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Synonyms: IMC-3G3 | Lartruvo® | LY3012207
olaratumab is an approved drug (EMA & FDA (2016))
Compound class: Antibody
Comment: Olaratumab is a fully human anti-platelet-derived growth factor receptor α (PDGFRα) monoclonal antibody, developed by Eli Lilly (link to Lilly's olaratumab webpage here), originally developed by ImClone Systems, Inc. .
Peptide sequences and structural information for this antibody are available from its IMGT/mAb-DB record. BLAST peptide sequence analysis reveals identical matches with sequences 8 and 16 from patent US8128929, and directly to clone IMC-3G3 . From patent US8128929 it appears that the epitope recognised by olaratumab overlaps the PDGFRα binding sites for PDGF-AA and PDGF-BB.
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|
|Soft tissue sarcoma (STS): Olaratumab plus doxorubicin was approved by the US FDA in October 2016, for patients with advanced STS. Additional clinical trials include Phase 1/2 NCT02659020 evaluating gemcitabine and docetaxel with or without olaratumab in patients with STS.
Other cancers: Phase 2 trials NCT01204710 (prostate cancer, plus mitoxantrone) and NCT00913835 (ovarian cancer, plus liposomal doxorubicin) have been completed. Paclitaxel plus carboplatin ± olaratumab in non-small cell lung cancer is in Phase 2 assessment. Recurrent glioblastoma multiforme and gastrointestinal stromal tumors (GIST) have also reached Phase 2 trials.
|Mechanism Of Action and Pharmacodynamic Effects|
|Coexpression of PDGFRα and PDGFs, consistent with autocrine-mediated growth, has been reported in sarcomas and glioblastomas. Hence PDGFRα antibodies are being developed to abbrogate aberrant PDGFRα signalling and uncontrolled proliferation in cancers expressing PDGFRα.
Eli Lilly have produced a mechanism of action video for olaratumab, which you can access here.
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT00913835||A Study of Liposomal Doxorubicin With or Without Olaratumab (IMC-3G3) in Platinum-Refractory or Resistant Advanced Ovarian Cancer||Phase 2 Interventional||Eli Lilly and Company|
|NCT01204710||A Study of Olaratumab (IMC-3G3) in Prostate Cancer||Phase 2 Interventional||Eli Lilly and Company|
|NCT02659020||A Study of Olaratumab (LY3012207) in Participants With Advanced Soft Tissue Sarcoma||Phase 1/Phase 2 Interventional||Eli Lilly and Company|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)