Delving into the Latest Updates on Bevirimat Dimeglumine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Bevirimat, Bevirimat dimeglumine (USAN)

+ [11]

Target

HIV-1 capsid

Action

inhibitors

Mechanism

HIV-1 capsid inhibitors(HIV-1 capsid inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesUrogenital Diseases

Active Indication-

Inactive Indication

HIV InfectionsHIV Seropositivity

Originator Organization

Myrexis, Inc.

Active Organization-

Inactive Organization

Myrexis, Inc.

License Organization

Panacos Pharmaceuticals, Inc.

Myrexis, Inc.

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC36H56O6

InChIKeyYJEJKUQEXFSVCJ-WRFMNRASSA-N

CAS Registry174022-42-5

View All Structures (2)

A Phase 2b Multicenter, Randomized, Open Label, Comparative Trial of MPC-4326 in Combination With a Two to Three Drug Optimized Background Regimen Versus an Optimized, Three to Four Drug Antiretroviral Regimen for the Treatment of Triple Class Antiretroviral Experienced, HIV-1 Infected Subjects Failing Current Therapy

This phase 2b study is designed to assess the long-term efficacy (24 weeks) of MPC-4326 in combination with a 2-3 drug optimized background regimen (OBR) relative to the efficacy of a 3-4 antiretroviral (ARV) regimen in treatment experienced, HIV-1 infected subjects.

Start Date01 Nov 2009

Sponsor / Collaborator

Myrexis, Inc.

NCT01097070

/ CompletedPhase 2

A Phase II Multicenter, Open-label, Randomized, Parrallel Group Study to Assess the Pharmacokinetics of Bevirimat (BVM) 100 mg Tablets Administered to HIV-1 Positive Patients for 15 Days

The purpose of this study is to evaluate the safety, tolerability, and pharmacokinetics (behavior in the body) of bevirimat administered for 15 days to HIV-positive individuals.

Start Date01 Nov 2008

Sponsor / Collaborator

Myrexis, Inc.

NCT00967187

/ CompletedPhase 2

A Phase II Multicenter, Open-label, Randomized, Parallel Group, Study of Bevirimat in HIV-1 Positive Patients to Evaluate the Safety, Efficacy, and Pharmacokinetics of MPC-4326 Administered as Monotherapy for 14 Days and as Part of an Optimized Background Regimen for up to 72 Weeks.

To evaluate the antiretroviral activity and safety of 200 mg BID and 300 mg BID doses of MPC-4326 administered as monotherapy for 14 days to HIV-1 positive patients. Patients with an initial treatment response will have the option to continue MPC-4326 in combination with an Optimized Backround Regimen for a maximum of 72 weeks.

Start Date01 May 2008

Sponsor / Collaborator

Myrexis, Inc.

100 Clinical Results associated with Bevirimat Dimeglumine

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100 Translational Medicine associated with Bevirimat Dimeglumine

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100 Patents (Medical) associated with Bevirimat Dimeglumine

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181

Literatures (Medical) associated with Bevirimat Dimeglumine

01 Apr 2025·Journal of Molecular Structure

Design, synthesis and biological evaluation of a 1,2,3-triazolyl-bearing betulinic acid derivatives as α-glucosidase inhibitors

Author: Xiong, Zhuang ; Chen, Wen-Hua ; Xu, Xuetao ; Zhang, Yufei ; Sun, Jinping ; Liu, Jingjing ; Min, Xiaofeng ; Liang, Bingwen ; Li, Jiangyi

In this study, a series of betulinic acid (BA) derivatives incorporating a 1,2,3-triazolyl unit, i.e., compounds c1 - c21 and d1 - d21 were synthesized and evaluated for their inhibitory activity toward α-glucosidase.All the derivatives exhibited excellent inhibition against α-glucosidase, and compound d2 was the most active (IC₅₀ = 0.89 ± 0.025 μM).Inhibition kinetics showed that compound d2 was a mixed-type inhibitor for α-glucosidase.The anal. of three-dimensional fluorescence and CD spectra suggested that compound d2 exerted its inhibitory activity by changing the conformation of α-glucosidase.Mol. docking revealed that compound d2 was well embedded into the active pocket of α-glucosidase through hydrogen-bonding and hydrophobic interactions.In vivo experiments showed that compound d2 not only reduced the level of fasting blood glucose, but also improved glucose tolerance and dyslipidemia.The present findings suggest that compound d2 has high potential as an α-glucosidase inhibitor for the treatment of type 2 diabetes.

21 Sep 2024·Journal of Biomolecular Structure and Dynamics

Construction of a HIV-1 subtype C 3D model using homology modeling and in-silico docking, molecular dynamics simulation, and MM-GBSA calculation of second-generation HIV-1 maturation inhibitor(s).

