Delving into the Latest Updates on Felbinac with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Felbinac (JP17/USAN/INN), Felbinac tape, Felbinac transdermal

+ [18]

Target

COX

Mechanism

COX inhibitors(Cyclooxygenases inhibitors)

Therapeutic Areas

Immune System DiseasesNervous System DiseasesSkin and Musculoskeletal Diseases+ [1]

Active Indication

Low Back PainBursitisMusculoskeletal Pain+ [3]

Inactive Indication

Soft Tissue Injuries

Originator Organization

Teikoku Seiyaku Co. Ltd.

Active Organization

Teikoku Seiyaku Co. Ltd.

Henan Lingrui Pharmaceutical Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

JP (25 Sep 1986),

BursitisMusculoskeletal PainOsteoarthritis+ [2]

Regulation-

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Structure

Molecular FormulaC14H12O2

InChIKeyQRZAKQDHEVVFRX-UHFFFAOYSA-N

CAS Registry5728-52-9

The clinical use of chemotherapy for refractory osteosarcoma (OS) is limited due to its multiorgan toxicity. To overcome this challenge, new dosage forms and combination treatments, such as phototherapy, are being explored to improve targeted delivery and cytocompatibility of chemotherapeutic agents. In addition, inducing ferroptosis in iron-rich tumors could be a promising strategy to enhance OS therapy. In this study, a novel formulation was developed using natural biological H-ferritin (HFn) encapsulating the photosensitizer IR-780 and the chemotherapy drug gemcitabine (Gem) for OS-specific targeted therapy (HFn@Gem/IR-780 NPs). HFn@Gem/IR-780 NPs were designed to specifically bind and internalize into OS cells by interacting with transferrin receptor 1 (TfR1) which is overexpressed on the surface of OS cell membranes. The Gem and IR-780 were then released responsively under mildly acidic conditions in tumors. HFn@Gem/IR-780 NPs achieved cascaded antitumor therapeutic efficacy through the combination of chemotherapy and phototherapy under near-infrared irradiation in vitro and in vivo. Importantly, HFn@Gem/IR-780 NPs demonstrated excellent safety profile with significantly decreased drug exposure to normal organs, indicating its potential for reducing systemic toxicity. Thus, utilizing HFn as a vehicle to encapsulate highly effective antitumor drugs provides a promising approach for the treatment of OS metastasis and relapse.

27 Nov 2023·Angewandte Chemie International Edition

Photoinduced [3+2] Cycloaddition of Carbenes and Nitriles: A Versatile Approach to Oxazole Synthesis

Article

Author: Maiti, Debajit ; Guin, Srimanta ; Sen, Chiranjit ; Saha, Argha ; Sen, Subhabrata ; Maiti, Debabrata ; Das, Chandan

AbstractWe have developed a photoinduced protocol for the synthesis of pharmaceutically important oxazole molecules using diazo‐ and nitrile‐containing reactants. The process involves the initial photolysis of the diazo compound to afford singlet carbenes, which are tapped by nitriles in a [3+2] cycloaddition fashion to give substituted oxazoles. With di‐nitrile compounds, useful bis‐oxazoles were obtained. The applicability of the transformation is showcased through the expedient synthesis of small‐molecule drugs and biologically relevant molecules such as felbinac, pimprinine, texamine, ugnenenazole etc. The protocol is also useful for the generation of 2H and 13C isotope labelled oxazoles. Merging photolysis with continuous‐flow chemistry was demonstrated for scaling up the reaction. The non‐requirement of metal catalysis or photosensitizers to harness the light energy with blue light sufficing the execution of the reaction makes it a versatile and general protocol for the synthesis of structurally diverse oxazoles

19 Jun 2023·Chemistry – A European Journal

Continuous‐Flow Suzuki‐Miyaura Coupling in Water and Organic Solvents Promoted by Blends of Stabilized Convoluted Polymeric Palladium Catalysts and Polymeric Auxiliary Materials

Article

Author: Takaya, Hikaru ; Yamada, Yoichi M A ; Zhang, Zhenzhong ; Ohno, Aya

AbstractGiven that heterogeneous palladium‐catalyzed C−C bond formation reactions under continuous‐flow conditions are well suited for the efficient and safe production of pharmaceuticals and functional materials, the development of active and durable catalysts for this purpose is a matter of high practical significance. Here, a previously established molecular convolution methodology was used to synthesize catalysts for Suzuki‐Miyaura coupling under flow conditions by blending convoluted polymeric palladium catalysts (prepared from copolymers of 4‐vinylpyridine and 4‐tert‐butylstyrene) and crosslinked polymeric auxiliary materials (prepared from copolymers of divinylbenzene and 4‐tert‐butylstyrene). The optimal catalyst exhibited high performance and durability and allowed numerous biaryl products such as liquid‐crystalline materials, organic electroluminescent materials, and pharmaceuticals to be continuously synthesized with turnover frequencies of up to 238 h−1. In a demonstration of practical utility, the developed catalytic system was used for the continuous synthesis of two pharmaceuticals (felbinac and fenbufen) in water as the sole solvent.

100 Deals associated with Felbinac

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External Link

KEGG	Wiki	ATC	Drug Bank
D01675	Felbinac	M02AA08	DB07477

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Low Back Pain	JP	Teikoku Seiyaku Co. Ltd.	28 Feb 1989
Bursitis	JP	Teikoku Seiyaku Co. Ltd.	25 Sep 1986
Musculoskeletal Pain	JP	Teikoku Seiyaku Co. Ltd.	25 Sep 1986
Osteoarthritis	JP	Teikoku Seiyaku Co. Ltd.	25 Sep 1986
Post-traumatic pain	JP	Teikoku Seiyaku Co. Ltd.	25 Sep 1986
Tenosynovitis	JP	Teikoku Seiyaku Co. Ltd.	25 Sep 1986

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Osteoarthritis	Phase 2	CN	Henan Lingrui Pharmaceutical Co., Ltd.	21 Jan 2014
Soft Tissue Injuries	Discovery	CN	Henan Lingrui Pharmaceutical Co., Ltd.	15 Nov 2011