Calcium Salt Hydrate Form of Orforglipron | Oral GLP-1R Agonist for Glycemic Control & Weight Management CAS 3008544-96-2

Orforglipron hemicalcium hydrate  More Info

Orforglipron hemicalcium hydrate, also identified by its developmental codes LY3502970 hemicalcium hydrate or GLP-1 receptor agonist 1 hemicalcium hydrate, represents the hemicalcium salt hydrate form of the parent compound Orforglipron. This pharmaceutical salt form is specifically designed to optimize the physicochemical properties of the active pharmaceutical ingredient for oral administration. The compound has a molecular formula of C₄₈H₄₈F₂N₁₀O₅·½Ca·H₂O and a molecular weight of approximately 921.02 g/mol. As a non-peptide small molecule, it belongs to a novel class of oral glucagon-like peptide-1 receptor (GLP-1R) agonists that offer a potential alternative to peptide-based therapies.

The primary mechanism of action for orforglipron involves selective and potent agonism of the glucagon-like peptide-1 receptor, a class B G protein-coupled receptor that plays a central role in glucose homeostasis. Unlike endogenous GLP-1 or peptide-based agonists, orforglipron is a partial agonist that demonstrates biased signaling toward G protein activation over β-arrestin recruitment. High-resolution structural studies have revealed that the compound binds within a unique pocket in the upper helical bundle of the GLP-1R, interacting with the extracellular domain and multiple transmembrane helices. This distinctive binding mechanism creates a unique receptor conformation that explains its partial agonism and biased signaling profile, as well as its selectivity for primate-specific receptor isoforms through interaction with Trp33 of the extracellular domain.

Preclinical studies have demonstrated the therapeutic potential of orforglipron in metabolic disease models. In cynomolgus monkeys, oral administration of orforglipron hemicalcium hydrate at doses ranging from 0.05 to 1.35 mg/kg produced dose-dependent reductions in food intake, enhanced glucose-stimulated insulin secretion, and lowered blood glucose levels. Pharmacokinetic evaluations showed that peak plasma concentrations are achieved approximately 2 hours after oral administration, with plasma drug exposure increasing roughly proportionally to the administered dose, indicating linear and dose-dependent gastrointestinal absorption. The compound exhibited an elimination half-life of 10.4 to 12.4 hours in rats and 3.4 to 4.7 hours in cynomolgus monkeys, with oral bioavailability calculated at 33-43% and 21-28%, respectively—substantially higher than the 0.4-1% oral bioavailability reported for peptide-based GLP-1R agonists in humans.

The pharmacokinetic profile of orforglipron is particularly noteworthy in the context of its development as an oral therapeutic. Unlike peptide-based GLP-1 receptor agonists, which typically require complex formulation strategies (such as co-formulation with absorption enhancers) or administration to achieve clinically relevant exposure, orforglipron demonstrates favorable oral pharmacokinetics as a small molecule. This property is derived from its non-peptide structure, which allows it to withstand proteolytic degradation in the gastrointestinal tract and be absorbed intact. The favorable pharmacokinetic profile, combined with high potency and selectivity against other class B GPCRs, positions orforglipron for once-daily oral administration without restrictions on food or water intake—a significant potential advantage over existing injectable or specially formulated oral peptide therapies.

The safety profile of orforglipron hemicalcium hydrate for laboratory use is considered manageable, with the compound classified as not a hazardous substance or mixture under the Globally Harmonized System of classification and labeling. Standard handling precautions include storage at 4°C in dry, sealed conditions, with transport recommended via ice packs. For research applications, the compound is soluble in DMSO at concentrations up to 25 mg/mL, and products are typically available with purity specifications of 99.0% or higher. It is important to note that this compound is strictly designated for research use only and is not intended for human or veterinary therapeutic applications unless explicitly formulated and approved for such use. The compound is currently being investigated in Phase 3 clinical trials for the treatment of type 2 diabetes and weight management in adults with obesity or overweight, with additional studies exploring potential applications in obstructive sleep apnea and hypertension.

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