Dalantercept

Fusion Protein / ALK1 Fc Fusion (activin Receptor Like Kinase 1 Extracellular Domain Fused To IgG1 Fc)Rx: ResearchCompound: Investigational

Also known as: ACE-041, ALK1-Fc

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

Summary

Dalantercept (ACE-041) is an investigational anti-angiogenic fusion protein consisting of the extracellular domain of ALK1 (activin receptor-like kinase 1) fused to a human IgG1 Fc region. It functions as a ligand trap for BMP9 and BMP10, inhibiting the ALK1 signaling pathway critical for tumor angiogenesis. It was evaluated in multiple solid tumor types including renal cell carcinoma and hepatocellular carcinoma. Clinical development was discontinued after Phase 2 trials did not demonstrate sufficient efficacy.

Mechanism of Action

Acts as a ligand trap for BMP9 and BMP10, binding to and inhibiting ALK1 (activin receptor-like kinase 1) signaling pathway, thereby blocking tumor angiogenesis by preventing endothelial cell proliferation and new blood vessel formation in tumors.

Routes of Administration

IntravenousSubcutaneous

Goals & Uses

  • Hepatocellular carcinoma treatmentOncologyLow
  • Renal cell carcinoma treatmentOncologyModerate
  • Anti-tumor angiogenesisOncologyModerate
  • Head and neck squamous cell carcinoma treatmentOncologyLow

Contraindications

  • Severe hepatic impairmentOrganModerateLiver function concerns
  • PregnancyPopulationHighPotential fetal risk or insufficient safety data
  • Hereditary hemorrhagic telangiectasia (HHT)Genetic Vascular DisorderHigh

Adverse Effects

  • TelangiectasiasDermatologic/vascularCommon
  • Peripheral edemaFluid BalanceCommonSwelling of the arms or legs
  • HypertensionCardiovascularUncommonHigh blood pressure
  • EpistaxisVascular/bleedingCommon
  • FatigueGeneralCommonLow energy or tiredness
  • Pulmonary hypertensionCardiovascular/pulmonaryRare

Drug Interactions

  • AxitinibModerate
  • Antihypertensive agentsModerate

Population Constraints

  • Patients with pre-existing vascular malformationsVascularRelative
  • Pediatric patientsAgeRelative
  • Pregnant womenReproductiveAbsolute

Regulatory Status

  • European UnionInvestigationalEvaluated in clinical trials; no marketing authorization sought or granted. Development discontinued.
  • United StatesInvestigationalInvestigated under IND; clinical development discontinued by Acceleron Pharma after Phase 2 failures. Never approved by FDA.

Never received regulatory approval in any jurisdiction. Clinical development discontinued by Acceleron Pharma following results of Phase 2 trials, including a Phase 2 study in renal cell carcinoma (DART trial) that did not meet primary endpoints.

Evidence & Sources

No sources recorded yet.

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