Evaluate Efficacy and Safety of Gosogliptin as Monotherapy and in Combination With Metformin vs. Vildagliptin as Monotherapy and in Combination With Metformin in Drug-naive Type 2 Diabetic Patients.

To demonstrate that efficacy of Gosogliptin as Monotherapy and in Combination with Metformin is non-inferior to efficacy of Vildagliptin as Monotherapy and in combination with Metformin in the effects on glycosilated hemoglobin (HbA1c) at Week 12 and Week 36 compared to baseline (Week 0).

Start Date23 Apr 2013

Sponsor / Collaborator

SatRx LLC

EUCTR2007-007588-26-PL / Not yet recruitingPhase 2

A PHASE 2, RANDOMIZED, DOUBLE-BLIND, PLACEBO-CONTROLLED, PARALLEL GROUP STUDY TO EVALUATE THE EFFICACY AND SAFETY OF 12-WEEK ADMINISTRATION OF PF-00734200 TO SUBJECTS WITH TYPE 2 DIABETES MELLITUS AND INSUFFICIENT GLYCEMIC CONTROL ON METFORMIN TREATMENT

Start Date04 Apr 2008

Sponsor / Collaborator

Pfizer Inc.

EUCTR2007-001922-28-DE / Not yet recruitingNot Applicable

A Phase 2A, Randomized, Placebo-controlled, Parallel group, Multiple-dose study to evaluate the Efficacy, Safety and Tolerability of 12-week oral administration of PF-00734200 tablets to subjects with Type 2 Diabetes Mellitus on stable treatment with Metformin - N/A

Start Date15 Oct 2007

Sponsor / Collaborator

Pfizer Inc.

100 Clinical Results associated with Gosogliptin

100 Translational Medicine associated with Gosogliptin

100 Patents (Medical) associated with Gosogliptin

Literatures (Medical) associated with Gosogliptin

01 May 2024·International journal of legal medicine

Severe 25E-NBOH intoxication associated with MDPHP intake: a case report, metabolism study, and literature review

Review

Author: Le Daré, Brendan ; Carvelli, Julien ; Bottinelli, Charline ; Pelletier, Romain ; Fabresse, Nicolas ; Balaz, Pierre ; Morel, Isabelle ; Pelissier-Alicot, Anne-Laure ; Gicquel, Thomas ; Solas, Caroline

N-Benzylphenethylamine derivatives are 5-HT2A receptor agonists with hallucinogenic properties, including NBOMe (N-(2-methoxybenzyl)-2-(3,4,5-trimethoxyphenyl)ethan-1-amine) and NBOH (2-(((2,5-dimethoxyphenethyl)amino)methyl)phenol). We reported here the case of a 23-year-old man who presented a serotoninergic syndrome and a loss of consciousness following the consumption of a powder labelled as 25I-NBOH. Toxicological analyses of biological samples were carried out using a liquid chromatography high-resolution mass spectrometry. Two new psychoactive substances were identified and confirmed with certified reference materials: 25E-NBOH (2-(((4-ethyl-2,5-dimethoxyphenethyl)amino)methyl)phenol) and MDPHP (1-(benzo[d][1,3]dioxol-5-yl)-2-(pyrrolidin-1-yl)hexan-1-one). Pharmaceuticals administered to the patient during his medical care were found in plasma and urine. 25E-NBOH and MDPHP concentrations were respectively at 2.3 ng/mL and 3.4 ng/mL in plasma, and 25.7 ng/mL and 30.5 ng/mL in urine. 25I-NBOH (2-(((4-iodo-2,5-dimethoxyphenethyl)amino)methyl)phenol) was specifically searched in both samples and was not detected. These results are discussed along with a literature review on human cases of exposure to N-benzylphenethylamine derivatives. Using molecular networking approach, we propose the first 25E-NBOH metabolism study using authentic biological samples (plasma and urine). We described seven metabolites (M1 to M7), including two phase I (m/z 330.172; m/z 288.160) and five phase II metabolites (m/z 464.191, m/z 478.207, m/z 492.223, m/z 508.218; m/z 396.156). The M6 (m/z 492.223) was the most intense ion detected in plasma and urine and could be proposed as a relevant 25E-NBOH consumption marker. Overall, we described an original case of 25E-NBOH poisoning and identified metabolites that could potentially be used as consumption markers to detect 25E-NBOH intoxications with a higher confidence level and probably a longer detection window.

