Product
Eloralintide

roduct Information:

CAS NO.: 2883634-40-8

Molecular Formula: C210H319N49O65S2

Molecular Weight: 4526.10

EINECS:/

Appearance: White or White-off Powder

Purity≥98% by HPLC.

Solubility

Soluble in DMSO at 100 mg/ ml, with ultrasonication. DMSO is hygroscopic and that has an impact in product solubility. We recommend using a freshly opened bottle of DMSO. 

 

Eloralintide

Efficacy and Function:

 

(I) Core Pharmacological Effects

As a highly selective amylin receptor agonist, Eloralintide preferentially activates the human amylin receptor 1 (AMY1R). Its activation potency for AMY1R is 12-fold that of the calcitonin receptor (CTR) and 11-fold that of the amylin receptor 3 (AMY3R), respectively. In rats, it exhibits superior activation efficacy for both AMY1R and AMY3R compared to CTR. Its mechanism of action is synergistic with endogenous amylin, exerting effects through dual central and peripheral regulation: at the central level, it acts on the nucleus tractus solitarius of the brainstem to transmit satiety signals, thereby reducing food intake; at the peripheral level, it delays gastric emptying and inhibits excessive postprandial glucagon secretion, synergistically regulating metabolism.

(II) Clinical Therapeutic Effects

1. Weight Loss Efficacy

Phase II clinical data demonstrate that its weight loss effect is significantly dose-dependent. During the 48-week treatment period, the weight loss rates in the 1mg, 3mg, 6mg, and 9mg dose groups reached 9.5%, 12.4%, 17.6%, and 20.1%, respectively, which were far superior to the 0.4% in the placebo group. Moreover, it mainly reduces fat mass. In Phase I clinical trials, the high-dose group achieved a weight loss of 11.3% within 12 weeks, showing stable and durable efficacy. A Phase III clinical trial (ENLIGHTEN-1) has been initiated to further verify its long-term weight loss efficacy in obese/overweight populations.

2. Metabolic Improvement

In addition to weight loss, it can improve multiple cardiovascular risk factors such as waist circumference, blood pressure, blood lipids, glycemic control, and inflammatory markers. It exerts a positive regulatory effect on indicators related to metabolic disorders, making it suitable for obese or overweight individuals with comorbid metabolic abnormalities.

3. Medication Advantages

It is administered subcutaneously once a week and can be used safely without dose titration, offering high medication convenience and patient compliance. Compared with non-selective amylin receptor agonists (e.g., cagrilintide), it has a lower incidence of gastrointestinal adverse reactions, and the incidence of serious risks such as hypoglycemia and acute kidney injury is extremely low, showing good tolerability.

(III) Potential Application Directions

Currently, in addition to monotherapy for obesity/overweight, a Phase II clinical study is underway to evaluate its efficacy in combination with tirzepatide, a GLP-1/GIP dual agonist. This study explores a combined weight loss regimen of "central satiety signal + multi-incretin synergy," which is expected to provide a new option for populations pursuing higher weight loss goals. Meanwhile, its potential in weight management for patients with type 2 diabetes mellitus complicated by obesity is also being explored.

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