Neladenoson bialanate (BAY1067197) is the first oral partial and highly selective A1R agonist that has entered clinical development for the treatment of heart failure. Neladenoson bialanate maintains the cardioprotective effects of adenosine without the undesired side effects of a full agonist. Of particular importance in this clinical development is the potential influence of concomitant use of β-blockers as they have the potential to increase the risk of AV conduction abnormalities with A1R agonist treatment. Two small phase 2a pilot studies evaluating the short-term safety of neladenoson bialanate in patients with HFrEF pretreated with β-blockers have recently completed, and the results are pending (ClinicalTrials.gov identifiers: NCT02040233 and NCT01945606). In a small phase 1 trial in healthy volunteers pretreated with the β-blocker metoprolol succinate, a single 50 mg oral dose of neladenoson bialanate administered together with metaprolol succinate was found to be well tolerated. Notably, no higher degree AV block, prolongation of the PR interval, or relevant decreases in heart rate or systemic blood pressure were observed.