Tesofensine

Areas of active research — not promised effects

Each tag links to other compounds with research into that goal. Research use only: these are areas of study, not human-use claims.

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Tesofensine is not FDA-approved for any indication in the United States. It is classified as an Investigational New Drug (IND). It is not a DEA-scheduled controlled substance. The FDA granted Orphan Drug Designation for hypothalamic obesity. Tesofensine is a small molecule (not a peptide) and was not among the 19 peptides subject to the 2025–2026 FDA Category-2 restricted-compounding rulemaking (docket FDA-2025-N-6895; fda19=false). There is no 503A or 503B compounding authorization. Commercial supply for human use outside an authorized clinical trial is not permitted. Sale for documented in vitro or laboratory research purposes only.

Transparent blend · bci-1.0 · never paid-placement

Primary name

Tesofensine

Origin

Fully synthetic phenyltropane compound (CAS 195875-84-4; INN: tesofensine) originally developed by NeuroSearch A/S (Denmark) as a candidate for Parkinson's disease and Alzheimer's disease. Weight-loss activity was discovered incidentally during neurological trials. Development was subsequently taken over by Saniona A/S, which is pursuing it for obesity (standalone) and as Tesomet (tesofensine/metoprolol combination) for hypothalamic obesity and Prader-Willi syndrome. Tesofensine has received FDA Orphan Drug Designation for hypothalamic obesity.

Registry IDs

PubChem CID

11370864

CAS

195875-84-4

InChIKey

VCVWXKKWDOJNIT-ZOMKSWQUSA-N

DrugBank

DB06156

ChEMBL

CHEMBL3989690

Molecular formula

C17H23Cl2NO

Molar mass

328.3 g/mol

Monoisotopic

327.1156697 Da

InChIKey

VCVWXKKWDOJNIT-ZOMKSWQUSA-N

Appearance

White to off-white crystalline solid (small molecule, MW ~328.3 g/mol)

Solubility

Solubility characteristics typical of phenyltropane small molecules; soluble in …

Sequence not available in current seed.

Stability: As a phenyltropane small molecule, tesofensine is relatively stable as a solid. The ethoxymethyl and tertiary amine functionality may be susceptible to oxidatio

Vial sizes

null mg · null mg

Purity grades

≥98% HPLC / ≥99% HPLC

Salt forms

Free base (primary)

• GHS hazard class on file
• PPE & spill response
• Disposal guidance
• Not-for-human-consumption posture

How much research exists, and of what maturity — never a verdict on whether it works.

Mechanism of action

• Tesofensine inhibits the presynaptic reuptake transporters for dopamine (DAT), norepinephrine (NET), and serotonin (SERT) simultaneously, raising synaptic concentrations of all three monoamines
• In diet-induced obese rat models, appetite suppression is mediated primarily through indirect activation of postsynaptic alpha-1 adrenoceptors and dopamine D1 receptors in the hypothalamus (PMID 20144252 analog; mechanism described in published preclinical studies)
• Recent cryo-EM structural data (Nature Communications, 2025) show that tesofensine stabilizes the dopamine transporter in an outward-facing conformation, providing mechanistic insight into its high DAT affinity
• Enhanced monoaminergic tone reduces food intake and increases energy expenditure, producing sustained negative energy balance in preclinical and clinical models

Pharmacokinetics (ADME)

Half-life

~9 days (parent compound, ~220 hours); active metabolite NS2360 (N-desmethyl-tesofensine) ~16 days (~374 hours) — from human PK modelling in Alzheimer's patients (PMID 17324246)

Clearance

Total body clearance after oral administration estimated at 30–40 mL/min (low clearance); protein binding ~91%

PK–PD note: Oral bioavailability is >90%; food does not significantly affect absorption. Tesofensine is metabolized predominantly by CYP3A4 to the pharmacologically active N-desmethyl metabolite NS2360, which acc…

Reading the evidence

• Evidence quality and gaps vary by application — see the cited grades above.
• Indexed-article counts span all evidence tiers, not only completed human trials.
• No first-party human-dosing, efficacy, or benefit claims are made here.

