Delving into the Latest Updates on Aminosalicylic acid with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

AMINOSALICYLIC ACID RESIN COMPLEX, Aminosalicylic acid (USP), para-aminosalicylic acid

+ [7]

Target-

Mechanism-

Therapeutic Areas

Infectious Diseases

Active Indication

Tuberculosis, Multidrug-Resistant

Inactive Indication

Crohn Disease

Originator Organization

Eurocept International B.V.

Active Organization

Eurocept International B.V.

Inactive Organization

Bristol Myers Squibb Co.Jacobus Pharmaceutical Co., Inc.

Drug Highest PhaseApproved

First Approval Date

EU (07 Apr 2014),

Tuberculosis, Multidrug-Resistant

RegulationOrphan Drug (EU)

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Structure

Molecular FormulaC7H7NO3

InChIKeyWUBBRNOQWQTFEX-UHFFFAOYSA-N

CAS Registry65-49-6

Para-aminosalicylic acid enteric-coated granules (4 g) produced by Chongqing Huabang Pharmaceutical Co., Ltd. was used as the test preparation (T). According to the relevant provisions of bioequivalence tests, a bioequivalence test was conducted with para-aminosalicylic acid enteric-coated granules (4 g, PASER®) produced by Jacobus Pharmaceutical as the reference preparation (R).

Start Date13 Sep 2018

Sponsor / Collaborator

Chongqing Huapont Pharmaceutical Co. Ltd.

CTR20181586 / Completed

对氨基水杨酸肠溶颗粒的随机、开放、单次给药、双周期、双交叉空腹预BE试验

[Translation] A randomized, open-label, single-dose, two-period, double-crossover fasting pre-BE trial of p-aminosalicylic acid enteric-coated granules

以重庆华邦制药有限公司生产的对氨基水杨酸肠溶颗粒为受试制剂，按有关生物等效性试验的规定，与JACOBUS PHARMACEUTICAL公司生产的对氨基水杨酸肠溶颗粒（商品名：PASER®）进行人体生物利用度与生物等效性试验，比较受试制剂和参比制剂是否生物等效。

[Translation]

Using p-aminosalicylic acid enteric-coated granules produced by Chongqing Huabang Pharmaceutical Co., Ltd. as the test preparation, human bioavailability and bioequivalence tests were conducted with p-aminosalicylic acid enteric-coated granules (trade name: PASER®) produced by Jacobus Pharmaceutical Co., Ltd. in accordance with the relevant provisions of bioequivalence tests to compare whether the test preparation and the reference preparation are bioequivalent.

Start Date15 Jan 2018

Sponsor / Collaborator

Chongqing Huapont Pharmaceutical Co. Ltd.

CTR20171464 / Completed

对氨基水杨酸肠溶颗粒的随机、开放、单次给药、双周期、双交叉空腹预BE试验

[Translation] A randomized, open-label, single-dose, two-period, double-crossover fasting pre-BE trial of p-aminosalicylic acid enteric-coated granules

以重庆华邦制药有限公司生产的对氨基水杨酸肠溶颗粒为受试制剂，与JACOBUS PHARMACEUTICAL公司生产的对氨基水杨酸肠溶颗粒（商品名：PASER）进行人体生物利用度与生物等效性试验，比较受试制剂和参比制剂是否生物等效。

[Translation]

The p-aminosalicylic acid enteric-coated granules produced by Chongqing Huabang Pharmaceutical Co., Ltd. were used as the test preparation, and a human bioavailability and bioequivalence study was conducted with p-aminosalicylic acid enteric-coated granules (trade name: PASER) produced by Jacobus Pharmaceutical to compare whether the test preparation and the reference preparation are bioequivalent.

Start Date13 Nov 2017

Sponsor / Collaborator

Chongqing Huapont Pharmaceutical Co. Ltd.

100 Clinical Results associated with Aminosalicylic acid

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100 Translational Medicine associated with Aminosalicylic acid

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100 Patents (Medical) associated with Aminosalicylic acid

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1,758

Literatures (Medical) associated with Aminosalicylic acid

31 Dec 2024·Emerging Microbes & Infections

The T120P or M172V mutation on rv2172c confers high level para -aminosalicylic acid resistance in Mycobacterium tuberculosis

Article

Author: Deng, Jiao-Yu ; Yu, Ji-Fang ; Yang, Ping ; Feng, Ao ; Yu, Hong-Jun ; Cheng, Tao ; Xu, Jin-Tian ; Gu, Jing

Although para-aminosalicylic acid (PAS) has been used to treat tuberculosis for decades, mechanisms of resistance to this drug in Mycobacterium tuberculosis (M. tuberculosis) clinical isolates have not been thoroughly investigated. Previously, we found that decreased methylenetetrahydrofolate reductase (MTHFR) activity of Rv2172c led to increased sensitivity to antifolates in M. tuberculosis. In this study, we collected the genome-sequencing data of 173 PAS-resistant and 803 PAS-sensitive clinical isolates and analyzed rv2172c mutations in those 976 isolates. The results showed that two mutations (T120P and M172V) on rv2172c could be identified in a certain proportion (6.36%) of PAS-resistant isolates. The results of AlphaFold2 prediction indicated that the T120P or M172V mutation might affect the enzymatic activity of Rv2172c by influencing nicotinamide adenine dinucleotide (NADH) binding, and this was verified by subsequent biochemical analysis, demonstrating the role of residues Thr120 and Met172 on NADH binding and enzymatic activity of Rv2172c. In addition, the effect of rv2172c T120P or M172V mutation on methionine production and PAS resistance was determined in M. tuberculosis. The results showed that both T120P and M172V mutations caused increased intracellular methionine concentrations and high level PAS resistance. In summary, we discovered new molecular markers and also a novel mechanism of PAS resistance in M. tuberculosis clinical isolates and broadened the understanding of the NADH-dependent MTHFR catalytic mechanism of Rv2172c in M. tuberculosis, which will facilitate the molecular diagnosis of PAS resistance and also the development of new drugs targeting Rv2172c.

