Gumarontinib: Difference between revisions

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{{Short description|A third-generation EGFR inhibitor used in cancer treatment}}
== Gumarontinib ==
{{Drugbox
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| caption = Chemical structure of Gumarontinib
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'''Gumarontinib''' is a third-generation [[epidermal growth factor receptor]] (EGFR) [[tyrosine kinase inhibitor]] (TKI) used in the treatment of certain types of [[non-small cell lung cancer]] (NSCLC). It is specifically designed to target and inhibit the activity of the EGFR with the T790M mutation, which is a common mechanism of resistance to first- and second-generation EGFR inhibitors.
[[File:Gumarontinib.svg|Chemical structure of Gumarontinib|thumb|right]]


==Mechanism of Action==
'''Gumarontinib''' is a small molecule [[tyrosine kinase inhibitor]] (TKI) that is primarily used in the treatment of certain types of [[non-small cell lung cancer]] (NSCLC). It is specifically designed to target mutations in the [[epidermal growth factor receptor]] (EGFR), which are commonly found in NSCLC patients.
Gumarontinib works by selectively binding to the mutated form of the EGFR, particularly the T790M mutation, which is often responsible for acquired resistance in patients who have been treated with earlier generation EGFR inhibitors. By inhibiting the kinase activity of the mutated receptor, gumarontinib effectively blocks the downstream signaling pathways that promote cancer cell proliferation and survival.


==Clinical Use==
== Mechanism of Action ==
Gumarontinib is indicated for the treatment of patients with metastatic NSCLC who have developed resistance to previous EGFR TKI therapy due to the T790M mutation. It is administered orally and has shown efficacy in shrinking tumors and prolonging progression-free survival in clinical trials.
Gumarontinib functions by inhibiting the activity of the EGFR tyrosine kinase. EGFR is a transmembrane protein that, when activated by binding to its specific ligands, triggers a cascade of downstream signaling pathways that promote cell proliferation and survival. In many cancers, including NSCLC, mutations in the EGFR gene lead to its constitutive activation, driving uncontrolled cell division and tumor growth. Gumarontinib binds to the ATP-binding site of the mutated EGFR, thereby blocking its kinase activity and inhibiting tumor cell proliferation.


==Pharmacokinetics==
== Clinical Use ==
Gumarontinib is absorbed orally and undergoes hepatic metabolism. It has a half-life that allows for once-daily dosing, which is convenient for patients. The drug is primarily excreted through the feces, with a smaller portion eliminated via the urine.
Gumarontinib is indicated for the treatment of adult patients with locally advanced or metastatic NSCLC with specific EGFR mutations. These mutations are typically identified through genetic testing of tumor samples. The drug is administered orally and is part of a class of targeted therapies that have improved outcomes for patients with EGFR-mutant NSCLC compared to traditional chemotherapy.


==Side Effects==
== Development and Approval ==
Common side effects of gumarontinib include diarrhea, rash, nausea, and fatigue. More serious adverse effects can include interstitial lung disease, hepatotoxicity, and cardiac effects. Patients are monitored regularly to manage these potential side effects.
Gumarontinib was developed following the discovery of resistance mechanisms to earlier generations of EGFR inhibitors. It is designed to overcome resistance conferred by the T790M mutation, a common secondary mutation that arises in patients treated with first-generation EGFR inhibitors. The development of Gumarontinib involved extensive preclinical studies and clinical trials to establish its efficacy and safety profile.


==Development==
== Side Effects ==
Gumarontinib was developed as part of an effort to overcome resistance mechanisms in EGFR-mutant NSCLC. Its development involved extensive research into the structure and function of the EGFR and the mutations that confer drug resistance.
Common side effects of Gumarontinib include diarrhea, rash, nausea, and fatigue. More serious adverse effects can include interstitial lung disease, liver toxicity, and cardiac effects. Patients receiving Gumarontinib require regular monitoring to manage these potential side effects effectively.


==Related Pages==
== Related Pages ==
* [[Epidermal growth factor receptor]]
* [[Epidermal growth factor receptor]]
* [[Non-small cell lung cancer]]
* [[Tyrosine kinase inhibitor]]
* [[Tyrosine kinase inhibitor]]
* [[Non-small cell lung cancer]]
* [[Cancer treatment]]
* [[Cancer treatment]]



Latest revision as of 01:28, 6 March 2025

Gumarontinib[edit]

Chemical structure of Gumarontinib

Gumarontinib is a small molecule tyrosine kinase inhibitor (TKI) that is primarily used in the treatment of certain types of non-small cell lung cancer (NSCLC). It is specifically designed to target mutations in the epidermal growth factor receptor (EGFR), which are commonly found in NSCLC patients.

Mechanism of Action[edit]

Gumarontinib functions by inhibiting the activity of the EGFR tyrosine kinase. EGFR is a transmembrane protein that, when activated by binding to its specific ligands, triggers a cascade of downstream signaling pathways that promote cell proliferation and survival. In many cancers, including NSCLC, mutations in the EGFR gene lead to its constitutive activation, driving uncontrolled cell division and tumor growth. Gumarontinib binds to the ATP-binding site of the mutated EGFR, thereby blocking its kinase activity and inhibiting tumor cell proliferation.

Clinical Use[edit]

Gumarontinib is indicated for the treatment of adult patients with locally advanced or metastatic NSCLC with specific EGFR mutations. These mutations are typically identified through genetic testing of tumor samples. The drug is administered orally and is part of a class of targeted therapies that have improved outcomes for patients with EGFR-mutant NSCLC compared to traditional chemotherapy.

Development and Approval[edit]

Gumarontinib was developed following the discovery of resistance mechanisms to earlier generations of EGFR inhibitors. It is designed to overcome resistance conferred by the T790M mutation, a common secondary mutation that arises in patients treated with first-generation EGFR inhibitors. The development of Gumarontinib involved extensive preclinical studies and clinical trials to establish its efficacy and safety profile.

Side Effects[edit]

Common side effects of Gumarontinib include diarrhea, rash, nausea, and fatigue. More serious adverse effects can include interstitial lung disease, liver toxicity, and cardiac effects. Patients receiving Gumarontinib require regular monitoring to manage these potential side effects effectively.

Related Pages[edit]