Figopitant(Figopitant) - 药物靶点：NK1R_专利_临床

概要

基本信息

药物类型

小分子化药

别名

BIIF-1149

靶点

NK1R

作用方式

拮抗剂

作用机制

NK1R 拮抗剂(神经激肽-1-受体拮抗剂)

治疗领域-

在研适应症-

非在研适应症-

原研机构

C.H. Boehringer Sohn AG & Co. KG

在研机构-

非在研机构

Boehringer Ingelheim GmbH

权益机构-

最高研发阶段无进展临床1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/序列

分子式C27H31F6N3O

InChIKeyHUTHJVYJUPXHDF-DEOSSOPVSA-N

CAS号502422-74-4

关联

3

项与 Figopitant 相关的临床试验

NCT02209714

/ Completed临床1期

A Single Increasing Dose Safety, Tolerability and Pharmacodynamics (Citric Acid Challenge) Study After Oral Administration of BIIF 1149 BS (Single Doses as Tablets: 40, 65, 100 mg) in Healthy Male Volunteers (Randomised, Double-blind Within Each Dose Group, Placebo-controlled, Parallel Groups)

The objective of the study is to obtain information about the safety and tolerability of BIIF 1149 BS45 (single dose: 40, 65, 100 mg), to determine the pharmacologically active dose (range) by performing a citric acid challenge test and to obtain preliminary pharmacokinetic data.

开始日期1999-11-01

申办/合作机构

Boehringer Ingelheim GmbH

NCT02203487

/ Completed临床1期

A Double-blind (Within Dose Groups), Randomised, Placebo-controlled, Parallel-group Study to Investigate the Safety, Tolerability and Preliminary Pharmacokinetics of Increasing Repeated Oral Doses (Nine Days Treatment of 5 mg and 10 mg and Eighteen Days Treatment of 25 mg and 40 mg) of BIIF 1149 BS in Healthy Male Volunteers

The objective of the present study was to obtain information about the safety and tolerability of BIIF 1149 BS after repeated dosing and to obtain preliminary pharmacokinetics data (steady state and accumulation factor)

开始日期1999-11-01

申办/合作机构

Boehringer Ingelheim GmbH

NCT02199899

/ Completed临床1期

A Single Increasing Dose Safety, Tolerability and Pharmacodynamics (Citric Acid Challenge) Study After Oral Administration of BIIF 1149 BS (Drinking Solution, Single Doses: 0.1 - 25 mg; in Addition, at 25 mg Also as a 25 mg Tablet) in Healthy Young Male Volunteers (Randomised, Double-blind, Placebo-controlled, Parallel Groups)

The objective of the present study is to obtain information about the safety and tolerability of BIIF 1149 BS, to determine the pharmacologically active dose (range) by performing a citric acid challenge test and to obtain preliminary pharmacokinetic data

开始日期1999-03-01

申办/合作机构

Boehringer Ingelheim GmbH

100 项与 Figopitant 相关的临床结果

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100 项与 Figopitant 相关的转化医学

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100 项与 Figopitant 相关的专利（医药）

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3

项与 Figopitant 相关的文献（医药）

2024-07-11·JOURNAL OF MEDICINAL CHEMISTRY

Occurrence of “Natural Selection” in Successful Small Molecule Drug Discovery

Article

作者: Zdrazil, Barbara ; Waldmann, Herbert ; Leeson, Paul D. ; Heinzke, A. Lina ; Pahl, Axel ; Young, Robert J. ; Leach, Andrew R.

Published compounds from ChEMBL version 32 are used to seek evidence for the occurrence of "natural selection" in drug discovery. Three measures of natural product (NP) character were applied, to compare time- and target-matched compounds reaching the clinic (clinical compounds in phase 1-3 development and approved drugs) with background compounds (reference compounds). Pseudo-NPs (PNPs), containing NP fragments combined in ways inaccessible by nature, are increasing over time, reaching 67% of clinical compounds first disclosed since 2010. PNPs are 54% more likely to be found in post-2008 clinical versus reference compounds. The majority of target classes show increased clinical compound NP character versus their reference compounds. Only 176 NP fragments appear in >1000 clinical compounds published since 2008, yet these make up on average 63% of the clinical compound's core scaffolds. There is untapped potential awaiting exploitation, by applying nature's building blocks─"natural intelligence"─to drug design.

2012-03-01·Drug metabolism and disposition: the biological fate of chemicals2区 · 医学

Investigation of Figopitant and Its Metabolites in Rat Tissue by Combining Whole-Body Autoradiography with Liquid Extraction Surface Analysis Mass Spectrometry

2区 · 医学

Article

作者: Sandel, Jan ; Kallbach, Susanne ; Schadt, Simone ; Almeida, Reinaldo

This article describes the combination of whole-body autoradiography with liquid extraction surface analysis (LESA) and mass spectrometry (MS) to study the distribution of the tachykinin neurokinin-1 antagonist figopitant and its metabolites in tissue sections of rats after intravenous administration of 5.0 mg/kg figopitant. An overview of autoradiography results is presented together with mass spectrometry identification and semiquantification of parent drug and its metabolites based on LESA-MS. The quality and accuracy of data generated by LESA-MS were assessed in comparison with classic tissue extraction, sample cleanup, and high-performance liquid chromatography analysis. The parent drug and the N-dealkylated metabolite M474(1) (BIIF 1148) in varying ratios were the predominant compounds in all tissues investigated. In addition, several metabolites formed by oxygenation, dealkylation, and a combination of oxygenation and dealkylation were identified. In summary, the LESA-MS technique was shown to be a powerful tool for identification and semiquantification of figopitant and its metabolites in different tissues and was complementary to quantitative whole-body autoradiography for studying the distribution.

ChemRxiv : the preprint server for chemistry

Occurrence of 'natural selection' in successful small molecule drug discovery

作者: Zdrazil, Barbara ; Waldmann, Herbert ; Leeson, Paul D. ; Heinzke, A. Lina ; Pahl, Axel ; Young, Robert J. ; Leach, Andrew R.

The historical application of mols. of natural origin as starting points for drug discovery has largely been replaced by today's primary hit-seeking strategies of library screening (diversity-based, fragment-based, knowledge-based, virtual) and exploitation of known compoundAccordingly, the computed natural product (NP) probability score of approved oral drugs has fallen significantly for drugs invented after 1990, when primary in vitro screening at cloned human targets began to be widely adopted.Pseudo-natural products (PNPs) provide a new approach to quantifying the appearance of NP structural elements.The aim of this work is to seek further support for the existence of natural selection in drug discovery.We employ a highly curated dataset 22 from ChEMBL (version 32) 23 to assess the impact of quant. NP measures, including the presence of PNPs, in marketed drugs and phase 1-3 clin. compounds in comparison with a background of relevant, target-matched reference compounds

100 项与 Figopitant 相关的药物交易

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