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Estradiol metabolites for the treatment of pulmonary hypertension

A technology for pulmonary hypertension and estradiol, which can be used in drug combination, drug delivery, cardiovascular system diseases, etc., and can solve problems such as poor response to therapy

Inactive Publication Date: 2006-04-26
UNIVERSITY OF PITTSBURGH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Unfortunately, many patients respond poorly to these therapies or stop responding to them after a while

Method used

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  • Estradiol metabolites for the treatment of pulmonary hypertension
  • Estradiol metabolites for the treatment of pulmonary hypertension
  • Estradiol metabolites for the treatment of pulmonary hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] experimental design

[0078]A total of 27 male Sprague Dawley rats (Charles River, Wilmington, MA) (378 + / - 12 grams) were used in this experiment. The animals were maintained in the animal husbandry laboratory facility of the University of Pittsburgh Medical Center (temperature 22°C, light cycle 12 hours, relative humidity 55%). Animals were fed Pro Lab RHM 3000 Rodent Diet (PMINutrition, Inc, St Louis, MO) and watered ad libitum. The experiments followed the guidelines of the Animal Welfare Regulations, and the experimental protocols approved by the Animal Care and Use Committee.

[0079] Animals were randomly assigned to receive subcutaneous administration of normal saline (1ml / kg, n=6) or monosugine (Sigma, St Louis, MO) (MCT, 60mg / kg subcutaneous administration) (n=21) . Monosugine is known to be an agent that induces pulmonary hypertension. 6 hours after the initial injection, implanted with osmotic minipumps (model 2ML4, Alza, Palo Alto, CA) containing vehi...

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PUM

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Abstract

Methods are provided for the treatment of pulmonary hypertension and other conditions associated therewith. In particular, the methods include treatment of pulmonary hypertension with estradiol metabolite or estradiol metabolite associated with biodegradable microparticles or nanoparticles alone or in combination with another therapeutic agent. Preferred estradiol metabolites include 2-methoxyestradiol, 4-methoxyestradiol, 2-hydroxyestradiol, and 4-hydroxyestradiol, and / or to synthetic derivatives and analogues thereof or prodrugs thereof. The compositions may also be in the form of a controlled release formulation.

Description

[0001] related application [0002] This application claims priority from US Provisional Application filed February 20, 2003 (Application No. 60 / 448,118). field of invention [0003] The present invention relates to methods of using estradiol metabolites for the treatment of pulmonary hypertension and its sequelae, which include heart failure, and pulmonary and cardiac dysfunction. More specifically, the present invention relates to estradiol metabolites (such as 2-hydroxyestradiol, 4-hydroxyestradiol, 2-methoxyestradiol and 4-methoxy Estradiol), these substances can be delivered in the form of controlled release formulations for the treatment of pulmonary hypertension and related diseases. Background of the invention [0004] Pulmonary hypertension (PH) is a comprehensive health problem characterized by elevated blood pressure in the pulmonary arteries. In patients with PH, blood pressure within the pulmonary arteries rises at rest to well above normal levels of approxima...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K31/58A61K9/00A61K31/00A61K31/565A61K47/10
CPCA61K9/0019A61K31/00A61K47/10A61K9/0024A61K31/565A61K31/56A61P9/04A61P9/12B82B3/00H01L21/027
Inventor 斯蒂文·P·托夫维克爱德文·K·杰克森
Owner UNIVERSITY OF PITTSBURGH
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