Generic Diabetes Drug Teneligliptin Proves Bioequivalent in Chinese Volunteers

A new generic version of teneligliptin hydrobromide, a widely used medication for type 2 diabetes mellitus, has passed a rigorous bioequivalence test against the branded original in healthy Chinese volunteers, according to a study published in BMC Pharmacology and Toxicology. The finding, reported by a research team based at The Affiliated Panyu Central Hospital of Guangzhou Medical University, showed that the generic tablet delivers essentially the same drug exposure as the reference product Tenelia, whether taken on an empty stomach or with food. For millions of patients across Asia who rely on this class of drugs to keep their blood glucose in check, the result is a meaningful step toward more affordable treatment without compromise in performance.

Teneligliptin belongs to a family of medicines known as dipeptidyl peptidase-4, or DPP-4, inhibitors. These drugs work by blocking an enzyme that normally degrades incretin hormones, the gut-derived chemical messengers that prompt the pancreas to release insulin after a meal and to suppress glucagon when blood sugar is already adequate. By preserving incretin activity, DPP-4 inhibitors produce a glucose-dependent enhancement of insulin secretion, which gives them a comparatively favorable safety profile relative to some older antidiabetic agents. Teneligliptin in particular has gained a substantial foothold in Asian markets, where it is prescribed for adults with type 2 diabetes whose glycemic control is inadequate through diet and exercise alone.

The scientific rationale for the new study rests on a fundamental principle of generic drug approval: before a copycat tablet can be substituted for the branded original, regulators demand quantitative proof that the two formulations behave identically inside the body. This property, called bioequivalence, is assessed by comparing how much drug reaches the bloodstream, how quickly it gets there, and how long it lingers. The standard benchmarks are the area under the plasma concentration-time curve, abbreviated AUC, which captures total systemic exposure, and the maximum observed plasma concentration, known as Cmax, which reflects the peak level achieved after a dose. Because a generic can be manufactured and sold at a fraction of the brand-name price, demonstrating bioequivalence is the gateway to cost savings that can ripple across entire health systems, a consideration that is especially acute in countries with large diabetic populations and constrained drug budgets.

To generate that proof, the researchers recruited 52 healthy Chinese adults and enrolled them in a randomized, open-label, single-dose, two-sequence, two-period crossover trial, with 26 participants assigned to each treatment sequence. In a crossover design, every volunteer eventually receives both formulations, with the order of administration randomized; this arrangement is prized in bioequivalence work because each participant serves as his or her own control, stripping away much of the noise introduced by individual differences in metabolism, body composition, and physiology. The washout interval between the two doses was set at seven days, long enough for the first dose to be fully eliminated before the second was taken, ensuring that lingering drug from one period could not contaminate measurements in the other.

The trial was conducted twice under deliberately different dietary conditions, once in the fasting state and once after food. This dual design matters because meals can alter gastric emptying, bile flow, and the solubility of orally administered compounds, sometimes shifting absorption in ways that change both the speed and the extent of drug uptake. Regulatory agencies typically require bioequivalence testing under fasting conditions, and add a fed arm when a drug is likely to be taken with meals or when food effects are anticipated. A single 40 mg dose of either the test generic or the reference Tenelia was administered in each condition, allowing the investigators to establish that the two tablets perform equivalently regardless of whether a patient swallows the pill before breakfast or alongside it.

Measuring the drug in plasma demanded a highly sensitive analytical technique. The team used liquid chromatography-tandem mass spectrometry, or LC-MS/MS, a method that first separates teneligliptin from the other components of blood plasma and then fragments the molecules in a way that allows precise quantification even at very low concentrations. The assay was validated before use, and the accuracy of the measurements was verified through incurred sample reanalysis, in which selected patient samples are tested a second time to confirm that the original results are reproducible. Such quality-control steps are indispensable, because a bioequivalence verdict is only as trustworthy as the concentration data on which the entire statistical comparison is built.

The statistical framework for the comparison follows internationally harmonized regulatory conventions. For each pharmacokinetic parameter, the researchers calculated the geometric mean ratio between the generic and the branded product, then determined the 90 percent confidence interval around that ratio after logarithmic transformation of the data. Equivalence is declared only when the entire confidence interval falls within the predefined acceptance boundaries of 80 to 125 percent for the parameters AUC from time zero to the last measurable concentration, AUC extrapolated to infinity, and Cmax. The analysis of variance, or ANOVA, framework used for this purpose formally accounts for the crossover structure of the trial, testing whether formulation, period, and sequence effects influence the observed differences. In both the fasting and the fed studies, every confidence interval landed squarely inside the acceptance window, satisfying the regulatory criterion for bioequivalence in full.

Safety was monitored alongside the pharmacokinetic measurements, with adverse events graded according to the Common Terminology Criteria for Adverse Events, version 5.0. No serious adverse events occurred during the trial, an outcome consistent with the generally well-tolerated character of DPP-4 inhibitors at single therapeutic doses in healthy volunteers. While a small crossover study in healthy adults cannot substitute for the broader safety record accumulated through post-marketing surveillance, the absence of serious events provides reassurance that the generic formulation introduces no novel tolerability concerns relative to the established product.

The study was carried out from April through September 2025 at The Affiliated Panyu Central Hospital of Guangzhou Medical University, conducted in accordance with the Declaration of Helsinki and approved in advance by the institution’s Drug Clinical Trial Ethics Committee. Each volunteer provided written informed consent before screening began, and the trial was registered in the Chinese Clinical Trial Registry under identifier ChiCTR2500112749, registered retrospectively on November 19, 2025, with an earlier entry on the Drug Clinical Trial Registration and Information Publicity Platform under CTR20252533. The conduct of the trial and the preparation of the manuscript adhered to the CONSORT 2025 reporting guidelines and their applicable bioequivalence extensions, reflecting the transparency standards now expected of clinical research.

The broader significance of the result extends well beyond a single tablet. Bioequivalence studies of this kind form the backbone of generic substitution policies worldwide, allowing pharmacists and physicians to swap in lower-cost alternatives with confidence that patients will experience the same therapeutic effect. For teneligliptin specifically, the availability of a demonstrated equivalent generic in China could ease the financial burden of long-term diabetes therapy for a patient population that continues to grow. The authors conclude that the pharmacokinetic comparison supports the generic product as an equivalent alternative to Tenelia under both fasting and fed conditions, and that the evidence should help inform the product’s acceptance in clinical practice. The study was funded entirely without external grants, and the authors declare no competing interests, with the article published open access under a Creative Commons license so that clinicians, regulators, and patients can examine the full data for themselves.

Subject of Research: Bioequivalence evaluation of generic teneligliptin hydrobromide tablets in healthy Chinese volunteers

Article Title: Pharmacokinetic and bioequivalence evaluation of teneligliptin hydrobromide tablets following single-dose administration in healthy Chinese volunteers under fasting and fed conditions

Article References: Guan, Z., Chen, M., Wei, B., Su, J., Tan, D., Ke, J., & Huang, G. (2026). Pharmacokinetic and bioequivalence evaluation of teneligliptin hydrobromide tablets following single-dose administration in healthy Chinese volunteers under fasting and fed conditions. BMC Pharmacology and Toxicology. https://doi.org/10.1186/s40360-026-01234-9

Image Credits: AI Generated

DOI: 10.1186/s40360-026-01234-9

Keywords: teneligliptin, bioequivalence, pharmacokinetics, type 2 diabetes, DPP-4 inhibitor, generic drugs, LC-MS/MS, clinical trial, Chinese volunteers, drug safety, crossover study, BMC Pharmacology and Toxicology