Delving into the Latest Updates on Tenofovir Alafenamide Fumarate/Elvitegravir with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

TAF/EVG, Tenofovir Alafenamide/Elvitegravir

Target

HIV integrase x RT

Action

inhibitors

Mechanism

HIV-1 integrase inhibitors(HIV integrase inhibitors), RT inhibitors(Viral reverse transcriptase inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication

HIV Infections

Inactive Indication-

Originator Organization

Eastern Virginia Medical School

Active Organization

Eastern Virginia Medical School

Inactive Organization

National Institute of Allergy & Infectious Diseases

License Organization-

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC23H23ClFNO5

InChIKeyJUZYLCPPVHEVSV-LJQANCHMSA-N

CAS Registry697761-98-1

View All Structures (2)

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 Deals associated with Tenofovir Alafenamide Fumarate/Elvitegravir

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
HIV Infections	Discovery	United States	National Institute of Allergy & Infectious Diseases	11 Dec 2019

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04047420 (MTN-039, Pubmed) Manual	Phase 1	HIV Infections	-	Tenofovir Alafenamide/Elvitegravir Insert	(mcsibkbyxb) = mbfsfkwrqh htpzodkofj (baojwtvlom ) View more	Positive	24 Apr 2024