Ensartinib (Ensacove)
General information
Class/mechanism from the NCI Drug Dictionary: An orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, ensartinib binds to and inhibits ALK kinase, ALK fusion proteins and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells.
Route: PO
Extravasation: n/a
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.
Preliminary data
ALK+ NSCLC
- X396-CLI-101: Horn L, Infante JR, Reckamp KL, Blumenshein GR, Leal TA, Waqar SN, Gitlitz BJ, Sanborn RE, Whisenant JG, Du L, Neal JW, Gockerman JP, Dukart G, Harrow K, Liang C, Gibbons JJ, Holzhausen A, Lovly CM, Wakelee HA. Ensartinib (X-396) in ALK-positive non-small cell lung cancer: results from a first-in-human phase I/II, multicenter study. Clin Cancer Res. 2018 Jun 15;24(12):2771-2779. Epub 2018 Mar 21. link to original article link to PMC article PubMed Clinical Trial Registry
- eXalt3: Horn L, Wang Z, Wu G, Poddubskaya E, Mok T, Reck M, Wakelee H, Chiappori AA, Lee DH, Breder V, Orlov S, Cicin I, Cheng Y, Liu Y, Fan Y, Whisenant JG, Zhou Y, Oertel V, Harrow K, Liang C, Mao L, Selvaggi G, Wu YL. Ensartinib vs Crizotinib for Patients With Anaplastic Lymphoma Kinase-Positive Non-Small Cell Lung Cancer: A Randomized Clinical Trial. JAMA Oncol. 2021 Nov 1;7(11):1617-1625. link to original article link to PMC article PubMed Clinical Trial Registry
History of changes in NMPA indication
- 2020-11-17: Initial approval for the second-line treatment of ALK-positive NSCLC after progression or intolerance of crizotinib. (Based on X396-CLI-101)
- 2022-03: Approved for the first-line treatment of ALK-positive non-small cell lung cancer (NSCLC). (Based on eXalt3)
Also known as
- Code name: X-396
- Brand name: Ensacove