Weight Loss + Appetite Control
Tesofensine
A triple monoamine reuptake inhibitor capsule suppressing appetite, increasing resting energy expenditure, and reducing cravings for high-calorie foods through simultaneous dopamine, serotonin, and noradrenaline modulation.
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Overview
Tesofensine
Tesofensine is a presynaptic triple reuptake inhibitor originally investigated for Parkinson's disease and Alzheimer's disease. While showing limited efficacy for those neurological indications, trial participants who were overweight consistently achieved significant weight loss, prompting its clinical redevelopment as a weight loss agent. It acts primarily as an appetite suppressant while simultaneously increasing fat oxidation and resting energy expenditure through central monoaminergic mechanisms. Phase 2 clinical data demonstrated weight loss exceeding that of other available pharmacological options over a six-month period.
Mechanism of Action
Tesofensine inhibits the presynaptic reuptake transporters for serotonin (SERT), noradrenaline (NET), and dopamine (DAT) simultaneously, increasing synaptic concentrations of all three monoamines in the hypothalamus and reward-related brain regions. Elevated hypothalamic noradrenaline and serotonin suppress appetite via the arcuate and paraventricular nuclei, reducing total caloric intake and meal size. Dopamine reuptake inhibition in mesolimbic circuits reduces hedonic cravings for sweet, fatty, and salty foods by normalizing the reward salience of high-calorie stimuli. Noradrenaline reuptake inhibition also activates beta-3 adrenergic receptors in adipose tissue, increasing resting energy expenditure and fat oxidation beyond the caloric deficit achieved through appetite suppression alone. In Phase 2 trials, patients achieved an average weight loss of 12.8 kg at 1 mg, 11.3 kg at 0.5 mg, and 6.7 kg at 0.25 mg over six months.
Oral
Capsule taken orally. No injection required.
Information presented here is for educational purposes only and not intended to replace or substitute guidance from a healthcare provider. Compounded medications are not FDA-approved nor evaluated by the FDA for safety, efficacy, or quality.
Benefits
Appetite Suppression
Increases hypothalamic serotonin and noradrenaline to reduce hunger signaling, meal size expectations, and total daily caloric intake.
Craving Reduction
Dopamine reuptake inhibition in mesolimbic reward circuits reduces desire for sweet, fatty, and salty foods by normalizing reward salience of high-calorie stimuli.
Energy Expenditure
Noradrenaline-driven beta-3 adrenergic activation in adipose tissue increases resting metabolic rate and fat oxidation independent of caloric restriction.
Quality of Life
Phase 2 data showed improvement across physical function, self-esteem, sexual life, public distress, and work performance domains alongside weight reduction.
Individual results may vary. Benefits described are based on clinical and pharmacological evidence and do not constitute a guarantee of treatment outcomes. All treatment requires evaluation and approval by a licensed provider.
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FAQs
What is Tesofensine?
Tesofensine is a prescription therapy used for weight management support.
Who should use Tesofensine?
Patients seeking support for weight management support may qualify after evaluation by a licensed provider.
Does Tesofensine Capsules require a prescription?
Yes. Tesofensine is a compounded prescription medication requiring a valid prescription from a licensed provider. Available in 250 mcg, 500 mcg, and 1000 mcg capsules.
What are the possible side effects?
The most commonly reported effects are dry mouth, nausea, constipation, insomnia, and elevated heart rate, consistent with triple monoamine reuptake inhibition. Mood changes and irritability may occur. Blood pressure and heart rate monitoring is recommended during treatment, particularly at initiation and dose titration.
Who should not use Tesofensine Capsules?
Not for patients with uncontrolled hypertension, cardiovascular disease, cardiac arrhythmias, or a history of stroke. Not for patients with a history of psychiatric disorders including bipolar disorder or psychosis without specialist evaluation. Contraindicated with MAOIs or within 14 days of MAOI discontinuation. Not recommended during pregnancy or breastfeeding.
Are there any drug interactions?
Contraindicated with MAOIs due to risk of serotonin syndrome. Concurrent use with other serotonergic agents including SSRIs, SNRIs, and triptans increases serotonin syndrome risk and requires provider evaluation. May potentiate stimulants and sympathomimetics. Patients on antihypertensives require blood pressure monitoring given noradrenergic activity.
Is Tesofensine Capsules safe if I have a pre-existing medical condition?
Patients with cardiovascular disease, hypertension, arrhythmias, psychiatric conditions, or hepatic impairment require individualized provider evaluation before starting. Periodic blood pressure, heart rate, and mood monitoring is recommended throughout treatment. Not appropriate for patients with a history of substance use disorder given dopaminergic activity.
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The information and clinical services described on this website are for educational and informational purposes only and are not intended to diagnose, treat, cure, or prevent any disease. All treatments require evaluation and approval by a licensed healthcare provider through a telemedicine consultation. Treatment approval is not guaranteed. Individual results may vary, and treatments may carry risks and side effects. Certain compounded medications, wellness treatments, or off-label uses may not be evaluated by the U.S. Food and Drug Administration (FDA) for safety, effectiveness, or quality unless explicitly stated. Testosterone Shots provides telehealth consultations, clinical review, care coordination, lab-related services, membership services, and ongoing treatment management. Testosterone Shots is not a pharmacy and does not manufacture, compound, dispense, sell, handle, warehouse, ship, or collect payment for prescription medication. Testosterone Shots collects payment only for consultations, clinical review, care coordination, lab-related services, membership services, and other non-pharmacy services. If treatment is approved, your prescription may be sent to a licensed pharmacy partner. The pharmacy contacts you directly to complete medication payment and shipping. Services are provided by licensed physicians, nurse practitioners, and/or other licensed healthcare providers in states where they are authorized to practice. This service is not intended for medical emergencies. If you are experiencing an emergency, call 911 or seek immediate medical care. We take reasonable measures to protect personal health information in accordance with applicable privacy laws, including HIPAA. By using this website or its services, you agree to our Terms of Service, Privacy Policy, Notice of Privacy Practices, Telehealth Consent, and Important Safety Information. You must be 18 years of age or older to use this service.