01 Mar 2024·Drug testing and analysis

Pharmacological profile, phase I metabolism, and excretion time profile of the new synthetic cathinone 3,4‐Pr‐PipVP

Article

Author: Persson, Mattias ; Pulver, Benedikt ; Auwärter, Volker ; Huß, Max Vincent ; Gréen, Henrik ; Schwelm, Hannes Max

Abstract:

1‐(2,3‐Dihydro‐1H‐inden‐5‐yl)‐2‐(piperidin‐1‐yl)pentan‐1‐one (3,4‐Pr‐PipVP), a novel synthetic cathinone (SCat), was first identified in 2022 in Germany. The product was marketed as 1‐(bicyclo[4.2.0]octa‐1,3,5‐trien‐3‐yl)‐2‐(pyrrolidin‐1‐yl)pentan‐1‐one (3,4‐EtPV), a substance not covered by the German New Psychoactive Substances Act (NpSG). Although originally intended to be an exploratory new synthetic cathinone containing the novel bicyclo[4.2.0]octatrienyl function, the compound was subsequently confirmed to contain an indanyl ring system scheduled under generic legislation like the NpSG. However, it is one of only a few marketed SCats carrying a piperidine ring. Inhibition experiments involving norepinephrine, dopamine, and serotonin transporters showed that 3,4‐Pr‐PipVP was a low potency blocker at all three monoamine transporters compared to related substances such as MDPV. Additionally, pharmacokinetic data were collected from pooled human liver microsomes incubations and from the analysis of authentic urine samples received after oral administration of 5 mg 3,4‐Pr‐PipVP hydrochloride. Phase I metabolites were tentatively identified in vitro and in vivo using liquid chromatography−time‐of‐flight mass spectrometry. Main metabolites were formed by metabolic reduction of the carbonyl function with and without additional hydroxylations at the propylene bridge of the molecule. Keto‐reduced H2–3,4‐Pr‐PipVP and H2‐piperidine‐OH‐3,4‐Pr‐PipVP as well as aryl‐OH‐3,4‐Pr‐PipVP, and indanyl‐OH‐piperidine‐OH‐3,4‐Pr‐PipVP are suggested as most suitable biomarkers for the detection of 3,4‐Pr‐PipVP since they were detected for much longer than the parent compound. 3,4‐Pr‐PipVP could be detected for up to 21 h whereas its metabolites were detectable for up to about 4 days.

01 Dec 2023·Chemistry & biodiversity

Benzothiazole‐Propanamide Linker Pyrrolidine (Morpholine) as Monoamine Oxidase‐B and Butyrylcholinesterase Inhibitors

Article

Author: Wu, Di ; Guan, Li-Ping ; He, Zhi-Wen ; Jiang, B S Kai-Yin ; Liu, Ya-Wen ; Sun, Xin-Hao ; Tang, Min

Abstract:

According to the fusion technique create effective multi‐target‐directed ligands, in this study, we designed and synthesized a series of benzo[d]thiazol‐2‐yl)‐3‐(pyrrolidin‐1‐yl) or 3‐(morph‐ olino‐1‐yl)propanamide derivatives, and evaluated their inhibitory potency against MAOs, AChE, BuChE by in vitro enzyme effect assays. Based on activity results, we found that derivatives N‐(5‐methylbenzo[d]thiazol‐2‐yl)‐3‐(pyrrolidin‐1‐yl)propanamide (2 c) and N‐(6‐bromobenzo[d]thiazol‐2‐yl)‐3‐(pyrrolidin‐1‐yl)propanamide (2 h) showed good inhibitory potency against BuChE with IC50 values of 15.12 μM and 12.33 μM, respectively. Besides, 2 c and 2 h also exhibited selective MAO‐B inhibitory effects with inhibition rates of 60.10 % and 66.30 % at 100 μM, respectively. In contrast, all designed derivatives were poor active against AChE and MAO‐A at a concentration of 100 μM. The toxicity analysis in vitro by MTT and AO/EB fluorescence staining confirmed that 2 c and 2 h were nontoxic up to 100 μM. Molecular modeling studies showed that 2 c and 2 h could bind to the active site of BuChE. This research paves the way for further study aimed at designing MAO‐B and BuChE inhibitors for the treatment of neurodegenerative disorders.

