Tyrosine-kinase inhibitor
Tyrosine-kinase inhibitors (TKIs) are a class of targeted therapies designed to block the activity of tyrosine kinases, enzymes that transmit growth, survival, and differentiation signals through phosphorylation-dependent signaling pathways.
Tyrosine-kinase inhibitors (TKIs) are a class of targeted therapies designed to block the activity of tyrosine kinases, enzymes that transmit growth, survival, and differentiation signals through phosphorylation-dependent signaling pathways. In oncology, TKIs are used to suppress aberrant kinase-driven tumor proliferation and are especially important in cancers driven by oncogenic kinase signaling, such as EGFR-mutant non-small-cell lung cancer, chronic myeloid leukemia, gastrointestinal stromal tumors, renal cell carcinoma, and hepatocellular carcinoma.
Clinically, TKIs are often used as monotherapy or in combination with other systemic treatments, including immunotherapy, checkpoint inhibitor, and antiangiogenic agents such as apatinib or sorafenib. Their use is shaped by substantial interpatient pharmacokinetic variability, narrow therapeutic windows for some agents, and the frequent emergence of acquired resistance. As a result, TKIs are also a major focus of therapeutic drug monitoring, resistance-genotyping, and biomarker-driven treatment selection.
Where the papers sit
16 papers from the last 6 months study tyrosine-kinase inhibitor directly · updated from PubMed 12 Oct 2026
Study type 3 clinical trials · 5 observational · 4 human data · 4 preclinical
Themes 3 themes
-
Precision Cancer Therapy
Combination and precision strategies are being tested across advanced cancers rather than relying on TKI monotherapy. In hepatocellular carcinoma, camrelizumab, apatinib and radiotherapy, or lenvatinib with ADI-PEG 20, target response and progression-free survival. Stromal remodeling and drug penetration, PIK3CA selection, and HER2 targeting broaden the approach. Hypertension remains a recurring safety issue during VEGF-directed treatment.
6 papers · 37.5%
-
EGFR Resistance in Lung Cancer
EGFR-mutant lung cancer treatment is moving toward resistance-directed sequencing and mutation-specific inhibitors. Acquired resistance recurs through T790M, C797S, NF-κB/ALDH1A1 signaling and altered sphingolipid metabolism after EGFR-TKIs. Mefatinib and gefitinib are being compared in first-line care, while new compounds target L858R/T790M/C797S disease. Biosensors aim to detect resistance mutations earlier and guide treatment selection.
5 papers · 31.2%
-
Leukemia TKI Outcomes
Leukemia TKI care is shifting from indefinite treatment toward molecularly guided remission and survivorship management. In chronic myeloid leukemia, treatment-free remission and molecular relapse are defined through comprehensive monitoring, while adherence remains a modifiable determinant of success. Arterial stiffness and other adverse health events highlight cumulative vascular and real-world toxicity. TKI maintenance after brexucabtagene autoleucel extends targeted therapy into Philadelphia chromosome-positive acute lymphoblastic leukemia.
5 papers · 31.2%
Papers
The 16 papers from the last 6 months that study tyrosine-kinase inhibitor directly, newest first, by theme and by study type. Study types come from PubMed publication types and MeSH headings.
By theme
Precision Cancer Therapy (6)
- Efficacy and safety of immune checkpoint inhibitors combined with TKIs for recurrent or metastatic cervical cancer with PIK3CA mutation. PloS one · 29 Sept 2026 PMID 42809552
- Beyond Amplification: Precision Approaches to Targeting HER2. Clinical cancer research : an official journal of the American Association for Cancer Research · 9 Jul 2026 PMID 42423636
- The Combined Therapeutic Effect of Lenvatinib and ADI-PEG 20 in Advanced Hepatocellular Carcinoma: A Case Report. In vivo (Athens, Greece) · 30 Jun 2026 PMID 42379775
- Camrelizumab, Apatinib, and Radiotherapy in Locally Advanced, Unresectable Hepatocellular Carcinoma: A Phase II Study. Clinical cancer research : an official journal of the American Association for Cancer Research · 30 Jun 2026 PMID 42377073
- FAP-α-Responsive Size-Transformable Lipid Nanoparticles for Stromal Remodeling and Enhanced Drug Penetration in Fibrotic Hepatocellular Carcinoma. ACS applied materials & interfaces · 22 Jun 2026 PMID 42328782
- Cluster Randomized Controlled Trial of Intensive Systolic Blood Pressure Control in Patients With Renal Cell or Thyroid Cancer Receiving VEGFR Tyrosine Kinase Inhibitors: ECOG-ACRIN EAQ191. Hypertension (Dallas, Tex. : 1979) · 20 May 2026 PMID 42158981
EGFR Resistance in Lung Cancer (5)
- Mefatinib versus gefitinib as a first-line treatment for EGFR-mutated non-small cell lung cancer: a randomized, double-blind, multicenter phase III study. Signal transduction and targeted therapy · 12 Aug 2026 PMID 42586967
- Activation of the NF-κB/ALDH1A1 signaling promotes non-mutational resistance to EGFR-TKIs in non-small cell lung cancer. Oncogene · 23 Jul 2026 PMID 42493544
