Side-by-side · Research reference

HexarelinvsTesofensine

Side-by-side comparison across mechanism, dosage, evidence, side effects, administration, and stack synergies. Citations on every claim where available.

APhase 1Reviewed19/45 cited

BPhase 3Draft10/40 cited

Hexarelin

Hexapeptide GHRP · Cardio-tropic

100–200 mcgPer doseSmith 1996

Phase 1Evidence levelGhigo 1997

~70 minHalf-lifeSemenistaya 2010

SQ · Multiple sites · 1–3×/day

Tesofensine

SNDRI · Phase 3 obesity candidate

0.25–0.5 mgDaily doseAstrup 2008

9.2 kgWeight ↓ (24 wk)Astrup 2008

Phase 3Evidence levelAstrup 2008

Oral · Once daily morning

01Mechanism of Action

Parameter

Hexarelin

Tesofensine

Primary target

Ghrelin receptor (GHS-R1a) + cardiac CD36Smith 1996 Ghigo 1997

Serotonin / norepinephrine / dopamine transporters (SERT / NET / DAT)Astrup 2008

Pathway

GHS-R1a → Gαq → Ca²⁺ → GH release. CD36 engagement → direct cardio-tropic actionGhigo 1997

Triple monoamine reuptake inhibition → ↑synaptic 5-HT, NE, DA → appetite suppression + thermogenesisAstrup 2008

Downstream effect

Strong GH pulse + IGF-1 elevation; cardio-protective effects in animal MI modelsGhigo 1997

Strong appetite suppression, mild thermogenic effect, weight lossAstrup 2008

Feedback intact?

Yes initially; tachyphylaxis with chronic useGhigo 1997

—

Origin

Synthetic hexapeptide His-D-2-Methyl-Trp-Ala-Trp-D-Phe-Lys-NH₂Smith 1996

Small molecule developed by NeuroSearch (Denmark) for CNS indications, repurposed for obesityAstrup 2008

Antibody development

—

02Dosage Protocols

Parameter

Hexarelin

Tesofensine

Standard dose

100–200 mcg per injectionSmith 1996

0.25–0.5 mg / dayAstrup 2008

Frequency

1–2× per day max (tachyphylaxis with chronic 3× daily)

Once daily, morning

Lower / starter dose

50 mcg per dose

0.125 mg / day

Evidence basis

Phase 1 / Phase 2 trialsSmith 1996 Ghigo 1997

Phase 2b + ongoing Phase 3Astrup 2008

Duration

4–8 weeks on / 4–8 weeks off (tachyphylaxis mitigation)

24 weeks per studied cycle

Reconstitution

Bacteriostatic water

—

Timing

Pre-sleep + fasted preferred

Morning to avoid sleep disruption

Half-life

~70 minSemenistaya 2010

~9 days (very long)

Form

—

Oral capsule

04Side Effects & Safety

Parameter

Hexarelin

Tesofensine

Cortisol elevation

Modest at high dosesGhigo 1997

—

Prolactin elevation

Modest at high dosesGhigo 1997

—

Hunger

Strong appetite increase via ghrelin agonism

—

Tachyphylaxis

Receptor desensitisation with chronic dosingGhigo 1997

—

Cardiac effects

Direct cardio-tropic; potential benefit in MI but unstudied in humansGhigo 1997

—

IGF-1 elevation

Strong; monitor with chronic high-dose use

—

Cancer risk

Contraindicated in active malignancy (GH/IGF-1 axis)

—

Pregnancy / OB

Avoid

Contraindicated

Heart rate / BP

—

Dose-dependent ↑ HR + BPAstrup 2008

Insomnia

—

Dose-related; mitigate with morning timing

Dry mouth

—

Common

Nausea

—

Common

Mood changes

—

Anxiety / agitation possible

Cardiovascular events

—

Phase 3 trial monitoring; not yet FDA-cleared

Absolute Contraindications

Hexarelin

·Active malignancy
·Pregnancy / breastfeeding
·Disrupted hypothalamic-pituitary axis

Tesofensine

·Pregnancy / breastfeeding
·Severe cardiovascular disease
·Concurrent MAOI use

Relative Contraindications

Hexarelin

·Untreated diabetes
·Severe hyperprolactinemia

Tesofensine

·Hypertension
·Anxiety disorder
·Insomnia

05Administration Protocol

Parameter

Hexarelin

Tesofensine

1. Reconstitution

Add 2 mL bacteriostatic water to 5 mg vial → 2.5 mg/mL = 250 mcg per 0.1 mL.

Oral capsule (investigational; not commercial).

2. Injection site

SQ — abdomen or thigh. Rotate sites.

Swallow whole with water, morning only.

3. Timing

Pre-sleep + fasted preferred. Cycle on/off to avoid tachyphylaxis.

Morning to mitigate insomnia. Do not dose evening.

4. Storage

Lyophilised: room temp, light-protected. Reconstituted: refrigerate ≤30 days.

Room temp ≤25 °C, dry place.

5. Needle

29–31G, 4–8 mm insulin syringe.

Monitor BP + HR + mood. Avoid stimulants + MAOIs.

06Stack Synergy

Hexarelin

+ CJC-1295 (no DAC)

Strong

View CJC-1295 (no DAC) →

Hexarelin (GHRP) + CJC-1295-no-DAC (GHRH analogue) is the higher-amplitude variant of the standard GHRH+GHRP stack. Hexarelin produces a stronger pulse than ipamorelin but with cortisol + prolactin signal — choose this stack for maximum GH amplitude when side-effect tolerance is acceptable. Cycle aggressively.

Hexarelin: 100 mcg SQ · pre-sleep
CJC-1295 (no DAC): 100 mcg SQ · same injection
Primary benefit: Maximum GH pulse amplitude (with side-effect signal)

Smith 1996 Teichman 2006

Tesofensine

— no documented stacks