Entrectinib

Entrectinib

Systematic (IUPAC) name
N-[5-[(3,5-Difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(oxan-4-ylamino)benzamide
Legal status
Legal status	Investigational
Identifiers
PubChem	CID 25141092
Chemical data
Formula	C31H34F2N6O2
Molar 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 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.

See also

• LOXO-101, another Trk inhibitor

References

1. Entrectinib defn
2. Ignyta Receives Orphan Drug Designation From FDA For Entrectinib For The Treatment Of Molecularly Defined Subsets Of Non-Small Cell Lung Cancer
3. Ignyta's entrectinib an Orphan Drug in Europe for neuroblastoma
4. Entrectinib: Targeting NTRKs, ROS1, ALK Appears Promising. April 2016
5. Dramatic Tumor Responses With Multitargeted TKI - Entrectinib shows activity in five different cancer types. April 2016