Your browser does not fully support modern features. Please upgrade for a smoother experience.
Submitted Successfully!
Thank you for your contribution! You can also upload a video entry or images related to this topic. For video creation, please contact our Academic Video Service.
Version Summary Created by Modification Content Size Created at Operation
1 handwiki Dean Liu -- 1129 2022-10-27 01:33:51

Video Upload Options

We provide professional Academic Video Service to translate complex research into visually appealing presentations. Would you like to try it?
No, upload directly Yes
Cite
If you have any further questions, please contact Encyclopedia Editorial Office.
HandWiki. ALK Inhibitor. Encyclopedia. Available online: https://encyclopedia.pub/entry/32096 (accessed on 15 October 2026).
HandWiki. ALK Inhibitor. Encyclopedia. Available at: https://encyclopedia.pub/entry/32096. Accessed October 15, 2026.
HandWiki. "ALK Inhibitor" Encyclopedia, https://encyclopedia.pub/entry/32096 (accessed October 15, 2026).
HandWiki. (2022, October 31). ALK Inhibitor. In Encyclopedia. https://encyclopedia.pub/entry/32096
HandWiki. "ALK Inhibitor." Encyclopedia. Web. 31 October, 2022.
ALK Inhibitor
Edit
The content is sourced from: https://handwiki.org/wiki/Chemistry:ALK_inhibitor

ALK inhibitors are anti-cancer drugs that act on tumours with variations of anaplastic lymphoma kinase (ALK) such as an EML4-ALK translocation. They fall under the category of tyrosine kinase inhibitors, which work by inhibiting proteins involved in the abnormal growth of tumour cells. All the current approved ALK inhibitors function by binding to the ATP pocket of the abnormal ALK protein, blocking its access to energy and deactivating it. A majority of ALK-rearranged NSCLC harbour the EML4-ALK fusion, although as of 2020, over 92 fusion partners have been discovered in ALK+ NSCLC. For each fusion partner, there can be several fusion variants depending on the position the two genes were fused at, and this may have implications on the response of the tumour and prognosis of the patient.

