Delving into the Latest Updates on Meisoindigo with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Natura-α

Target-

Action-

Mechanism-

Therapeutic Areas

Neoplasms

Active Indication

Neoplasms

Inactive Indication

Colitis, UlcerativeProstatic CancerSystemic Lupus Erythematosus+ [1]

Originator Organization

Beijing Union Pharmaceutical Factory

Active Organization

Beijing Union Pharmaceutical Factory

Inactive Organization

Natrogen Therapeutics International, Inc.Takeda Pharmaceuticals International AG

Takeda Pharmaceutical Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

China (01 Jan 2001),

Neoplasms

Regulation-

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Structure/Sequence

Molecular FormulaC17H12N2O2

InChIKeyQNOCRUSVMMAKSC-UHFFFAOYSA-N

CAS Registry97207-47-1

This study is to evaluate the efficacy and tolerability of multiple oral doses of Natura-alpha capsule administered to patients with active ulcerative colitis. This will be a randomized, double-blind, placebo-controlled, parallel-design study. Up to 75 patients will complete this study (20 to 25 patients per treatment group) at approximately 10-12 clinical sites in the Unites States. Patients will be assigned at a 1:1:1 ratio to receive placebo, Natura-alpha 10 mg or Natura-alpha 20 mg, b.i.d. Replacement patients may be added, pending Sponsor approval, if it appears that less than 60 patients will complete the study.

Start Date01 Jul 2010

Sponsor / Collaborator

Natrogen Therapeutics International, Inc.

100 Clinical Results associated with Meisoindigo

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100 Translational Medicine associated with Meisoindigo

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100 Patents (Medical) associated with Meisoindigo

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78

Literatures (Medical) associated with Meisoindigo

01 Feb 2025·Journal of Medical Virology

Systematic Reevaluation of Repurposed Drugs Against the Main Protease of SARS‐CoV‐2 via Combined Experiments

Article

Author: Zhou, Jiahao ; Xu, Tao ; Ye, Jiankai ; Chen, Yunyu ; Liu, Xiaoping ; Zhang, Rui

ABSTRACTThe main protease (Mpro) of SARS‐CoV‐2 is an attractive drug target for antivirals, as this enzyme plays a key role in virus replication. Drug repurposing is a promising option for the treatment of coronavirus disease 2019 (COVID‐19). Recently, a number of FDA‐approved drugs have been identified as Mpro inhibitors, but stringent hit validation is lacking. In this study, we rigorously reevaluated the in vitro inhibition of the Mpro enzyme by repurposed drugs via combined experiments, including the fluorescence resonance energy transfer (FRET) assay, fluorescence polarization (FP) assay, and protease biosensor cleavage assay. Our results from a set of in vitro assays revealed that boceprevir is a potential Mpro inhibitor, but other repurposed drugs, including atazanavir, dipyridamole, entrectinib, ethacridine, glecaprevir, hydroxychloroquine, ivermectin, meisoindigo, pelitinib, raloxifene, roxatidine acetate, saquinavir, teicoplanin, thonzonium bromide, and valacyclovir, are not. Our research highlights that the use of candidate Mpro inhibitors from primary screening warrants further comprehensive studies before the reporting of new findings.

01 Oct 2024·Dyes and Pigments

From indigo to isoindigo: Rationalizing the high efficiency of photoprotective molecular mechanisms

Author: Seixas de Melo, J. Sergio ; Cunha, Carla

Indigo (IND) and its natural derivatives, including Tyrian purple and indirubin (INR), are examples of mols. with a history of millions of years.They also illustrate mol. evolution and longevity, linked to their extraordinary mol. stability associated with excited state decay mechanisms.In the excited state, these mols. efficiently undergo a radiationless deactivation process resulting in negligible fluorescence and triplet state formation (less than 0.1% of the quantum loss in indigo for both processes).Here, we demonstrate that in isoindigo (ISO) this process is even more efficient than in IND, resulting in nearly 100% of the excited state deactivation.In IND, the mol. mechanism behind this decay process involves intramol. proton transfer (ESPT).In the case of INR, ESPT efficiently competes with the formation of a conformational species -the syn-rotamer- for deactivation to the ground state.With ISO, the ESPT process is absent.Instead, the deactivation mechanism involves a rotation of a few degrees around the central C-C bond, aRotational Isomerization (RI).This rotation leads to a sloped conical intersection (CI), making the radiationless deactivation process more efficient than the ESPT found with IND.

01 Jul 2024·European Journal of Medicinal Chemistry

Discovery of meisoindigo derivatives as noncovalent and orally available Mpro inhibitors: their therapeutic implications in the treatment of COVID-19

Article

Author: Zhou, Yuzheng ; Xia, Zanxian ; Fan, Jinbao ; Ke, Shufen ; Wang, Yuxuan ; Liu, Sixu ; Fan, Kaiqiang ; Deng, Xu ; Zhou, Yingjun ; Gao, Qingtian ; Zhou, Yuqing

The progressive emergence of SARS-CoV-2 variants has necessitated the urgent exploration of novel therapeutic strategies to combat the COVID-19 pandemic. The SARS-CoV-2 main protease (M^pro) represents an evolutionarily conserved therapeutic target for drug discovery. This study highlights the discovery of meisoindigo (Mei), derived from the traditional Chinese medicine (TCM) Indigo naturalis, as a novel non-covalent and nonpeptidic M^pro inhibitor. Substantial optimizations and structure-activity relationship (SAR) studies, guided by a structure-based drug design approach, led to the identification of several Mei derivatives, including S5-27 and S5-28, exhibiting low micromolar inhibition against SARS-CoV-2 M^pro with high binding affinity. Notably, S5-28 provided significant protection against wild-type SARS-CoV-2 in HeLa-hACE2 cells, with EC₅₀ up to 2.66 μM. Furthermore, it displayed favorable physiochemical properties and remarkable gastrointestinal and metabolic stability, demonstrating its potential as an orally bioavailable drug for anti-COVID-19 therapy. This research presents a promising avenue for the development of new antiviral agents, offering hope in the ongoing battle against COVID-19.

100 Deals associated with Meisoindigo

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External Link

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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Neoplasms	China	Beijing Union Pharmaceutical Factory	01 Jan 2001

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Ulcerative colitis, active severe	Phase 2	United States	Natrogen Therapeutics International, Inc.	01 Jul 2010
Colitis, Ulcerative	Phase 2	United States	Takeda Pharmaceuticals International AG	-
Colitis, Ulcerative	Phase 2	European Union	Takeda Pharmaceuticals International AG	-
Prostatic Cancer	Phase 2	United States	Natrogen Therapeutics International, Inc.	-
Systemic Lupus Erythematosus	Phase 2	United States	Natrogen Therapeutics International, Inc.	-