Desmetramadol(Desmetramadol) - 药物靶点：NET x μ opioid receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名

O-DSMT、O-demethyl-tramadol、O-desmethyl-tramadol

+ [4]

靶点

NET x μ opioid receptor

作用机制

NET抑制剂(去甲肾上腺素转运蛋白抑制剂)、μ opioid receptor激动剂(μ-阿片受体激动剂)

治疗领域

神经系统疾病内分泌与代谢疾病遗传病与畸形

在研适应症-

非在研适应症

慢性疼痛糖尿病性神经病变与 CYP2D6 相关的药物代谢不良+ [1]

原研机构

Syntrix Biosystems, Inc.

在研机构-

非在研机构

Syntrix Biosystems, Inc.

最高研发阶段无进展临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C15H23NO2

InChIKeyUWJUQVWARXYRCG-UYWMCZCJSA-N

CAS号80456-81-1

关联

5

项与 Desmetramadol 相关的临床试验

NCT04683926 / Completed临床1期

A Phase 1 Randomized Single Oral Dose Cross-Over Study Investigating Desmetramadol Dose Proportionality And Food Effect In Normal Human Subjects

The purpose of the study is to investigate in healthy human subjects how much desmetramadol (Omnitram) gets in the blood after different oral doses are taken with or without food.

开始日期2021-01-08

申办/合作机构

Syntrix Biosystems, Inc.

[+2]

NCT03664921 / Completed临床2期

A Phase II Randomized, Double-Blind, Placebo-Controlled, Cross-Over Study Investigating the Safety and Efficacy of Omnitram in Diabetic Neuropathy

This study evaluates the analgesic effect of Omnitram for the treatment of painful diabetic neuropathy. Each subject with diabetic neuropathy will be treated for four weeks with Omnitram and for four weeks with placebo. The order of the Omnitram and placebo treatment will be random.

开始日期2018-11-15

申办/合作机构

Syntrix Biosystems, Inc.

[+2]

NCT03312777 / Completed临床1期

A Phase 1b, Double-Blind, Randomized, Placebo-Controlled, Three Segment Cross-Over Study Investigating Oral Steady-State Pharmacokinetics And Hypoalgesic Effect Of 20 Mg Omnitram And 50 Mg Tramadol In Normal Human Subjects Made Cyp2d6 Deficient By Paroxetine

This study evaluates the analgesic effect of Omnitram and tramadol during concurrent administration of paroxetine. Paroxetine administration is expected to diminish the analgesic effect of tramadol, but not Omnitram. Each participant will receive paroxetine before and during treatment with Omnitram, tramadol, and placebo.

开始日期2017-10-31

申办/合作机构

Syntrix Biosystems, Inc.

[+2]

100 项与 Desmetramadol 相关的临床结果

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100 项与 Desmetramadol 相关的转化医学

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100 项与 Desmetramadol 相关的专利（医药）

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115

项与 Desmetramadol 相关的文献（医药）

2024-10-01·Saudi Journal of Medicine & Medical Sciences

Achievement of No Evidence of Disease Activity-3 with Oral Disease-Modifying Treatment in Patients with Relapsing–Remitting Multiple Sclerosis

Article

作者: Alshamrani, Foziah Jabbar Gossab ; Soltan, Nehad Mahmoud ; Shahid, Rizwana ; Yasawy, Zakia ; Nazish, Saima ; Shariff, Erum ; Alsawad, Rahmah Majed ; Zafar, Azra

AbstractBackground:There is scant data regarding the use of oral disease-modifying treatments (oDMT) in patients with relapsing–remitting multiple sclerosis (PwRRMS) from Saudi Arabia.Objective:This study aimed to identify the response rate to oDMT in PwRRMS compared to interferon (IFN) in terms of achieving no evidence of disease activity-3 (NEDA-3).Methods:This retrospective study was conducted at a tertiary care hospital in Saudi Arabia and included all adult PwRRMS over a 2-year period who were on oDMTs or IFN for <1 year. The achievement of overall NEDA-3 and its components (namely, relapse, disability progression, and focal MRI activity) were assessed for each treatment.Results:A total of 231 patients were included for the analysis of NEDA-3 status, of which 78 (33.8%) were on oDMTs (namely, dimethyl fumarate, teriflunomide, and fingolimod). NEDA-3 status was achieved in 51.3% (OR: 1.86, 95% CI: 1.28–2.71) of patients on oDMTs and in 32% of patients on IFN (OR: 0.72, 95% CI: 0.58–0.89) (P < 0.001). Compared to the IFN group, the oDMT group had significantly lower rates of clinical relapse (P < 0.001), disability progression (P = 0.004), and new focal MRI activity (P = 0.01). Patients on dimethyl-fumarate had higher odds of achieving NEDA-3 (OR: 2.18, 95% CI = 1.09–4.34; P =0.02) compared with those on fingolimod (OR 2.15, 95% CI = 0.70–6.58; P =0.16) and teriflunomide (OR: 1.53, 95% CI = 0.81–2.91; P =0.18).Conclusion:More than half of the patients with relapsing–remitting multiple sclerosis on oral DMTs achieved NEDA-3 status in this study. Significant differences were observed in NEDA-3 status parameters and achievement between patients on oral DMTs and interferon, with the likeliness being highest among patients treated with dimethyl-fumarate.

