MedPath

Entrectinib

Generic Name
Entrectinib
Brand Names
Rozlytrek
Drug Type
Small Molecule
Chemical Formula
C31H34F2N6O2
CAS Number
1108743-60-7
Unique Ingredient Identifier
L5ORF0AN1I

Overview

Entrectinib is a tropomyosin receptor tyrosine kinase (TRK) TRKA, TRKB, TRKC, proto-oncogene tyrosine-protein kinase ROS1, and anaplastic lymphoma kinase (ALK) inhibitor. It was approved by the FDA in August 2019 for use in the treatment of ROS1-positive metastatic non-small cell lung cancer and NTRK gene fusion positive solid tumors. Entrectinib's approved use is meant as a last line of therapy due to its accelerated approval based on early trial data. This therapy offers benefit over similar ALK inhibitors such as alectinib, ceritinib, and lorlatinib due to a wider range of targets.

Background

Entrectinib is a tropomyosin receptor tyrosine kinase (TRK) TRKA, TRKB, TRKC, proto-oncogene tyrosine-protein kinase ROS1, and anaplastic lymphoma kinase (ALK) inhibitor. It was approved by the FDA in August 2019 for use in the treatment of ROS1-positive metastatic non-small cell lung cancer and NTRK gene fusion positive solid tumors. Entrectinib's approved use is meant as a last line of therapy due to its accelerated approval based on early trial data. This therapy offers benefit over similar ALK inhibitors such as alectinib, ceritinib, and lorlatinib due to a wider range of targets.

Indication

Entrectinib is indicated for the treatment of metastatic ROS1-positive non-small cell lung cancer in adults. Entrectinib is also indicated in adults and children over 12 years old for the treatment of NTRK gene fusion-positive solid tumors which have metastasized or for which surgical resection is likely to result in severe morbidity and for which has progressed on previous therapies or for which no comparable alternative therapies are available. FoundationOne®Liquid CDx is the only FDA-approved test for the detection of ROS1 rearrangement(s) in NSCLC for selecting patients for treatment with entrectinib.

Associated Conditions

  • Metastatic Non-Small Cell Lung Cancer
  • Metastatic Solid Neoplasm
  • Solid Tumors

FDA Approved Products

Rozlytrek
Manufacturer:Genentech, Inc.
Route:ORAL
Strength:100 mg in 1 1
Approved: 2024/02/06
NDC:50242-091
Rozlytrek
Manufacturer:Genentech, Inc.
Route:ORAL
Strength:200 mg in 1 1
Approved: 2024/02/06
NDC:50242-094
Rozlytrek
Manufacturer:Genentech, Inc.
Route:ORAL
Strength:50 mg in 20 1
Approved: 2024/02/06
NDC:50242-623

Singapore Approved Products

ROZLYTREK HARD CAPSULE 200MG
Manufacturer:Mayne Pharma Inc., F. Hoffmann-La Roche Ltd (Primary and secondary packaging)
Form:CAPSULE
Strength:200.00mg
Online:Yes
Approved: 2021/01/27
Approval:SIN16087P
ROZLYTREK HARD CAPSULE 100MG
Manufacturer:Mayne Pharma Inc., F. Hoffmann-La Roche Ltd (Primary and secondary packaging)
Form:CAPSULE
Strength:100.000mg
Online:Yes
Approved: 2021/01/27
Approval:SIN16086P

Drug Development Updates

Stay informed with timely notifications on clinical trials and research advancements.

© Copyright 2025. All Rights Reserved by MedPath