News (Medical) associated with Gosogliptin

09 Jul 2012

·www.biospace.com

Pfizer Inc. Licenses Diabetes Drug to Russia's SatRx

MOSCOW--(Marketwire - July 05, 2012) - ChemRar Hi-Tech Centre, the Russian pharmaceutical investment and R&D group, announced today that Pfizer granted exclusive development and marketing rights to SatRx for their DPP(1)-IVi compound, PF-00734200. SatRX, a ChemRar group company, is developing PF-00734200 for type 2 diabetes (T2D), one of the most burdensome chronic non-communicable diseases, which is fast reaching epidemic proportions throughout the world. Under the terms of the license, signed during the St. Petersburg Economic Forum on June 23, Pfizer granted exclusive worldwide rights (ex-China) development and commercialization of PF-00734200 as monotherapy or in combination with certain other. Pfizer will receive royalties and milestone payments based on commercialization activities. The agreement was developed as partial fulfillment of a Memorandum of Understanding reached in March 2011, under which Pfizer and ChemRar agreed to explore collaborations focused on research, development and commercialization of innovative compounds and vaccines to treat cardiometabolic, infectious and oncologic diseases in Russia and other countries. "We welcome this licensing agreement between SatRx and Pfizer. SatRx is going to register the new drug to the Russian market and will further establish breakthrough therapies for treating diabetes synergistically combining DPP-IVi with TGR5 agonists and other novel small molecule drug candidates in its R&D portfolio. ChemRar is committed to investing in development of innovative medicines, diagnostics and devices to control and treat type 2 and type 1 diabetes," confirmed Nikolay Savchuk, board member of ChemRar HTC. "We aspire to further expand our collaboration with Pfizer in the framework of the MOU we signed in 2011." "This licensing agreement with Pfizer provides SatRx with essential background for development of fully innovative tools to tune the metabolism of patients with T2D and obesity. Synergistic actions of DPP-IVi and proprietary new SatRx molecules active in the incretin metabolic cascade will provide significant therapeutic benefits and promises to increase patient compliance and quality of life," said Yulia Baybikova, General Manager of SatRx. The World Health Organization (WHO)(2) considers diabetes among the four most socially significant diseases, along with cardiovascular and respiratory diseases and cancers; responsible for 80% of deaths from non-communicable diseases worldwide. One of ten people in the world has diabetes, and T2D, formerly called non-insulin-dependent or adult-onset diabetes, comprises 90% of those cases. Based on Russian Endocrinology Association data(3), the prevalence of T2D is increasing in the Russian Federation in parallel with overall global trends. As of January 1, 2011 more than 3.3 million diabetes cases were registered in Russia, and 90% are T2D. Control-and-epidemiological studies by the State Federal Endocrinology Center from 2005-2010 indicate that the number of diabetic patients exceed the number of registered cases by 2-3 times. During the last 10 years the number of patients with diabetes in Russia has doubled. About ChemRar ChemRar High Tech Center is a unique group of biotech start up, R&D service and venture investment companies developing and commercializing innovative medicines for treatment of cardiometabolic and infectious diseases, oncology, and CNS pathologies in Russia and abroad. ChemRar Ventures is a Russian venture company, managing a diversified investment portfolio of biopharma, diagnostic and medical device companies developing treatments for unmet medical needs. SatRx is an R&D company focused on development in the area of diabetes and obesity. About SatRx SatRx is a Russian start-up company established in 2010 on the basis of ChemRar High Tech Center which aims to develop novel medicines and their synergistic combinations to treat diabetes, obesity and other metabolic diseases. (1) DPP4i (dipeptidyl peptidase) inhibitors provide a class of therapies that manage blood-glucose levels without the associated risk of hypoglycaemia that may be experienced with other diabetes medication. (2) The World health statistics 2012 report (3) I. Dedov and co-authors, Monograph "Consensus of experts of Russian association of endocrinologists on initiation of intensification of sugar-decreasing treatment for patients with type 2 diabetes", p.7, 2011 ChemRar Russia Elena Surina Email Contact +7 (926) 206-78-71 ChemRar US Olga Dmitrieva Email Contact (858) 794-48-60

CollaborateVaccineSmall molecular drug

100 Deals associated with Gosogliptin

External Link

KEGG	Wiki	ATC	Drug Bank
D09625	Gosogliptin	-	DB08382

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	RU	SatRx LLC	16 May 2016

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Noninsulin-Dependent, 2	Phase 3	RU	SatRx LLC	23 Apr 2013
Chronic Kidney Diseases	Phase 1	US	Pfizer Inc.	01 Oct 2007

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03088670 (SRX-1374-02, Literature) Manual	Phase 3	Diabetes Mellitus, Type 2	299	Metformin+Gosogliptin	emcjziycxy(wxdcbhaaob) = zgvnllazzn bycofibetl (mdcnimruhr ) View more	Superior	01 Jan 2016
				Metformin+Vildagliptin	emcjziycxy(wxdcbhaaob) = offqaiesck bycofibetl (mdcnimruhr ) View more

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