Pharmaceutical formulations and systems for delivery of androgen agents and aromatase inhibitors and methods of use

A technology of aromatase inhibitors and pharmaceutical preparations, which is applied in drug combination, drug delivery, and pharmaceutical formulations, and can solve problems such as side effects and decreased serum estradiol levels

Pending Publication Date: 2022-06-07
HAVAH THERAPEUTICS PTY LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, if the manufacture and concentration of the compound results in the delivery of the active ingredient via zero-order kinetics, the end result is a reduction in serum est

Method used

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  • Pharmaceutical formulations and systems for delivery of androgen agents and aromatase inhibitors and methods of use
  • Pharmaceutical formulations and systems for delivery of androgen agents and aromatase inhibitors and methods of use
  • Pharmaceutical formulations and systems for delivery of androgen agents and aromatase inhibitors and methods of use

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0304] Example 1 : Single-dose trial to evaluate the pharmacokinetics of testosterone and anastrozole from subcutaneous testosterone and anastrozole implants (80 mg / 4 mg (T+Ai)) in women

[0305] Pharmacokinetic analysis was performed on subcutaneous testosterone 80 g and anastrozole 4 mg implants in 11 healthy volunteers with high mammographic breast density. This study evaluated the pattern of both anastrozole and testosterone and allowed modeling of the pharmacokinetics of this exemplary implant to demonstrate the pattern and end-organ pharmacodynamics known to exist in excess of aromatase activity Response, ie, end-organ pharmacodynamic response in tissue of women with high mammographic breast density. This is assessed by direct measurement of breast tissue elasticity in relation to mammographic breast density.

[0306] Ultrasonic evaluation of pellet dissolution was performed to demonstrate how to perform a comprehensive analysis of infusion dissolution of reproductive h...

example 2

[0334] Example 2: Testosterone and Anastrozole Combination Therapy for MBD Reduction in Women

[0335] This example provides an analysis of the use of testosterone and anastrozole combination therapy to reduce mammographic breast density (MBD) in women. The study was conducted at the Wellend Clinic (Burnside War Memorial Hospital, Adelaide, South Australia). The main indications for therapeutic intervention are one or more of the following: perimenopausal hormonal dysfunction, high MBD, which is considered a factor in reducing breast cancer (BC) risk.

[0336] The 652 patients were all female, and the mean age at first T+Ai implantation was 52 years (range, 23 to 79 years).

[0337] MBD / BC risk reduction was the primary indication for treatment in 89 patients (14%), adjunctive hormonal dysfunction in 334 patients (51%), and both indications in 177 patients (27%) . Fifty-two patients did not provide primary indications.

[0338]A history of BC was noted in 90 patients (14% ...

example 3

[0394] Example 3: Pharmacokinetic profile of anastrozole using a modeling approach

[0395] This example provides an analysis of the pharmacokinetic profile of anastrozole using a modeling approach to evaluate the best input function describing the absorption of the assay described in Example 1. Table 6 lists the sampling schedule for anastrozole and testosterone. At least 8 mL of blood samples were collected by venipuncture for serum testosterone / DHT and plasma anastrozole at each time point indicated in Table 6. Figure 7A-B Anastrozole absorption rate is described. Data in these figures are expressed as mean + / - standard deviation. Figure 7A shows the Y-axis on a log scale. Figure 7B shows the Y-axis on a linear scale. This number was generated using the pellet absorption data summarized in Table 2 of Example 1. The percent change from baseline in mean volume was calculated and plotted against time in months. Figure 8A -B plots post-implantation plasma anastrozole co...

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Abstract

The present disclosure relates to formulations, delivery systems, and/or methods of use with a novel sustained release multiphase concentration pattern that can be used, among other things, to reduce mammography breast density and/or breast stiffness in warm-blooded animals. For example, the formulation may comprise administering to the subject an effective amount of an androgen agent and an effective amount of an aromatase inhibitor that provides a multiphase concentration pattern of sustained release over time in the blood of the subject, as measured by serum concentration of the androgen and plasma concentration of the aromatase inhibitor, and, among other things, improves breast tissue stability and/or increases androgen receptor expression levels. The disclosure also relates to the use of an effective amount of an androgen agent in combination with an effective amount of an aromatase inhibitor for preventing or treating autoimmune inflammatory mastitis (AIM) in a patient in need thereof. The autoimmune inflammatory mastitis includes conditions of idiopathic inflammatory mastitis, plasma cell mastitis, and granulomatous mastitis.

Description

technical field [0001] The present disclosure generally relates to pharmaceutical formulations and / or drug delivery systems with novel multiphase release profiles when delivered to warm-blooded animals. The disclosed compositions can be used in warm-blooded animals in which it is desired to increase organ-specific or serum androgen levels without increasing or significantly increasing organ-specific and / or serum estradiol levels. The present disclosure also relates to implants or transdermal patches comprising an effective amount of an androgen and an aromatase inhibitor that provide delivery of a multiphase release profile or pharmacokinetics, which can be used in a desire to increase organ-specific or serum androgen Warm-blooded animals with no or significantly elevated organ-specific and / or serum estradiol levels. Also disclosed are methods of use, including methods related to tissue-specific autoimmune inflammatory conditions. [0002] Related References [0003] Boyd ...

Claims

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Application Information

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IPC IPC(8): A61K31/568A61K31/5685A61K31/4196A61K47/12A61K9/00A61P5/26A61P43/00
CPCA61K31/568A61K9/0019A61P37/02A61P5/24A61K31/4196A61K31/5685A61K2300/00A61K9/0024A61K45/06
Inventor S·N·比勒尔
Owner HAVAH THERAPEUTICS PTY LTD
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