Adagrasib
- MRTX849
- Adagrasib
- 2326521-71-3
- MRTX-849
- KRAZATI
- Create:2019-07-20
- Modify:2025-01-04
- 2-((S)-4-(7-(8-chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile
- 2-Piperazineacetonitrile, 4-(7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-(((2S)-1-methyl-2-pyrrolidinyl)methoxy)pyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-
- adagrasib
- MRTX-849
- MRTX849
- MRTX849
- Adagrasib
- 2326521-71-3
- MRTX-849
- KRAZATI
- Kras G12C inhibitor MRTX849
- 8EOO6HQF8Y
- Adagrasib [USAN]
- UNII-8EOO6HQF8Y
- 2-((S)-4-(7-(8-Chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile
- 2-[(2S)-4-[7-(8-chloronaphthalen-1-yl)-2-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoroprop-2-enoyl)piperazin-2-yl]acetonitrile
- 2-Piperazineacetonitrile, 4-[7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-
- 2-Piperazineacetonitrile, 4-(7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-(((2S)-1-methyl-2-pyrrolidinyl)methoxy)pyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-
- MFCD32263433
- compound 20 (PMID: 32250617)
- compound 20 [PMID: 32250617]
- 2-[(2S)-4-[7-(8-chloronaphthalen-1-yl)-2-{[(2S)-1-methylpyrrolidin-2-yl]methoxy}-5H,6H,7H,8H-pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoroprop-2-enoyl)piperazin-2-yl]acetonitrile
- 2-((S)-4-(7-(8-chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile
- 2-[(2S)-4-[7-(8-chloronaphthalen-1-yl)-2-{[(2S)-1-methylpyrrolidin-2-yl]methoxy}-5H,6H,8H-pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoroprop-2-enoyl)piperazin-2-yl]acetonitrile
- Krazati (TN)
- ADAGRASIB [INN]
- Adagrasib (USAN/INN)
- Adagrasib (MRTX849)
- MRTX849(Adagrasib)?
- ADAGRASIB [WHO-DD]
- MRTX 849
- CHEMBL4594350
- SCHEMBL20974691
- GTPL10888
- DTXSID801336759
- BCP31538
- EX-A3258
- MRTX-849; MRTX 849
- BDBM50539763
- NSC831453
- WHO 11519
- AKOS037648997
- AT23561
- NSC-831453
- AC-35659
- BM177692
- BS-16211
- HY-130149
- CS-0105265
- D12301
- EN300-26953032
- Z4145344023
- ((2S)-4-(7-(8-CHLORONAPHTHALEN-1-YL)-2-(((2S)-1- METHYLPYRROLIDIN-2-YL)METHOXY)-5,6,7,8- TETRAHYDROPYRIDO(3,4-D)PYRIMIDIN-4-YL)-1-(2-FLUOROPROP2-ENOYL)PIPERAZIN-2-YL)ACETONITRILE
- ((2S)-4-(7-(8-CHLORONAPHTHALEN-1-YL)-2-(((2S)-1-METHYLPYRROLIDIN-2-YL)METHOXY)-5,6,7,8-TETRAHYDROPYRIDO(3,4-D)PYRIMIDIN-4-YL)-1-(2-FLUOROPROP2-ENOYL)PIPERAZIN-2-YL)ACETONITRILE
Adagrasib is approved to treat adults with cancer that has spread and has an abnormal KRAS gene, including:
• non-small cell lung cancer (NSCLC). It is used in patients who have received at least one other systemic therapy
• colorectal cancer. It is used with cetuximab in patients who have received chemotherapy that included a fluoropyrimidine, oxaliplatin, and irinotecan hydrochloride
These uses are approved under FDA’s Accelerated Approval Program. As a condition of approval, a confirmatory trial(s) must show that adagrasib provides a clinical benefit in these patients.Adagrasib is also being studied in the treatment of other types of cancer.
H302 (66.7%): Harmful if swallowed [Warning Acute toxicity, oral]
H315 (66.7%): Causes skin irritation [Warning Skin corrosion/irritation]
H319 (66.7%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]
H335 (66.7%): May cause respiratory irritation [Warning Specific target organ toxicity, single exposure; Respiratory tract irritation]
P261, P264, P264+P265, P270, P271, P280, P301+P317, P302+P352, P304+P340, P305+P351+P338, P319, P321, P330, P332+P317, P337+P317, P362+P364, P403+P233, P405, and P501
(The corresponding statement to each P-code can be found at the GHS Classification page.)
Aggregated GHS information provided per 3 reports by companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
Reported as not meeting GHS hazard criteria per 1 of 3 reports by companies. For more detailed information, please visit ECHA C&L website.
There is 1 notification provided by 2 of 3 reports by companies with hazard statement code(s).
Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.
Acute Tox. 4 (66.7%)
Skin Irrit. 2 (66.7%)
Eye Irrit. 2A (66.7%)
STOT SE 3 (66.7%)
In the prelicensure clinical trials of adagrasib in patients with solid tumors harboring KRAS G12C mutations, liver test abnormalities were frequent although usually self-limited and mild. Some degree of ALT elevations arose in 28% to 46% of adagrasib treated patients and elevations above 5 times the upper limit of normal (ULN) were seen in 5% to 7%. In these trials that enrolled approximately 366 patients, adagrasib was discontinued early due to increased AST or ALT in 8% of patients. In addition, a small proportion of patients developed clinically apparent hepatotoxicity requiring adagrasib discontinuation. The liver test abnormalities had a median onset of 3 weeks after initiation of therapy. While serum aminotransferase elevations were occasionally quite high (5 to 20 times ULN), there were no accompanying elevations in serum bilirubin and no patient developed clinically apparent liver injury with jaundice. The product label for adagrasib recommends monitoring for routine liver tests before, at 3 week intervals during the first 3 months of therapy, and thereafter as clinically indicated.
Likelihood score: D (possible but infrequent cause of clinically apparent liver injury).
Patents are available for this chemical structure:
https://patentscope.wipo.int/search/en/result.jsf?inchikey=PEMUGDMSUDYLHU-ZEQRLZLVSA-N
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