Difference between revisions of "Adagrasib (Krazati)"
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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. | ||
| − | ==Diseases for which it is | + | *[https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10888 IUPHAR/BPS] |
| + | |||
| + | ==Diseases for which it is used== | ||
| + | *[[Colorectal cancer, KRAS-mutated]] | ||
*[[Non-small cell lung cancer, KRAS-mutated]] | *[[Non-small cell lung cancer, KRAS-mutated]] | ||
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
| − | *2022-12-12: Granted accelerated approval for adult patients with [[Biomarkers#KRAS|KRAS]] [[Biomarkers#G12C| | + | *2022-12-12: 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<sub>NSCLC</sub>)'' |
| + | *2024-06-21: Granted accelerated approval in combination with cetuximab for adults with KRAS G12C-mutated locally advanced or metastatic [[Colorectal cancer|colorectal cancer (CRC)]], as determined by an FDA-approved test, who have received prior treatment with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy. ''(Based on KRYSTAL-1<sub>CRC</sub>)'' | ||
| + | |||
| + | ==History of changes in EMA indication== | ||
| + | *2023-11-09: CHMP recommendation for conditional marketing authorisation - KRAZATI as monotherapy is indicated for the treatment of adult patients with advanced [[Non-small cell lung cancer|non-small cell lung cancer (NSCLC)]] with KRAS G12C mutation and disease progression after at least one prior systemic therapy. | ||
==Also known as== | ==Also known as== | ||
| − | *'''Code name:''' | + | *'''Code name:''' MRTX-849 |
*'''Brand name:''' Krazati | *'''Brand name:''' Krazati | ||
| Line 16: | Line 23: | ||
[[Category:KRAS inhibitors]] | [[Category:KRAS inhibitors]] | ||
| + | [[Category:Colorectal cancer medications]] | ||
[[Category:Non-small cell lung cancer medications]] | [[Category:Non-small cell lung cancer medications]] | ||
[[Category:FDA approved in 2022]] | [[Category:FDA approved in 2022]] | ||
Latest revision as of 13:55, 25 June 2024
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 used
History of changes in FDA indication
- 2022-12-12: 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-1NSCLC)
- 2024-06-21: Granted accelerated approval in combination with cetuximab for adults with KRAS G12C-mutated locally advanced or metastatic colorectal cancer (CRC), as determined by an FDA-approved test, who have received prior treatment with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy. (Based on KRYSTAL-1CRC)
History of changes in EMA indication
- 2023-11-09: CHMP recommendation for conditional marketing authorisation - KRAZATI as monotherapy is indicated for the treatment of adult patients with advanced non-small cell lung cancer (NSCLC) with KRAS G12C mutation and disease progression after at least one prior systemic therapy.
Also known as
- Code name: MRTX-849
- Brand name: Krazati