Last update 01 Jul 2024
Sitagliptin Phosphate
Last update 01 Jul 2024
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms Glactiv, Sitagliptin phosphate (USAN), Sitagliptin Phosphate Hydrate + [19] |
Target |
Mechanism DPP-4 inhibitors(Dipeptidyl peptidase IV inhibitors) |
Therapeutic Areas |
Active Indication |
Inactive Indication |
Originator Organization |
Active Organization |
Inactive Organization |
Drug Highest PhaseApproved |
First Approval Date US (16 Oct 2006), |
RegulationPriority Review (CN) |
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Structure
Molecular FormulaC16H20F6N5O6P |
InChIKeyGQPYTJVDPQTBQC-KLQYNRQASA-N |
CAS Registry654671-77-9 |
Related
562
Clinical Trials associated with Sitagliptin PhosphateDoxycycline in Combination With Sitagliptin on the Glycemic and Cardiac Indices in Patients With Type 2 Diabetes Mellitus
An Open Label, Randomized, Two-Period, Single Oral Dose, Crossover BE Study of SITAGAVIA (100 mg) of the GPO, Thailand with Januvia of ORGANON PHARMA (UK) LIMITED, United Kingdom in Normal, Healthy, Adult Human Subjects under Fasting Conditions
磷酸西格列汀片在健康受试者中的单剂量、随机、开放、交叉、两周期空腹和餐后人体生物等效性试验
[Translation] A single-dose, randomized, open-label, crossover, two-period fasting and fed bioequivalence study of sitagliptin phosphate tablets in healthy subjects
100 Clinical Results associated with Sitagliptin Phosphate
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100 Translational Medicine associated with Sitagliptin Phosphate
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100 Patents (Medical) associated with Sitagliptin Phosphate
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125
Literatures (Medical) associated with Sitagliptin Phosphate01 Feb 2024Journal of pharmaceutical sciences
Solid-State Phase Transformation of Monohydrate and Anhydrous Form II of Sitagliptin Phosphate into a Novel Anhydrous Form IV – Solvent-Driven, Temperature-Induced and Stress Testings
Article
Author: Petrushevski, Gjorgji ; Chachorovska, Marina ; Geskovski, Nikola ; Makreski, Petre ; Lefton, Jonathan B ; Jakimovska, Viktorija
The solid form landscape of sitagliptin phosphate was systematically evaluated by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier transform infrared spectroscopy (FTIR), Raman spectroscopy and X-ray powder diffraction (XRPD), supported by a plethora of auxiliary analytical techniques. The preformulation experiments resulted in the transition of sitagliptin phosphate monohydrate into a new anhydrous form (designated as form IV), obtained after recrystallization from absolute ethanol. The anhydrous form IV remained stable under stressed conditions (1 month at 25 °C/60 %RH and 40 °C/75 %RH). On the other hand, thermal heating (dehydration) of sitagliptin phosphate monohydrate resulted in conversion into another anhydrous form II. Form II was found to be metastable, because after melting, under exposure at 40 °C/75 %RH for 1 month, or when dissolved in absolute ethanol converted to the stable anhydrous form IV of sitagliptin phosphate. A monotropic relationship was found between both studied anhydrous forms. Intrinsic dissolution tests revealed differences in the dissolution rates between the monohydrate and the anhydrous forms of sitagliptin phosphate. This research corrects the record with an accurate chemical composition of the anhydrous form IV of sitagliptin phosphate that was previously regarded as a hemiethanolate. In addition, the crystal structure of anhydrous form II of sitagliptin phosphate has been solved and reported for the first time.
