Fotagliptin Benzoate API is a synthetic small-molecule dipeptidyl peptidase-4 (DPP-4) inhibitor belonging to the gliptin class of antidiabetic compounds. It is also known by the development code SAL067 or FCN-005. Fotagliptin is designed as a long-acting, orally active DPP-4 inhibitor for the management of type 2 diabetes mellitus (T2DM).
Fotagliptin inhibits the DPP-4 enzyme, which normally degrades the incretin hormones GLP-1 and GIP. Inhibition of DPP-4 increases the activity of these endogenous incretin hormones, supporting glucose-dependent insulin secretion and reducing glucagon secretion. This mechanism contributes to improved glycemic control in patients with type 2 diabetes.
The pharmaceutical substance Fotagliptin Benzoate consists of the fotagliptin molecule associated with benzoic acid. It has the molecular formula C₂₄H₂₅FN₆O₃ and molecular weight 464.49 g/mol. The reported CAS Registry Number is 1403496-40-1.
| Property | Value |
|---|---|
| API Name | Fotagliptin Benzoate |
| Synonyms | SAL067, FCN-005, SAL-067 |
| CAS Number | 1403496-40-1 |
| Molecular Formula | C₂₄H₂₅FN₆O₃ |
| Molecular Weight | 464.49 g/mol |
| API Class | DPP-4 Inhibitor |
| Therapeutic Area | Type 2 Diabetes Mellitus |
| Salt Form | Benzoate |
| Appearance | White to off-white solid |
The identity and physicochemical data are independently reported by multiple chemical databases and research suppliers.
Fotagliptin is a selective DPP-4 inhibitor. DPP-4 is an enzyme responsible for the rapid degradation of incretin hormones such as GLP-1 and GIP.
By inhibiting DPP-4:
Fotagliptin has demonstrated potent DPP-4 inhibition, with an experimentally reported IC₅₀ of approximately 2.27 nM in the cited research-product literature.
Fotagliptin has undergone clinical development for type 2 diabetes mellitus. A randomized phase 3 study evaluated fotagliptin monotherapy against alogliptin and placebo in patients with uncontrolled T2DM. After 24 weeks, HbA1c decreased by approximately 0.70% from baseline in the fotagliptin group, compared with 0.26% with placebo.
A subsequent phase 3 study evaluated fotagliptin as an add-on to metformin. At 24 weeks, the least-squares mean HbA1c change was −0.81% with fotagliptin versus −0.28% with placebo, demonstrating improved glycemic control in the studied population.
Fotagliptin was approved in China in June 2024 for the management of type 2 diabetes mellitus.
Fotagliptin is a once-daily, orally bioavailable DPP-4 inhibitor. Clinical pharmacology research involving fotagliptin benzoate demonstrated rapid absorption, with a reported median time to maximum plasma concentration of approximately 1.5 hours. Pharmacodynamic evaluation showed sustained DPP-4 inhibition over the dosing interval.
Its pharmacological profile makes Fotagliptin Benzoate relevant to pharmaceutical development programs focused on oral antidiabetic therapies.
Fotagliptin Benzoate can be used as an active pharmaceutical substance for:
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | ≥99.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.5% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 5.0 – 7.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |