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ATG-017 (tizaterkib, also known as AZD0364) is an orally bioavailable, potent, and highly selective small molecule inhibitor of extracellular signal-regulated kinases 1 and 2 (ERK1/2), which are terminal kinases in the RAS-RAF-MEK-ERK signaling pathway. By inhibiting ERK1/2 activity, ATG-017 disrupts a key oncogenic driver pathway implicated in the growth and survival of various cancers. The drug is being developed primarily for the treatment of advanced solid tumors and hematological malignancies with activating alterations in the RAS-MAPK pathway. Preclinical studies have shown that ATG-017 can overcome resistance to RAF and MEK inhibitors. Clinical trials are ongoing both as monotherapy and in combination with immune checkpoint inhibitors such as nivolumab[2][3][4][5][6][8].
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