- A tri-modal biosensor based on alkyne-functionalized gold nanoparticles and molecular beacon for detection of resistance-related point mutations in epidermal growth factor receptor-tyrosine kinase inhibitors. Molecular biology reports · 22 May 2026 PMID 42171913
- Design, synthesis and biological evaluation of selective inhibitors against the L858R/T790 M/C797S mutant EGFR kinase based on the scaffold of brigatinib. European journal of medicinal chemistry · 5 May 2026 PMID 42085935
- Altered Sphingolipid Metabolism is Associated with Osimertinib Resistance in Nonsmall-Cell Lung Cancer. Journal of proteome research · 16 Apr 2026 PMID 41988688
Leukemia TKI Outcomes (5)
- Modifiable determinants of adherence to tyrosine kinase inhibitors in classical myeloproliferative neoplasms: A mixed-methods systematic review protocol. PloS one · 18 Sept 2026 PMID 42758748
- Arterial stiffness in patients with chronic myeloid leukemia receiving tyrosine kinase inhibitors: An exploratory prospective observational study. Leukemia research · 4 Aug 2026 PMID 42551129
- Improved outcomes with TKI maintenance after brexucabtagene autoleucel in Philadelphia chromosome ALL. Blood advances · 25 Jun 2026 PMID 42349018
- Comprehensive molecular characterization of treatment-free remission and molecular relapse in chronic myeloid leukemia patients: the EURO-SKI Biomarker Study. Leukemia · 18 Jun 2026 PMID 42315627
- Adverse Health Events in Chronic Myeloid Leukaemia Patients Treated With Tyrosine Kinase Inhibitors 2009-2019: A Real-World Study From the UK's Haematological Malignancy Research Network. International journal of cancer · 30 Apr 2026 PMID 42057558
By study type
Clinical trials (3)
- Mefatinib versus gefitinib as a first-line treatment for EGFR-mutated non-small cell lung cancer: a randomized, double-blind, multicenter phase III study. Signal transduction and targeted therapy · 12 Aug 2026 PMID 42586967
- Camrelizumab, Apatinib, and Radiotherapy in Locally Advanced, Unresectable Hepatocellular Carcinoma: A Phase II Study. Clinical cancer research : an official journal of the American Association for Cancer Research · 30 Jun 2026 PMID 42377073
- Cluster Randomized Controlled Trial of Intensive Systolic Blood Pressure Control in Patients With Renal Cell or Thyroid Cancer Receiving VEGFR Tyrosine Kinase Inhibitors: ECOG-ACRIN EAQ191. Hypertension (Dallas, Tex. : 1979) · 20 May 2026 PMID 42158981
Observational studies and case reports (5)
- Efficacy and safety of immune checkpoint inhibitors combined with TKIs for recurrent or metastatic cervical cancer with PIK3CA mutation. PloS one · 29 Sept 2026 PMID 42809552
- Arterial stiffness in patients with chronic myeloid leukemia receiving tyrosine kinase inhibitors: An exploratory prospective observational study. Leukemia research · 4 Aug 2026 PMID 42551129
- The Combined Therapeutic Effect of Lenvatinib and ADI-PEG 20 in Advanced Hepatocellular Carcinoma: A Case Report. In vivo (Athens, Greece) · 30 Jun 2026 PMID 42379775
- Comprehensive molecular characterization of treatment-free remission and molecular relapse in chronic myeloid leukemia patients: the EURO-SKI Biomarker Study. Leukemia · 18 Jun 2026 PMID 42315627
- Adverse Health Events in Chronic Myeloid Leukaemia Patients Treated With Tyrosine Kinase Inhibitors 2009-2019: A Real-World Study From the UK's Haematological Malignancy Research Network. International journal of cancer · 30 Apr 2026 PMID 42057558
Human data, design not indexed (4)
- Modifiable determinants of adherence to tyrosine kinase inhibitors in classical myeloproliferative neoplasms: A mixed-methods systematic review protocol. PloS one · 18 Sept 2026 PMID 42758748
- Beyond Amplification: Precision Approaches to Targeting HER2. Clinical cancer research : an official journal of the American Association for Cancer Research · 9 Jul 2026 PMID 42423636
- Improved outcomes with TKI maintenance after brexucabtagene autoleucel in Philadelphia chromosome ALL. Blood advances · 25 Jun 2026 PMID 42349018
- A tri-modal biosensor based on alkyne-functionalized gold nanoparticles and molecular beacon for detection of resistance-related point mutations in epidermal growth factor receptor-tyrosine kinase inhibitors. Molecular biology reports · 22 May 2026 PMID 42171913
Preclinical: animal, cell and lab studies (4)
- Activation of the NF-κB/ALDH1A1 signaling promotes non-mutational resistance to EGFR-TKIs in non-small cell lung cancer. Oncogene · 23 Jul 2026 PMID 42493544
- FAP-α-Responsive Size-Transformable Lipid Nanoparticles for Stromal Remodeling and Enhanced Drug Penetration in Fibrotic Hepatocellular Carcinoma. ACS applied materials & interfaces · 22 Jun 2026 PMID 42328782
- Design, synthesis and biological evaluation of selective inhibitors against the L858R/T790 M/C797S mutant EGFR kinase based on the scaffold of brigatinib. European journal of medicinal chemistry · 5 May 2026 PMID 42085935
- Altered Sphingolipid Metabolism is Associated with Osimertinib Resistance in Nonsmall-Cell Lung Cancer. Journal of proteome research · 16 Apr 2026 PMID 41988688
Written from 16 PubMed abstracts, each one listed by PMID above. Published: 2026-06-15. Last written: 2026-09-20 by GPT. Drafted by language models from published abstracts; not medical advice.