alk eml4-alk anti-cancer drugs

References

  1. Chustecka (2010). "Crizotinib in ALK-NSCLC; Response Rate "Unprecedented"". http://www.medscape.com/viewarticle/723075. 
  2. "Crizotinib Clinical Trials – Currently Ongoing and/or Enrolling". Fact Sheet. Pfizer. http://www.pfizer.com/files/news/asco/crizotinib_fact_sheet.pdf. 
  3. Clinical trial number NCT00932451 for "An Investigational Drug, PF-02341066, Is Being Studied In Patients With Advanced Non-Small Cell Lung Cancer With A Specific Gene Profile Involving The Anaplastic Lymphoma Kinase (ALK) Gene" at ClinicalTrials.gov https://www.clinicaltrials.gov/show/NCT00932451
  4. "Pfizer Oncology To Present New Clinical Data From Ten Molecules Across Multiple Tumor Types" (PDF) (Press release). Pfizer Oncology. 2010-05-20. Archived from the original (PDF) on 2010-06-12. Retrieved 2010-06-07. https://web.archive.org/web/20100612203421/http://media.pfizer.com/files/news/press_releases/2010/asco_curtain_raiser_052010.pdf
  5. Clinical trial number NCT00932893 for "An Investigational Drug, PF-02341066 Is Being Studied Versus Standard Of Care In Patients With Advanced Non-Small Cell Lung Cancer With A Specific Gene Profile Involving The Anaplastic Lymphoma Kinase (ALK) Gene" at ClinicalTrials.gov https://www.clinicaltrials.gov/show/NCT00932893
  6. Farmer (2010). "Non-Small-Cell Lung Cancer Standards of Care Challenged by a Cornucopia of New Drugs". http://www.genengnews.com/gen-articles/treatment-paradigm-shifting-for-nsclc/3423?page=1. 
  7. "FDA Approves Ceritinib for ALK-Positive Lung Cancer". Medscape. April 29, 2014. http://www.medscape.com/viewarticle/824305. 
  8. Soria, Jean-Charles (March 4, 2017). "First-line ceritinib versus platinum-based chemotherapy in advanced ALK-rearranged non-small-cell lung cancer (ASCEND-4): a randomised, open-label, phase 3 study.". The Lancet 389 (10072): 917–929. doi:10.1016/s0140-6736(17)30123-x. PMID 28126333.  https://dx.doi.org/10.1016%2Fs0140-6736%2817%2930123-x
  9. FDA approves Alecensa for ALK-positive metastatic non-small cell lung cancer Nov 2017 https://www.healio.com/hematology-oncology/lung-cancer/news/online/%7Ba97a3d66-e12d-42a5-9b72-4d330b151aaf%7D/fda-approves-alecensa-for-alk--positive-metastatic-non-small-cell-lung-cancer
  10. "Novel Drug Approvals for 2017". FDA. 25 January 2021. https://www.fda.gov/Drugs/DevelopmentApprovalProcess/DrugInnovation/ucm537040.htm. 
  11. Hrustanovic, G; Bivona, TG (2015). "RAS-MAPK in ALK Targeted Therapy Resistance". Cell Cycle 14 (23): 3661–3662. doi:10.1080/15384101.2015.1096103. PMID 26654768.  http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=4825705
  12. Clinical trial number NCT04005144 for "Brigatinib and Binimetinib in Treating Patients With Stage IIIB-IV ALK or ROS1-Rearranged Non-small Cell Lung Cancer" at ClinicalTrials.gov https://www.clinicaltrials.gov/show/NCT04005144
  13. Clinical trial number NCT03087448 for "Ceritinib + Trametinib in Patients With Advanced ALK-Positive Non-Small Cell Lung Cancer (NSCLC)" at ClinicalTrials.gov https://www.clinicaltrials.gov/show/NCT03087448
  14. Clinical trial number NCT03202940 for "A Phase IB/II Study of Alectinib Combined With Cobimetinib in Advanced ALK-Rearranged (ALK+) NSCLC" at ClinicalTrials.gov https://www.clinicaltrials.gov/show/NCT03202940
  15. Velde, RV; Yoon, N (2020). "Resistance to targeted therapies as a multifactorial, gradual adaptation to inhibitor specific selective pressures". Nature Communications 11 (1): 2393. doi:10.1038/s41467-020-16212-w. PMID 32409712. Bibcode: 2020NatCo..11.2393V.  http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=7224215
  16. Xuyuan, D; Fernandez-Salas, E (2015). "Elucidation of Resistance Mechanisms to Second-Generation ALK Inhibitors Alectinib and Ceritinib in Non–Small Cell Lung Cancer Cells". Neoplasia 18 (3): 162–171. doi:10.1016/j.neo.2016.02.001. PMID 26992917.  http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=4796802
  17. Clinical trial number NCT02521051 for "Phase I/II Trial of Alectinib and Bevacizumab in Patients With Advanced, Anaplastic Lymphoma Kinase (ALK)-Positive, Non-Small Cell Lung Cancer" at ClinicalTrials.gov https://www.clinicaltrials.gov/show/NCT02521051
  18. Clinical trial number NCT03779191 for "Alectinib in Combination With Bevacizumab in ALK Positive NSCLC" at ClinicalTrials.gov https://www.clinicaltrials.gov/show/NCT03779191
  19. Clinical trial number NCT04227028 for "Brigatinib and Bevacizumab for the Treatment of ALK-Rearranged Locally Advanced, Metastatic, or Recurrent Non-small Cell Lung Cancer" at ClinicalTrials.gov https://www.clinicaltrials.gov/show/NCT04227028
  20. Clinical trial number NCT03707938 for "Local Consolidative Therapy and Brigatinib in Treating Patients With Stage IV or Recurrent Non-small Cell Lung Cancer" at ClinicalTrials.gov https://www.clinicaltrials.gov/show/NCT03707938
  21. Galkin (2007). "Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK". Proceedings of the National Academy of Sciences of the United States of America 104 (1): 270–5. doi:10.1073/pnas.0609412103. PMID 17185414. Bibcode: 2007PNAS..104..270G.  http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1765448
  22. "Archived copy". http://www.axonmedchem.com/product/1416tae684.html. 
More
©Text is available under the terms and conditions of the Creative Commons-Attribution ShareAlike (CC BY-SA) license; additional terms may apply. By using this site, you agree to the Terms and Conditions and Privacy Policy.
Upload a video for this entry
Information
Subjects: Others
Contributor MDPI registered users' name will be linked to their SciProfiles pages. To register with us, please refer to https://encyclopedia.pub/register :
HandWiki
View Times: 1.6K
Entry Collection: HandWiki
Revision: 1 time (View History)
Update Date: 31 Oct 2022
Table of Contents
    Notice
    You are not a member of the advisory board for this topic. If you want to update advisory board member profile, please contact office@encyclopedia.pub.
    OK
    Confirm
    Only members of the Encyclopedia advisory board for this topic are allowed to note entries. Would you like to become an advisory board member of the Encyclopedia?
    Yes
    No
    ${ textCharacter }/${ maxCharacter }
    Submit
    Cancel
    There is no comment~
    ${ textCharacter }/${ maxCharacter }
    Submit
    Cancel
    ${ selectedItem.replyTextCharacter }/${ selectedItem.replyMaxCharacter }
    Submit
    Cancel
    Confirm
    Are you sure to Delete?
    Yes No
    Academic Video Service
    Feedback