Difference between revisions of "Asciminib (Scemblix)"

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From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/allosteric-bcr-abl-tyrosine-kinase-inhibitor-abl001 NCI Drug Dictionary]: An orally bioavailable, allosteric Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity. Designed to overcome resistance, asciminib binds to the Abl portion of the Bcr-Abl fusion protein at a location that is distinct from the ATP-binding domain. This binding results in the inhibition of Bcr-Abl-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies.
 
From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/allosteric-bcr-abl-tyrosine-kinase-inhibitor-abl001 NCI Drug Dictionary]: An orally bioavailable, allosteric Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity. Designed to overcome resistance, asciminib binds to the Abl portion of the Bcr-Abl fusion protein at a location that is distinct from the ATP-binding domain. This binding results in the inhibition of Bcr-Abl-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies.
  
==Preliminary data==
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==Diseases for which it is used==
===[[Chronic myelogenous leukemia]]===
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*[[Chronic myelogenous leukemia]]
# '''CABL001X2101:''' Hughes TP, Mauro MJ, Cortes JE, Minami H, Rea D, DeAngelo DJ, Breccia M, Goh YT, Talpaz M, Hochhaus A, le Coutre P, Ottmann O, Heinrich MC, Steegmann JL, Deininger MWN, Janssen JJWM, Mahon FX, Minami Y, Yeung D, Ross DM, Tallman MS, Park JH, Druker BJ, Hynds D, Duan Y, Meille C, Hourcade-Potelleret F, Vanasse KG, Lang F, Kim DW. Asciminib in Chronic Myeloid Leukemia after ABL Kinase Inhibitor Failure. N Engl J Med. 2019 Dec 12;381(24):2315-2326. [https://www.nejm.org/doi/full/10.1056/NEJMoa1902328 link to original article] [https://pubmed.ncbi.nlm.nih.gov/31826340 PubMed]
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==History of changes in FDA indication==
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*10/29/2021: Granted accelerated approval for patients with [[Biomarkers#BCR-ABL1|Philadelphia chromosome-positive]] [[Chronic myelogenous leukemia|chronic myeloid leukemia]] (Ph+ CML) in chronic phase (CP), previously treated with two or more tyrosine kinase inhibitors (TKIs). ''(Based on ASCEMBL)''
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*10/29/2021: Approved for adult patients with [[Biomarkers#BCR-ABL1|Ph+]] [[Chronic myelogenous leukemia|CML]] in CP with the [[Biomarkers#T315I|T315I]] mutation. ''(Based on CABL001X2101)''
  
 
==Also known as==
 
==Also known as==
 
*'''Code name:''' ABL001
 
*'''Code name:''' ABL001
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*'''Brand name:''' Scemblix
  
 
[[Category:Drugs]]
 
[[Category:Drugs]]
 
[[Category:Oral medications]]
 
[[Category:Oral medications]]
 
  
 
[[Category:Bcr-Abl inhibitors]]
 
[[Category:Bcr-Abl inhibitors]]
 
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[[Category:Chronic myelogenous leukemia medications]]
[[Category:Investigational drugs]]
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[[Category:FDA approved in 2021]]

Revision as of 21:42, 29 October 2021

Mechanism of action

From the NCI Drug Dictionary: An orally bioavailable, allosteric Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity. Designed to overcome resistance, asciminib binds to the Abl portion of the Bcr-Abl fusion protein at a location that is distinct from the ATP-binding domain. This binding results in the inhibition of Bcr-Abl-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies.

Diseases for which it is used

History of changes in FDA indication

  • 10/29/2021: Granted accelerated approval for patients with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP), previously treated with two or more tyrosine kinase inhibitors (TKIs). (Based on ASCEMBL)
  • 10/29/2021: Approved for adult patients with Ph+ CML in CP with the T315I mutation. (Based on CABL001X2101)

Also known as

  • Code name: ABL001
  • Brand name: Scemblix