Taminadenant

Taminadenant

Identifiers
IUPAC name 5-bromo-2,6-di(pyrazol-1-yl)pyrimidin-4-amine
CAS Number	1337962-47-6
PubChem CID	53466958
DrugBank	DB18811
ChemSpider	58810193
UNII	84I5UEP321
ChEMBL	ChEMBL3694769
Chemical and physical data
Formula	C10H8BrN7
Molar mass	306.127 g·mol−1
3D model (JSmol)	Interactive image
SMILES C1=CN(N=C1)C2=NC(=NC(=C2Br)N)N3C=CC=N3
InChI 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 the adenosine A2A receptor. It is in clinical trials for the treatment of lung cancer, and has also shown potential for applications in the treatment of movement disorders. ^{[1] [2] [3] [4]}

References

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 A_2A 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.