Key reviews & evidence-gap sources

• Doggrell SA. Tesofensine--a novel potent weight loss medicine. Expert Opin Investig Drugs. 2009;18(7):1043-6 (evaluation of Astrup/Lancet 2008 RCT) — Anchoring expert commentary on the pivotal Phase IIB Lancet RCT.
• ScienceDirect Topics overview: Tesofensine (triple monoamine reuptake inhibitor; PWS Phase 2b data; cardiovascular risk-benefit context) — Aggregator topic overview, not a peer-reviewed systematic review.
• Wikipedia: Tesofensine (history, pharmacology, clinical trials summary) — Tertiary aggregator; useful for cross-check of trial timeline and IC50 values.

5 registered trials — 0 currently recruiting.

Phase 2
NCT03149445
Co-administration of Tesofensine/Metoprolol in Subjects With Prader-Willi Syndrome (PWS)

COMPLETED

Phase 2
NCT00148512
A Randomized, Double-blind, Placebo-controlled, Five Parallel Groups Efficacy and Safety Study of NS 2330 (Tesofensine) (0.125 mg, 0.25 mg, 0.5 mg and 1.0 mg) Administered Orally Once Daily Over 14 Weeks in Levodopa Treated Parkinson Patients With Motor Fluctuations

COMPLETED

Phase 2
NCT00153010
An Evaluation of Three Doses of NS 2330 in Patients With Mild to Moderate Dementia of the Alzheimer's Type

COMPLETED

Phase 2
NCT03845075
48 Weeks, Study to Evaluate Overall Safety and Tolerability of Co-administration of Tesofensine and Metoprolol in Subjects With Hypothalamic Injury-induced Obesity (HIO)

COMPLETED

Phase 1
NCT03286829
Study to Investigate the Pharmacokinetic Profile

COMPLETED

Summary (literature)

The most consistent adverse effects across Phase 2 trials are cardiovascular: heart rate increases of 7–10 bpm and systolic blood pressure increases of 3–5 mmHg at the 0.5 mg/day dose. Non-cardiovascular adverse effects include dry mouth, nausea, insomnia, headache, diarrhea, and…

WADA status

Prohibited — WADA 2025 Prohibited List, S6.b Specified Stimulants (in-competition). Tesofensine was added as an explicit example of a specified stimulant effect…

Dominant research route: Oral (PO)

Phase I, II, and III clinical trials in healthy volunteers and patients (obesity, Alzheimer's, Parkinson's); population PK model from 320 subjects with multiple oral dosing

Bioavailability: Absolute bioavailability estimated >90% by cross-study comparison of separate oral and intravenous studies; relative bioavailability not significantly affected by food intake

Dominant route across all clinical development programs; oral tablet formulation used in TIPO-1 Phase IIb and subsequent Phase III obesity trials

Single rising-dose IV infusion study in 21 healthy subjects (0.3, 0.6, 0.9, 1.2 mg over 6 hours); IV infusion up to 1.2 mg in volunteers in Phase 1 studies

Bioavailability: IV data used as reference for absolute bioavailability estimation; after IV administration, high volume of distribution ~600 L and low oral clearance 30-40 mL/min reported

IV route studied solely for pharmacokinetic characterization and bioavailability determination, not for therapeutic use; no commercial IV formulation

Subcutaneous administration in mice (subcutaneous catheter) and rats (2 mg/kg injected subcutaneously for 15 consecutive days) in preclinical obesity mechanism studies

Bioavailability: No human SC bioavailability data; SC route used only in preclinical animal models for mechanistic and weight-loss studies

SC route employed in rodent pharmacology studies investigating hypothalamic GABAergic neuron silencing and weight-loss mechanisms; not studied in humans

Animal & human figures are kept visibly separate so studied animal doses are never misread as human guidance.

Sorted A–Z by vendor — never by price

Weekly median $/mg from the live vendor crawl.

