General Information

Linagliptin Impurities and Linagliptin

For evaluating the purity and safety of Linagliptin, an essential active pharmaceutical ingredient, Daicel Pharma offers a customized synthesis of Linagliptin impurity standards. These impurity standards include crucial compounds such as 8-Bromo-3-methyl-7-(2-butynyl)-xanthine, Linagliptin impurity E, Linagliptin Methyldimer, Linagliptin N-glucose impurity, Linagliptin Nitroso impurity’s internal STD, Linagliptin S-isomer, N-Acetyl Linagliptin, N-Boc Linagliptin, N-Carbamoyl Linagliptin, and N-Formyl Linagliptin. Additionally, Daicel Pharma provides worldwide delivery options for Linagliptin impurity standards.

Linagliptin [CAS: 668270-12-0], a potent dihydropurinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), is orally bioavailable and exhibits hypoglycemic activity. It treats type 2 diabetes in combination with diet and exercise alone or with other oral hypoglycemic agents.

Linagliptin: Use and Commercial Availability 

Linagliptin, marketed under Tradjenta, treats type 2 diabetes mellitus to improve glycemic control in adults. It acts as a monotherapy in patients inadequately controlled by diet and exercise alone and for whom metformin is unsuitable or contraindicated due to renal impairment.

Linagliptin Structure and Mechanism of Action

The chemical name of Linagliptin is 8-[(3R)-3-Amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione. Its chemical formula is C₂₅H₂₈N₈O_2, and its molecular weight is approximately 472.5 g/mol.

Linagliptin degrades the incretin hormone, glucagon-like peptide-1 (GLP-1). It stimulates insulin release in a glucose-dependent manner and decreases glucagon levels in circulation. 

Linagliptin Impurities and Synthesis 

Linagliptin impurities refer to unintended substances that may be present in Linagliptin formulations. They can originate from manufacturing¹, raw materials, or storage conditions. Their presence can potentially affect its purity, potency, and overall quality. Rigorous quality control measures by pharmaceutical manufacturers help ensure the safety and efficacy of the medication. These measures include thorough testing and analysis to identify and quantify impurities and strict adherence to regulatory guidelines and standards. By controlling impurity levels within acceptable limits, pharmaceutical companies strive to provide patients with high-quality Linagliptin formulations for treating type 2 diabetes mellitus, minimizing any potential risks associated with impurities.

Daicel Pharma strictly adheres to cGMP standards and operates an analytical facility for preparing Linagliptin impurity standards, which include 8-Bromo-3-methyl-7-(2-butynyl)-xanthine, Linagliptin impurity E, Linagliptin Methyldimer, Linagliptin N-glucose impurity, Linagliptin Nitroso impurity’s internal STD, Linagliptin S-isomer, N-Acetyl Linagliptin, N-Boc Linagliptin, N-Carbamoyl Linagliptin, and N-Formyl Linagliptin. Our Linagliptin impurity standards have a detailed Certificate of Analysis (CoA) that provides a comprehensive characterization report. This report includes data obtained through techniques,1H NMR, 13C NMR, IR, MASS, and HPLC purity analysis². Upon request, we give additional data like 13C-DEPT. Moreover, we can synthesize unknown Linagliptin impurity standards and degradation products. Each delivery has a comprehensive characterization report.