Ensartinib

Ensartinib, sold under the brand name Ensacove, is an anti-cancer medication used for the treatment of non-small cell lung cancer.^[1] Ensartinib is an Anaplastic lymphoma kinase (ALK) inhibitor used as the salt ensartinib hydrochloride.^[1] It is taken by mouth.^[1]

Ensartinib

Clinical data
Trade names	Ensacove
Other names	X-396
AHFS/Drugs.com	Monograph
MedlinePlus	a625004
License data	US DailyMed: Ensartinib
Routes of administration	By mouth
ATC code	None
Legal status
Legal status	US: ℞-only[1]
Identifiers
CAS Number	1370651-20-9
PubChem CID	56960363
DrugBank	DB14860
ChemSpider	58828042
UNII	SMA5ZS5B22
KEGG	D11346
ChEMBL	ChEMBL4113131
ECHA InfoCard	100.306.918
Chemical and physical data
Formula	C26H27Cl2FN6O3
Molar mass	561.44 g·mol−1
3D model (JSmol)	Interactive image
SMILES C[C@@H](OC1=C(N)N=NC(=C1)C(=O)NC2=CC=C(C=C2)C(=O)N3C[C@H](C)N[C@H](C)C3)C4=C(Cl)C(F)=CC=C4Cl
InChI InChI=1S/C26H27Cl2FN6O3/c1-13-11-35(12-14(2)31-13)26(37)16-4-6-17(7-5-16)32-25(36)20-10-21(24(30)34-33-20)38-15(3)22-18(27)8-9-19(29)23(22)28/h4-10,13-15,31H,11-12H2,1-3H3,(H2,30,34)(H,32,36)/t13-,14+,15-/m1/s1 Key:GLYMPHUVMRFTFV-QLFBSQMISA-N

The most common adverse reactions include rash, musculoskeletal pain, constipation, cough, pruritis, nausea, edema, pyrexia, and fatigue.^[2]

Ensartinib was approved for medical use in the United States in December 2024.^[1][2][3][4]

Medical uses

Ensartinib is indicated for the treatment of adults with anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer who have not previously received an ALK-inhibitor.^[1][2]

History

Efficacy was evaluated in eXALT3 (NCT02767804), an open-label, randomized, active-controlled, multicenter trial in 290 participants with locally advanced or metastatic ALK-positive non-small cell lung cancer who had not previously received an ALK-targeted therapy.^[2] Participants were randomized 1:1 to receive ensartinib or crizotinib.^[2]

Society and culture

Legal status

Ensartinib was approved for medical use in the United States in December 2024.^[2][3][5]

Names

Ensartinib is the international nonproprietary name.^[6]

Ensartinib is sold under the brand name Ensacove.^[1][2][3]