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Drugs Fut 2022, 47(4): 247
ISSN 0377-8282
e-ISSN 2013-0368
Copyright 2022 Clarivate
CCC: 0377-8282
DOI: 10.1358/dof.2022.47.4.3381587
 
 
Navtemadlin. MDM2-p53 interaction inhibitor, Treatment of cancer
Price, S., Al-Bahou, A.
 
 
The p53 tumor suppressor pathway has been an area of interest in drug development, since upon activation, it can eradicate tumors. Murine double minute 2 (MDM2) inhibits p53 activity and results in the downregulation of p53; inhibition of MDM2 results in the reactivation of the p53 function. Navtemadlin or KRT-232, previously known as AMG-232, is an oral potent, selective inhibitor of MDM2 in patients with wild-type p53. KRT-232 has shown activity in brain neoplasms, sarcomas, leukemia, multiple myeloma and myelofibrosis. Studies to date have shown promising data with an acceptable toxicity profile including mild to moderate nausea, vomiting, diarrhea, fatigue, decreased appetite and anemia as the most common adverse events. KRT- 232 is being evaluated as monotherapy and in combination with other anticancer agents in phase Ib/II and phase II studies.


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