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Gonadotropin-releasing hormone antagonist dosing regimens for treating uterine fibroids and reducing menstrual blood loss

A technology for menstrual blood loss and uterine fibroids, which can be used in pharmaceutical formulations, sexual diseases, drug combinations, etc., and can solve problems such as chronic administration incompatibility

Pending Publication Date: 2020-04-10
KISSEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Therapeutics currently approved for the treatment of uterine fibroid symptoms provide only short-term beneficial effects and are usually indicated for administration only prior to surgical intervention or are incompatible with chronic administration due to deleterious side effects

Method used

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  • Gonadotropin-releasing hormone antagonist dosing regimens for treating uterine fibroids and reducing menstrual blood loss
  • Gonadotropin-releasing hormone antagonist dosing regimens for treating uterine fibroids and reducing menstrual blood loss
  • Gonadotropin-releasing hormone antagonist dosing regimens for treating uterine fibroids and reducing menstrual blood loss

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0345] Example 1. Choline 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo - Evaluation of the effect of 1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylate on serum estradiol and menstrual blood loss in female human subjects

[0346] Subject population and study design

[0347] To assess the effect of Compound (II) on serum β17-estradiol concentrations and menstrual blood loss, a total of 75 healthy female human subjects were divided into five treatment groups, as described in Table 1 below. Subjects were screened for a period of four weeks prior to initiation of treatment with Compound (II). At the end of the four-week screening period, subjects in each treatment group were administered an equal dose of norethindrone acetate, 5 mg x 3 times daily. This 15 mg / day dose was administered for 11 days to allow synchronization of menstruation between subjects. Subjects were then left without treatment for the next 4 days. Following this drug holiday...

Embodiment 2

[0372] Example 2. Use of GnRH Antagonist Dosing Regimen for Treating Patients with Uterine Fibroids and Concomitant Anemia

[0373] Human patients with uterine fibroids with concomitant anemia, such as iron deficiency anemia, can be effectively treated to exhibit reduced menstrual blood loss using the dosing regimens described herein. For example, after a patient is identified as suffering from uterine fibroids and anemia caused by heavy menstrual blood loss, a skilled clinician in the art may prescribe Compound (I) or a pharmaceutically acceptable salt thereof, such as its choline salt, to the patient. daily dose. The compound can be administered to the patient daily, for example, at a dose of 100 mg / day, as a stand-alone treatment or in combination with add-back therapy such as 1.0 mg / day of β17-estradiol and 0.5 mg / day Norethindrone acetate per day or β17-estradiol at 0.5 mg / day and norethindrone acetate at 0.1 mg / day. In an alternative example, a patient may be administe...

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Abstract

The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxypheny I]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.

Description

technical field [0001] The present invention relates to a method of reducing menstrual blood loss in a patient, such as a patient presenting or diagnosed with uterine fibroids, by administering a gonadotropin releasing hormone antagonist. Background technique [0002] Uterine fibroids, also known as leiomyomas, are the most common benign tumors in women. Uterine fibroids are highly prevalent in women of reproductive age and are identified in more than 50% of women between the ages of 35 and 50. The incidence of this pathology is positively related to age and is usually resolved by means of surgical intervention, such as hysterectomy (Buttram et al., Fertil Steril. 36:433-445 (1981); and Day Baird et al., Am. J. Obstet. Gynecol. 188:100-107 (2003)). Symptoms associated with uterine fibroids often include heavy or prolonged menstrual bleeding, pelvic pressure and squeezing of pelvic organs, back pain, and adverse reproductive outcome. Heavy menstrual bleeding, which can man...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61P15/00
CPCA61K31/519A61P15/00A61K31/565A61K31/57A61K45/06A61P15/02A61K2300/00A61P5/00
Inventor E·卢马耶J-P·戈特兰德O·波尔
Owner KISSEI PHARMA
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