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tropomyosin receptor kinase (trk) proto-oncogene protein (NTRK)
Pharmacology:
- larotrectinib is a trk inhibitor with activity in trk fusion-positive cancers [1]
- repotrectinib (Augtyro) is FDA-aproved for all locally advanced, unresectable, or metastatic solid tumors with an NTRK gene fusion* that have progressed after initial treatment or have no alternative treatment
* NTRK gene-fusions are rare, but found in many tumor types [2]
Specific
BDNF/NT-3 growth factors receptor; EC=2.7.10.1; neurotrophic tyrosine kinase receptor type 2; TrkB tyrosine kinase; GP145-TrkB; Trk-B (NTRK2 TRKB)
trk A protein; high affinity nerve growth factor receptor; neurotrophic tyrosine kinase receptor type 1; TRK1-transforming tyrosine kinase protein; p140-TrkA; Trk-A (NTRK1, TRK)
trk C protein; NT-3 growth factor receptor; neurotrophic tyrosine kinase receptor type 3; TrkC tyrosine kinase; GP145-TrkC; Trk-C (NTRK3, TRKC)
trk E proto-oncogene protein or neurotrophic tyrosine kinase, receptor-4
General
glycoprotein
proto oncogene protein
tyrosine kinase receptor (RTK)
Properties
COMPARTMENT: plasma membrane
STATE: active state
MOTIF: ligand-binding site
glycosylation site
transmembrane domain
Tyr phosphorylation site
kinase domain
MOTIF: ATP-binding site
NAME: ATP-binding site
References
- Drilon A, Laetsch TW, Kummar S et al
Efficacy of Larotrectinib in TRK Fusion-Positive Cancers in
Adults and Children.
N Engl J Med 2018; 378:731-739. February 22, 2018
PMID: 29466156
http://www.nejm.org/doi/full/10.1056/NEJMoa1714448
- Alexander Otto M
FDA Expands Repotrectinib Label to All NTRK Gene Fusion+ Solid Tumors.
Medscape. June 13, 2024
https://www.medscape.com/viewarticle/fda-expands-repotrectinib-label-all-ntrk-gene-fusion-solid-2024a1000b3q