PeptideTrace
Research CompoundNative TRH Peptide (Diagnostic, Withdrawn)

Protirelin

Thypinone, Relefact TRH

B

Evidence Grade B — Strong clinical evidence. 121 published studies, 102 human. 15 registered clinical trials.

15 trials121 studiesUSEUCA

Overview

Protirelin (previously sold as Thypinone and Relefact TRH) is synthetic TRH — the brain hormone that controls thyroid function. It was used as a diagnostic injection to test pituitary function but has been discontinued from the US market after advances in blood test sensitivity made the provocative test unnecessary. It is notable as one of the smallest biologically active hormones known (just three amino acids), and its discovery contributed to a Nobel Prize in 1977.

Research Activity

121studies
Human 102
Animal 13
In-vitro 4
Reviews 6

121 published studies: 102 human, 13 animal, 4 in-vitro, 6 reviews

Regulatory Status

US
Not approved by FDA(FDA)
EU
Not authorised by EMA(EMA)
CA
Cancelled in Canada(Health Canada)

Legal Status

USNot applicable (not approved)
EUNot applicable (not authorised)
CAPrescription drug

Summary

Protirelin was previously marketed as Thypinone (Abbott) and Relefact TRH (Hoechst). The TRH stimulation test was a standard endocrine diagnostic procedure from the 1970s through the 1990s. It was discontinued from the US market in the early 2000s after advances in laboratory TSH measurement eliminated the need for a provocative test in most clinical scenarios.

Protirelin is notable as the smallest known biologically active peptide hormone (just three amino acids) and its discovery contributed to a Nobel Prize in Physiology or Medicine in 1977.

Mechanism of Action

When injected intravenously, protirelin stimulates the pituitary to release TSH. In a healthy person, TSH rises predictably within 20–30 minutes. The pattern of response — whether exaggerated, normal, or absent — helped clinicians distinguish between different types of thyroid and pituitary disorders. This diagnostic utility was replaced by third-generation TSH assays that can detect extremely low TSH levels directly from a blood sample.

Research Summary

Research suggests protirelin's diagnostic utility was well established from the 1970s through the 1990s but was made obsolete by third-generation TSH assays that can detect extremely low TSH levels directly from a blood sample, eliminating the need for an injection-based test. Rare but serious adverse events included pituitary apoplexy in patients with undiagnosed large pituitary tumours. A related compound (taltirelin, an oral TRH analogue) is approved in Japan for a neurological condition, and TRH-based approaches are being explored for traumatic brain injury. No active development exists for protirelin itself in major markets.

Clinical Trials

NCT01970124Phase IIICompleted

A Long-Term Study of KPS-0373 in Patients With Spinocerebellar Degeneration (SCD)

Kissei Pharmaceutical Co., Ltd.Endpoint: SARA (Scale for the Assessment and Rating of Ataxia)
NCT01004016Phase IICompleted

A Study of KPS-0373 in Patients With Spinocerebellar Degeneration (SCD)

Kissei Pharmaceutical Co., Ltd.Endpoint: Scale for Assessment and Rating of Ataxia (SARA)
NCT01970137Phase IIICompleted

A 24-week Open-label Study of KPS-0373 in Patients With Spinocerebellar Degeneration (SCD)

Kissei Pharmaceutical Co., Ltd.Endpoint: SARA (Scale for the Assessment and Rating of Ataxia)
NCT01970111Phase IIICompleted

An Extension Study of KPS-0373 in Patients With Spinocerebellar Degeneration (SCD)

Kissei Pharmaceutical Co., Ltd.Endpoint: SARA (Scale for the Assessment and Rating of Ataxia)
NCT00863538Phase IICompleted

Phase II Study of KPS-0373 in Patients With Spinocerebellar Degeneration (SCD)

Kissei Pharmaceutical Co., Ltd.Endpoint: Scale for the assessment and rating of ataxia (SARA), ADL(Flow-FIM), Patient Improvement Impression
View all 15 trials on ClinicalTrials.gov →

Regulatory Timeline

1976
Regulatory

Health Canada Market Authorisation

The information on this page is provided for educational and research reference purposes only. This is not medical advice. Always consult a qualified healthcare professional before making any health-related decisions.

Related Compounds

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Approved
GLP-1 Receptor Agonist

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Pramlintide

Approved
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