Difference between revisions of "Capivasertib (Truqap)"

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From the [https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=688304 NCI Drug Dictionary]: A novel pyrrolopyrimidine derivative, and an orally available inhibitor of the serine/threonine protein kinase AKT (protein kinase B) with potential antineoplastic activity. AKT inhibitor AZD5363 binds to and inhibits all AKT isoforms. Inhibition of AKT prevents the phosphorylation of AKT substrates that mediate cellular processes, such as cell division, apoptosis, and glucose and fatty acid metabolism.
 
From the [https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=688304 NCI Drug Dictionary]: A novel pyrrolopyrimidine derivative, and an orally available inhibitor of the serine/threonine protein kinase AKT (protein kinase B) with potential antineoplastic activity. AKT inhibitor AZD5363 binds to and inhibits all AKT isoforms. Inhibition of AKT prevents the phosphorylation of AKT substrates that mediate cellular processes, such as cell division, apoptosis, and glucose and fatty acid metabolism.
  
==Preliminary data==
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==Diseases for which it is established==
# Hyman DM, Smyth LM, Donoghue MTA, Westin SN, Bedard PL, Dean EJ, Bando H, El-Khoueiry AB, Pérez-Fidalgo JA, Mita A, Schellens JHM, Chang MT, Reichel JB, Bouvier N, Selcuklu SD, Soumerai TE, Torrisi J, Erinjeri JP, Ambrose H, Barrett JC, Dougherty B, Foxley A, Lindemann JPO, McEwen R, Pass M, Schiavon G, Berger MF, Chandarlapaty S, Solit DB, Banerji U, Baselga J, Taylor BS. AKT inhibition in solid tumors with AKT1 mutations. J Clin Oncol. 2017 Jul 10;35(20):2251-2259. Epub 2017 May 10. [https://ascopubs.org/doi/full/10.1200/JCO.2017.73.0143 link to original article] [https://www.ncbi.nlm.nih.gov/pubmed/28489509 PubMed]
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*[[Breast cancer]]
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==History of changes in FDA indication==
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*2023-11-16: Approved with fulvestrant for adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic [[breast cancer]] with one or more PIK3CA/AKT1/PTEN-alterations, as detected by an FDA-approved test, following progression on at least one endocrine-based regimen in the metastatic setting. ''(Based on CAPItello-291)''
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*2023-11-16: Approved with fulvestrant for adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic [[breast cancer]] with one or more PIK3CA/AKT1/PTEN-alterations, as detected by an FDA-approved test, following recurrence on or within 12 months of completing adjuvant therapy. ''(Based on CAPItello-291)''
  
 
==Also known as==
 
==Also known as==
*'''Code name:''' AZD5363
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*'''Code name:''' AZD-5363
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*'''Brand name:''' Truqap
  
 
[[Category:Drugs]]
 
[[Category:Drugs]]
[[Category:Chemotherapeutic]]
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[[Category:Oral medications]]
 
[[Category:Oral medications]]
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[[Category:Mutation-specific medications]]
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[[Category:Protein expression-specific medications]]
  
[[Category:Kinase inhibitors]]
 
 
[[Category:AKT1 inhibitors]]
 
[[Category:AKT1 inhibitors]]
  
[[Category:Investigational drugs]]
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[[Category:Breast cancer medications]]
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[[Category:FDA approved in 2023]]

Latest revision as of 17:19, 26 January 2024

Mechanism of action

From the NCI Drug Dictionary: A novel pyrrolopyrimidine derivative, and an orally available inhibitor of the serine/threonine protein kinase AKT (protein kinase B) with potential antineoplastic activity. AKT inhibitor AZD5363 binds to and inhibits all AKT isoforms. Inhibition of AKT prevents the phosphorylation of AKT substrates that mediate cellular processes, such as cell division, apoptosis, and glucose and fatty acid metabolism.

Diseases for which it is established

History of changes in FDA indication

  • 2023-11-16: Approved with fulvestrant for adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer with one or more PIK3CA/AKT1/PTEN-alterations, as detected by an FDA-approved test, following progression on at least one endocrine-based regimen in the metastatic setting. (Based on CAPItello-291)
  • 2023-11-16: Approved with fulvestrant for adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer with one or more PIK3CA/AKT1/PTEN-alterations, as detected by an FDA-approved test, following recurrence on or within 12 months of completing adjuvant therapy. (Based on CAPItello-291)

Also known as

  • Code name: AZD-5363
  • Brand name: Truqap