LTP·01learntopeptide
Metabolic & GLP-1Small moleculeEvidence B2 cited

Tesofensine

aka NS2330 · TE · triple monoamine reuptake inhibitor

A triple monoamine reuptake inhibitor researched for significant appetite suppression and weight reduction.

Molecular wt
328.3g/mol
Formula
C17H23Cl2NO
CAS
195875-84-4
Half-life
9.2 days
clinical
Tmax
8 h
Route
Oral
PubChem
11370864

Sequence

Read this before quoting the sequence
Not a peptide. Tesofensine is a small-molecule tropane derivative, (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(ethoxymethyl)-8-methyl-8-azabicyclo[3.2.1]octane, acting as a triple (serotonin/noradrenaline/dopamine) monoamine reuptake inhibitor. No amino acid sequence exists.
Source ↗

Mechanism of action

Tesofensine works by inhibiting the reuptake of neurotransmitters such as dopamine, norepinephrine, and serotonin in the brain. This leads to increased levels of these neurotransmitters, which are associated with reduced appetite and increased energy expenditure. The compound primarily acts on the central nervous system to modulate appetite control centers.

What the evidence actually shows

Grade B

There are several human clinical trials that have demonstrated tesofensine's efficacy in promoting weight loss through appetite suppression. These studies generally show significant weight reduction compared to placebo. However, long-term safety data and studies on diverse populations are limited.

Regulatory status

Status
Not approved. No FDA-approved product (no record in Drugs@FDA or DailyMed) and no EMA authorisation located.
Clinical stage
Phase 3 completed by partner Medix in Mexico (0.25 and 0.50 mg daily in obesity). A new drug application was filed with COFEPRIS; in February 2023 the COFEPRIS technical committee gave a favourable opinion, but marketing authorisation had not been granted as of the source page. ClinicalTrials.gov lists 13 registered studies (phases 1-2).
WADA
Not named on the WADA 2026 Prohibited List. Note that stimulants are prohibited in-competition under S6 as a class, so class capture cannot be ruled out from the named-substance list alone; no explicit WADA ruling on tesofensine was located.
UK
research_compound

In the UK, tesofensine is not approved for clinical use and is considered a research compound. It is not licensed for weight loss treatment.

Source ↗

Pharmacokinetics

Half-life
9.2 days
Tmax
8 h
Absorption
oral
Elimination
hepatic
Washout
60 days
Titration
Start 0.25mg increase to 0.5mg
Low-confidence pharmacokinetics
These figures are recorded as clinical rather than measured in a published PK study. Treat them as an order of magnitude. Anything downstream of them — accumulation, steady state, washout — inherits that uncertainty.

Dosing — what backs each figure

Tesofensine is an oral small molecule (not a peptide) with real phase 2 human dosing: 0.25-1.0 mg once daily for 24 weeks in obesity, with 0.5 mg once daily carried forward as the candidate dose. It is not approved by FDA, EMA or MHRA, so no labelled dose exists.

ClinicalApproved labelling or a published human trial
No established human dose
No approved label or completed human trial establishes a dosing regimen for this compound. Anything presented as a standard protocol for it — anywhere — is someone's convention rather than a finding.

Handling and storage

No compound-specific stability data exists
No approved product label exists anywhere, so there is no authoritative storage specification. Tesofensine is an orally dosed small molecule (tablet/capsule in trials), not a lyophilised peptide, so lyophilised/reconstituted storage categories do not apply. No compound-specific stability data located from a citable regulatory or peer-reviewed source. General peptide handling still applies — reconstitute gently, keep it cold, keep it dark — but any specific figure you see quoted for this compound elsewhere is someone's assumption, not a measurement.
→ Reconstitution walkthrough→ Reconstitution calculator

Safety

Commonly reported
  • ·Dry mouth
  • ·Insomnia
  • ·Increased heart rate
Rarely reported
  • ·Hypertensive crisis
  • ·Serotonin syndrome
Contraindications
  • ·Pregnancy
  • ·Breastfeeding
  • ·"Severe cardiovascular disease"
  • ·"Uncontrolled hypertension"
Drug interactions
  • ·Monoamine oxidase inhibitors (MAOIs) - risk of hypertensive crisis
  • ·Selective serotonin reuptake inhibitors (SSRIs) - risk of serotonin syndrome

Reported combinations

Reported as synergistic
  • ·Caffeine - may enhance energy expenditure
Reported as antagonistic
  • ·Antihypertensives - may counteract blood pressure effects

Combination claims in this dataset are largely unsourced and should be treated as folk knowledge until a citation appears beside them.

References (2)

Data provenance

Chemistry and citations on this page were checked against primary sources on 2026-08-14. Values that could not be verified were left blank rather than filled with a plausible guess.

Could not verify
storage.lyophilized, storage.reconstituted, storage.lightSensitive, reconstitution.solvent

Research use only
This profile is educational reference material. It is not medical advice, not a prescription, and not an endorsement of self-administration. Compounds discussed here are research chemicals and most are not approved for human therapeutic use.

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