Entrectinib

Systematic (IUPAC) name
	N-[5-[(3,5-Difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(oxan-4-ylamino)benzamide
Clinical data
Legal status	Investigational;
Identifiers
PubChem	CID: 25141092
Chemical data
Formula	C31H34F2N6O2
Molecular mass	560.64 g/mol
	InChI InChI=1S/C31H34F2N6O2/c1-38-8-10-39(11-9-38)25-3-4-26(29(19-25)34-24-6-12-41-13-7-24)31(40)35-30-27-17-20(2-5-28(27)36-37-30)14-21-15-22(32)18-23(33)16-21/h2-5,15-19,24,34H,6-14H2,1H3,(H2,35,36,37,40) ; Key:HAYYBYPASCDWEQ-UHFFFAOYSA-N ;

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

Originally it was designated by Nerviano Medical Sciences as NMS-E628, then licensed by Ignyta and renamed RXDX-101.

In the U.S., it 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).^[2] It has an EU orphan designation for neuroblastoma.^[3]

It has had two phase I clinical studies : STARTRK-1 and ALKA-372-001,^[4] (with encouraging results^[5]) which are progressing to phase II.

References

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