitinib, and the duration of treatment.

Points to Note Regarding Application to Real Life

Gefitinib is an effective drug for treating EGFR-mutant positive lung cancer, but it can cause some side effects. When taking gefitinib, it is important to follow your doctor's instructions and be aware of side effects. If you are concerned about side effects, talk to your doctor.

Limitations of Current Research

The side effects of gefitinib are not yet fully understood. Further research is needed to better understand the side effects of gefitinib.

Future Research Directions

Future research is needed to reduce the side effects of gefitinib. For example, optimizing the dose and administration method of gefitinib may reduce side effects. The development of drugs that prevent gefitinib side effects is also expected.

Conclusion

Gefitinib is an effective drug for treating EGFR-mutant positive lung cancer, but it can cause some side effects. When taking gefitinib, it is important to follow your doctor's instructions and be aware of side effects. If you are concerned about side effects, talk to your doctor. Further research is needed to better understand the side effects of gefitinib.

Literature analysis of 24 papers
Positive Content
19
Neutral Content
2
Negative Content
3
Article Type
0
0
0
4
23
1.

Gefitinib initiates sterile inflammation by promoting IL-1β and HMGB1 release via two distinct mechanisms.

Author: NoguchiTakuya, SekiguchiYuto, KudohYuki, NaganumaRio, KagiTomohiro, NishidateAkiko, MaedaKazuhiro, IshiiChizuru, ToyamaTakashi, HirataYusuke, HwangGi-Wook, MatsuzawaAtsushi

Inflammation
Interstitial pneumonitis

Gefitinib, an anticancer drug, induces inflammation by promoting the release of mature IL-1β and HMGB1. This process involves mitochondrial reactive oxygen species (mtROS) which stimulate NLRP3 inflammasome activation for IL-1β release and γH2AX accumulation for HMGB1 release through PARP-1 activation.

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.

Language : English

2.

A novel cyclic NP1 reveals obstruction of EGFR kinase activity and attenuation of EGFR-driven cell lines.

Author: JiwacharoenchaiNattanan, TabtimmaiLueacha, KiriwanDuangnapa, SuwattanasophonChonticha, SeetahaSupaphorn, SinthuvanichChomdao, ChoowongkomonKiattawee

NP1 EGFR inhibitor

This study screened cyclic peptides against the tyrosine kinase domain of EGFR (TK-EGFR) using a phage display library. The study identified a novel peptide inhibitor, NP1, which demonstrated an inhibitory effect against TK-EGFR at IC50 within the nanomolar range.

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.

Language : English

3.

Eyelashes Trichomegaly: An Unusual Side Effect of Gefitinib Therapy.

Author: AgrawalChaturbhuj R, GoyalPankaj, DovalDinesh Chandra, DuttaKumardeep, DomadiaKshitij, KothiwalSilky

Diarrhea
Fatigability
Liver function tests
Skin rashes

This case report describes a 52-year-old female patient with metastatic lung carcinoma who developed trichomegaly of eyelashes while on gefitinib therapy. Trichomegaly is a rare side effect of epidermal growth factor receptor inhibitors.

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.

Language : English

6.

c(RGDfK) anchored surface manipulated liposome for tumor-targeted tyrosine kinase inhibitor (TKI) delivery to potentiate liver anticancer activity.

Author: DeepakPayal, KumarPraveen, AryaDilip Kumar, PandeyPrashant, KumarShiv, ParidaBishnu Prasad, NarayanGopeshwar, SinghSanjay, RajinikanthParuvathanahalli Siddalingam

Improved HCC targeting
Increased anticancer efficacy
Reduced toxicity

This study developed and assessed c(RGDfK) surface modified liposomes for targeted delivery of Gefitinib, an EGFR inhibitor, to hepatocellular carcinoma cells. The modified liposomes showed enhanced cytotoxicity and tumor accumulation compared to conventional liposomes.

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

Language : English

7.

Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.

Author: AmrheinJennifer A, BeyettTyler S, FengWilliam W, KrämerAndreas, WeckesserJanik, SchaeffnerIlse K, RanaJaimin K, JännePasi A, EckMichael J, KnappStefan, HankeThomas

Kinome selectivity
NSCLC treatment

This study describes the development of a new EGFR inhibitor with improved selectivity for EGFR mutations. Activating mutations in the epidermal growth factor receptor (EGFR) are common drivers of non-small-cell lung cancer (NSCLC). EGFR inhibitors like gefitinib and erlotinib are effective but have off-target effects and can inhibit wild-type EGFR, leading to side effects. This study utilizes a macrocyclic strategy to enhance selectivity for EGFR mutations, potentially improving treatment efficacy while minimizing side effects.

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.
Research Support, U.S. Gov't, Non-P.H.S.Research funding provided by US government agencies other than the Public Health Service.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.

Language : English

9.

Long-Term Effect of Erlotinib Therapy in the Third Line of Anticancer Treatment in a Patient with Non-Small-Cell Lung Cancer - a Case Report.

Author: ŠťastnáNela, JakubíkováLenka, BratKristián

Improved prognosis

This article discusses the treatment of malignant tumors of the trachea, lungs, and bronchus in the Czech Republic, focusing on the use of tyrosine kinase inhibitors (TKIs). TKIs are targeted therapies that can be effective in treating non-small-cell lung cancer with specific mutations. The article highlights the importance of early diagnosis and treatment with appropriate TKIs to improve prognosis for patients with these tumors.

