Neladenoson bialanate

Adenosine A1 Receptor Partial Agonist (prodrug; Small Molecule Peptide Conjugated)Rx: InvestigationalCompound: Investigational

Also known as: BAY 1067197, BAY-1067197, neladenoson bialanate

Educational Only — Not medical advice. Consult a qualified clinician before using any peptide.

Summary

Neladenoson bialanate (BAY 1067197) is an oral prodrug of neladenoson, a selective adenosine A1 receptor partial agonist developed by Bayer AG. It was investigated primarily for the treatment of chronic heart failure with reduced ejection fraction (HFrEF) and heart failure with preserved ejection fraction (HFpEF). Phase II clinical trials (PANTHEON and PANACHE) showed it was well tolerated but did not demonstrate significant improvement in primary endpoints, limiting further development.

Mechanism of Action

Neladenoson bialanate is an oral prodrug that is converted to neladenoson, a selective partial agonist of the adenosine A1 receptor (A1AR). Activation of A1AR mediates cardioprotective effects including reduction of heart rate, modulation of cardiac energy metabolism, and attenuation of maladaptive remodeling in heart failure.

Routes of Administration

Oral

Goals & Uses

  • Chronic heart failure with reduced ejection fraction (HFrEF)CardiovascularModerate
  • CardioprotectionCardiovascularLow
  • Heart rate reductionCardiovascularModerate
  • Heart failure with preserved ejection fraction (HFpEF)CardiovascularLow

Contraindications

  • Severe bradycardiaCardiacHigh
  • Known hypersensitivity to neladenoson or excipientsAllergyHigh
  • Second or third degree AV blockCardiac ConductionHigh

Adverse Effects

  • HypotensionCardiovascularUncommonLow blood pressure
  • NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit
  • AV conduction prolongationCardiovascularUncommon
  • DizzinessNeurologicUncommonFeeling faint, lightheaded, or unsteady
  • BradycardiaCardiovascularCommon

Drug Interactions

  • Calcium channel blockers (non-dihydropyridine)Moderate
  • Beta-blockersModerate
  • DigoxinModerate
  • Methylxanthines (e.g., theophylline, caffeine)Moderate

Population Constraints

  • PregnancyReproductive SafetyRelative
  • Severe renal impairmentOrgan ImpairmentRelative
  • Pediatric patientsAgeRelative
  • Severe hepatic impairmentOrgan ImpairmentRelative

Regulatory Status

  • European UnionInvestigationalPhase II trials conducted in EU under Bayer AG sponsorship; no marketing authorization sought.
  • United StatesInvestigationalIND-level investigations only; Phase II completed; no NDA filed.
  • United KingdomInvestigationalNo approval; investigational use only in clinical trial context.

Not approved in any jurisdiction. Investigated in Phase II trials (PANTHEON for HFrEF, PANACHE for HFpEF). Development was not advanced to Phase III based on Phase II results.

Evidence & Sources

No sources recorded yet.

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