MRTX849 was identified as a potent, selective, and covalent KRAS G12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRAS G12C, and inhibits KRAS-dependent signaling.

Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction [1] [2] .

2020年4月6日 · The discovery of the clinical development candidate MRTX849 as a potent, selective covalent inhibitor of KRAS G12C is described. This paper was published ASAP on April 6, 2020. Scheme 8 Reagents and Conditions were updated. The …

Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction.

2025年2月14日 · KRAZATI 与 西妥昔单抗 联合用于治疗经 FDA 批准的检测确定为KRAS G12C 突变的局部晚期或转移性结直肠癌（CRC）的成年患者 [见用法用量（2.1） ]，且该类患者先前接受过氟嘧啶、奥沙利铂和伊立替康为基础的化疗。 该适应症根据 ORR 和 DOR 获得加速审批 [见临床研究 (14.2) ]。 该适应症的继续审批可能取决于确认性试验中临床益处的验证和描述。 非小细胞肺癌. 根据血浆或肿瘤标本中是否存在 KRAS G12C 突变，选择使用 KRAZATI 治疗局部晚期或 …

MRTX849 is a Potent and Selective Inhibitor of KRAS G12C, KRAS-Dependent Signal Transduction and Cell Viability In Vitro. A structure-based drug design approach, including optimization for favorable drug-like properties, lead to the discovery of MRTX849 as a potent, covalent KRAS G12C inhibitor (Figure 1A and Table S1).

2022年12月13日 · 代号：MRTX849. 靶点：KRAS G12C. 美国首次获批时间：2022年12月. 中国首次获批时间：未获批. 规格：200mg*120片、200mg*180片. 获批适应症：KRAS G12C突变非小细胞肺癌. 推荐剂量：每次600mg，口服，每天两次，随餐或不随餐均可，直到疾病进展或出现不可接受的毒性反应。

2023年2月1日 · A concise, transition-metal and protection-free synthesis of adagrasib (MRTX849), a novel KRAS G12C inhibitor drug recently approved by the FDA, is reported. Introduction of two chiral building blocks to the tetrahydropyridopyrimidine core was accomplished via two sequential S N Ar reactions.

2020年7月9日 · The discovery of the clinical development candidate MRTX849 as a potent, selective covalent inhibitor of KRAS G12C is described. Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new technologies and strategies are aiding in the target's resurgence.

Krazati(adagrasib，MRTX849，阿达格拉西布) 【KRAZATI适应症和用法】 KRAZATI是 RAS GTP酶家族 的抑制剂，用于治疗经FDA批准的检测确定的患有KRAS G12C突变，且既往至少接受过一次全身性治疗的局部晚期或转移性非小细胞肺癌(NSCLC)的成年患者。