CROSS REFERENCE TO RELATED APPLICATIONS

This Non-provisional application claims priority under 35 U.S.C. § 119(a) on Patent Application No(s). 108121743 filed in Taiwan, Republic of China on Jun. 21, 2019, the entire contents of which are hereby incorporated by reference.

BACKGROUND OF THE INVENTION

Field of Invention

The invention relates to a pharmaceutical composition for treating a patient with phosphodiesterase 4-mediated disease and inhibiting phosphodiesterase 4 activity and use thereof.

Related Art

Phosphodiesterase (PDE) family can hydrolyze cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) to AMP and GMP, and thus inactivated them. In the said family, the phosphodiesterase 4 is a specific enzyme for cAMP. The phosphodiesterase 4 is ubiquitously present in inflammation and immune cells.

cAMP is a critical second messenger in the cells. It is known that increased concentration of cAMP can inhibit pro-inflammatory responses in various types of inflammatory and immune cells, including lymphocytes, monocytes, macrophages, neutrophils, eosinophils, basophils, and the lung epithelial cells and so on.

However, phosphodiesterase 4 (PDE4) may reduce the concentration of cAMP, which may reduce its effect on inhibiting various types of inflammation and proinflammatory response in immune cells, and thus leading to cause inflammatory diseases and allergic diseases easily. It is currently known that increased activity of PDE4 is associated with certain inflammatory diseases or allergic diseases, such as asthma, chronic bronchitis, emphysema, atopic dermatitis, urticaria, allergic rhinitis, allergic conjunctivitis, psoriasis, rheumatoid arthritis, chronic obstructive pulmonary disease (COPD), acute respiratory distress syndrome, multiple sclerosis and so on.

Accordingly, it is an urgent need to provide a pharmaceutical composition for inhibiting PDE4 activity and use thereof. The pharmaceutical composition can reduce PDE4 activity in a patient for avoiding the effect of PDE4 to the function of the immune system, and thus achieves the efficacy of treating the diseases related to the PDE4 activity.

SUMMARY OF THE INVENTION

In view of the foregoing objectives, a purpose of the invention is to provide a pharmaceutical composition for inhibiting PDE4 activity and use thereof. The pharmaceutical composition can reduce PDE4 activity in an individual for avoiding the effect of PDE4 to the function of the immune system, and thus achieves the efficacy of treating phosphodiesterase 4-mediated (PDE4-mediated) diseases.

To achieve the above objective, the invention provides a pharmaceutical composition for treating a phosphodiesterase 4-mediated (PDE4-mediated) disease in a patient. The pharmaceutical composition comprises an effective amount of Ribociclib and a pharmaceutically acceptable carrier.

To achieve the above objective, the invention also provides a pharmaceutical composition for use in the treatment of a PDE4-mediated disease in a patient, wherein the pharmaceutical composition comprises an effective amount of Ribociclib and a pharmaceutically acceptable carrier.

To achieve the above objective, the invention further provides a pharmaceutical composition for inhibiting PDE4 activity. The pharmaceutical composition comprises an effective amount of Ribociclib and a pharmaceutically acceptable carrier.

To achieve the above objective, the invention further provides a method for treating a PDE4-mediated disease in a patient. The method comprises a step of providing a pharmaceutical composition to the patient. The pharmaceutical composition comprises an effective amount of Ribociclib and a pharmaceutically acceptable carrier.

In one embodiment, the PDE4-mediated disease is acute lung injury, acute respiratory distress syndrome, psoriasis, chronic obstructive pulmonary disease, pulmonary fibrosis, liver injury, fatty liver disease, liver fibrosis, myocardial infarction, shock, stroke, vasculitis, sepsis, inflammatory bowel disease, rheumatoid arthritis, systemic lupus erythematosus or atopic dermatitis.

In one embodiment, Ribociclib is used to treat the PDE4-mediated disease by inhibiting neutrophils activity.

In one embodiment, Ribociclib is used to treat the PDE4-mediated disease by inhibiting phosphodiesterase 4 (PDE4) pathway.

In one embodiment, Ribociclib is used to treat the PDE4-mediated disease by inhibiting phosphodiesterase 4A (PDE4A) activity, phosphodiesterase 4B (PDE4B) activity, phosphodiesterase 4C (PDE4C) activity or phosphodiesterase 4D (PDE4D) activity of the PDE4 pathway.

In one embodiment, the effective amount of Ribociclib is from 1 μg/kg of the body weight/per day to 100 mg/kg of the body weight/per day.

As mentioned above, the efficacy of this invention is to provide a pharmaceutical composition for inhibiting PDE4 activity and use thereof. The pharmaceutical composition can reduce PDE4 activity in a patient for avoiding the effect of PDE4 to the function of the immune system, and thus achieves the efficacy of treating PDE4-mediated diseases.

