dirozalkib

Dirozalkib is an orally administered, next‑generation small‑molecule anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor, and likely dual ALK/ROS1 inhibitor, independently developed by Xuanzhu Biopharmaceutical (a subsidiary of Sihuan Pharmaceutical) for the treatment of ALK‑positive non‑small cell lung cancer (NSCLC).[4][7][12][13] Designed with a unique structural scaffold to enhance potency and selectivity, dirozalkib demonstrates strong inhibitory activity against ALK, including key resistance mutations such as G1202R and I1171N that limit first‑ and some second‑generation ALK TKIs, and shows activity against ROS1 in preclinical profiling.[4][9][13] In a head‑to‑head phase III trial versus crizotinib in treatment‑naive, ALK‑positive advanced NSCLC, dirozalkib significantly improved objective response rate and progression‑free survival and exhibited robust intracranial efficacy, reflecting its ability to cross the blood–brain barrier.[1][2][7][9] The drug has a generally favorable safety profile, with mostly grade 1–2 gastrointestinal adverse events such as diarrhea and vomiting, and reduced risks of pleural effusion and hepatotoxicity compared with earlier ALK inhibitors, supporting its use as a frontline targeted therapy option in ALK‑rearranged NSCLC.[1][7][9][15]

Brand names

Xuan Fei Ning

Other names

Dexitinib达希替尼