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Home > A. Molecular pathology > Targeted therapy > Small molecules > entrectinib


Tuesday 24 January 2017

RXDX-101, NMS-E628 ; Rozlytrek


Definition: Entrectinib is an investigational drug with preliminary antitumor activity. It is a selective tyrosine kinase inhibitor (TKI), of the tropomyosin receptor kinases (Trk) A, B and C, C-ros oncogene 1 (ROS1 ) and anaplastic lymphoma kinase (ALK ).

In the U.S., entrectinib has orphan drug designation and rare pediatric disease designation for the treatment of neuroblastoma and orphan drug designation for treatment of TrkA-, TrkB-, TrkC-, ROS1- and ALK-positive non-small cell lung cancer (NSCLC) and metastatic colorectal cancer (mCRC). It has an EU orphan designation for neuroblastoma.

Open references

- Sensitivity to Entrectinib Associated With a Novel LMNA-NTRK1 Gene Fusion in Metastatic Colorectal Cancer. Sartore-Bianchi A, Ardini E, Bosotti R, Amatu A, Valtorta E, Somaschini A, Raddrizzani L, Palmeri L, Banfi P, Bonazzina E, Misale S, Marrapese G, Leone A, Alzani R, Luo D, Hornby Z, Lim J, Veronese S, Vanzulli A, Bardelli A, Martignoni M, Davite C, Galvani A, Isacchi A, Siena S. J Natl Cancer Inst. 2015 Nov 12;108(1). pii: djv306. doi : 10.1093/jnci/djv306 PMID: 26563355 Free

- Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors. Liu D, Offin M, Harnicar S, Li BT, Drilon A. Ther Clin Risk Manag. 2018 Jul 20;14:1247-1252. doi : 10.2147/TCRM.S147381. eCollection 2018. Review PMID: 30050303 Free