Selepressin

Vasopressin Analogue (selective V1a Receptor Agonist)Rx: ResearchCompound: Investigational

Also known as: [Phe2,Ile3,Hom(Cys)6]-oxytocin, FE 202158, FE202158

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

Summary

Selepressin is a selective V1a vasopressin receptor agonist developed as an alternative to norepinephrine and vasopressin for vasodilatory shock, particularly septic shock. It aims to restore vascular tone without the off-target V2-mediated effects. Phase II/III clinical trials (SEPSIS-ACT) did not demonstrate significant improvement in ventilator-free or vasopressor-free days compared to placebo, leading to setbacks in development.

Mechanism of Action

Selective agonist of vasopressin V1a receptors, causing vasoconstriction via Gq-coupled signaling and smooth muscle contraction without significant V2 receptor activation, thereby avoiding V2-mediated fluid retention, coagulation effects, and immunosuppression seen with non-selective vasopressin.

Routes of Administration

Intravenous

Goals & Uses

  • Reduction of norepinephrine requirementsCatecholamine SparingModerate
  • Avoidance of V2-mediated adverse effectsSafety Improvement Over VasopressinModerate
  • Treatment of vasodilatory/septic shockHemodynamic SupportModerate
  • Restoration of vascular tone in distributive shockHemodynamic SupportLow

Contraindications

  • Hypersensitivity to selepressin or vasopressin analoguesAllergyHigh
  • Cardiogenic shockCardiovascularHigh
  • Severe peripheral vascular diseaseVascularHigh

Adverse Effects

  • HypertensionCardiovascularCommonHigh blood pressure
  • Digital/mesenteric ischemiaVascularUncommon
  • HyponatremiaElectrolyteRare
  • Skin necrosis at infusion siteDermatologicalRare
  • BradycardiaCardiovascularUncommon

Drug Interactions

  • Indomethacin and NSAIDsModerate
  • NorepinephrineModerate
  • EpinephrineModerate

Population Constraints

  • PregnancyReproductive SafetyRelative
  • Pediatric patientsAgeRelative
  • Patients with known coronary artery diseaseCardiovascularRelative
  • Severe hepatic impairmentOrgan ImpairmentRelative

Regulatory Status

  • European UnionInvestigationalNot approved; studied in multi-national trials including EU sites.
  • United StatesInvestigationalInvestigated under IND; Phase IIb/III trial (SEPSIS-ACT) failed primary endpoints; no NDA filed as of last available data.
  • United KingdomInvestigationalNot approved; participated in international SEPSIS-ACT trial.

Not approved by FDA, EMA, or MHRA. Investigated in Phase IIb/III trials (SEPSIS-ACT, NCT02508649). Development largely stalled following negative primary endpoint results in 2018–2019.

Evidence & Sources

No sources recorded yet.

Browse All PeptidesBuild My Stack