Preferred Label : pan-TRK/ROS1 Dual Inhibitor XZP-5955;
NCIt synonyms : pan-TRK/ROS1 Inhibitor XZP-5955;
NCIt definition : An orally available dual inhibitor of the receptor tyrosine kinase c-ros oncogene
1 (ROS1) and the tropomyosin-related-kinase (tyrosine receptor kinase; TRK), with
potential antineoplastic activity. Upon oral administration, pan-TRK/ROS1 dual inhibitor
XZP-5955 targets, binds to and inhibits wild-type, point mutants and fusion proteins
of ROS1 and TRK, including fusion proteins containing sequences from neurotrophic
tyrosine receptor kinase (NTRK) types 1 (NTRK1; TrkA), 2 (NTRK2; TrkB), and 3 (NTRK3;
TrkC). It specifically inhibits proliferation of tumor cells harboring certain TRK
and ROS1 resistance mutations, such as TRKA G595R, TRKC G623R, TRKA G667C and ROS1
G2032R. Inhibition of these kinases leads to the disruption of downstream signaling
pathways and the inhibition of cell growth of tumors in which these kinases are overexpressed,
rearranged or mutated. TRK, a family of receptor tyrosine kinases (RTKs) activated
by neurotrophins, is encoded by NTRK family genes. The expression of either mutated
forms of, or fusion proteins involving, NTRK family members results in uncontrolled
TRK signaling, which plays an important role in tumor cell growth, survival, invasion
and treatment resistance. ROS1, overexpressed in certain cancer cells, plays a key
role in cell growth and survival of cancer cells. XZP-5955 is able to penetrate the
blood-brain barrier (BBB).;
Molecule name : XZP-5955; XZP 5955;
NCI Metathesaurus CUI : CL1770681;
Origin ID : C182074;
UMLS CUI : C5666879;
Semantic type(s)
- concept_is_in_subset
- has_target
