Peptide LibraryTabimorelin
Tabimorelin is an oral growth hormone secretagogue. Tabimorelin is a peptidomimetic agonist at the growth hormone secretagogue receptor with sufficient oral bioavailability for once-daily administration. It raises growth hormone and IGF-1, but development stopped after findings including hepatic enzyme elevation and inhibition of cytochrome P450 3A4, which raised interaction and safety concerns.
For research use only.
Key Facts
- CAS
- 193079-69-5
- Molecular Weight (MW)
- 528.7 g/mol
- Half-life
- —
- FDA status
- Withdrawn / Rejected
- Evidence level
- Limited Human Evidence
- Human dose established
- Yes
- Administration Route
- Oral
- Frequency
- Single dose or once daily
- Last updated
- Nov 7, 2026
- Reviewed
- Nov 7, 2026
Research summary
Orally active growth hormone secretagogue investigated for growth hormone deficiency. Development was discontinued. Not FDA-approved.
Research evidence
- Regulatory review (FDA label)None in reviewed sources
- Controlled human trials3 reviewed sources
- Early or uncontrolled human studies1 reviewed source
- Lab & animal studiesNone in reviewed sources
How it works
Each step shows whether the sources Peptide Library has reviewed include that kind of research. Counts are reviewed sources, not every study ever published. Reviews and programme summaries that describe human use are shown as "reported", not as trials, and registered trials without published results are listed but not counted. A higher step means research has progressed further; it does not mean a compound works better or is safer. Compounds whose evidence has not been reviewed yet show "Not reviewed" instead of a guess.
Peptide Library's Tabimorelin profile summarises 5 cited studies listed in the Science section, the compound's regulatory status, and research-protocol parameters reported for it. It is a research reference, not medical advice.
Tabimorelin dosage evidence
Tabimorelin (NN703) has no approved dosage. Its human dosing comes from small studies published in 2000–2003 of an oral, weight-based dose: single doses of 0.05–12 mg/kg and 7 days of 1.71–6.86 mg/kg in healthy men, and 1 week of 1.5–3 mg/kg a day in 97 adults with growth hormone deficiency, of whom only 11% had a meaningful growth hormone response. No later trials are indexed.
| Human dosing established | Yes |
|---|---|
| Route | Oral |
| Frequency | Single dose or once daily |
| Duration studied | Single dose to 7 days |
| Evidence level | Limited Human Evidence |
| Last reviewed | 2026-11-07 |
Research-reported dosing
Doses as studied, one row per regimen. Different trials used different regimens; they are listed separately rather than averaged.
| Study / context | Population | Dose | Route | Frequency | Duration | Outcome studied | Source |
|---|---|---|---|---|---|---|---|
| Adults with growth hormone deficiency (2003)Clinical trial · Multicentre, randomized, double-blind, placebo-controlled study | Adults with growth hormone deficiency (n=97; 83 tabimorelin, 14 placebo) | 3 mg/kg on the first and last day and 1.5 mg/kg a day on the 6 days between | Oral | Once daily | 1 week | Generally well tolerated; 11% of treated patients reached a peak growth hormone of at least 5 mcg/L; IGF-1 unchanged | Oral administration of the growth hormone secretagogue NN703 in adult patients with growth hormone deficiency. Clin Endocrinol (Oxf). 2003. |
| Single ascending dose study (2000)Clinical trial · Double-blind, randomized, placebo-controlled study | Healthy male volunteers (n not stated in the indexed abstract) | Eight escalating doses from 0.05 to 12 mg/kg body weight | Oral | Single dose | Single dose, sampling to 24 hours | Growth hormone raised at 1.5 mg/kg and above; IGF-1 raised at 6 and 12 mg/kg; well tolerated | The pharmacokinetics, pharmacodynamics, safety and tolerability of a single dose of NN703, a novel orally active growth hormone secretagogue in healthy male volunteers. Growth Horm IGF Res. 2000. |
| 7-day repeated dose study (2001)Clinical trial · Randomized, double-blind, placebo-controlled study | Healthy male subjects (n not stated in the indexed abstract) | 1.71, 3.0, 4.5 or 6.86 mg/kg body weight | Oral | Once daily | 7 days | Dose-related growth hormone rise that declined from day 1 to day 7; IGF-1 higher than placebo at the three highest doses | The pharmacokinetics, pharmacodynamics, safety and tolerability following 7 days daily oral treatment with NN703 in healthy male subjects. Growth Horm IGF Res. 2001. |
| Drug interaction study with midazolam (2003)Clinical trial · Clinical pharmacokinetic interaction study | Adult male subjects (n=17) | Dose not stated in the indexed abstract | Oral | Single dose, then once daily for 7 days | 7 days, with a 7-day washout | Midazolam exposure rose up to 93%, consistent with inhibition of the liver enzyme CYP3A4 | A clinical study investigating the pharmacokinetic interaction between NN703 (tabimorelin), a potential inhibitor of CYP3A4 activity, and midazolam, a CYP3A4 substrate. Eur J Clin Pharmacol. 2003. |
Where sources disagree
- All human doses are weight-based oral doses in milligrams per kilogram, studied for a week at most. They do not convert into a fixed dose or an injected dose.
