entrectinib

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Associated Genetic Biomarkers

Associated Diseases

Overview

Trade Name(s):

Rozlytrek

NCI Definition [1]:

An orally bioavailable inhibitor of the tyrosine kinases tropomyosin receptor kinases (Trk) A, B and C, C-ros oncogene 1 (ROS1) and anaplastic lymphoma kinase (ALK), with potential antineoplastic activity. Upon administration, entrectinib binds to and inhibits TrkA, TrkB, TrkC, ROS1 and ALK. Inhibition of these kinases may result in a disruption of TrkA-, TrkB-, TrkC-, ROS1-, and ALK-mediated signaling. This leads to an induction of apoptosis and an inhibition of tumor cell proliferation in tumor cells that express these kinases. TrkA, TrkB, TrkC, ROS1 and ALK are overexpressed in a variety of cancer cell types.

Biomarker-Directed Therapies

Entrectinib can be used in the treatment of malignant solid tumor and non-small cell lung carcinoma. NTRK1, NTRK1 Fusion, and NTRK2 are the most frequent biomarker inclusion criteria for use of entrectinib [2].

Malignant Solid Tumor +

Disease is predicted to be sensitive to entrectinib: -

Biomarker Criteria:

Sample must match one or more of the following:

NTRK1/2/3 Fusion

Clinical Setting(s): Metastatic (FDA)

Note: Approved for patients with solid tumors that have a neurotrophic receptor tyrosine kinase (NTRK) gene fusion without a known acquired resistance mutation, that are metastatic or unresectable, and that have progressed following treatment or have no satisfactory alternative therapy.

Biomarker Criteria: Sample must match one or more of the following: NTRK1/2/3 Fusion	Clinical Setting(s): Metastatic (FDA)
	Note: Approved for patients with solid tumors that have a neurotrophic receptor tyrosine kinase (NTRK) gene fusion without a known acquired resistance mutation, that are metastatic or unresectable, and that have progressed following treatment or have no satisfactory alternative therapy.

Disease is predicted to be resistant to entrectinib: -

Biomarker Criteria:

Sample must match all of the following:

NTRK1/2/3 Fusion

Sample must match one or more of the following:

NTRK1 G595R, NTRK3 G623E, NTRK3 G623R

Clinical Setting(s): Metastatic (FDA, MCG)

Note: Secondary mutations in the NTRK genes confer resistance to entrectinib.

Biomarker Criteria: Sample must match all of the following: Sample must match all of the following: NTRK1/2/3 Fusion Sample must match one or more of the following: NTRK1 G595R, NTRK3 G623E, NTRK3 G623R	Clinical Setting(s): Metastatic (FDA, MCG)
	Note: Secondary mutations in the NTRK genes confer resistance to entrectinib.

Non-Small Cell Lung Carcinoma +

Clinical Trials

View Clinical Trials for entrectinib

Entrectinib has been investigated in 12 clinical trials, of which 12 are open and 0 are closed. Of the trials investigating entrectinib, 1 is phase 1 (1 open), 2 are phase 1/phase 2 (2 open), 8 are phase 2 (8 open), and 1 is phase 2/phase 3 (1 open).

ROS1 Fusion, NTRK1 Fusion, and NTRK2 Fusion are the most frequent biomarker inclusion criteria for entrectinib clinical trials.

Malignant solid tumor, non-small cell lung carcinoma, and acute lymphoblastic leukemia are the most common diseases being investigated in entrectinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Entrectinib

This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating entrectinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:

rxdx-101, entrectinib, n-(5-(3,5-difluorobenzyl)-1h-indazol-3-yl)-4-(4-methylpiperazin-1yl)-2-(tetrahydro-2h-pyran-4-ylamino)benzamide, trka/b/c/ros1/alk tyrosine kinase inhibitor rxdx-101, Rozlytrek

Drug Target(s) [2]:

ALK, JAK2, NTRK1, NTRK2, NTRK3, ROS1, TNK2

NCIT ID [1]:

C114984

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.

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