Difference between revisions of "Tucatinib (Tukysa)"

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(Created page with "==Mechanism of action== From the [https://www.annalsofoncology.org/article/S0923-7534(19)32228-8/fulltext NCI Drug Dictionary]: An orally bioavailable inhibitor of the human e...")
 
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From the [https://www.annalsofoncology.org/article/S0923-7534(19)32228-8/fulltext NCI Drug Dictionary]: An orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. Tucatinib selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells.  
 
From the [https://www.annalsofoncology.org/article/S0923-7534(19)32228-8/fulltext NCI Drug Dictionary]: An orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. Tucatinib selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells.  
  
==Preliminary data==
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==Diseases for which it is used==
 
===[[Breast cancer, HER2-positive|HER2+ breast cancer]]===
 
===[[Breast cancer, HER2-positive|HER2+ breast cancer]]===
 
# '''HER2CLIMB:''' Murthy RK, Loi S, Okines A, Paplomata E, Hamilton E, Hurvitz SA, Lin NU, Borges V, Abramson V, Anders C, Bedard PL, Oliveira M, Jakobsen E, Bachelot T, Shachar SS, Müller V, Braga S, Duhoux FP, Greil R, Cameron D, Carey LA, Curigliano G, Gelmon K, Hortobagyi G, Krop I, Loibl S, Pegram M, Slamon D, Palanca-Wessels MC, Walker L, Feng W, Winer EP. Tucatinib, Trastuzumab, and Capecitabine for HER2-Positive Metastatic Breast Cancer. N Engl J Med. 2020 Feb 13;382(7):597-609. Epub 2019 Dec 11. Erratum in: N Engl J Med. 2020 Feb 6;382(6):586. [https://doi.org/10.1056/nejmoa1914609 link to original article] '''contains verified protocol''' [https://pubmed.ncbi.nlm.nih.gov/31825569 PubMed] NCT02614794
 
# '''HER2CLIMB:''' Murthy RK, Loi S, Okines A, Paplomata E, Hamilton E, Hurvitz SA, Lin NU, Borges V, Abramson V, Anders C, Bedard PL, Oliveira M, Jakobsen E, Bachelot T, Shachar SS, Müller V, Braga S, Duhoux FP, Greil R, Cameron D, Carey LA, Curigliano G, Gelmon K, Hortobagyi G, Krop I, Loibl S, Pegram M, Slamon D, Palanca-Wessels MC, Walker L, Feng W, Winer EP. Tucatinib, Trastuzumab, and Capecitabine for HER2-Positive Metastatic Breast Cancer. N Engl J Med. 2020 Feb 13;382(7):597-609. Epub 2019 Dec 11. Erratum in: N Engl J Med. 2020 Feb 6;382(6):586. [https://doi.org/10.1056/nejmoa1914609 link to original article] '''contains verified protocol''' [https://pubmed.ncbi.nlm.nih.gov/31825569 PubMed] NCT02614794
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==History of changes in FDA indication==
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*4/17/2020: Initial approval in combination with trastuzumab and capecitabine, for adult patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic setting.
  
 
==Also known as==
 
==Also known as==
 
*'''Code name:''' ARRY-380, ONT-380
 
*'''Code name:''' ARRY-380, ONT-380
 
*'''Generic name:''' irbinitinib
 
*'''Generic name:''' irbinitinib
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*'''Brand name:''' Tukysa
  
 
[[Category:Drugs]]
 
[[Category:Drugs]]
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[[Category:ERBB2 inhibitors]]
 
[[Category:ERBB2 inhibitors]]
  
[[Category:Investigational drugs]]
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[[Category:Breast cancer medications]]
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[[Category:FDA approved in 2020]]

Revision as of 14:46, 18 April 2020

Mechanism of action

From the NCI Drug Dictionary: An orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. Tucatinib selectively binds to and inhibits the phosphorylation of ErbB-2, which may prevent the activation of ErbB-2 signal transduction pathways, resulting in growth inhibition and death of ErbB-2-expressing tumor cells.

Diseases for which it is used

HER2+ breast cancer

  1. HER2CLIMB: Murthy RK, Loi S, Okines A, Paplomata E, Hamilton E, Hurvitz SA, Lin NU, Borges V, Abramson V, Anders C, Bedard PL, Oliveira M, Jakobsen E, Bachelot T, Shachar SS, Müller V, Braga S, Duhoux FP, Greil R, Cameron D, Carey LA, Curigliano G, Gelmon K, Hortobagyi G, Krop I, Loibl S, Pegram M, Slamon D, Palanca-Wessels MC, Walker L, Feng W, Winer EP. Tucatinib, Trastuzumab, and Capecitabine for HER2-Positive Metastatic Breast Cancer. N Engl J Med. 2020 Feb 13;382(7):597-609. Epub 2019 Dec 11. Erratum in: N Engl J Med. 2020 Feb 6;382(6):586. link to original article contains verified protocol PubMed NCT02614794

History of changes in FDA indication

  • 4/17/2020: Initial approval in combination with trastuzumab and capecitabine, for adult patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic setting.

Also known as

  • Code name: ARRY-380, ONT-380
  • Generic name: irbinitinib
  • Brand name: Tukysa