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Neoplasms

Respiratory Diseases

Small molecule drug

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

Most used technologies in drug development

Targets

Most frequently developed targets

Disease Domain	Count

Neoplasms	2

Top 5 Drug Type	Count

Small molecule drug	2

Top 5 Target	Count

ALK5(Transforming growth factor beta receptor 1)	1
IGF2BP1(insulin like growth factor 2 mRNA binding protein 1)	1

Background:Linagliptin (LNG) exhibits poor bioavailability and numerous side effects, significantly limiting its use. Transdermal drug delivery systems (TDDS) offer a potential solution to overcome the first-pass effect and gastrointestinal reactions associated with oral formulations.Objective:The aim of this study was to develop LNG microparticle gels to enhance drug bioavailability and mitigate side effects.Methods:Linagliptin hyaluronic acid (LNG-HA) microparticles were prepared by spray drying method and their formulation was optimized via a one-factor method. The solubility and release were investigated using the slurry method. LNG-HA microparticle gels were prepared and optimised using in vitro transdermal permeation assay. The hypoglycaemic effect of the LNG-HA microparticle gel was examined on diabetic mice.Results:The results indicated that the LNG-HA microparticle encapsulation rate was 84.46%. Carbomer was selected as the gel matrix for the microparticle gels. Compared to the oral API, the microparticle gel formulation demonstrated a distinct biphasic release pattern. In the first 30 minutes, only 43.56% of the drug was released, followed by a gradual release. This indicates that the formulation achieved a slow-release effect from a dual reservoir system. Furthermore, pharmacodynamic studies revealed a sustained hypoglycemic effect lasting for 48 hours with the LNG microparticle gel formulation.Conclusion:These findings signify that the LNG microparticle gel holds significant clinical value for providing sustained release and justifies its practical application.

01 Dec 2024·Journal of Pharmaceutical and Biomedical Analysis

Simultaneous determination of free DL-amino acids in human hair with a novel DBD-M-Pro derivatization by UHPLC-HRMS: An application in diabetes patients

Article

Author: Nan, Jun ; Zhou, Xin ; Wang, Songze ; Cheng, Shengyu ; Wang, Xin ; Li, Xi-Ling ; Min, Jun Zhe

Human hair is a non-invasive biological sample that is easy to collect and store and can reflect long-term body health. However, the correlation between DL-amino acids and metabolic diseases in hair samples has not been studied. Therefore, we propose a novel UHPLC-HRMS method for analyzing seven free chiral amino acids (DL-Thr, DL-Glu, DL-Ala, DL-Val, DL-Pro, DL-Leu, and DL-Phe) simultaneously in hair samples by derivatization of chiral probe 4-(N,N-dmethylaminosulfonyl)-2,1,3-benzoxadiazole-trans-2-methyl-L-proline (DBD-M-Pro) labeled with targeted amino functional groups. Gradient elution was carried out using an ACQUITYTM BEH C18 (100×2.1 mm,1.7 μm) column with a mobile phase of 0.15 % formic acid (FA) in 10 mM ammonium acetate (CH₃-COONH₄) and 0.2 % FA in acetonitrile. The labelled DL-amino acid diastereoisomers could be completely separated, with a resolution (Rs) of 1.59-11.44. These amino acids show a strong linear correlation within the range of 3.1-99.2 pmol (R² ≥ 0.9990). Intraday and interday precision was 1.87 %-14.87 %. The average recovery was 96.12 %-105.33 %. The limit of detection (LOD) ranged from 0.29 to 2.11 pmol. We then employed the method to determine the concentration of free chiral amino acids in hair samples from 30 healthy volunteers (HVs) and 30 diabetes patients (DPs). Male diabetes patients had significantly higher levels of L-Thr, L-Val, L-Leu (p < 0.05), and D-Ala (p < 0.01) in their hair samples than male healthy volunteers and female diabetes patients had significantly higher levels of D-Ala (p < 0.05) in their hair samples than female healthy volunteers. This is the first study to confirm the feasibility of using free DL-amino acids in human hair as potential biomarkers for diabetes.

100 Deals associated with Yanbian University

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100 Translational Medicine associated with Yanbian University

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Pipeline

Pipeline Snapshot as of 26 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Discovery

1

Preclinical

Other

2

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

J-1012 ( ALK5 )	Neoplasms More	Preclinical
A-11(Yanbian University) ( IGF2BP1 )	Non-Small Cell Lung Cancer More	Discovery
QUAN-0806	Epilepsy More	Pending
J-1090 ( ALK5 x p38α )	Glioma More	Pending