Article

Author: Pal, Sapna ; Gaur, Ritu ; Nitz, T J ; K C, Yuvraj ; Wild, Carl

Maturation inhibitors (MIs) efficiently block HIV-1 maturation by inhibiting the cleavage of the capsid protein and spacer peptide 1 (CA-SP1) leading to the production of immature and non-infectious virus particles. We have previously reported that second-generation MIs were more potent than bevirimat (BVM) against HIV-1 subtype C. In-silico studies on interaction of with BVM and their analogs have been limited to HIV-1 subtype B(5I4T) due to lack of an available 3D structure for HIV-1 subtype C virus. In our current study, we have developed a 3D model of HIV-1C Gag CA-SP1 region using protein homology modeling with HIV-1 subtype B(514T) as a template. The HIV-1 C homology model generated was extensively validated using several online tools and served as a template to perform molecular docking studies with eight well-characterized MIs. The docked complex of HIV-1C and all nine MIs was subjected to molecular dynamics simulation for 100 ns using AMBER and binding free energy calculations were done using MM-GBSA. Based on our data, CV8611 exhibited highest binding energy of -6.5 Kcal/mol among all BVM analogs. CV8611 formed strong interactions with Gly222 and Met235 of HIV-1C Gag CA-SP1 during MD simulation and remained intact. The root mean square deviation and root mean square fluctuation values of the complex were stable during the simulations. Our study is the first to report construction and validation of 3D model for the HIV-1C Gag CA-SP1, which could serve as a crucial tool in the structure-aided design of novel and broadly acting maturation inhibitors.Communicated by Ramaswamy H. Sarma.

01 May 2023·Chemical and Pharmaceutical Bulletin

Computational Screening of Inhibitory Compounds for SARS-Cov-2 3CL Protease with a Database Consisting of Approved and Investigational Chemicals

Article

Author: Hata, Masayuki ; Hoshino, Tyuji ; Yamamoto, Norio ; Miwa, Kazunori ; Guo, Yan

Computational screening is one of the fundamental techniques in drug discovery. Each compound in a chemical database is bound to the target protein in virtual, and candidate compounds are selected from the binding scores. In this work, we carried out combinational computation of docking simulation to generate binding poses and molecular mechanics calculation to estimate binding scores. The coronavirus infectious disease has spread worldwide, and effective chemotherapy is strongly required. The viral 3-chymotrypsin-like (3CL) protease is a good target of low molecular-weight inhibitors. Hence, computational screening was performed to search for inhibitory compounds acting on the 3CL protease. As a preliminary assessment of the performance of this approach, we used 51 compounds for which inhibitory activity had already been confirmed. Docking simulations and molecular mechanics calculations were performed to evaluate binding scores. The preliminary evaluation suggested that our approach successfully selected the inhibitory compounds identified by the experiments. The same approach was applied to 8820 compounds in a database consisting of approved and investigational chemicals. Hence, docking simulations, molecular mechanics calculations, and re-evaluation of binding scores including solvation effects were performed, and the top 200 poses were selected as candidates for experimental assays. Consequently, 25 compounds were chosen for in vitro measurement of the enzymatic inhibitory activity. From the enzymatic assay, 5 compounds were identified to have inhibitory activities against the 3CL protease. The present work demonstrated the feasibility of a combination of docking simulation and molecular mechanics calculation for practical use in computational virtual screening.

100 Deals associated with Bevirimat Dimeglumine

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External Link

KEGG	Wiki	ATC	Drug Bank
D06564	Bevirimat Dimeglumine	-	DB06581

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
HIV Seropositivity	Phase 2	Australia	Myrexis, Inc.	01 May 2008
HIV Infections	Phase 2	United States	Myrexis, Inc.	01 Apr 2006

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


IAS2011	Not Applicable	HIV Infections	-	Bevirimat	dsuozmvput(emuysyoyqd) = kxsakkqzhf ihlkbsjffh (nzdsrtraik )	-	01 Jan 2011
IAS2007	Not Applicable	HIV Infections	165	Bevirimat (BVM) 25-200mg	jzybssvebp(fzskyevliq) = headache, 6-24%; dizziness, 0-24% siuludokae (pfkmzucfud ) View more	-	01 Jan 2007
IAS2006	Not Applicable	-	-	450 mg/kg/day PA-457	(eiwpkucuvv) = loaclhwjbl lwwwviovgz (yvoazaycfy ) View more	-	01 Jan 2006
IAS2006	Not Applicable	-	-	900 mg/kg/day PA-457	(eiwpkucuvv) = nqrnophnzm lwwwviovgz (yvoazaycfy ) View more	-	01 Jan 2006