Evidence map›Paper›PMID 41920754›Full record

ReviewMini reviews in medicinal chemistry2026

Medicinal Chemistry of Fourth-generation Tyrosine Kinase Inhibitors.

Mohamed F Zayed

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In one paragraph

Review in Mini reviews in medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

1 author.

Mohamed F ZayedPharmaceutical Sciences Department, Fakeeh College for Medical Sciences, Fakeeh Care Group, Jeddah 21461, Saudi Arabia.ORCID 0000-0001-8683-5460

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Introduction / Objectives: Resistance to chemotherapies represents a critical challenge in the treatment of Non-Small Cell Lung Cancer (NSCLC). This clinical imperative drove the discovery of Fourth-Generation Tyrosine Kinase Inhibitors (FGTKIs) to defeat such resistance mechanisms. The study comprehensively reviews and critically analyzes the medicinal chemistry of FGTKIs, focusing on their rational design, mechanisms of action, Structure-Activity Relationships (SARs), and therapeutic potential for overcoming resistance mutations in oncology.

methodsA systematic search of major medical databases was conducted to recognize and integrate related literature.

resultsFGTKIs represent a class of structurally efficient anticancer agents that function through the allosteric inhibition of TKs via reversible interactions. This mechanism confers potent inhibitory activity along with improved pharmacokinetic and pharmacodynamic properties. DISCUSSION: They target the mutant-EGFR to overcome the tertiary resistant mutations (Del19/T790M/C797S), which represent a major clinical challenge against other Tyrosine Kinase Inhibitors (TKIs). They have definite molecular designs and pharmacokinetic properties supporting their action.

conclusionFGTKIs have altered the therapeutic concept for mutant NSCLC patients and offered unprecedented efficacy and durability compared to earlier-generation inhibitors.

Indexed as

Antineoplastic AgentsCarcinoma, Non-Small-Cell LungLung NeoplasmsProtein Kinase InhibitorsAnimalsChemistry, PharmaceuticalErbB ReceptorsHumansProtein-Tyrosine KinasesStructure-Activity RelationshipAntineoplastic AgentsErbB ReceptorsProtein Kinase InhibitorsProtein-Tyrosine Kinasesanti-cancer agentcancer cellfourth-generationMedicinal chemistryreceptortyrosine kinase inhibitors

Identifiers

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.