Difference between revisions of "Adagrasib (Krazati)"

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m (Jwarner moved page Adagrasib (MRTX849) to Adagrasib (Krazati): FDA approval)
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From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/adagrasib NCI Drug Dictionary]: An orally available, small molecule inhibitor that targets the oncogenic KRAS substitution mutation, G12C, with potential antineoplastic activity. Upon oral administration adagrasib covalently binds to cytosine 12 within the switch II pocket of GDP-bound KRAS G12C, thereby inhibiting mutant KRAS-dependent signaling.
 
From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/adagrasib NCI Drug Dictionary]: An orally available, small molecule inhibitor that targets the oncogenic KRAS substitution mutation, G12C, with potential antineoplastic activity. Upon oral administration adagrasib covalently binds to cytosine 12 within the switch II pocket of GDP-bound KRAS G12C, thereby inhibiting mutant KRAS-dependent signaling.
  
==Preliminary data==
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==Diseases for which it is established==
 
*[[Non-small cell lung cancer, KRAS-mutated]]
 
*[[Non-small cell lung cancer, KRAS-mutated]]
#'''KRYSTAL-1:''' Jänne PA, Riely GJ, Gadgeel SM, Heist RS, Ou SI, Pacheco JM, Johnson ML, Sabari JK, Leventakos K, Yau E, Bazhenova L, Negrao MV, Pennell NA, Zhang J, Anderes K, Der-Torossian H, Kheoh T, Velastegui K, Yan X, Christensen JG, Chao RC, Spira AI. Adagrasib in Non-Small-Cell Lung Cancer Harboring a KRASG12C Mutation. N Engl J Med. 2022 Jul 14;387(2):120-131. Epub 2022 Jun 3. [https://doi.org/10.1056/nejmoa2204619 link to original article] [https://pubmed.ncbi.nlm.nih.gov/35658005/ PubMed] NCT03785249
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==History of changes in FDA indication==
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*12/12/2022: Granted accelerated approval for adult patients with [[Biomarkers#KRAS|KRAS]] [[Biomarkers#G12C|G12C­-mutated]] locally advanced or metastatic [[Non-small cell lung cancer|non-small cell lung cancer (NSCLC)]], as determined by an FDA-approved test, who have received at least one prior systemic therapy. ''(Based on KRYSTAL-1)''
  
 
==Also known as==
 
==Also known as==
 
*'''Code name:''' MRTX849
 
*'''Code name:''' MRTX849
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*'''Brand name:''' Krazati
  
 
[[Category:Drugs]]
 
[[Category:Drugs]]
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[[Category:KRAS inhibitors]]
 
[[Category:KRAS inhibitors]]
  
[[Category:Non-small cell lung cancer medications (investigational)]]
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[[Category:Non-small cell lung cancer medications]]
  
[[Category:Investigational drugs]]
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[[Category:FDA approved in 2022]]

Revision as of 21:13, 26 December 2022

Mechanism of action

From the NCI Drug Dictionary: An orally available, small molecule inhibitor that targets the oncogenic KRAS substitution mutation, G12C, with potential antineoplastic activity. Upon oral administration adagrasib covalently binds to cytosine 12 within the switch II pocket of GDP-bound KRAS G12C, thereby inhibiting mutant KRAS-dependent signaling.

Diseases for which it is established

History of changes in FDA indication

  • 12/12/2022: Granted accelerated approval for adult patients with KRAS G12C­-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC), as determined by an FDA-approved test, who have received at least one prior systemic therapy. (Based on KRYSTAL-1)

Also known as

  • Code name: MRTX849
  • Brand name: Krazati