01 Oct 2024·Analytica Chimica Acta

New screen-printed electrodes for Raman spectroelectrochemistry. Determination of p-aminosalicylic acid

Article

Author: Perales-Rondon, Juan V ; del Campo, F. Javier ; Colina, Alvaro ; Nuñez-Marinero, Pello ; Heras, Aranzazu ; Del Campo, F Javier ; Romay, Luis ; Perales-Rondon, Juan V.

BACKGROUNDThe availability of new surface enhanced Raman scattering (SERS) substrates is essential to develop quantitative analytical methods. Electrochemistry is an easy, fast and reproducible methodology to prepare SERS substrates on screen-printed electrodes (SPEs).RESULTSThis work proposes new SPEs based on a three-electrode system all made of silver. Using the same ink for the whole electrode system facilitates the fabrication process, reduces production costs, and leads to excellent analytical performance. The results showed that Raman enhancement depends strongly on the type of silver ink. To demonstrate the capabilities of the new electrodes developed, 4-aminosalicylic acid was determined in complex matrices and in the presence of strong interfering compounds such as salicylic acid and acetylsalicylic acid. The proposed analytical method is based on the electrochemical surface oxidation enhanced Raman scattering (EC-SOERS) strategy. AgCl nanocrystals are generated on the working electrode surface, which amplify the Raman signal of 4-aminosalicylic acid. Good figures of merit were obtained both in the absence and in the presence of the interfering compounds, achieving a correct estimation of a 4-aminosalicylic test sample in complex matrices.SIGNIFICANCEThe new SPEs have been demonstrated to be very sensitive and reproducible which, together to the high specificity of the Raman signal, makes this methodology very attractive for chemical analysis.

06 Aug 2024·Microbiology Spectrum

Evaluation of WHO catalog of mutations and five WGS analysis tools for drug resistance prediction of Mycobacterium tuberculosis isolates from China

Article

Author: Yang, Yang ; He, Guiqing ; Zheng, Qingyong ; Shi, Jichan ; Wu, Lianpeng ; Huang, Bei

ABSTRACT The continuous advancement of molecular diagnostic techniques, particularly whole-genome sequencing (WGS), has greatly facilitated the early diagnosis of drug-resistant tuberculosis patients. Nonetheless, the interpretation of results from various types of mutations in drug-resistant-associated genes has become the primary challenge in the field of molecular drug-resistance diagnostics. In this study, our primary objective is to evaluate the diagnosis accuracy of the World Health Organization (WHO) catalog of mutations and five WGS analysis tools (PhyResSE, Mykrobe, TB Profiler, Gen-TB, and SAM-TB) in drug resistance to 10 anti- Mycobacterium tuberculosis (MTB) drugs. We utilized the data of WGS collected between 2014 and 2017 in Zhejiang Province, consisting of 110 MTB isolates as detailed in our previous study. Based on phenotypic drug susceptibility testing (DST) results using the proportion method on Löwenstein-Jensen medium with antibiotics, we evaluated the predictive accuracy of genotypic DST obtained by these tools. The results revealed that the WHO catalog of mutations and five WGS analysis tools exhibit robust predictive capabilities concerning resistance to isoniazid, rifampicin, ethambutol, streptomycin, amikacin, kanamycin, and capreomycin. Notably, Mykrobe, SAM-TB, and TB Profiler demonstrate the most accurate predictions for resistance to pyrazinamide, prothionamide, and para-aminosalicylic acid, respectively. These findings are poised to significantly guide and influence future clinical treatment strategies and resistance monitoring protocols. IMPORTANCEWhole-genome sequencing (WGS) has the potential for the early diagnosis of drug-resistant tuberculosis. However, the interpretation of mutations of drug-resistant-associated genes represents a significant challenge as the amount and complexity of WGS data. We evaluated the accuracy of the World Health Organization catalog of mutations and five WGS analysis tools in predicting drug resistance to first-line and second-line anti-TB drugs. Our results offer clinicians guidance on selecting appropriate WGS analysis tools for predicting resistance to specific anti-TB drugs.

100 Deals associated with Aminosalicylic acid

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External Link

KEGG	Wiki	ATC	Drug Bank
D00162	Aminosalicylic acid	J04AA01	DB00233

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Tuberculosis, Multidrug-Resistant	NO	Eurocept International B.V.	07 Apr 2014
Tuberculosis, Multidrug-Resistant	LI	Eurocept International B.V.	07 Apr 2014
Tuberculosis, Multidrug-Resistant	IS	Eurocept International B.V.	07 Apr 2014
Tuberculosis, Multidrug-Resistant	EU	Eurocept International B.V.	07 Apr 2014

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Crohn Disease	Phase 2	US	Jacobus Pharmaceutical Co., Inc.	01 Jan 2007
Crohn Disease	Phase 1	IL	Jacobus Pharmaceutical Co., Inc.	01 Jan 2007

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00495521 (CTgov)	Phase 2	Crohn Disease	2	4-Aminosalicylic acid extended release granules (Active)	ebbrqylzys(mdwghxspxq) = yrjbwmdful osirwdocdw (ulburwohvd, dvaqwgrfjq - tibmtpkimt) View more	-	21 Sep 2017
				4-Aminosalicylic acid extended release granules (Placebo)	ebbrqylzys(mdwghxspxq) = myducoyvbt osirwdocdw (ulburwohvd, zougvepvgb - kyqjumothi) View more