Reversin 121

P Glycoprotein Inhibitor Peptide / MDR Reversal AgentRx: ResearchCompound: Research

Also known as: P-gp inhibitor peptide 121, Reversin-121

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

Summary

Reversin 121 is a short cyclic peptide identified as a potent modulator of P-glycoprotein (MDR1/ABCB1). It was discovered through combinatorial peptide library screening and demonstrated ability to sensitize multidrug-resistant cancer cell lines to chemotherapeutic agents such as doxorubicin and vinblastine by blocking P-gp efflux activity. It remains a research tool compound with no clinical development reported.

Mechanism of Action

Inhibits P-glycoprotein (P-gp/ABCB1)-mediated drug efflux by binding to the transporter, thereby reversing multidrug resistance (MDR) in cancer cells and increasing intracellular accumulation of cytotoxic agents.

Routes of Administration

In Vitro

Goals & Uses

  • Reversal of multidrug resistance in cancerOncology / Pharmacology ResearchLow
  • Increased intracellular accumulation of chemotherapeuticsDrug Delivery / Pharmacokinetics ResearchLow

Contraindications

  • Human clinical useRegulatoryHigh

Adverse Effects

  • Unknown systemic toxicityGeneralUnknown

Drug Interactions

  • P-glycoprotein substrates (e.g., doxorubicin, vinblastine, paclitaxel)High

Population Constraints

  • General human populationRegulatory/safetyAbsolute

Regulatory Status

  • European UnionUnapprovedNo EMA filing; research use only.
  • United StatesUnapprovedNo IND or regulatory filing; research use only.
  • United KingdomUnapprovedNo MHRA filing; research use only.

No regulatory filings identified in any jurisdiction. Strictly a research/in vitro tool compound.

Evidence & Sources

No sources recorded yet.

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