Montirelin
Also known as: 3-methyl-His2-TRH, Ceredist, CG-3703, montirelin hydrate, RX-77368
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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
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.
Frequently Asked Questions
What is Montirelin?
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.
What is Montirelin used for?
Montirelin is educationally associated with: Neuroprotection, Disorders of consciousness / arousal, Treatment of spinocerebellar degeneration, Pituitary function testing. Educational only — not medical advice.
How is Montirelin administered?
Recorded routes of administration: Oral.
What are the potential side effects of Montirelin?
Reported adverse effects include: Urinary urgency, Increased prolactin levels, Headache, Flushing, Increased blood pressure, Nausea. This list is not exhaustive — consult a qualified clinician.
Who should avoid Montirelin?
Recorded contraindications: Thyroid disease (hyperthyroidism), Pregnancy, Severe cardiovascular disease, Hypersensitivity to montirelin or TRH analogues. Consult a qualified clinician before use.