A Randomized, Open-Label Study to Evaluate the Bioavailability of a BMS-986205 Tablet Containing Free Base Relative to a Reference Tablet in Healthy Participants

This is a Phase 1, open-label, randomized study in healthy participants to evaluate the absorption of a BMS-986205 tablet into the bloodstream compared to a reference tablet. Eligible participants will be randomly assigned to 1 of 2 treatment sequences and will receive a single, oral dose of BMS-986205 twice over 22 days. Participants must remain at the clinical facility for the duration of the study.

开始日期2017-12-21

申办/合作机构

Bristol Myers Squibb Co.

NCT01043263 / Completed临床2期

A Phase IIB, Randomized, Double-blind, Two-arm, Multi-center, Placebo-controlled, Study to Assess the Efficacy and Safety of EN3324 (Axomadol) in Subjects With Moderate to Severe Chronic Low Back Pain

The purpose of this study is to determine the efficacy and safety of EN3324 (axomadol) in subjects with moderate to severe chronic low back pain

开始日期2009-12-01

申办/合作机构

Grünenthal GmbH

NCT03768024 / Completed临床1期

A Single-Dose, Randomized, Double Blind, Placebo and Active Controlled Cross-Over Study to Evaluate the Abuse Potential of Three Doses of GRT0151Y in Adult Non-dependent Recreational Opiate Users

The purpose of this clinical study was to evaluate whether healthy adults, who sometimes take drugs for pleasure, are likely to abuse GRT0151Y. This abuse potential is assessed at three different doses of GRT0151Y.
During a Qualification Phase, a single dose of hydromorphone IR 8 mg and a single dose of placebo were separately administered orally over 4 days in a randomized, double-blinded manner.
During the Treatment Phase, single doses of GRT0151Y free base (100 mg, 200 mg and 400 mg), hydromorphone Immediate-release (IR) (4 mg, 8 mg, and 16 mg), and placebo were administered orally over 7 Treatment Periods.
Participants received the treatments according to a 7-sequence, 7-period balanced design.

开始日期2007-06-21

申办/合作机构

Grünenthal GmbH

100 项与阿索马多相关的临床结果

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100 项与阿索马多相关的转化医学

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100 项与阿索马多相关的专利（医药）

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项与阿索马多相关的文献（医药）

2016-07-01·British Journal of Clinical Pharmacology2区 · 医学

Population pharmacokinetic/pharmacodynamic modelling of the effects of axomadol and its O‐demethyl metabolite on pupil diameter and nociception in healthy subjects

2区 · 医学

Article

作者: Bursi, Roberta ; Pastor, José Martín ; Mangas‐Sanjuan, Víctor ; Rengelshausen, Jens ; Troconiz, Iñaki F.

AimThe aim of the present study was to characterize the pharmacokinetic/pharmacodynamic (PK/PD) properties of the active components of axomadol and to quantify their contribution to observed the pupillometric and analgesic (measured through the cold pressor test) effects linking the PD engagement biomarker with clinical response.MethodsHealthy subjects (n = 74) received either placebo or axomadol orally at doses ranging from 66 mg to 225 mg following multiple dosing regimens in two separate clinical trials. Plasma concentrations of the two enantiomers of axomadol and their metabolites, and PD responses were measured at specific times. The population analysis was performed using NONMEM 7.2.ResultsThe kinetics of the parent drug and its metabolite could be described simultaneously using an extra compartment mimicking the liver, where the metabolite is formed. The SS parent compound elicited a plasma concentration‐dependent increase in pupil diameter, with estimates (percentage relative standard errors) of maximal effect (Emax) and plasma concentration exerting a half‐maximal effect (C50) of 0.79 (17.4) mm, and 90.7 (27) ng ml−1, respectively. The predicted effect site concentrations of the RR O‐demethyl metabolite decreased the pupil diameter linearly, with an estimate of the slope of 0.00967 (18.7) mm·ml ng−1. An additive model, integrating the net effect on pupil diameter, described adequately the reduction in pain with a linear function. The PK/PD model revealed that each 0.5 mm change in pupil diameter is associated with a 10% decrease in cold pressor area under the concentration–time curve effects.ConclusionsThe PK/PD analysis performed enabled the individual contributions of the active compounds to the observed effects to be identified and quantified. These effects were in accordance with the known mechanisms of action – namely, opioid agonism and noradrenaline reuptake inhibition.

100 项与阿索马多相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D03219	阿索马多	-	DB16100

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
腰痛	临床2期	美国	Grünenthal GmbH	2009-12-01
腰痛	临床2期	美国	Grunenthal SA	2009-12-01
急性疼痛	临床2期	法国	Grunenthal SA	2004-12-30
急性疼痛	临床2期	法国	Grünenthal GmbH	2004-12-30
神经痛	临床2期	欧洲	Grünenthal GmbH	-
术后疼痛	临床2期	-	Grunenthal SA	-
术后疼痛	临床2期	欧洲	Grünenthal GmbH	-