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Gonadotropin-releasing hormone antagonist dosing regimens for the treatment of endometriosis

A technology of endometrium and antagonists, which is applied in the direction of pharmaceutical formulations, diseases, drug combinations, etc., and can solve problems such as adverse side effects, receptor insensitivity, and restrictions

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

[0006] Other therapies that have proven effective in treating pain associated with endometriosis are often limited by adverse side effects
For example, GnRH agonists cause a constant stimulation of the GnRH receptor at the level of the pituitary gland, thus desensitizing this receptor and ultimately leading to inhibition of ovulation and reduction of serum estrogen levels

Method used

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  • Gonadotropin-releasing hormone antagonist dosing regimens for the treatment of endometriosis
  • Gonadotropin-releasing hormone antagonist dosing regimens for the treatment of endometriosis
  • Gonadotropin-releasing hormone antagonist dosing regimens for the treatment of endometriosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0572] Example 1. Determination of initial doses of GnRH antagonists for the treatment of endometriosis in human subjects based on AMH levels

[0573] Using the methods of the present invention, a clinician skilled in the art can assess a patient's AMH levels prior to initiation of GnRH antagonist therapy for the treatment of endometriosis. The GnRH antagonist to be administered to the patient may be a compound represented by formula (III), namely choline 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4 -Methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylate. A clinician skilled in the art can draw blood from a patient and can then perform one or more analytical techniques, such as immunoassays known in the art or described herein, to determine the concentration of AMH in a blood sample isolated from the patient. Quantitative. If it is determined that the concentration of AMH in the sample is elevated relative to the AMH reference range of 15pM to 35...

Embodiment 2

[0577] Example 2. Dosage titration of GnRH antagonists for the treatment of endometriosis in human subjects based on E2 levels

[0578] Using the methods of the present invention, a clinician skilled in the art can assess E2 levels in a patient currently undergoing GnRH antagonist therapy for the treatment of endometriosis in order to determine whether the same dose of GnRH antagonist should continue to be administered to the patient. agent, or whether different doses of a GnRH antagonist should be administered to the patient in order to be effective in reducing one or more symptoms of endometriosis. The GnRH antagonist to be administered to the patient may be a compound represented by formula (III), namely choline 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4 -Methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylate. A clinician skilled in the art can draw blood from a patient and can then perform one or more analytical techniques, such as immunoass...

Embodiment 3

[0582] Example 3. Administration of GnRH Antagonists to Endometriosis Patients Presenting Different AMH Levels

[0583] To study the effect of GnRH antagonists, such as compounds (I), (II), and their pharmaceutically acceptable salts, such as their choline salt (compound (III)) on endometriosis exhibiting different initial values ​​of serum AMH To determine the effect on patients with the disease, a series of experiments were carried out in which the patients were divided into treatment groups and compound (III) or placebo was administered orally. Specifically, a series of n=327 female human patients with endometriosis were divided into five groups and received placebo, 50 mg / day of Compound (III), 75 mg / day of Compound (III) by oral delivery ), 100 mg / day of Compound (III) or 200 mg / day of Compound (III). Treatment with placebo or compound (III) at the doses specified above was continued over a period of 12 weeks.

[0584] At various time points throughout these experiments...

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Abstract

The invention provides methods of treating endometriosis in a patient by administration of a gonadotropin-releasing hormone (GnRH) antagonist, for instance, according to dosing regimens predicated onthe patient's level of anti-Mullerian hormone (AMH) or beta 17-estradiol (E2).

Description

technical field [0001] The present invention relates to methods for determining the dosing regimen of a gonadotropin releasing hormone antagonist for use in the treatment of endometriosis. Background technique [0002] Endometriosis is an estrogen-dependent gynecological condition characterized by the presence of endometrium-like tissue on the outside of the uterus and is one of the most common sex hormone-dependent diseases. The condition is mainly observed in women of reproductive age and disappears spontaneously after menopause. A chronic inflammatory response caused by ectopic endometrial cells Endometriosis can lead to infertility and a variety of painful symptoms, including dysmenorrhea, dyspareunia, chronic pelvic pain, and difficulty urinating and defecating. [0003] The main goal of treating endometriosis is to achieve symptom relief. Treatment options for women with endometriosis-related pain are diverse and include analgesic therapy, hormone therapy, conservati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61P15/00
CPCA61K31/519A61K38/09A61P15/00A61K31/565A61K31/57A61K45/06A61P15/02G01N33/74A61K2300/00
Inventor E·卢马耶J-P·戈特兰德
Owner KISSEI PHARMA
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