Eloralintide (LY-3841136) is a novel long-acting amylin receptor agonist used to treat obesity/overweight.

Eloralintide (LY-3841136) is a novel, long-acting, selective islet amyloid receptor agonist currently in clinical development for the treatment of obesity. Its core strategy involves activating amylin receptors to mimic the satiety and appetite-suppressing effects of natural hormones, while selectively reducing activation of calcitonin receptors (CTRs) to improve gastrointestinal tolerance.

Basic Drug Properties

Key Identification: Eloralintide (USAN name), research code LY-3841136. Its UNII registration number is 73G3354J8W.

Molecular Characteristics: It is an engineered 37-amino acid peptide analog.

Structural Modifications: To enhance stability and achieve long-lasting action, its polypeptide chain underwent several specific modifications, including replacing the natural disulfide bond with a chemically more chemically stable methylthioacet**bridge, and attaching a C20 fatty acid diacid moiety to the 26th lysine residue, enabling it to bind to albumin and support once-weekly dosing.

Mechanism of Action and Preclinical Data

Receptor Selectivity: Eloralintide exerts its effect by activating amylin receptors, particularly the AMY1R subtype. In vitro studies have shown that it is approximately 12 times more potent in activating human AMY1R than in activating the calcitonin receptor (CTR), achieving functional selectivity.

Weight Loss and Tolerability Advantages: In preclinical animal models, compared to the non-selective amylin analogue Cagrilintide, which has entered clinical trials, Eloralintide demonstrated superior gastrointestinal tolerability and less muscle loss while achieving comparable weight loss results. The weight loss primarily resulted from a reduction in fat mass.

Eloralintide (LY-3841136) is a novel long-acting amylin receptor agonist used to treat obesity/overweight.

. Core Functions (Pharmacological Actions)

1. Type of Action
Amylin receptor agonist
Main target: AMY1R (selective enhancement)

2. Main Physiological Functions

✔ Appetite control
Strongly enhances satiety
Reduces food intake (↓)

✔ Gastric emptying
Delays gastric emptying (↓)

✔ Weight loss
Primarily reduces fat mass loss

3. Clinical Efficacy (Key Data)

Phase 2:

👉 Approximately -20% weight loss at maximum dose (48 weeks)
Additional improvements:
Waistline reduction
Blood glucose improvement
Blood lipid improvement
Blood pressure reduction

Storage Conditions (Important)

1. Powder (lyophilized state)

-20°C: Stable for approximately 2–3 years

4°C: Stable for approximately 1–2 years (short-term)

Protect from light

Protect from moisture (critical)

👉 Recommendation:

Long-term storage requires freezing at -20°C