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Taminadenant

From Wikipedia, the free encyclopedia

Pharmaceutical compound
Taminadenant
Identifiers
  • 5-bromo-2,6-di(pyrazol-1-yl)pyrimidin-4-amine
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC10H8BrN7
Molar mass306.127 g·mol−1
3D model (JSmol)
  • C1=CN(N=C1)C2=NC(=NC(=C2Br)N)N3C=CC=N3
  • InChI=1S/C10H8BrN7/c11-7-8(12)15-10(18-6-2-4-14-18)16-9(7)17-5-1-3-13-17/h1-6H,(H2,12,15,16)
  • Key:ATFXVNUWQOXRRU-UHFFFAOYSA-N

Taminadenant (PBF509) is an experimental drug which acts as a selective inhibitor of theadenosine A2A receptor. It is inclinical trials for the treatment oflung cancer, and has also shown potential for applications in the treatment ofmovement disorders.[1][2][3][4]

References

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  1. ^Mediavilla-Varela M, Castro J, Chiappori A, Noyes D, Hernandez DC, Allard B, et al. (July 2017)."A Novel Antagonist of the Immune Checkpoint Protein Adenosine A2a Receptor Restores Tumor-Infiltrating Lymphocyte Activity in the Context of the Tumor Microenvironment".Neoplasia.19 (7):530–536.doi:10.1016/j.neo.2017.02.004.PMC 5458644.PMID 28582704.
  2. ^Núñez F, Taura J, Camacho J, López-Cano M, Fernández-Dueñas V, Castro N, et al. (2018)."PBF509, an Adenosine A2A Receptor Antagonist With Efficacy in Rodent Models of Movement Disorders".Frontiers in Pharmacology.9: 1200.doi:10.3389/fphar.2018.01200.PMC 6202948.PMID 30405415.
  3. ^Chiappori AA, Creelan B, Tanvetyanon T, Gray JE, Haura EB, Thapa R, et al. (June 2022)."Phase I Study of Taminadenant (PBF509/NIR178), an Adenosine 2A Receptor Antagonist, with or without Spartalizumab (PDR001), in Patients with Advanced Non-Small Cell Lung Cancer".Clinical Cancer Research.28 (11):2313–2320.doi:10.1158/1078-0432.CCR-21-2742.PMC 9167697.PMID 35254415.
  4. ^Chen DT, Saltos AN, Rose T, Thompson ZJ, Thapa R, Chiappori A, et al. (April 2023)."Early Adverse Event Derived Biomarkers in Predicting Clinical Outcomes in Patients with Advanced Non-Small Cell Lung Cancer Treated with Immunotherapy".Cancers.15 (9): 2521.doi:10.3390/cancers15092521.PMC 10177532.PMID 37173987.
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