Taltirelin
An oral form of the brain hormone TRH, approved in Japan for a rare movement disorder
Taltirelin is a modified thyrotropin-releasing hormone that works by mouth and lasts longer than TRH. Approved in Japan since 2000 as Ceredist for ataxia in spinocerebellar degeneration, it is not approved in the US or EU.
What is it?
Thyrotropin-releasing hormone (TRH) is a three-amino-acid brain hormone best known for telling the pituitary to release thyroid-stimulating hormone. It also acts as a messenger within the brain, which is why researchers have looked for forms of it that reach the brain and last longer. Spinocerebellar degeneration, the condition taltirelin is approved for in Japan, is a group of disorders that cause progressive loss of coordination.
Taltirelin is a modified TRH designed to survive being taken by mouth and to act more on the brain than on the thyroid. According to a 2001 drug profile, it was approved in Japan in July 2000 and launched that September as Ceredist, the first oral drug for spinocerebellar degeneration. In a small study of people after stroke, eight weeks of daily oral doses left thyroid and pituitary hormones within the normal range.
The best modern trial is Korean: in 149 patients with ataxia, 24 weeks of taltirelin slowed worsening on an ataxia rating scale slightly compared with controls. Animal studies have explored it as a breathing stimulant against opioid-induced respiratory depression and as an anti-itch agent, but there are no human data for those uses.
At a Glance
Every value in this table is printed from the Grey Peptides dataset, the same record the compound explorer and comparison tool read, so the three can never disagree.
Educational information, not medical advice. The doses on this page come from approved labels, published studies and, where no study exists, amounts reported by users. None is a recommendation for you. An unapproved compound has no established safe or effective human dose, and products sold for “research use only” are not made or tested for people. Talk to a doctor before acting on anything on this site, including before you start, stop or change any medicine or dose. Full medical disclaimer.
Published Research
The studies behind taltirelin, read from their PubMed abstracts.
Approval in Japan
A drug profile records that a new drug application was filed in Japan in April 1999 for spinocerebellar degeneration, approved in July 2000, and launched in September 2000 as the first orally administered drug for the condition.
Korean trial in ataxia, 149 patients
Patients randomised to taltirelin 5 mg twice daily or control for 24 weeks; the ataxia score changed by -0.51 on taltirelin against +0.36 on control (p = 0.032), with gains in stance and speech, but no significant differences in the other secondary outcomes.
Speech in Machado-Joseph disease
In 10 patients, four weeks of taltirelin made the timing of repeated syllables more regular on acoustic analysis, more so in milder cases, while the overall ataxia rating did not change significantly.
Thyroid axis after stroke
In people after stroke given 2.5 to 20 mg by mouth daily for eight weeks, thyroid hormones and TSH stayed within normal ranges and the TSH response to TRH was not significantly changed.
A possible opioid-breathing reversal agent
A review of 52 papers found TRH and taltirelin stimulated breathing in animals given opioids, but intravenous TRH did not reverse opioid-induced respiratory depression in humans, and no human data exist for taltirelin.
Itch in mice
Taltirelin reduced scratching after a chemical itch trigger in a dose-dependent way and eased a model of chronic itch in mice.
Side Effects & Contraindications
Reported Side Effects
From the studies above.
Contraindications & Cautions
Taltirelin has no US label. Points from the research.
Legal Status
Taltirelin is approved in Japan and not in the US.
Frequently Asked Questions
?What is taltirelin?
An orally active analogue of thyrotropin-releasing hormone, approved in Japan in 2000 as Ceredist for ataxia in spinocerebellar degeneration.
?Does taltirelin work for ataxia?
In a 24-week Korean trial of 149 patients, it slowed worsening on an ataxia scale slightly compared with controls, with gains in stance and speech but not in other measures.
?Is taltirelin approved in the US?
No. Drugs@FDA holds no record for it, and it has no central EU authorisation.
References
- [fda] US FDA, Drugs@FDA (openFDA): no application for taltirelin. Read October 3, 2026.
- [pubmed] Brown WM. "Taltirelin (Tanabe Seiyaku)." IDrugs, 2001;4(12):1389-400. PMID: 15931571.
- [clinical-trial] Cho JW, et al. "Efficacy and Safety of Taltirelin Hydrate in Patients With Ataxia Due to Spinocerebellar Degeneration." J Mov Disord, 2025;18(1):35-44. PMID: 39428104.
- [clinical-trial] Shirasaki H, et al. "[A quantitative evaluation of spinocerebellar degeneration by an acoustic analysis--the effect of taltirelin hydrate on patients with Machado-Joseph disease]." Rinsho Shinkeigaku, 2003;43(4):143-8. PMID: 12884823.
- [pubmed] Miyashita K, et al. "Alteration by prolonged oral administration of a thyrotropin-releasing hormone analog, TA-0910, of the pituitary-thyroid axis in subjects with brain stroke." Intern Med, 1993;32(9):681-5. PMID: 8142670.
- [pubmed] Algera MH, et al. "Are thyrotropin-releasing hormone (TRH) and analog taltirelin viable reversal agents of opioid-induced respiratory depression?." Pharmacol Res Perspect, 2022;10(3):e00974. PMID: 35621218.
- [pubmed] Eto K, et al. "Thyrotropin-Releasing Hormone Analog Taltirelin Inhibits Acute and Chronic Itch in Mice." Biol Pharm Bull, 2024;47(11):1927-1930. PMID: 39603612.
Sources & Citations
Studies were read from their PubMed records; regulatory sources are listed below, read October 3, 2026.
Medical Disclaimer: This content is for educational and informational purposes only. It is not medical advice, and nothing here is an instruction to obtain or use any compound. Consult a licensed healthcare provider before making health decisions.