- Tabimorelin inhibited CYP3A4 in people, raising blood levels of a drug cleared by that enzyme. That interaction was reported in the same research programme.
- Development did not continue past these early studies, and no later trial is indexed on PubMed or registered on ClinicalTrials.gov. The sources reviewed here do not state why it stopped.
Sequence & molecular data
| Molecular formula | C32H40N4O3 |
|---|---|
| Molecular weight | 528.7 g/mol |
| CAS number | 193079-69-5 |
| PubChem CID | 9810101 |
| FDA UNII | L51CBE03KF |
| ChEMBL | CHEMBL281764 |
Identifiers link to the public PubChem, FDA Substance Registration (UNII), ChEMBL and DrugBank records for the same entity.
Science
Mechanism of Action
Tabimorelin is a peptidomimetic agonist at the growth hormone secretagogue receptor with sufficient oral bioavailability for once-daily administration. It raises growth hormone and IGF-1, but development stopped after findings including hepatic enzyme elevation and inhibition of cytochrome P450 3A4, which raised interaction and safety concerns.
Studies
- Oral administration of the growth hormone secretagogue NN703 in adult patients with growth hormone deficiency
- Pharmacokinetic and pharmacodynamic modeling of NN703, a growth hormone secretagogue, after a single po dose to human volunteers
- The pharmacokinetics, pharmacodynamics, safety and tolerability following 7 days daily oral treatment with NN703 in healthy male subjects
- The pharmacokinetics, pharmacodynamics, safety and tolerability of a single dose of NN703, a novel orally active growth hormone secretagogue in healthy male volunteers
- A clinical study investigating the pharmacokinetic interaction between NN703 (tabimorelin), a potential inhibitor of CYP3A4 activity, and midazolam, a CYP3A4 substrate
Research statistics
18 PubMed publications · 33.3% human clinical research · 0 registered trials
Counts of published research through 2026-11-01, not evidence that it works. Publications by year, study types and trials · How publications are counted
Regulatory & research status
Tabimorelin was withdrawn from the market or rejected for approval. It is not an approved product.
| FDA status | Withdrawn / Rejected |
|---|---|
| Research status | Development discontinued |
| Availability | Research-Only |
| WADA (sport) | Unknown / Not Listed |
| Library classification | Clinical Trial |
How FDA approval, compounding and research-only status differ
Benefits
—
Tabimorelin side effects
No side effects listed yet for this entry.
Storage & stability
This compound is not supplied as a powder to be mixed, so the freeze-dried powder and reconstitution handling described for research peptides does not apply. Storage conditions are product-specific: follow the label or packaging of the product itself.
Tabimorelin: frequently asked questions
What is Tabimorelin?
Orally active growth hormone secretagogue investigated for growth hormone deficiency. Development was discontinued. Not FDA-approved.
How does Tabimorelin work?
Tabimorelin is a peptidomimetic agonist at the growth hormone secretagogue receptor with sufficient oral bioavailability for once-daily administration. It raises growth hormone and IGF-1, but development stopped after findings including hepatic enzyme elevation and inhibition of cytochrome P450 3A4, which raised interaction and safety concerns.
Is Tabimorelin FDA approved?
No. Tabimorelin is not currently FDA-approved. Its development or marketing was discontinued, which can happen for commercial reasons as well as safety or efficacy ones. Any material available today is not an approved product.
What peptides are similar to Tabimorelin?
Compounds most often compared with Tabimorelin include MK-677, Macimorelin, Anamorelin and Relamorelin. They are grouped by shared mechanism or research area rather than by equivalence, and their regulatory status and evidence base differ.
References
- Oral administration of the growth hormone secretagogue NN703 in adult patients with growth hormone deficiency — Clin Endocrinol (Oxf), 2003External reference
- Pharmacokinetic and pharmacodynamic modeling of NN703, a growth hormone secretagogue, after a single po dose to human volunteers — J Clin Pharmacol, 2001External reference
- The pharmacokinetics, pharmacodynamics, safety and tolerability following 7 days daily oral treatment with NN703 in healthy male subjects — Growth Horm IGF Res, 2001External reference
- The pharmacokinetics, pharmacodynamics, safety and tolerability of a single dose of NN703, a novel orally active growth hormone secretagogue in healthy male volunteers — Growth Horm IGF Res, 2000External reference
- A clinical study investigating the pharmacokinetic interaction between NN703 (tabimorelin), a potential inhibitor of CYP3A4 activity, and midazolam, a CYP3A4 substrate — Eur J Clin Pharmacol, 2003External reference
Related research, comparisons & guides
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Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Nov 7, 2026 · Version 2
This Tabimorelin profile is compiled from published literature (5 cited studies linked above), public regulatory records and chemical registries. It describes what research reports; it is not medical advice, and nothing here is a dosing recommendation for humans. Peptide Library does not sell peptides. Editorial policy · How profiles are compiled · Report an error
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