2024-04-01·Medicina Clínica

Análisis retrospectivo de las hipoglucemias inducidas por venlafaxina en pacientes con sobredosis

Article

作者: Elorza Guerrero, Miguel Ángel ; Guiu Marti, Alexandra M ; Socias Crespí, Lorenzo ; Barceló Martín, Bernardino ; Puiguriguer Ferrando, Jordi ; Gomila Muñiz, Isabel

INTRODUCTIONRecent publications relate the presence of hypoglycemia in venlafaxine (VLX) poisoning depending on the dose. Our aim was to analyze the clinical characteristics of patients who presented hypoglycemia induced by VLF overdose.PATIENTS AND METHODSRetrospective study carried out in the Balearic Islands (2020-2023).INCLUSION CRITERIAserum concentrations of VLX + O-desmethyl-venlafaxine (O-VLX)>800 ng/mL. The characteristics of patients with and without hypoglycemia were compared.RESULTSTwenty-one patients were included, 8 (38.1%) with hypoglycemia. No differences were found in the doses referred to in both groups. Peak concentrations of VLX + O-VLX (ng/mL) were 9,783 [4,459-17,976] in patients with hypoglycemia and 1,413 [930-1,719] in patients without hypoglycemia (p<0.0001). The presence of hypoglycemia was associated with: lower age and level of consciousness; and higher frequency of suicide attempts, seizures, mydriasis, tachycardia and serotonin syndrome, invasive respiratory support, fluid therapy and ICU admission (p<0.05).CONCLUSIONSThe detection of hypoglycemia in a VLX overdose case is a readily available marker to suspect the severity of the patient. In any case, serum concentrations when available allow us to confirm intoxication.

2023-12-01·International Journal of Biological Macromolecules

Active coatings based on oxidized chitin nanocrystals and silk fibroins for the control of anthracnose in ‘Hass’ avocados

Article

作者: Besoain, Ximena ; Funes, Catalina Ferreira ; Larach, Alejandra ; Van Nhien, Albert Nguyen ; Hadad, Caroline ; Serrano, Daniela Duarte ; Fuentealba, Claudia ; Pedreschi, Romina

Postharvest avocado losses are mainly due to anthracnose disease caused by Colletotrichum gloeosporioides. Chemical fungicides are effective, but their negative effects on health and the environment have led to the search for sustainable alternatives such as biopolymer-based coatings and natural compounds. Therefore, chitin nanocrystals (NCChit) were extracted using a sustainable deep eutectic solvent (DES) and chemically modified into oxidized chitin nanocrystals (O-NCChit) or deacetylated chitin nanocrystals (D-NCChit) to modulate and increase the charge surface density and the dispersibility of the crystals. The modified NCChits were dispersed with silk fibroins (SF), essential oil (EO), melatonin (MT) and/or phenylalanine (Phe) to elaborate active coatings. Antioxidant and antifungal in vitro analyses showed that the O-NCChit/SF-based coating had the best performance. In addition, in vivo tests were carried out through the artificial inoculation of C. gloeosporioides on coated avocados. O-NCChit/SF/MT-based coatings reduced the severity of anthracnose by 45 %, the same effect as the chemical fungicide (Prochloraz®). Moreover, avocado quality parameters during cold storage and the shelf-life period were also evaluated, where nonsignificant differences were observed. Therefore, this study demonstrates the great potential of O-NCChit and SF in combination with active compounds for the control of anthracnose in 'Hass' avocados.

100 项与 Desmetramadol 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	Desmetramadol	-	-

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
慢性疼痛	临床2期	美国	Syntrix Biosystems, Inc.	2018-11-15
糖尿病性神经病变	临床2期	美国	Syntrix Biosystems, Inc.	2018-11-15
神经痛	临床2期	美国	Syntrix Biosystems, Inc.	2018-11-15
与 CYP2D6 相关的药物代谢不良	临床2期	美国	Syntrix Biosystems, Inc.	2017-10-31

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT04683926 (CTgov)	临床1期	疼痛	24	Desmetramadol (Desmetramadol 10 mg, Fasted)	鬱襯艱淵觸衊築鏇鹽醖(觸餘簾選壓築繭窪衊顧) = 廠壓顧簾窪鏇遞獵廠繭選範鬱積壓鑰夢鏇願願 (築觸選衊糧鏇窪艱糧齋, 壓膚製築簾鏇築淵壓艱 ~ 蓋觸衊遞淵鑰鬱淵壓構) 更多	-	2023-04-04
				Desmetramadol (Desmetramadol 20 mg, Fasted)	鬱襯艱淵觸衊築鏇鹽醖(觸餘簾選壓築繭窪衊顧) = 淵鏇積衊鑰選觸簾齋蓋選範鬱積壓鑰夢鏇願願 (築觸選衊糧鏇窪艱糧齋, 淵製鹽簾艱齋簾網窪願 ~ 窪築遞齋願鹽鹽齋衊窪) 更多