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On November 10, 2022, the registration application for inhaled aerosol of class 1 new drug PA9159 was implicitly approved by the State Food and Drug Administration for the prevention and treatment of bronchial asthma
.
This is a new indication acquired after PA9159 nasal spray for the treatment of rhinitis
.
.
This is a new indication acquired after PA9159 nasal spray for the treatment of rhinitis
.
PA9159 is a new chemical entity licensed by Shanghai Institute of Materia Medica, Van Andel Research Institute in 2016 to Plaatu Pharmaceuticals for global R&D and promotion, which will develop indications for the prevention and treatment of seasonal and perennial allergic rhinitis, asthma and chronic obstructive pulmonary disease (COPD), eczema, neurodermatitis, atopic dermatitis and pruritus
.
.
In addition to the clinical indications for rhinitis and bronchial asthma, PA9159 plans to submit a clinical trial registration application
for dermatitis indications in December this year.
for dermatitis indications in December this year.
PA9159 inhaled aerosol for asthma indications approved clinically
PA9159 is a glucocorticoid drug
.
Over the years, people's understanding of glucocorticoid drugs has mostly been in-depth research
on the function and efficacy of glucocorticoid receptor protein (GR).
The industry has been exploring the relationship between the protein structure and function of GR, but has struggled with no good way to resolve the protein structure
of GR.
.
Over the years, people's understanding of glucocorticoid drugs has mostly been in-depth research
on the function and efficacy of glucocorticoid receptor protein (GR).
The industry has been exploring the relationship between the protein structure and function of GR, but has struggled with no good way to resolve the protein structure
of GR.
Xu Huaqiang's research group of Shanghai Institute of Materia Medica, has been in-depth research on the mechanism of action of glucocorticoids for more than ten years
.
In 2002, Professor Xu Huaqiang was the first to obtain the structure of high-definition GR protein-bound dexamethasone drug by X-ray diffraction, which was published in the journal Cell in 2002 and laid the foundation
for designing drugs based on the structure of GR protein.
The figure below shows the structure
of GR disomy protein.
.
In 2002, Professor Xu Huaqiang was the first to obtain the structure of high-definition GR protein-bound dexamethasone drug by X-ray diffraction, which was published in the journal Cell in 2002 and laid the foundation
for designing drugs based on the structure of GR protein.
The figure below shows the structure
of GR disomy protein.
Gr disomy protein structure
In 2008, researcher Xu Huaqiang obtained the high-definition protein structure
of glucocorticoid drugs deaccortifazole (DAC) and dexamethasone (DEX) and GR complexes based on previous research.
of glucocorticoid drugs deaccortifazole (DAC) and dexamethasone (DEX) and GR complexes based on previous research.
Structural diagram of GR combined with DAC and DEX
Based on the deep understanding of the high-definition structure of GR and drug interaction, Xu Huaqiang's research group synthesized a large number of lead compounds in more than ten years of continuous exploration, and further in-depth research on the efficacy and side effects of compounds, and finally found the ideal compound PA9159
with high efficacy and low toxic side effects.
with high efficacy and low toxic side effects.
The innovation of glucocorticoid drug PA9159 is that it uses the technology of combining atomic-level protein structure with drug computer simulation docking to find atomic sites that may enhance drug activity and reduce drug side effects, and apply them to the design of
new drug molecules.
Preclinical studies have shown that PA9159 inhalation aerosol has high safety and low toxic side effects, and is expected to become a new generation of hormonal drugs
.
new drug molecules.
Preclinical studies have shown that PA9159 inhalation aerosol has high safety and low toxic side effects, and is expected to become a new generation of hormonal drugs
.
(Contributing department: Xu Huaqiang research group)
