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Activated blood coagulation factor X (FXa) inhibitor

An anticoagulant, dosage technology, applied in the fields of organic chemistry, blood diseases, organic active ingredients, etc., can solve the problems of being affected by food, time-consuming and so on

Inactive Publication Date: 2012-01-18
DAIICHI SANKYO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the other hand, warfarin has the following problems: it takes time to exert its effect; its effect greatly varies with individual recipient patients; combined use requires caution due to its drug interaction with other agents; it is affected by food; It requires monitoring of PT-INR (Prothrombin Time-International Normalized Ratio) in recipient patients
On the other hand, most orally administered drugs have very different dose-increasing increases in serum concentrations among recipient patients

Method used

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  • Activated blood coagulation factor X (FXa) inhibitor
  • Activated blood coagulation factor X (FXa) inhibitor
  • Activated blood coagulation factor X (FXa) inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0286] Patients undergoing total knee arthroplasty were enrolled in a placebo-controlled randomized double-blind dose comparison study to verify their effect of compound (1a) on deep vein thrombosis (DVT ) and pulmonary embolism (PE) prophylaxis (efficacy) and examine the safety of compound (1a).

[0287] In terms of dosage and administration, dosing begins 6 to 24 hours after surgery and usually begins in the morning from the day after the first dose. A preparation containing compound (1a) as an active ingredient was orally administered once a day for 11 to 14 days as a test new drug.

[0288] The administration group was divided into a total of 5 groups: a placebo group and a compound (1a) group (5 mg, 15 mg, 30 mg and 60 mg [each dose is based on the amount of compound (1) in free form]).

[0289] The clinical trial was conducted by a method that included conducting a preliminary test within 14 days before surgery, starting drug or placebo administration within 6 to 24 hou...

Embodiment 2

[0300] Patients with non-valvular atrial fibrillation were used as test subjects to compare the incidence of bleeding events between the group administered with compound (1a) and warfarin potassium (hereinafter referred to as warfarin) as a control. In addition, for efficacy, secondary assessments were performed by comparing the incidence of thromboembolic events, pharmacodynamic indices, and biomarkers, and for safety, by comparing the incidence of adverse events and adverse reactions. This clinical trial is a multicenter randomized dose comparison study conducted as a double-blind trial in the case of the group administered with compound (1a) and as an open-label trial in the case of the group administered with warfarin. Due to dose adjustment difficulties, the comparator drug warfarin was evaluated in an open-label fashion despite its demonstrated efficacy for embolization in patients with nonvalvular atrial fibrillation. Therefore, only the group that had been administered...

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Abstract

Disclosed is an activated blood coagulation factor X (FXa) inhibitor which is reduced in the risk of bleeding in the treatment of thromboembolism. Specifically disclosed is a blood coagulation inhibitor for oral administration, which comprises a compound represented by formula (1), a pharmacologically acceptable salt thereof, or a hydrate of the compound or the pharmacologically acceptable salt as an active ingredient. The blood coagulation inhibitor is characterized in that the dosage of the blood coagulation inhibitor can be determined by the following steps (A) to (D): (A) a factor associated with the risk of bleeding of the blood coagulation inhibitor is selected as a dosage determination factor; (B) a standard value for the dosage determination factor is set; (C) the level of the dosage determination factor is measured in a patient who needs the administration of the blood coagulation inhibitor; and (D) the dosage for the patient is determined by employing the standard value as a measure.

Description

technical field [0001] The present invention relates to inhibitors of activated coagulation factor X (FXa) for reducing the risk of bleeding caused by thromboembolic therapy in recipient patients, wherein the dose of the agent can be selected based on reference values ​​for dose-determining factors of the patient in need of administration. Background technique [0002] N shown in the following formula (1) 1 -(5-chloropyridin-2-yl)-N 2 -((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c ]pyridin-2-yl)carbonyl]amino}cyclohexyl)oxalamide or a pharmaceutically acceptable salt thereof or a hydrate thereof exhibits a strong direct inhibitory effect on activated coagulation factor X (FXa) as a prophylactic agent for thromboembolism , especially based on the prophylaxis and treatment of thromboembolism in deep vein thrombosis (DVT), venous thromboembolism (VTE) or nonvalvular atrial fibrillation (NVAF), the usefulness of drugs is becoming increa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/437A61P7/02A61P9/08A61P9/10A61P11/00C07D513/04
CPCA61K31/444C07D513/04A61K31/437A61P11/00A61P7/02A61P9/08A61P9/10
Inventor 安孙子尚史内山和久本桥知子松田智子须田朱春
Owner DAIICHI SANKYO CO LTD
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