cintirorgon   Click here for help

GtoPdb Ligand ID: 10045

Synonyms: compound 32J [WO2016201225A1] | LYC-55716 | LYC55716
Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: Cintirorgon (LYC-55716) is a first-in-class, oral, selective RORγ agonist that is being developed by Lycera as a novel immuno-oncology agent. It is one of the chemical structures claimed in Lycera's patent WO2016201225A1 [1].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 5
Hydrogen bond donors 1
Rotatable bonds 9
Topological polar surface area 101.52
Molecular weight 603.12
XLogP 7.19
No. Lipinski's rules broken 1
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Canonical SMILES FC(Oc1cc(F)cc(c1)c1ccc2c(c1)N(CC(O2)CC(C(=O)O)(C)C)S(=O)(=O)c1cccc(c1)C(F)(F)F)F
Isomeric SMILES FC(Oc1cc(F)cc(c1)c1ccc2c(c1)N(C[C@@H](O2)CC(C(=O)O)(C)C)S(=O)(=O)c1cccc(c1)C(F)(F)F)F
InChI InChI=1S/C27H23F6NO6S/c1-26(2,24(35)36)13-20-14-34(41(37,38)21-5-3-4-17(11-21)27(31,32)33)22-10-15(6-7-23(22)39-20)16-8-18(28)12-19(9-16)40-25(29)30/h3-12,20,25H,13-14H2,1-2H3,(H,35,36)/t20-/m0/s1
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Summary of Clinical Use Click here for help
Phase 1 and 1/2 clinical trials testing LYC-55716 are recruiting patients (August 2018). Phase 1 NCT03396497 is evaluating LYC-55716 plus the checkpoint inhibitor pembrolizumab in NSCLC, whereas Phase 1/2 NCT02929862 will evaluate LYC-55716 as a monotherapy in a selection of locally advanced or metastatic solid tumours that are considered the most likely to be responsive to RORγ agonist therapy.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
RORγ is a nuclear receptor transcription factor that acts as an immune cell master control switch. Activation of this switch by RORγ agonists mediates improved immune cell function and decreases immunosuppressive mechanisms, actions which synergise to bring about enhanced tumour cell killing.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02929862 Study of LYC-55716 in Adult Subjects With Locally Advanced or Metastatic Cancer Phase 1/Phase 2 Interventional Lycera Corp.
NCT03396497 Study of LYC-55716 With Pembrolizumab in Adult Subjects With Non-Small Cell Lung Cancer Phase 1 Interventional Lycera Corp.