Prusogliptin, also known as DBPR-108, is an orally bioavailable dipeptidyl peptidase-4 (DPP-4) inhibitor developed for the treatment of type 2 diabetes mellitus. It is a small-molecule antidiabetic pharmaceutical API with selective inhibitory activity against DPP-4.
Prusogliptin has the molecular formula C₁₆H₂₅FN₄O₂ and a molecular weight of 324.3937 g/mol. The compound has two defined stereocenters with absolute stereochemistry.
Prusogliptin tablets received marketing approval from China's National Medical Products Administration (NMPA) in 2025 for improving glycemic control in adults with type 2 diabetes.
Prusogliptin belongs to the DPP-4 inhibitor class of oral antihyperglycemic agents. It is designed to inhibit the enzyme dipeptidyl peptidase-4, an important regulator of incretin hormone activity.
Prusogliptin selectively inhibits DPP-4. DPP-4 inhibition reduces the enzymatic degradation of incretin hormones, including GLP-1 and GIP. Increased incretin activity supports glucose-dependent insulin secretion and contributes to improved glycemic control.
Prusogliptin has been described as a potent and selective DPP-4 inhibitor, with an IC₅₀ of approximately 15 nM in reported pharmacological studies.
Prusogliptin is used as an active pharmaceutical ingredient for development and manufacture of oral antidiabetic formulations.
Its principal pharmaceutical application is the treatment of type 2 diabetes mellitus (T2DM). China NMPA approved Prusogliptin tablets for improving blood glucose control in adult patients with type 2 diabetes.
Clinical development has included once-daily oral doses of 50 mg, 100 mg, and 200 mg in pharmacokinetic/pharmacodynamic studies.
Prusogliptin is a defined stereochemical small molecule with molecular weight 324.3937 g/mol. IUPHAR/BPS reports:
A universal melting point, water solubility value, or API-grade appearance specification was not identified from the authoritative sources reviewed. These should therefore be controlled according to the applicable registered API specification rather than assigned an unsupported numerical value.
Prusogliptin API can be characterized using a combination of:
The analytical package should demonstrate identity, assay, purity, stereochemical integrity and control of process-related impurities.
Prusogliptin API quality control should include:
Because Prusogliptin does not have a publicly verified universal USP/Ph. Eur. API monograph in the sources reviewed, specific assay and impurity acceptance limits should be taken from the applicable approved/registered API specification rather than presenting unsupported limits as universal standards.
API manufacturing and quality systems should follow applicable GMP principles for active pharmaceutical ingredients. FDA's ICH Q7 guidance provides GMP guidance specifically for API manufacturing.
Prusogliptin possesses two defined stereocenters out of two, with absolute stereochemistry. The registered chemical identity corresponds to the (2S,4S) configuration.
Stereochemical integrity is therefore an important quality attribute for Prusogliptin API, and suitable chiral or stereospecific analytical controls should be applied where required by the registered specification.
Storage conditions should be based on the validated stability data and approved API specification for the particular manufactured material.
General handling practices include:
Typical documentation for Prusogliptin API may include:
Prusogliptin API manufacturing requires controlled synthesis, purification, drying and analytical testing, with particular attention to stereochemical integrity and impurity control.
The finished API should comply with its approved or customer-specific specification for identity, assay, related substances, residual solvents, stereochemical purity and other applicable critical quality attributes.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 0.5% |