ulocuplumab   Click here for help

GtoPdb Ligand ID: 9161

Synonyms: BMS-936564 | MDX-1338
Immunopharmacology Ligand
Compound class: Antibody
Comment: Ulocuplumab is an IgG4 kappa anti-CXCR4 monoclonal, being developed by Bristol-Myers Squibb as a potential oncolgy therapeutic.
Peptide sequences and structural details for this antibody are available from its IMGT/mAb-DB record.
BLAST sequence analysis of the heavy and light chain peptide sequences of ulocuplumab, reveal identical matches with sequences claimed in patent US8450464 [5]. This identifies clone F7GL as the likely candidate for ulocuplumab.
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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.

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View interactive charts of activity data across species
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Summary of Clinical Use Click here for help
First in human study NCT01120457, evaluating ulocuplumab (BMS-936564) in patients with acute myelogenous leukemia (AML) and selected B-cell cancers has been completed. A Phase 1/2 study (NCT02472977) in combination with nivolumab in patients with advanced/metastatic solid tumours is underway. Trial NCT02666209 is allowing extended access to ulocuplumab therapy for patients with relapsed/ refractory multiple myeloma who had taken part in completed trial NCT01359657.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
CXCR4 is the cytokine receptor for CXCL12 (stromal cell-derived factor-1 (SDF-1)). CXCR4 has been shown to be expressed by a variety of cancer types (amongst others, breast, ovarian, prostate, pancreatic, and non-small cell lung cancers, neuroblastoma and glioblastoma as well as lymphoma, AML and acute lymphoblastic leukemia (ALL), is known to be involved in tumour metastasis, and can be a negative indicator of survival. Anti-CXCR4 antibodies are expected to dampen aberrant CXCR4-SDF-1 signalling in cancer cells. The CXCR4-SDF-1 pathway has also been shown to play a role in a variety of inflammatory conditions (e.g. inflammatory liver disease [7], autoimmune joint inflammation [6], allergic airway disease [1] and periodontal disease [3]), so anti-CXCR4 biologics such as ulocuplumab may also have potential anti-inflammatory actions of use in the clinical setting, and may have useful anti-angiogenic action [2,4].
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT01120457 First in Human Study to Determine the Safety, Tolerability and Preliminary Efficacy of an Anti-CXCR4 Antibody in Subjects With Acute Myelogenous Leukemia and Selected B-cell Cancers Phase 1 Interventional Bristol-Myers Squibb
NCT01359657 Anti-CXCR4 (BMS-936564) Alone and in Combination With Lenalidomide/Dexamethasone or Bortezomib/Dexamethasone in Relapsed/Refractory Multiple Myeloma Phase 1 Interventional Bristol-Myers Squibb
NCT02472977 Safety and Efficacy Study of Ulocuplumab and Nivolumab in Subjects With Solid Tumors Phase 1/Phase 2 Interventional Bristol-Myers Squibb
NCT02666209 Early Patient Access Single Named Patient Program for the Use of Ulocuplumab for the Treatment of Multiple Myeloma Expanded Access Dana-Farber Cancer Institute