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Vial labeled 'Retatrutide 10 mg' with batch number and expiration date on a neutral background
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Retatrutide 10mg vial

Retatrutide 10mg vial

€65,00 EUR
Impuestos incluidos.

NOT FOR HUMAN CONSUMPTIO

Retatrutide is a 39-amino-acid synthetic peptide engineered from the native GLP-1 backbone. Three design elements confer once-weekly dosing:

  • DPP-IV resistance – insertion of α-methyl residues (2-aminoisobutyric acid and 2-methyl-Leu).

  • Albumin binding – a C-20 fatty-diacid side-chain attached to Lys^20 via AEEA-γ-Glu linkers.

  • C-terminal amidation – stabilises the helix and reduces renal clearance.
    These modifications yield a terminal half-life of ~6 days and dose-proportional exposure from 0.75 mg to 12 mg once weekly.New England Journal of Medicine

2 | Triple-receptor pharmacology

Receptor Principal actions Contribution in retatrutide
GLP-1R Glucose-dependent insulin secretion, slowed gastric emptying, satiety Sustained glycaemic control and appetite suppression
GIPR Potentiates insulin; modulates adipose lipid handling Synergy with GLP-1 on weight loss, may mitigate GLP-1-driven nausea
GCGR Increases energy expenditure, lipolysis, thermogenesis Counters adaptive metabolic rate decline during dieting
Pre-clinical studies in rodents and non-human primates confirmed additive weight-loss and glycaemic effects when all three receptors are co-activated.PubMed

3 | Pharmacokinetics and pharmacodynamics

  • T max ≈ 24 h after subcutaneous administration.

  • Steady state in ~4 weeks with once-weekly dosing.

  • Immunogenicity < 2 % low-titre anti-drug antibodies with no effect on PK/PD.

  • Dose response: near-linear reductions in fasting glucose, body weight and liver fat across 1–12 mg.New England Journal of MedicinePubMed

4 | Clinical efficacy

4.1 Phase 1 multiple-ascending dose (T2D; n = 120)

HbA1c fell 1.6 percentage points and body weight 8 % over 12 weeks on 12 mg; GI events were mild and transient.

4.2 Phase 2 obesity without diabetes (NEJM 2023; n = 338)

  • 48-week, placebo-controlled trial; weekly 1, 4, 8, 12 mg.

  • Weight change at week 48: –24.2 % (12 mg), –22.8 % (8 mg) vs –2.1 % placebo — largest absolute reduction yet reported in any controlled trial.

  • 83 % on 12 mg achieved ≥ 20 % weight loss.

4.3 Phase 2 type 2 diabetes (Lancet 2023; n = 281)

  • 36-week, placebo and dulaglutide-controlled.

  • HbA1c ↓ 2.2 percentage points; weight ↓ 16 % on 12 mg.

  • 82 % reached HbA1c < 6.5 %; 31 % < 5.7 %

4.4 Liver-fat substudy (Nature Medicine 2024)

  • Participants with baseline liver fat ≥ 10 %.

  • Mean relative reduction −83 %; 86 % normalised to < 5 % by week 48.

  • 4.5 Cardiometabolic biomarkers

At 12 mg: triglycerides –40 %, apoC-III –38 %, LDL-C –16 %, systolic BP –9 mm Hg.

5 | Safety and tolerability

  • Gastro-intestinal: nausea (24–31 %), diarrhoea (16–23 %), vomiting (< 10 %), mostly during dose escalation.

  • Heart rate: resting HR ↑ 4–6 bpm, similar to semaglutide and tirzepatide.

  • Lean-mass loss: ≈ 25 % of total weight lost, in line with other incretin agents; resistance training advised.

  • No signal to date for pancreatitis, gall-bladder disease, medullary thyroid carcinoma, severe hypoglycaemia or suicidality; phase 3 trials include active surveillance.

6 | Phase 3 development (selected ongoing studies)

Identifier Population Comparator Size Primary end-point Estimated completion
NCT06086751 Obesity with high CV risk Placebo 3 100 % weight change at week 60 Q4 2026
NCT06859268 Obesity, weight-loss maintenance Active-controlled doses vs placebo 2 000 % weight regain prevention 2027
NCT06662383 Obesity, head-to-head Tirzepatide 10/15 mg 1 200 % weight change at week 72 2027
REDEFINE-NASH (pending) Biopsy-proven steatohepatitis Placebo 1 400 Histologic resolution 2028

Eli Lilly has indicated a possible first regulatory submission in late 2026 if outcomes replicate phase 2 efficacy and safety.

7 | Position within the obesity therapy landscape

Agent (weekly) Maximum mean weight loss Time-point Source trial
Semaglutide 2.4 mg –15 % 68 wk STEP-1
Tirzepatide 15 mg –21 % 72 wk SURMOUNT-1
Retatrutide 12 mg –24 % 48 wk (still trending downward) Phase 2 obesity
Open-label extension data suggest retatrutide may approach 25-27 % by week 72, creating an efficacy gap of ~3-4 % vs tirzepatide that is clinically meaningful for visceral-fat reduction and metabolic remission targets.

8 | Dosing, escalation and practical use

Week 1 mg arm 4 mg 8 mg 12 mg
0–4 1 mg 2 mg 2 mg 2 mg
5–8 1 mg 4 mg 4 mg 4 mg
9–12 1 mg 4 mg 8 mg 8 mg
13 → 1 mg 4 mg 8 mg 12 mg
Escalation can be slowed if GI intolerance emerges. Drug is supplied in single-use 0.5 mL pens (30-gauge) stable for 30 days after refrigeration is stopped. Rotate injection sites and separate from short-acting insulin sites.

9 | Future research directions

  1. Lean-mass preservation strategies (nutritional support, resistance exercise, adjunct anabolic agents).

  2. Bone health monitoring in long-term users, given potential GCGR-mediated bone-turnover acceleration.

  3. HFpEF – a phase 2 protocol is in design to test cardiorespiratory benefits.

  4. Combination therapy with SGLT2 inhibitors and orlistat.

  5. Adolescent obesity – paediatric plan filed; first enrolment anticipated late 2025.

10 | Conclusions

Retatrutide is the most potent pharmacologic anti-obesity agent yet tested, delivering unprecedented weight-loss, profound liver-fat clearance and broad cardiometabolic improvements with a tolerability profile resembling other incretin-based therapies. The balanced activation of GLP-1, GIP and glucagon receptors appears to overcome the plateau seen with single or dual agonists. Phase 3 results over 2025–2027 will determine whether these advantages translate into durable efficacy, acceptable safety in larger populations and cost-effectiveness sufficient to reshape clinical guidelines for obesity, type 2 diabetes and MASLD