imaradenant   Click here for help

GtoPdb Ligand ID: 11153

Synonyms: AZD-4635 | AZD4635
PDB Ligand Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: Imaradenant (AZD4635) is an orally bioavailable adenosine A2A receptor (A2AR) antagonist [2]. It was developed as a potential immuno-oncology (immunotherapy) drug. Imaradenant reduces the immunosuppressive effects of adenosine within the tumour microenvironment, an activity that rescues immune cell function and it enhances the efficacy of checkpoint inhibitors in syngeneic mouse tumour models [2].
In 2021 AstraZeneca decided to stop a number of their midphase studies of imaradenant in patients with prostate cancer.
Click here for help
2D Structure
Click here for help
Click here for structure editor
Physico-chemical Properties
Click here for help
Hydrogen bond acceptors 5
Hydrogen bond donors 1
Rotatable bonds 2
Topological polar surface area 77.58
Molecular weight 315.07
XLogP 2.8
No. Lipinski's rules broken 0
Click here for help
Canonical SMILES Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl
Isomeric SMILES Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl
InChI InChI=1S/C15H11ClFN5/c1-8-6-10(7-12(16)19-8)14-13(20-15(18)22-21-14)9-2-4-11(17)5-3-9/h2-7H,1H3,(H2,18,20,22)
No information available.
Summary of Clinical Use Click here for help
AZD4635 is being evaluated in combination with other therapeutic agents in patients with solid tumours.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03980821 A Phase I Study of AZD4635 in Japanese Patients With Advanced Solid Malignancies Phase 1 Interventional AstraZeneca
NCT03381274 Oleclumab (MEDI9447) EGFRm NSCLC Novel Combination Study Phase 1/Phase 2 Interventional MedImmune LLC
NCT02740985 A Phase 1 Clinical Study of AZD4635 in Patients With Advanced Solid Malignancies Phase 1 Interventional AstraZeneca
NCT04089553 An Open-label, Phase II Study of AZD4635 in Patients With Prostate Cancer Phase 2 Interventional AstraZeneca