Tesofensine Capsules 500mcg 30ct by Omnix Peptides — research-grade capsules

Tesofensine Capsules 500mcg

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Tesofensine (NS2330) is a centrally acting triple monoamine reuptake inhibitor that blocks the presynaptic reuptake of dopamine, norepinephrine, and serotonin.

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Research goals: Metabolic & Weight

Description

Tesofensine (NS2330) is a centrally acting triple monoamine reuptake inhibitor that blocks the presynaptic reuptake of dopamine, norepinephrine, and serotonin. Originally developed by NeuroSearch (now licensed to Saniona) for Alzheimer’s and Parkinson’s disease, tesofensine was repurposed for obesity after substantial weight loss was consistently observed in early CNS trials. It has been studied in human Phase 2 randomized controlled trials and in Phase 3 registrational trials in Mexico, with regulatory submission to COFEPRIS receiving a favorable technical opinion in 2023.

The strongest peer-reviewed human finding comes from the Astrup et al. Phase 2 RCT in The Lancet: at 24 weeks, tesofensine 0.5 mg produced a mean diet-adjusted weight loss of 9.2%, and at 1.0 mg a loss of 10.6%, compared with 2.0% for diet plus placebo (p<0.0001).1

Important Note on the Evidence Base

Tesofensine has a well-developed Phase 2 evidence base in peer-reviewed Western journals (The Lancet, Obesity, International Journal of Obesity), but the Phase 3 registrational trial conducted by Medix in Mexico was reported only via press release and regulatory filing, not peer-reviewed publication. Additionally, the original 2008 Astrup et al. Lancet paper was the subject of an Expression of Concern issued by the journal in 2013 (Lancet 2013;381(9873):1167) relating to investigator conduct; the underlying efficacy data were not retracted, but the notice should be considered when interpreting the trial. Tesofensine is not approved by the FDA or EMA. Most published mechanism-of-action work is preclinical (rat models). All limitations are disclosed below alongside the findings.

Published Research on Tesofensine

Phase 2 Obesity Randomized Controlled Trial — Astrup et al., The Lancet (2008)

This double-blind, placebo-controlled trial enrolled 203 adults with obesity across five Danish obesity management centers, randomizing them to placebo or tesofensine 0.25, 0.5, or 1.0 mg once daily for 24 weeks. Mean diet-adjusted weight loss was 4.5%, 9.2%, and 10.6% across the escalating-amount arms, respectively, all significantly greater than placebo. The authors concluded that tesofensine 0.5 mg has the potential to produce a weight loss twice that of currently approved drugs. The most common adverse events were dry mouth, nausea, constipation, hard stools, diarrhea, and insomnia. The 0.5 mg amount increased mean heart rate by 7.4 bpm without significant change in blood pressure; the 1.0 mg amount produced larger heart rate increases.1

Pooled Analysis in Parkinson’s and Alzheimer’s Disease — Astrup et al., Obesity (2008)

This meta-analysis of four randomized double-blind multicenter trials originally designed for Parkinson’s or Alzheimer’s disease pooled 740 tesofensine-treated and 228 placebo-treated participants, all administered once daily for 14 weeks without weight loss counseling. Adjusted mean weight change ranged from −0.5% at 0.125 mg to −2.8% at 1.0 mg versus +0.5% on placebo. In the obese subgroup, the highest amount produced a placebo-subtracted weight loss of 3.5% and increased the proportion of patients achieving ≥5% weight loss from 2% to 32% — the original observation that prompted the obesity development program.2

Energy Metabolism and Appetite — Sjödin et al., International Journal of Obesity (2010)

This study used whole-room indirect calorimetry to measure 24-hour energy expenditure, fat oxidation, and spontaneous physical activity in overweight and moderately obese men before and after tesofensine treatment. The findings indicated that tesofensine’s weight loss effect is driven both by appetite suppression and by a modest preservation or increase in 24-hour energy expenditure, distinguishing it from purely anorectic agents.3

Mechanism of Action in Diet-Induced Obese Rats — Hansen et al., European Journal of Pharmacology (2010)

This animal study compared tesofensine, sibutramine, and rimonabant in diet-induced obese rats. Tesofensine produced sustained weight loss and improved glycemic control across a 16-day administration protocol, with the hypophagic effect substantially blocked by α1-adrenergic and dopamine D1 receptor antagonists — implicating indirect activation of those pathways as the primary mechanism of appetite suppression rather than direct serotonergic effects.4

About the Compound

Tesofensine is a phenyltropane-class small molecule with intrinsic inhibitory activity on the dopamine, norepinephrine, and serotonin transporters (DAT, NET, SERT), with reported transporter inhibition IC50 values in the low single-digit nanomolar range. Positron emission tomography studies in humans have shown concentration-dependent DAT occupancy at oral amounts of 0.125–1.0 mg. Its weight-loss effect appears to combine appetite suppression (mediated indirectly through α1-adrenergic and dopamine D1 receptor pathways) with sustained energy expenditure. Pharmacokinetics are characterized by a long terminal half-life (approximately 9 days), making once-daily administration practical without titration after a brief lead-in.

  • Compound class: small-molecule triple monoamine reuptake inhibitor (DAT/NET/SERT); phenyltropane derivative
  • Mechanism: presynaptic blockade of dopamine, norepinephrine, and serotonin reuptake; centrally-acting appetite suppression and energy expenditure modulation
  • Synonyms: NS2330, NS-2330
  • CAS Number: 195875-84-4 (free base)
  • Molecular Formula: C17H23Cl2NO
  • Molecular Weight: 328.27 g/mol
  • Originator: NeuroSearch A/S; licensed to Saniona AB; Mexico/Argentina commercial rights with Productos Medix
  • Administration: once daily, oral
  • Phase 3 status: Medix registrational trial completed (Mexico, 372 patients, 24 weeks)
  • Regulatory status: not approved by the FDA or EMA. Mexico — COFEPRIS technical committee favorable opinion (2023). Phase 3 registrational data not yet peer-reviewed
  • Common adverse events: dry mouth, insomnia, constipation, headache, increased heart rate

Product Specifications

  • Format: capsules
  • Strength: 500 mcg per capsule
  • Count: 30 capsules per bottle
  • Purity: ≥99% (HPLC verified)
  • Container: sealed amber bottle
  • Certificate of Analysis: lot-specific COA available

See the FDA Disclosure, Storage Instructions, and RUO tabs for handling, storage, and regulatory information.

References

  1. Astrup A, Madsbad S, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet. 2008;372(9653):1906-1913. doi:10.1016/S0140-6736(08)61525-1 (See Expression of Concern: Lancet. 2013;381(9873):1167.)
  2. Astrup A, Meier DH, Mikkelsen BO, Villumsen JS, Larsen TM. Weight loss produced by tesofensine in patients with Parkinson’s or Alzheimer’s disease. Obesity (Silver Spring). 2008;16(6):1363-1369. doi:10.1038/oby.2008.56
  3. Sjödin A, Gasteyger C, Nielsen AL, et al. The effect of the triple monoamine reuptake inhibitor tesofensine on energy metabolism and appetite in overweight and moderately obese men. Int J Obes (Lond). 2010;34(11):1634-1643. doi:10.1038/ijo.2010.87
  4. Hansen HH, Hansen G, Tang-Christensen M, et al. The novel triple monoamine reuptake inhibitor tesofensine induces sustained weight loss and improves glycemic control in the diet-induced obese rat: comparison to sibutramine and rimonabant. Eur J Pharmacol. 2010;636(1-3):88-95. doi:10.1016/j.ejphar.2010.03.026

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For research use only. Not for human consumption.