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Synonyms: Ex. 3-15 [US9174986B2] | GR389988 | GZ389988 | GZ389988A
Compound class: Synthetic organic
Comment: GR-389988 (a.k.a. GZ389988) is a neurotrophic receptor tyrosine kinase/Trk inhibitor that was developed by Genzyme. It blocks nerve growth factor (NGF)/Trk pathway activation. The chemical structure is claimed in Genzyme's patent US9174986B2 for utility in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and especially for the management of osteoarthritis and osteoarthritis pain. GR-389988 also inhibits c-FMS, the cellular receptor for colony stimulating factor-1 (CSF-1).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.
|Summary of Clinical Use
|GZ389988 has completed Phase 2 proof-of-concept evaluation in patients with knee osteoarthritis (see NCT02845271), for which results were published in 2019 . As of August 2021, there were no active studies of GZ389988 listed on ClinicalTrials.gov.
|Clinical Trial ID
|Proof-of-concept Study to Assess the Efficacy, Tolerability and Safety of a Single Intraarticular Dose of GZ389988 Versus Placebo in Patients With Painful Osteoarthritis of the Knee
|Phase 2 Interventional
|In this study a single intra-articular injection of GZ389988A reduced pain and improved function compared to placebo, in participants with painful knee osteoarthritis, with an acceptable safety profile.