01 Jan 2024Gerontology
Sitagliptin Extends Lifespan of Caenorhabditis elegans by Inhibiting Insulin/Insulin-Like Signaling and Activating Dietary Restriction-Like Signaling Pathways
Article
Author: Yang, Jing ; Li, Yimin ; Wang, Cheng ; Zheng, Jingming ; Ye, Qunshan ; Wan, Qin-Li ; Qiao, Jing
Introduction: The discovery of longevity molecules that delay aging and prolong lifespan has always been a dream of humanity. Sitagliptin phosphate (SIT), an oral dipeptidyl peptidase-4 (DPP-4) inhibitor, is an oral drug commonly used in the treatment of type 2 diabetes (T2D). In addition to being antidiabetic, previous studies have reported that SIT has shown potential to improve health. However, whether SIT plays a role in the amelioration of aging and the underlying molecular mechanism remain undetermined. Methods: Caenorhabditis elegans (C. elegans) was used as a model of aging. Lifespan assays were performed with adult-stage worms on nematode growth medium plates containing FUdR with or without the specific concentration of SIT. The period of fast body movement, body bending rates, and pharyngeal pumping rates were recorded to assess the healthspan of C. elegans. Gene expression was confirmed by GFP fluorescence signal of transgenic worms and qPCR. In addition, the intracellular reactive oxygen species levels were measured using a free radical sensor H2DCF-DA. Results: We found that SIT significantly extended lifespan and healthspan of C. elegans. Mechanistically, we found that several age-related pathways and genes were involved in SIT-induced lifespan extension. The transcription factors DAF-16/FOXO, SKN-1/NRF2, and HSF-1 played important roles in SIT-induced longevity. Moreover, our findings illustrated that SIT-induced survival benefits by inhibiting the insulin/insulin-like signaling pathway and activating the dietary restriction-related and mitochondrial function-related signaling pathways. Conclusion: Our work may provide a theoretical basis for the development of anti-T2D drugs as antiaging drugs, especially for the treatment of age-related disease in diabetic patients.
01 Nov 2023Pakistan journal of pharmaceutical sciences
Synthesis, characterization and in-vitro cytotoxic potential of sitagliptin phosphate nanoparticles against advanced breast cancer cell line - MCF-7.
Article
Author: Nasir Kalam, Muhammad ; Shahid, Nariman ; Daoud Butt, Muhammad ; Rafiq, Azra ; Munir, Yusra ; Saeed, Hamid ; Abdullah, Muhammad
Pharmaceutical substance sitagliptin has long been used to treat diabetes. However, subsequent researches have shown that sitagliptin has additional therapeutic effects. Anti-inflammatory effects are observed. Combining sitagliptin with biodegradable polymers like nanoparticles for chemotherapy may be effective. This method enhances therapeutic agent pharmacokinetics. This study tests sitagliptin (SIT) chitosan base nanoparticles against MCF-7 cancer cell lines for anti-cancer effects. Sitagliptin chitosan-based nanoparticles are tested for their ability to suppress MCF-7 cancer cell proliferation. Ionic gelation, a typical nanoparticle manufacturing method, was used. A detailed examination of the nanoparticles followed, using particle-size measurement, FTIR and SEM. Entrapment efficiency, drug-loading, and in-vitro drug release were assessed. Loaded with chitosan and sitagliptin, the nanoparticles averaged 500nm and 534nm in diameter. Sitagliptin has little effect on particle size. Chitosan-based Sitagliptin nanoparticles grew slightly, suggesting Sitagliptin is present. SIT-SC-NPs had 32% encapsulation efficiency and 30% drug content due to their high polymer-to-drug ratio. SEM analysis showed that both drug-free and sitagliptin-loaded nanoparticles are spherical, as shown by the different bands in the photos. The SIT-CS-NPs had a 120-hour release efficiency of up to 80%. This suggests that these nanoparticles could cure hepatocellular carcinoma, specifically MCF-7 cell lines.
74
News (Medical) associated with Sitagliptin Phosphate25 Apr 2024