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

10.

Study on the hepatotoxicity and potential mechanism of gefitinib based on CYP450 in mice and AML12 cells.

Author: YinXiaoting, MaSuzhen, LiMengyuan, LuShuaifei, ZhangChangjing, LiuHui, LiCaiyin, SuPan, BaiMing, LiYucheng

Hepatotoxicity

Gefitinib-induced hepatotoxicity may be associated with CYP1A1, CYP2D9, and CYP2D10, suggesting a potential mechanism for the side effect.

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

Language : English

12.

Clinically actionable genotypes for anticancer prescribing among >1500 patients with pharmacogenomic testing.

Author: ReizineNatalie M, DanaheyKeith, TruongTien M, GeorgeDavid, HouseLarry K, KarrisonTheodore G, van WijkXander M R, YeoKiang-Teck J, RatainMark J, O'DonnellPeter H

Predict toxicity

This study argues that comprehensive germline pharmacogenomic profiling could be highly relevant for cancer care due to increasing evidence supporting the role of such factors in predicting toxicity for anticancer therapies.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

14.

Lung adenocarcinoma concomitant with xeroderma pigmentosum: a case report.

Author: MatsumotoMasataka, KaneshiroKazumi, TakatsukiKiyonobu

Lung cancer
Xeroderma pigmentosum

This report describes a patient with xeroderma pigmentosum, a rare photosensitive dermatosis, who developed lung cancer. Patients with xeroderma pigmentosum are at increased risk for certain cancers.

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

15.

Recent Progress in Drug Delivery Systems for Tyrosine Kinase Inhibitors in the Treatment of Lung Cancer.

Author: Korucu AktasPelinsu, BaysalIpek, Yabanoglu-CiftciSamiye, LamprechtAlf, AricaBetul

Enhanced lung cancer treatment
Improved drug delivery

This review focuses on advancements in drug delivery systems for tyrosine kinase inhibitors (TKIs) used in lung cancer treatment. Nanoparticle-based delivery systems enhance bioavailability, stability, and retention, potentially improving treatment efficacy.

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

17.

Nitrogen-Containing Heterocycles as Anticancer Agents: An Overview.

Author: LangDamanpreet K, KaurRajwinder, AroraRashmi, SainiBalraj, AroraSandeep

cancer treatment
side effects

Cancer is a leading cause of death globally. Kinase inhibitors are a common strategy in anti-cancer drug development, but researchers are working to minimize side effects. Various factors contribute to cancer, including environmental factors and lifestyle choices. Treatment options include chemotherapy, radiotherapy, surgery, and immunotherapy, often in combination.

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

18.

Combination therapy with afatinib and bevacizumab in an EGFR-mutated non-small cell lung cancer patient with acquired ERBB2 amplification: A case report.

Author: ChenSixian, XiangTianmin, LuWei, HongShuiqiang, LiYuanyuan, LuYuan, ZhangQiongyue, ChenYongfeng, ZhouSuli, WangGehui, ZhangZhenzhen, CaiYongguang

EGFR mutation treatment

This review discusses the challenges of acquired resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in patients with non-small cell lung cancer (NSCLC).

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

21.

Gefitinib successfully administered in a lung cancer patient with leptomeningeal carcinomatosis after erlotinib-induced pneumatosis intestinalis.

Author: UrugaHironori, MoriguchiShuhei, TakahashiYui, OgawaKazumasa, MuraseKyoko, MochizukiSayaka, HanadaShigeo, TakayaHisashi, MiyamotoAtsushi, MorokawaNasa, KishiKazuma

Gefitinib administration
PI resolution
Pneumatosis intestinalis

Pneumatosis intestinalis (PI) is a side effect of erlotinib. In a case report of a 71-year-old woman with lung adenocarcinoma, PI occurred twice after erlotinib administration, but resolved after conservative therapies. Gefitinib was successfully administered after erlotinib-induced PI.

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

22.

A long-term survival case after resection of the pancreatic metastasis from lung cancer.

Author: KageyamaYumiko, YamaguchiRyuzo, WatanabeShinya, AizuKeiji, SatoFumiya, FujiedaHironori, YamadaMihoko, ToyodaYoshitaka, IwataTsutomu

Pancreatic metastasis treatment

This case report describes a long-term survivor of pancreatic metastasis from lung cancer after pancreatectomy. Pancreatic metastasis is not typically an indication for surgical resection, but this case suggests that resection may be a viable option for some patients.

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

Language : English

23.

A Transcriptomic Approach to Elucidate the Mechanisms of Gefitinib-Induced Toxicity in Healthy Human Intestinal Organoids.

Author: RodriguesDaniela, HerpersBram, FerreiraSofia, JoHeeseung, FisherCiarán, CoyleLuke, ChungSeung-Wook, KleinjansJos C S, JennenDanyel G J, de KokTheo M

Cancer treatment
EGFR inhibition
Drug safety concerns
Intestinal toxicity

Gefitinib induced toxicity in intestinal organoids by perturbing signal transduction pathways, apoptosis, cell cycle, FOXO-mediated transcription, p53 signaling pathway, and metabolic pathways. The study provides an avenue for drug screening and development.

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

Language : English

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