Researched storefront prices, bucketed

p25 $2.40 · median $2.80 · p75 $4.00 · 7 researched vendors

Legit, COA-backed band: $2.30–$4.00/mg.

Value rule: don't just buy the cheapest — a price under $3/mg is a red flag. Pair price with COA and independent-test grade.

Estimated cost of research (10 mg)

Vial (best researched price)

$23

Bacteriostatic water (generic estimate)

$6

Syringes / supplies (generic estimate)

$12

What each test proves — general guidance, plus this compound's researched purity data

Independent labs cited for this compound

No FDA recalls, warning letters, or seizure actions specifically naming tesofensine were found in the sources retrieved; tesofensine has no US-approved product to recall. None found.

Buyer red-flag checklist

• No FDA-approved tesofensine product exists in the US; any US retail 'tesofensine' is an unapproved new drug and misbranded under the FD&C Act
• Sold through 'research chemical'/'not for human consumption' channels with weight-loss claims
• Cardiovascular safety signal (blood pressure and heart rate elevations) blocked US development
• Lancet Expression of Concern (2013, unresolved) on the pivotal Phase II trial for adverse-event under-reporting
• WADA Prohibited List S6 specified stimulant (2025) — doping-positive risk for tested athletes
• Mexican-approved Tesomet/Nupenta product accessible only under Mexican regulatory authority; gray-market US import carries legal and quality risk
• Suppliers may lack batch-specific CoAs from independent HPLC/GC-MS labs

GMP vs research-grade: the chemistry (SPPS + HPLC + MS) is identical — the difference is the quality system.

Underdosing / mislabeling: No independent lab-test aggregates (Janoshik/MZ Biolabs/Finnrick) reporting tesofensine underdosing prevalence were located. Janoshik lists a tesofensine analysis service but notes it is not a peptide and therefore will not have peptide purity measured; no public tesofensine batch results were retrieved.

• FDA Import Alert 66-41 'Detention Without Physical Examination of Unapproved New Drugs Promoted In The U.S.' is the general DWPE alert covering unapproved new drugs; tesofensine (an unapproved new drug in the US with no approved NDA) falls within this general framework, though it is not specifically named on the retrieved Red List.66-41
• An RUO label is not an import exemption — CBP judges actual intended use.
• Lyophilized powder is ambient-stable in transit; temperature control needed for > 7-day transit.
• US-warehouse vendors dodge import scrutiny — they cost more but ship more reliably.

Every item dated & sourced

Prohibited — listed as an example under S6. Stimulants on the WADA Prohibited List (2025 and 2026 editions, in force 1 Jan 2025 and 1 Jan 2026 respectively).

No granted patents identified in current seed. Composition-of-matter coverage is limited given the peptide's synthetic origin.

• IACUC / IRB research context
• RUO buyer responsibilities & documentation
• Veterinary / alternative-use where lawful
• Jurisdiction-aware "who may lawfully obtain"

What people discuss

Reported concerns — discussion, not established effects

Reading caveats

• self-selection bias (posters self-experiment with grey-market compound)
• unverified sourcing (research-chemical / no-prescription supply)
• self-reported outcomes without blinding or control
• survivorship bias toward strong responders posting
• possible placebo / mislabeled-product confounding

Manually researched from reddit, youtube— theme weights are research estimates, not live counts; aggregated & de-identified. No individual posts, quotes, or usernames are ever shown.

Relative research / market volume — populated once the activity stream is wired

Inline tooltips for lyophilized, RUO, EU/mg, SPPS, 503A and more.

Toggle plain-language ↔ scientific in the header.

• How to read a COA
• Free base vs acetate
• Understanding evidence grades

Oral triple monoamine reuptake inhibitor in Phase 3 investigation for obesity; not FDA-approved; WADA S6 specified stimulant from 2025. Approximately 55 articles are indexed (literature last scanned 2026-05-29). US regulatory status: Investigational New Drug — not FDA-approved; no compounding authorization. Research use only.

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