VaccineFinancial StatementClinical Result
100 Deals associated with Sitagliptin Phosphate
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External Link
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D06645 | Sitagliptin Phosphate |
R&D Status
Approved
10 top approved records. to view more data
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| Indication | Country/Location | Organization | Date |
|---|---|---|---|
| Diabetes Mellitus, Type 2 | US | 16 Oct 2006 |
Developing
10 top R&D records. to view more data
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Diabetes Mellitus | Phase 3 | US | 01 Apr 2012 | |
| Diabetes Mellitus | Phase 3 | AU | 01 Apr 2012 | |
| Diabetes Mellitus | Phase 3 | BG | 01 Apr 2012 | |
| Diabetes Mellitus | Phase 3 | HR | 01 Apr 2012 | |
| Diabetes Mellitus | Phase 3 | CZ | 01 Apr 2012 | |
| Diabetes Mellitus | Phase 3 | HU | 01 Apr 2012 | |
| Diabetes Mellitus | Phase 3 | IT | 01 Apr 2012 | |
| Diabetes Mellitus | Phase 3 | MY | 01 Apr 2012 | |
| Diabetes Mellitus | Phase 3 | SK | 01 Apr 2012 | |
| Diabetes Mellitus | Phase 3 | KR | 01 Apr 2012 |
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Clinical Result
Clinical Result
Indication
Phase
Evaluation
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Phase 4 | - | tzlxxvhxvk(rfpprshhmq) = uxnxdhzteg dfrjoptfno (tkgzuuycan ) | - | 07 Dec 2022 | |||
(Control group) | tzlxxvhxvk(rfpprshhmq) = wsqcfmljtb dfrjoptfno (tkgzuuycan ) | ||||||
Not Applicable | 22 | (Januvia 100mg) | tamdijakkn(uuyypjylli) = gvdabruudw mdrdxqoodn (imqtaimtkw, ukdgsdhpzh - wuiqbebife) View more | - | 21 Jul 2022 | ||
Placebo (Placebo) | tamdijakkn(uuyypjylli) = peqgrzjple mdrdxqoodn (imqtaimtkw, wdohiicuxq - nneltkxpak) View more | ||||||
Not Applicable | 26 | (Sitagliptin) | pulypsoxup(lfofrkyyvk) = rmoiusdugb lgkfrtpxfs (gxfenbujfv, pqybdkkbsh - czvsnfiwjb) View more | - | 09 Feb 2022 | ||
placebo (Placebo) | pulypsoxup(lfofrkyyvk) = djsoawkuwa lgkfrtpxfs (gxfenbujfv, qzsxyldxys - fpoquxzaqb) View more | ||||||
Phase 4 | 61 | (Sitagliptin) | ouxbzimypc(ibnruzaazv) = xunwgbhfcs zvvbepacqi (qhvvseyexc, wjnosmqcsd - tupsmjfqfh) View more | - | 29 Jun 2021 | ||
Placebo (Placebo) | ouxbzimypc(ibnruzaazv) = ofxpscalgm zvvbepacqi (qhvvseyexc, ykvcgmahop - pnqxeodgmj) View more | ||||||
Phase 4 | 348 | Placebo to match sitagliptin+Saxagliptin (Saxagliptin) | kybdqtwnyf(xddakjchzn) = tefmqqcsfg orxollwnzt (sglsidgnrs, kmuuywucru - naixisdjlj) View more | - | 18 Jun 2021 | ||
Placebo to match saxagliptin (Placebo) | kybdqtwnyf(xddakjchzn) = echquitjfi orxollwnzt (sglsidgnrs, poknpyokbm - holupjaukw) View more | ||||||
Not Applicable | - | 20 | fyafvvibrp(vjhujowtyi) = joatomtwqp csqvhfqafw (gytkzlkicw ) View more | - | 01 Jun 2021 | ||
Placebo | fyafvvibrp(vjhujowtyi) = rzsvxpgbgc csqvhfqafw (gytkzlkicw ) View more | ||||||
Phase 1 | - | 40 | (Sitagliptin) | oahwtnoces(gtcmrhvioy) = xeyrgkymqa mpmamoumlr (saienislos, bhmwatnwkv - gcrpbezilu) View more | - | 03 May 2021 | |
Placebo Comparator - No Sitagliptin (Non-Sitagliptin) | oahwtnoces(gtcmrhvioy) = yeuavdpjhg mpmamoumlr (saienislos, iysvtxwuty - tqsekrhstu) View more | ||||||
Not Applicable | 26 | (Impaired Fasting Glucose) | ixfsqaylha(lxbeholwvj) = dkxsbdbnzc yivtwgxiji (nxjzleaeuu, usywpqgbiz - fhtvfghtaj) View more | - | 05 Apr 2021 | ||
(Normal Glucose Tolerance) | ixfsqaylha(lxbeholwvj) = atqwyldtab yivtwgxiji (nxjzleaeuu, yitgmfeqzi - rsvdvhedpy) View more | ||||||
Phase 4 | - | oetelsuipr(ovqvvwuddt) = kumjyavbfx nyasopbxry (letijwlvgo ) | - | 24 Feb 2021 | |||
(Control group) | oetelsuipr(ovqvvwuddt) = pshjvpazjr nyasopbxry (letijwlvgo ) | ||||||
Phase 2 | 20 | (Sitagliptin Arm) | umbnlxfivk(zbkglqgfwk) = qitfuetcbe pwevqyhzet (qghoacgkct, khmzsppwoq - tzusfasfyc) View more | - | 21 Feb 2021 | ||
Placebo (Placebo Arm) | umbnlxfivk(zbkglqgfwk) = vfoiitxsqh pwevqyhzet (qghoacgkct, arndflbbpm - uzglispmwr) View more |
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