Overview

Generic Name(s):
gilteritinib
Trade Name(s):
Xospata
NCI Definition [1]:
An orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) FMS-related tyrosine kinase 3 (FLT3, STK1, or FLK2), AXL (UFO or JTK11) and anaplastic lymphoma kinase (ALK or CD246), with potential antineoplastic activity. Gilteritinib binds to and inhibits both the wild-type and mutated forms of FLT3, AXL and ALK. This may result in an inhibition of FLT3, AXL, and ALK-mediated signal transduction pathways and reduces tumor cell proliferation in cancer cell types that overexpress these RTKs. FLT3, AXL and ALK, overexpressed or mutated in a variety of cancer cell types, play a key role in tumor cell growth and survival.

Biomarker-Directed Therapies

Gilteritinib has been investigated in 19 clinical trials, of which 17 are open and 2 are closed. Of the trials investigating gilteritinib, 4 are phase 1 (3 open), 7 are phase 1/phase 2 (6 open), 2 are phase 2 (2 open), 5 are phase 3 (5 open), and 1 is no phase specified (1 open).

FLT3 ITD, FLT3 Codon 835 Missense, and FLT3 Codon 836 Missense are the most frequent biomarker inclusion criteria for gilteritinib clinical trials.

Acute myeloid leukemia, myelodysplastic syndromes, and acute promyelocytic leukemia are the most common diseases being investigated in gilteritinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Gilteritinib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Gilteritinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating gilteritinib 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]:
asp2215, 6-ethyl-3-((3-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-5-((tetrahydro-2h-pyran-4-yl)amino)pyrazine-2-carboxamide, flt3/axl/alk kinase inhibitor asp2215, gilteritinib, asp-2215, Xospata
Drug Categories [2]:
ALK inhibitors, Tyrosine kinase inhibitors
Drug Target(s) [2]:
ALK, AXL, FLT3
NCIT ID [1]:
C116722

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.