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Pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity

a technology of thrombopoietin and compound, which is applied in the direction of drug composition, extracellular fluid disorder, biocide, etc., can solve the problems of thrombocytopenia patients not being able to receive anti-virus therapy using interferon, bleeding tendency, and reducing the number of platelets, so as to avoid thrombosis risk, increase platelet count, and increase platelet count

Inactive Publication Date: 2015-05-28
SHIONOGI & CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The pharmaceutical composition described in this patent has the advantage of increasing platelets without causing an excessive increase in the risk of blood clotting.

Problems solved by technology

Thrombocytopenia is a disease in which platelet destruction is promoted or platelets are insufficiently produced, causing a reduction in the number of platelets and resulting in bleeding tendency.
Upon treatment for hepatitis or liver cancer, patients with thrombocytopenia may not be able to receive anti-virus therapy using interferons or may require splenectomy, partial splenic embolization (PSE) or platelet transfusion when undergoing invasive procedures such as laparotomy and local therapy.
However, these procedures have the following problems, and thus are not always safe and convenient:
platelet transfusion has risks of transfusion-related side effects (transfusion-related acute lung injury and infection), and platelet products have a short expiration date (4 days after blood collection).
It is also known that repeated platelet transfusion may promote antibody production, causing platelet transfusion refractoriness.
However, it induced a neutralizing antibody directed to endogenous TPO, and thus the development thereof was stopped due to antigenicity.
However, the approved indication thereof is limited to improvement of thrombocytopenia caused by bone-marrow suppression after chemotherapy because of side effects including fluid accumulation, palpitation, edema and the like.
Thus it is suggested that an increase in the platelet count in patients having thrombocytopenia resulting from development of chronic hepatitis to 20×104 / μL or higher may increase the risk of onset of portal vein thrombosis.

Method used

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  • Pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity
  • Pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity
  • Pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity

Examples

Experimental program
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Effect test

example 1

Prediction of Profile of a Platelet Count by Monte-Carlo Simulation

[0216]An excessive increase in the platelet count is considered to increase a risk of thrombosis. In order to ensure the safety of patients who receive drugs, we designed an administration discontinuating criteria based on the platelet count. Using the data of pharmacokinetics and profile of a platelet count from single administration and repeated administration trials of lusutrombopag carried out to healthy adults, a profile of a platelet count during repeated administration of lusutrombopag for 7 days to chronic liver disease patients was predicted by Monte-Carlo simulation. In simulation, the PK / PD model parameters of healthy adults were estimated based on the data obtained from healthy adults (Test Example 1), and model parameters in chronic liver disease patients were calculated based on the PK / PD model in healthy adults (Test Example 2). Based on the calculated parameters, we verified the criteria in which admi...

example 2

Test Example 1

[0256]To patients with thrombocytopenia caused by chronic liver disease, lusutrombopag as a pretreatment of percutaneous liver ablation was orally administered repeatedly for 7 days while applying the discontinuation criteria designed in Example 1 and profile of the platelet count was studied. In the present Example, the term “ablation” refers to radiofrequency ablation.

(Target Disease)

[0257]Patients with thrombocytopenia caused by chronic liver disease who are scheduled to undergo percutaneous liver ablation.

(Inclusion Criteria)

[0258]Patients who meet the following inclusion criteria are included.

1) Age: 20 years of age or older (at the time of signing informed consent);

2) Patients who themselves can give a consent in writing;

3) Patients who have a complication or a history of chronic liver disease caused by hepatitis B or C virus;

4) Patients who are scheduled to undergo percutaneous liver ablation for primary liver cancer;

5) Patients having a platelet count which is ...

formulation examples

[0290]The following Formulation Examples are only exemplified and not intended to limit the scope of the invention.

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Abstract

The present inventor has found out that the following criteria enable to ensure an effect for increasing the platelet count while preventing an excessive increase in the platelet count;“when the platelet count has increased by a certain amount and reached to a sufficient level of the platelet count during administration of a pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity, administration of the pharmaceutical composition is discontinued thereafter”.

Description

FIELD OF THE INVENTION[0001]The present invention relates to a pharmaceutical composition containing a compound having a thrombopoietin receptor agonistic activity.BACKGROUND OF THE INVENTION[0002]Thrombocytopenia is a disease in which platelet destruction is promoted or platelets are insufficiently produced, causing a reduction in the number of platelets and resulting in bleeding tendency. Hemorrhagic events include brain hemorrhage, internal hemorrhage, petechia, purpura, mucosal hemorrhages (nasal hemorrhage, gastrointestinal hemorrhage, genital hemorrhage) and the like, and in some cases, excessive bleeding may be observed after surgery.[0003]It is known that one of the causes of thrombocytopenia is chronic liver disease. In chronic liver disease patients, a decrease in hepatic spare ability with the development of disease stages, and a decrease in the platelet count with hypersplenism are observed. Most of chronic hepatitis is caused by hepatitis B or C virus infection, of whic...

Claims

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Application Information

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IPC IPC(8): A61K31/426
CPCA61K31/426A61K9/06A61K9/08A61K31/4152A61K31/4155A61K31/496A61P1/16A61P7/00A61P7/04A61P31/14A61P31/20A61P35/00A61P43/00
Inventor KANO, TAKESHIFUKUHARA, TAKAHIROKATSUBE, TAKAYUKI
Owner SHIONOGI & CO LTD
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