Abiraterone prodrugs

A technology of abiraterone and pharmacy, applied in the field of parenteral preparations, and can solve the problem of no abiraterone and the like

Pending Publication Date: 2022-02-08
PROPELLA THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, to date, there is no sustained-release injectable prodrug formulation of abiraterone

Method used

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  • Abiraterone prodrugs
  • Abiraterone prodrugs
  • Abiraterone prodrugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach 1

[0238] Embodiment 1. A formulation of abiraterone suitable for parenteral administration to a subject with a hormone-dependent benign or malignant disease comprising:

[0239] (a) one or more lipophilic ester forms of abiraterone, and

[0240] (b) one or more pharmaceutically acceptable carriers, diluents or excipients,

[0241] Wherein after said administering to said subject, said abiraterone prodrug formulation reaches a therapeutic plasma concentration of abiraterone.

Embodiment approach 2

[0242] Embodiment 2. The abiraterone prodrug formulation of embodiment 1, wherein said abiraterone has a therapeutic plasma concentration of at least 1.0 ng / ml.

Embodiment approach 3

[0243] Embodiment 3. The abiraterone prodrug formulation of embodiment 1, wherein said abiraterone has a therapeutic plasma concentration of at least 8 ng / ml.

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Abstract

Sustained-release abiraterone prodrug formulations, methods, and kits for parenteral administration to a subject having a sex hormone-dependent benign or malignant disorder such as prostate cancer, a syndrome due to androgen excess, and / or a syndrome due to glucocorticoid excess such as hypercortisolemia.

Description

[0001] This application claims the benefit of U.S. Provisional Application No. 62 / 814,568, filed March 6, 2019, and U.S. Provisional Application No. 62 / 849,259, filed May 17, 2019, the contents of each provisional application being incorporated by reference in their entirety Incorporated into this article. [0002] The present disclosure generally relates to novel abiraterone prodrugs and long-acting, depot-based parenteral formulations of abiraterone prodrugs. The present disclosure pertains to a wide range of applications, such as for intramuscular (IM) injection in patients with androgen- or estrogen-dependent benign or malignant conditions, including various cancers (such as prostate cancer, bladder cancer, hepatocellular carcinoma, lung cancer, etc.) , breast and ovarian cancer, etc.)), and for the treatment of non-neoplastic syndromes caused by androgen excess (including classic and non-classic congenital adrenal hyperplasia, endometriosis, polycystic ovary syndrome, sexua...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J43/00A61K31/58A61P5/28A61P5/46A61P35/00
CPCC07J43/003A61K31/58A61K47/14A61K47/44A61K9/0019
Inventor M·J·夏普W·R·摩尔
Owner PROPELLA THERAPEUTICS INC
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