Synonyms: compound 12 [PMID: 30380863] | KZR-616 | KZR616
Compound class:
Synthetic organic
Comment: Zetomipzomib (KZR-616) is a first-in-class, selective and irreversible immunoproteasome inhibitor that results in anti-inflammatory activity in vitro and models of inflammatory conditions. It is a tripeptide epoxyketone-based molecule. At the molecular level KZR-616 inhibits the proteolytic activities of the low molecular mass polypeptide-7 (LMP7, a.k.a. proteasome subunit β8) and low molecular mass polypeptide-2 (LMP2, a.k.a. proteasome subunit β9) subunits of the 20S immunoproteasome complex [1-2]. Inhibition of a secondary immunoproteasome subunit, in this case LMP2 is required to achieve a multicytokine inhibitory effect.
![]() Ligand Activity Visualisation ChartsThese 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. ✖ |
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No information available. |
Summary of Clinical Use ![]() |
KZR-616 is being developed as a potential treatment for multiple autoimmune and inflammatory diseases. Click here to link to ClinicalTrials.gov's full list of KZR-616 studies. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT04033926 | A Phase 2 Study of KZR-616 to Evaluate Safety and Efficacy in Patients With Active Polymyositis or Dermatomyositis | Phase 2 Interventional | Kezar Life Sciences, Inc. | ||
NCT03393013 | A Study of KZR-616 in Patients With SLE With and Without Lupus Nephritis | Phase 1/Phase 2 Interventional | Kezar Life Sciences, Inc. | ||
NCT04628936 | Open-label Extension to the Phase 2 Crossover Study (PRESIDIO) Evaluating KZR-616 in Patients With PM and DM. | Phase 2 Interventional | Kezar Life Sciences, Inc. |