Delving into the Latest Updates on L-756423 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

HIV-1 protease

Mechanism

HIV-1 protease inhibitors(HIV protease inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication-

Inactive Indication

HIV Infections

Originator Organization

Merck & Co., Inc.

Active Organization-

Inactive Organization

Merck Sharp & Dohme Corp.

Drug Highest PhaseSuspendedPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC39H48N4O5

InChIKeyAOMZDQMIOCTPQP-QHQMVRJISA-N

CAS Registry216863-66-0

This study will see how safe and effective against HIV the drugs L-756423 plus indinavir (IDV) are compared to just IDV when taken with stavudine (d4T) and lamivudine (3TC). The study will also see whether taking 1 large dose of L-756423/IDV once a day is as safe and effective as taking 2 smaller doses twice a day.

Start Date-

Sponsor / Collaborator

Merck Sharp & Dohme Corp.

100 Clinical Results associated with L-756423

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100 Translational Medicine associated with L-756423

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100 Patents (Medical) associated with L-756423

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3

Literatures (Medical) associated with L-756423

01 Apr 2002·Nihon rinsho. Japanese journal of clinical medicine

[New HIV-1 protease inhibitors in development].

Review

Author: Maeda, Kenji ; Yoshimura, Kazuhisa

Protease inhibitors block the protease enzyme of HIV-1. When new viral particles break off from an infected cell, protease cuts long protein strands into the parts needed to assemble a mature virus. When protease is blocked, the new viral particles cannot mature. Protease inhibitors being tested in humans include Atazanavir, GW433908, L-756,423, Mozenavir(DMP-450), Tipranavir and more. Several firms are trying to develop a new type of protease inhibitor that will be the more favorable pharmacokinetic and resistance profiles compared with currently available drugs. We cannot expect that every one of the drugs listed in this paper will be successfully developed. However, it is likely that significant clinical advancements can be made with those that are proven to be active and safe for patients in need.

01 Dec 2000·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

High-throughput simultaneous determination of the HIV protease inhibitors indinavir and L-756423 in human plasma using semi-automated 96-well solid phase extraction and LC–MS/MS

Q3 · MEDICINE

Article

Author: K.C Yeh ; B.K Matuszewski ; L Lin ; M.P Braun ; R Eisenhandler ; E.J Woolf ; M.J Rose ; J Hsieh ; W Fang ; G.J Gatto ; S.A Merschman

A method for the simultaneous determination of the HIV protease inhibitors indinavir and L-756423, in human plasma has been developed. Plasma samples (0.5 ml) were extracted using a 3M Empore 96-well plate in the mixed phase cation exchange (MPC) format. The extraction method was automated through the application of both the Packard 204DT and TOMTEC Quadra 96 work stations, and the resulting extracts were analyzed using a PE-Sciex API-3000 LC-MS/MS with a heated nebulizer interface (500 degrees C). The assay was linear in the concentration range 1-2500 ng/ml for indinavir and 5 2500 ng/ml for L-756423 when 0.5-ml aliquots of plasma were extracted. Recoveries of indinavir and L-756423 were greater than 76 and 80%, respectively, over the calibration curve range when using the described sample preparation method. Within-batch precision and accuracy for the quantitation of indinavir over the range 1-2500 ng/ml were 5.4% R.S.D. or less and within 4.0%, respectively. Within-batch precision and accuracy for the quantitation of L-756423 over the range 5-2500 ng/ml were 5.3% R.S.D. or less and within 3.4%, respectively. Interbatch variability for the analysis of indinavir QC samples at low (3 ng/ml), middle (250 ng/ml) and high (2250 ng/ml) were 3.2, 2.9, and 1.9%, respectively. Interbatch variability for the analysis of L-756423 QC samples at low (15 ng/ml), middle (250 ng/ml) and high (2250 ng/ml) concentration were 2.0, 2.5, and 3.3%, respectively. The validated assay was used in support of human clinical trials.

01 Sep 1999·Journal of Chromatography B: Biomedical Sciences and Applications

Determination of L-756 423, a novel HIV protease inhibitor, in human plasma and urine using high-performance liquid chromatography with fluorescence detection

Article

Author: Bogdan K Matuszewski ; Mark J Rose ; Sheila A Merschman ; Eric J Woolf

A method for the determination of L-756 423, a novel HIV protease inhibitor, in human plasma and urine is described. Plasma and urine samples were extracted using 3M Empore extraction disk cartridges in the C18 and MPC (mixed-phase cation-exchange) formats, respectively. The extract was analyzed using HPLC with fluorescence detection (ex 248 nm, em 300 nm), and included a column switching procedure to reduce run-time. The assay was linear in the concentration range 5 to 1000 ng/ml when 1-ml aliquots of plasma and urine were extracted. Recoveries of L-756 423 were greater than 84% over the calibration curve range using the described sample preparation procedures. Intra-day precision and accuracy for this assay was less than 9% RSD and within 7%, respectively. Inter-day variabilities for the plasma (n=17) and urine (n= 10) were less than 5% and 3% for low (15 ng/ml) and high (750 ng/ml) quality control samples. Bovine serum albumin (0.5%) was used as an additive to urine to prevent precipitation of L-756 423 during the storage of clinical samples. The assay was used in support of human clinical trials.

100 Deals associated with L-756423

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