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Antitumor agent for acute myeloid leukemia

A technology of myeloid leukemia and anti-tumor agent, which is applied in the field of anti-tumor agent for acute myeloid leukemia, and can solve the problems that no research has been carried out.

Pending Publication Date: 2021-05-25
FUJIFILM CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order for Compound A to exert its medicinal effect on patients with acute myelogenous leukemia, it is very important to maintain the prescribed blood concentration for more than 24 hours, but how much dosage can be used to achieve its medicinal effect. Those skilled in the art cannot imagine
Also, with regard to compound A, no study has been conducted so far on the value of maintaining a predetermined blood concentration for 24 hours or more in order to exhibit an actual therapeutic effect on patients with acute myelogenous leukemia.

Method used

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  • Antitumor agent for acute myeloid leukemia
  • Antitumor agent for acute myeloid leukemia
  • Antitumor agent for acute myeloid leukemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0285] Population pharmacokinetic analysis was performed using plasma concentration data of 198 compounds A1 obtained from 10 acute myelogenous leukemia patients. As the population pharmacokinetic analysis software, NONMEM (registered trademark) (ICON Development Solutions Co., Ltd., software version 7.3) was used. A QD of 50 mg once a day (QD) will be implemented in order to study the dose that can achieve a plasma drug concentration exceeding 40 ng / mL (the target value of the expected drug effect) using the parameters estimated from the population pharmacokinetic analysis During the administration, the simulation results of the simulation of drug concentration changes when 25 to 75 mg BID was administered twice a day and 10 to 75 mg TID were administered three times a day are shown in Figure 2 ~ Figure 4 . exist Figure 2 ~ Figure 4 In , the dashed line represents the line at 40 ng / mL.

[0286] As a result of the simulation, it was predicted that the dose of the overall ...

Embodiment 2

[0288]

[0289] For patients with acute myelogenous leukemia, compound A1 was administered twice a day, 25-225 mg once, BID before meals. Good effects (for example, a reduction in the ratio of blast cells in the bone marrow, a therapeutic effect of PR or higher) were confirmed. The specific dosage is 50mg, 75mg, 100mg or 150mg each time.

[0290] As the initial treatment, patients received chemotherapy based on cytarabine, daunorubicin, idarubicin, etc., and some patients did not achieve CR, CRi, CRp, or PR after the initial treatment.

[0291]

[0292] The therapeutic effect was judged by the following criteria.

[0293] The bone marrow aspiration subjects were evaluated and judged by the following criteria.

[0294]CR (Complete Response): 5% or less of bone marrow blast cells with no Auer rods confirmed, and the number of neutrophils and platelets is 1,000 / μL or more and 100,000 / μL or more state.

[0295] CRp (Complete Response with incomplete platelet recovery): Bon...

Embodiment 3

[0300]

[0301] For patients with acute myelogenous leukemia, compound A1 was administered TID in an amount of 20-150 mg three times a day before meals. Good effects (for example, reduction of blast cell ratio in bone marrow, therapeutic effect of PR or higher) were confirmed.

[0302] As the initial treatment, patients received chemotherapy based on cytarabine, daunorubicin, idarubicin, etc., and some patients failed to achieve CR, CRi or CRp after the initial treatment.

[0303]

[0304] For patients with acute myelogenous leukemia, compound A1 was administered QD before meals in an amount of 50-300 mg once a day. More specifically, the dosage is 50, 75, 100, 150, 225, 300 mg. A relatively good effect (for example, a reduction in the blast cell ratio in the bone marrow, a therapeutic effect of PR or higher) was confirmed.

[0305] As the initial treatment, patients received chemotherapy based on cytarabine, daunorubicin, idarubicin, etc., and some patients failed to ac...

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Abstract

The present invention addresses the problem of providing an antitumor agent for acute myeloid leukemia, the antitumor agent exhibiting practical effects on acute myeloid leukemia. According to the present invention, provided is an antitumor agent for acute myeloid leukemia, the antitumor agent containing a compound, such as (S,E)-N-(1-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)-4-pentyn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methyl-2-butenamide, represented by general formula [1] specified in the present specification, or a salt thereof, wherein the amount of the antitumor agent administered per dose is within a predetermined range.

Description

technical field [0001] The invention relates to an antitumor agent for acute myelogenous leukemia. Background technique [0002] Nitrogen-containing heterocyclic compounds having excellent Fms-like tyrosine kinase 3 (FLT3) inhibitory activity and useful as raw materials for pharmaceuticals have been reported (Patent Document 1 and Patent Document 2). Also, a pharmaceutical composition for treating FLT3 mutation-positive cancer comprising the above nitrogen-containing heterocyclic compound has been reported (Patent Document 3). Furthermore, a production method of a nitrogen-containing heterocyclic compound and an intermediate thereof have been reported (Patent Document 4). Hereinafter, the compound represented by the general formula [1] described in Patent Document 3 or its salt may be abbreviated as compound A in some cases. [0003] prior art literature [0004] patent documents [0005] Patent Document 1: International Publication No. 2013 / 157540 Pamphlet [0006] Pat...

Claims

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Application Information

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IPC IPC(8): A61K31/505A61P35/02A61P43/00
CPCA61P43/00A61K31/505A61P35/02A61K9/0053A61K9/48
Inventor 安东诚渡部智之
Owner FUJIFILM CORP
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