ATN-161

Integrin Antagonist PeptideRx: ResearchCompound: Investigational

Also known as: Ac-PHSCN-NH2, ATN161, PHSCN

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

Summary

ATN-161 is a non-RGD peptidomimetic acetylated pentapeptide (Ac-PHSCN-NH2) derived from the synergy region of fibronectin. It acts as an integrin α5β1 and αvβ3 antagonist and has demonstrated antitumor and antiangiogenic activity in preclinical models. It was evaluated in Phase I and Phase II clinical trials for solid tumors, including glioblastoma, in combination with chemotherapy agents such as temozolomide and carboplatin.

Mechanism of Action

Inhibits integrin α5β1 and αvβ3 by binding to fibronectin-derived sequences, blocking integrin-mediated cell adhesion, migration, and angiogenesis; also modulates integrin signaling to suppress tumor vasculature formation and cancer cell invasion.

Routes of Administration

Intravenous

Goals & Uses

  • Glioblastoma treatmentNeuro OncologyLow
  • Metastasis inhibitionOncologyModerate
  • Anti-angiogenesisOncology / VascularModerate
  • Combination chemotherapy sensitizationOncologyLow
  • Antitumor activity in solid tumorsOncologyModerate

Contraindications

  • Hypersensitivity to ATN-161 or fibronectin-derived peptidesAllergyHigh
  • PregnancyPopulationHighPotential fetal risk or insufficient safety data
  • Active bleeding disordersHematologyModerate

Adverse Effects

  • ThrombocytopeniaHematologicUncommonLow platelet count
  • NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
  • FatigueGeneralCommonLow energy or tiredness
  • Elevated liver enzymesHepaticUncommonIncrease in AST/ALT or other hepatic markers
  • Infusion-related reactionsHypersensitivityUncommon

Drug Interactions

  • CarboplatinLow
  • Anticoagulants / antiplatelet agentsModerate
  • TemozolomideLow

Population Constraints

  • Severe renal impairmentOrgan ImpairmentRelative
  • Pediatric patientsAgeRelative
  • Pregnant or breastfeeding womenReproductiveRelative
  • Severe hepatic impairmentOrgan ImpairmentRelative

Regulatory Status

  • European UnionInvestigationalNo EMA approval or marketing authorization; investigational use only.
  • United StatesInvestigationalEvaluated in Phase I and Phase II clinical trials; IND held by Attenuon LLC; no NDA filed or approved.
  • United KingdomUnknownNo MHRA approval; likely follows investigational status consistent with EU.

ATN-161 has not received FDA, EMA, or any other regulatory approval. It remains an investigational compound. Clinical development appears to have stalled after Phase II trials.

Evidence & Sources

No sources recorded yet.

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