Taminadenant

Taminadenant is an adenosine A_2A receptor antagonist (K_i = 12 nM).¹ It is selective for adenosine A_2A receptors over adenosine A₁-, A_2B-, and A₃ receptors (K_is = 2,500, 1,000, and 5,000 nM, respectively). Taminadenant (1 µM) increases the levels of IFN-γ secreted by tumor-associated T cells isolated from patient-derived lung tumors when used in combination with an antibody targeting programmed cell death protein 1 (PD-1) or PD-1 ligand (PD-L1). It reduces the number of lung nodules in an MCA-205 murine fibrosarcoma model of lung metastasis when administered at a dose of 15 mg/kg per day. Taminadenant (3, 10, or 30 mg/kg) inhibits catalepsy induced by haloperidol (Item No. 12014) in a rat model of Parkinson's disease motor symptoms.²

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1. Mediavilla-Varela, M., Castro, J., Chiappori, A., et al. 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 (2017).

2. Núñez, F., Taura, J., Camacho, J., et al. PBF509, an adenosine A_2A receptor antagonist with efficacy in rodent models of movement disorders. Front. Pharmacol. 9, 1200 (2018).