Pharmacokinetic and protein binding profile of peptidomimetic DPP-4 inhibitor – Teneligliptin in rats using liquid chromatography–tandem mass spectrometry

Saladi, Shantikumar; Satheeshkumar, N.; Srinivas, R.

doi:10.1016/j.jchromb.2015.08.023

Cited by 21 publications

(11 citation statements)

References 21 publications

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“…Although the drug entered the market, there is no much information available about its degradation studies and its degraded products. Few have reported its metabolism and pharmacokinetic studies (Halabi et al 2013;Reddy et al 2014;Luhar et al 2016;Shanthikumar et al 2015). Identification of the degraded products helps in future metabolic studies and also related impurity determination during its bulk synthesis.…”

Section: Introductionmentioning

confidence: 99%

Method development, validation, and stability studies of teneligliptin by RP-HPLC and identification of degradation products by UPLC tandem mass spectroscopy

Kumar¹,

Vidyadhara²,

Narkhede

et al. 2016

J Anal Sci Technol

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Background: Teneligliptin is a new FDA approved drug for treating Diabetes Mellitus. There are no reported evidences for its degradation products during stability studies and their effects on humans. Methods: A simple and new stability indicating RP-HPLC method was developed and validated for identification of Teneligliptin and its degradants on Kromasil 100-5C 18 (250 × 4.6 mm, 5 μm) column using pH 6.0 phosphate buffer and acetonitrile (60:40 v/v) as a mobile phase in isocratic mode of elution at a flow rate of 1.0 mL/min. The column effluents were monitored by a variable wavelength UV detector at 246 nm. The method was validated as per ICH guidelines. Forced degradation studies of Teneligliptin were carried out under acidic, basic, neutral (peroxide), photo and thermal conditions for 48 hours at room temperature. The degradation products were identified by HPLC and characterized by UPLC with tandem mass spectroscopy (LC/MS/MS). Results: UPLC MS/MS data shown major peaks, observed at 375.72, 354.30, 310.30, 214.19, 155.65, 138.08 and 136.18 m/z. Their structural elucidation was depicted. Conclusion: Degradation was observed in base, peroxide and thermal stressed samples, but not in acid and photolytic stressed samples.

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Section: Introductionmentioning

confidence: 99%

Method development, validation, and stability studies of teneligliptin by RP-HPLC and identification of degradation products by UPLC tandem mass spectroscopy

Kumar¹,

Vidyadhara²,

Narkhede

et al. 2016

J Anal Sci Technol

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show abstract

“…[490][491][492] Experimental approaches based on intermolecular interactions Proteomic techniques using affinity chromatography combined with mass spectrometry, showing protein interactions based on intermolecular force have been widely used for target validation, facilitating drug repurposing due to an experimentally based pharmacological analysis. 493,494 In this approach, cells or animals are treated with drugs followed by deep proteome analysis to differentially quantify proteins changes that occurred. 495,496 With the development of labeling (including metabolic labeling and chemical labeling) or label-free approaches, proteins targeted by the drug can be detected in an unbiased fashion.…”

Section: Technological Approaches To Drug Repurposing For Cancer Therapymentioning

confidence: 99%

Overcoming cancer therapeutic bottleneck by drug repurposing

Zhang

Zhou

Xie

et al. 2020

Sig Transduct Target Ther

366

315

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Ever present hurdles for the discovery of new drugs for cancer therapy have necessitated the development of the alternative strategy of drug repurposing, the development of old drugs for new therapeutic purposes. This strategy with a cost-effective way offers a rare opportunity for the treatment of human neoplastic disease, facilitating rapid clinical translation. With an increased understanding of the hallmarks of cancer and the development of various data-driven approaches, drug repurposing further promotes the holistic productivity of drug discovery and reasonably focuses on target-defined antineoplastic compounds. The "treasure trove" of non-oncology drugs should not be ignored since they could target not only known but also hitherto unknown vulnerabilities of cancer. Indeed, different from targeted drugs, these old generic drugs, usually used in a multi-target strategy may bring benefit to patients. In this review, aiming to demonstrate the full potential of drug repurposing, we present various promising repurposed non-oncology drugs for clinical cancer management and classify these candidates into their proposed administration for either mono-or drug combination therapy. We also summarize approaches used for drug repurposing and discuss the main barriers to its uptake.

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“…Although the drug entered the market, there is no much information available about its degradation studies and its degraded products. Few have reported its metabolism and pharmacokinetic studies (Halabi et al 2013;Reddy and Rao 2014;Luhar et al 2016;Shanthikumar et al 2015). Identification of the degraded products helps in future metabolic studies and also related impurity determination during its bulk synthesis.…”

Section: Introductionmentioning

confidence: 99%

RETRACTED ARTICLE: Method development, validation, and stability studies of teneligliptin by RP-HPLC and identification of degradation products by UPLC tandem mass spectroscopy

Kumar¹,

Vidyadhara²,

Narkhede

et al. 2016

J Anal Sci Technol

View full text Add to dashboard Cite

Background: Teneligliptin is a new FDA approved drug for treating Diabetes Mellitus. There are no reported evidences for their identified degradation products and their effects on humans. Methods: A simple and new stability indicating RP-HPLC method was developed and validated for identification of Teneligliptin and its degradants on Kromasil 100-5C18 (250×4.6mm, 5μm) column using pH 6.0 phosphate buffer and acetonitrile (60:40 v/v) as a mobile phase in isocratic mode of elution at a flow rate of 1.0 mL/min. The column effluents were monitored by a variable wavelength UV detector at 246 nm. The method was validated as per ICH guidelines. Forced degradation studies of Teneligliptin were carried out under acidic, basic, neutral (peroxide), photo and thermal conditions for 48 hours at room temperature. The degradation products were identified by HPLC and characterized by UPLC with tandem mass spectroscopy (LC/MS/MS). Results: UPLC MS/MS data shown major peaks, observed at 375. 72, 354.30, 310.30, 214.19, 155.65, 138.08 and 136.18 m/z. Conclusion: Degradation was observed in base, peroxide and thermal stressed samples, but not in acid and photolytic stressed samples.

show abstract

Pharmacokinetic and protein binding profile of peptidomimetic DPP-4 inhibitor – Teneligliptin in rats using liquid chromatography–tandem mass spectrometry

Cited by 21 publications

References 21 publications

Method development, validation, and stability studies of teneligliptin by RP-HPLC and identification of degradation products by UPLC tandem mass spectroscopy

Method development, validation, and stability studies of teneligliptin by RP-HPLC and identification of degradation products by UPLC tandem mass spectroscopy

Overcoming cancer therapeutic bottleneck by drug repurposing

RETRACTED ARTICLE: Method development, validation, and stability studies of teneligliptin by RP-HPLC and identification of degradation products by UPLC tandem mass spectroscopy

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