Taltirelin

Thyrotropin Releasing Hormone (TRH) AnalogueRx: PrescriptionCompound: Approved

Also known as: Ceredist, N-[(4S)-hexahydro-2,6-dioxo-4-pyrimidinylcarbonyl]-L-histidyl-L-prolinamide, TA-0910

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

Summary

Taltirelin (also known as TA-0910) is a synthetic TRH analogue approved in Japan for the treatment of spinocerebellar degeneration. It is more resistant to enzymatic degradation and has a longer duration of action compared to native TRH. It improves cerebellar ataxia and related neurological symptoms.

Mechanism of Action

Synthetic TRH analogue that binds to TRH receptors in the CNS, stimulating thyrotropin release and exerting direct neurotropic effects; enhances cholinergic, dopaminergic, and noradrenergic neurotransmission; more potent and longer-acting than endogenous TRH with greater CNS selectivity.

Routes of Administration

Oral

Goals & Uses

  • NeuroprotectionNeurologyLow
  • Spinocerebellar degeneration treatmentNeurologicalModerate
  • Amyotrophic lateral sclerosis (ALS) treatmentNeurologicalLow
  • Cerebellar ataxia symptom reliefNeurologicalModerate

Contraindications

  • HyperthyroidismEndocrineModerate
  • Hypersensitivity to taltirelin or TRH analoguesAllergyHigh
  • Pituitary apoplexy or pituitary tumorsEndocrineHigh

Adverse Effects

  • Urinary urgencyGenitourinaryUncommon
  • HeadacheNeurologicUncommonPain in the head or upper neck
  • Increased blood pressureCardiovascularUncommon
  • NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
  • Elevation of thyroid-stimulating hormone (TSH)EndocrineCommon
  • Hot flush / warmth sensationAutonomicCommon

Drug Interactions

  • Antihypertensive agentsModerate
  • Thyroid hormone medications (levothyroxine)Moderate

Population Constraints

  • PregnancyReproductive SafetyRelative
  • Patients with cardiac diseaseCardiovascularRelative
  • Elderly patientsAgeRelative
  • Renal or hepatic impairmentOrgan DysfunctionRelative

Regulatory Status

  • European UnionUnapprovedNot approved by the EMA.
  • United StatesUnapprovedNot FDA-approved; no active NDA on record. May be available via research channels.
  • United KingdomUnapprovedNot approved by the MHRA.

Approved in Japan (marketed as Ceredist) for spinocerebellar degeneration. Not approved by the FDA or EMA. Classified as a prescription drug in Japan.

Evidence & Sources

No sources recorded yet.

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