富马酸丙酚替诺福韦/埃替格韦(Tenofovir Alafenamide Fumarate/Elvitegravir) - 药物靶点：HIV integrase x RT_在研适应症：HIV感染_专利_临床

概要

基本信息

药物类型

小分子化药

别名

TAF/EVG、Tenofovir Alafenamide/Elvitegravir

靶点

HIV integrase x RT

作用方式

抑制剂

作用机制

HIV-1 integrase抑制剂(HIV整合酶抑制剂)、RT抑制剂(逆转录酶抑制剂)

治疗领域

免疫系统疾病感染泌尿生殖系统疾病

在研适应症

HIV感染

非在研适应症-

原研机构

Eastern Virginia Medical School

在研机构

Eastern Virginia Medical School

非在研机构

National Institute of Allergy & Infectious Diseases

最高研发阶段临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

登录后查看时间轴

结构/序列

分子式C23H23ClFNO5

InChIKeyJUZYLCPPVHEVSV-LJQANCHMSA-N

CAS号697761-98-1

查看全部结构式(2)

关联

2

项与富马酸丙酚替诺福韦/埃替格韦相关的临床试验

NCT06274398

/ Recruiting临床1期IIT

A Double-Blind, Placebo-Controlled, Randomized Phase 1 Study to Evaluate the Safety and Pharmacokinetics of Rectally Administered Tenofovir Alafenamide/Elvitegravir Inserts

This is a double-blind, placebo-controlled, randomized two-phase study to evaluate the safety and pharmacokinetics (PK) of two TAF/EVG inserts administered rectally for 3 consecutive days, then every other day for 14 days.

开始日期2024-01-16

申办/合作机构

Eastern Virginia Medical School

[+3]

NCT04047420

/ Completed临床1期IIT

A Phase 1 Open Label Safety and Pharmacokinetic Study of Rectal Administration of a Tenofovir Alafenamide/Elvitegravir Insert at Two Dose Levels

The purpose of this study is to evaluate the safety and pharmacokinetics of rectal administration of a tenofovir alafenamide (TAF)/elvitegravir (EVG) insert at two dose levels in HIV-uninfected individuals.

开始日期2019-12-11

申办/合作机构

National Institute of Allergy & Infectious Diseases

[+1]

100 项与富马酸丙酚替诺福韦/埃替格韦相关的临床结果

登录后查看更多信息

100 项与富马酸丙酚替诺福韦/埃替格韦相关的转化医学

登录后查看更多信息

100 项与富马酸丙酚替诺福韦/埃替格韦相关的专利（医药）

登录后查看更多信息

1

项与富马酸丙酚替诺福韦/埃替格韦相关的文献（医药）

2024-09-23·The Journal of Infectious Diseases

A Phase 1 Clinical Trial to Assess the Safety and Pharmacokinetics of a Tenofovir Alafenamide/Elvitegravir Insert Administered Rectally for HIV Prevention

Article

作者: Riddler, Sharon A ; Hoesley, Craig J ; Heard, Faye ; Bauermeister, José A ; Johnson, Sherri ; Brand, Rhonda M ; Hillier, Sharon L ; Hendrix, Craig W ; Kunjara Na Ayudhya, Ratiya Pamela ; Ho, Ken S ; Kelly, Clifton W ; Piper, Jeanna M ; Edick, Stacey ; Anderson, Peter L ; Doncel, Gustavo F

AbstractBackgroundOn-demand topical products could be an important tool for human immunodeficiency virus (HIV) prevention. We evaluated the safety, pharmacokinetics, and ex vivo pharmacodynamics of a tenofovir alafenamide/elvitegravir (TAF/EVG, 20 mg/16 mg) insert administered rectally.MethodsMTN-039 was a phase 1, open-label, single-arm, 2-dose study. Blood, rectal fluid, and rectal tissue were collected over 72 hours following rectal administration of 1 and 2 TAF/EVG inserts for each participant.ResultsTAF/EVG inserts were safe and well tolerated. EVG and tenofovir (TFV) were detected in blood plasma at low concentrations: median peak concentrations after 2 inserts were EVG 2.4 ng/mL and TFV 4.4 ng/mL. Rectal tissue EVG peaked at 2 hours (median, 2 inserts = 9 ng/mg) but declined to below limit of quantification in the majority of samples at 24 hours, whereas tenofovir diphosphate (TFV-DP) remained high >2000 fmol/million cells for 72 hours with 2 inserts. Compared to baseline, median cumulative log10 HIV p24 antigen of ex vivo rectal tissue HIV infection was reduced at each time point for both 1 and 2 inserts (P < .065 and P < .039, respectively).DiscussionRectal administration of TAF/EVG inserts achieved high rectal tissue concentrations of EVG and TFV-DP with low systemic drug exposure and demonstrable ex vivo inhibition of HIV infection for 72 hours.Clinical Trials Registration . NCT04047420.

100 项与富马酸丙酚替诺福韦/埃替格韦相关的药物交易

登录后查看更多信息

研发状态

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
HIV感染	药物发现	美国	National Institute of Allergy & Infectious Diseases	2019-12-11

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT04047420 (MTN-039, Pubmed) 人工标引	临床1期	HIV感染	-	Tenofovir Alafenamide/Elvitegravir Insert	(鬱獵醖憲廠窪簾鑰顧構) = 膚鹹鏇蓋壓襯遞衊繭壓艱襯範顧糧願選鹽鏇鏇 (淵壓壓淵淵憲顧網積顧 ) 更多	积极	2024-04-24