Montirelin

Thyrotropin Releasing Hormone (TRH) AnalogueRx: PrescriptionCompound: Approved

Also known as: 3-methyl-His2-TRH, Ceredist, CG-3703, montirelin hydrate, RX-77368

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

Summary

Montirelin (also known as CG-3703 or RX-77368) is a synthetic TRH analogue with greater metabolic stability and potency than endogenous TRH. It is approved in Japan (as montirelin hydrate, brand name Ceredist) for the treatment of spinocerebellar degeneration. It has been investigated for other CNS conditions including disorders of consciousness.

Mechanism of Action

Synthetic analogue of thyrotropin-releasing hormone (TRH) that acts as a TRH receptor agonist, stimulating the release of TSH and prolactin from the anterior pituitary. Also exhibits CNS activity including neuroprotective and analeptic effects, potentially through direct receptor-mediated actions in the brain.

Routes of Administration

Oral

Goals & Uses

  • NeuroprotectionNeurologyLow
  • Disorders of consciousness / arousalNeurological / Critical CareLow
  • Treatment of spinocerebellar degenerationNeurological / Movement DisordersModerate
  • Pituitary function testingEndocrinology / DiagnosticModerate

Contraindications

  • Thyroid disease (hyperthyroidism)EndocrineModerate
  • PregnancyPopulationModeratePotential fetal risk or insufficient safety data
  • Severe cardiovascular diseaseCardiovascularModerate
  • Hypersensitivity to montirelin or TRH analoguesAllergy / ImmunologicHigh

Adverse Effects

  • Urinary urgencyGenitourinaryUncommon
  • Increased prolactin levelsEndocrineCommon
  • HeadacheNeurologicUncommonPain in the head or upper neck
  • FlushingVascularCommonWarmth and redness of the skin
  • Increased blood pressureCardiovascularUncommon
  • NauseaGastrointestinalCommonFeeling of sickness or urge to vomit

Drug Interactions

  • Thyroid hormone preparations (levothyroxine)Low
  • Dopamine agonists (bromocriptine, cabergoline)Low
  • Antithyroid drugs (methimazole, propylthiouracil)Moderate

Population Constraints

  • Hepatic impairmentOrgan FunctionRelative
  • Renal impairmentOrgan ImpairmentRelative
  • Pediatric patientsAgeRelative
  • Elderly patientsAgeRelative

Regulatory Status

  • European UnionUnapprovedNot approved by the EMA; no marketing authorization in the European Union.
  • United StatesUnapprovedNot approved by the FDA; classified as investigational/research compound in the US.
  • United KingdomUnapprovedNot approved by the MHRA in the United Kingdom.

Approved in Japan for spinocerebellar degeneration. Not approved by the FDA or EMA. Research and investigational use in other jurisdictions.

Evidence & Sources

No sources recorded yet.

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