Oral testosterone therapy
Inventors
Chidambaram, Nachiappan • Nachaegari, Satish K. • Patel, Mahesh V. • Kim, Kilyoung
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-12161651-B1
Publication Date
2024-12-10
Expiration Date
Abstract
Disclosed are methods and compositions for testosterone replacement therapy, especially for use in administration to hypogonadal males. The methods and compositions employ an untitrated dose dosing regimen that does not require titration or dose adjustments and that can provide a therapeutically effective amount of a testosterone ester, such as a non-undecanoate testosterone ester, while avoiding unacceptably high testosterone levels.
Core Innovation
The invention relates to an oral testosterone replacement therapy for subjects having a condition associated with depression, insomnia, obesity, fatigue, a reduction in muscle size, a reduction in muscle mass, a reduction in muscle strength, a reduction in endurance, reduction in bone size, a reduction in bone mass, and a reduction in bone density. The method comprises orally administering a pharmaceutical composition comprising a therapeutically effective amount of a non-undecanoate testosterone ester in an untitrated dose administration regimen.
A central aspect is that the non-undecanoate testosterone ester is administered in an untitrated regimen, including an orally administered therapeutically effective amount without dose titration. The approach encompasses fixed dose administration regimens, including once daily or other untitrated dosing regimens, with target serum testosterone metrics including daily average serum testosterone (Cavg) in a normal eugonadal range and maximum serum testosterone concentration (Cmax) thresholds used to define target and discontinuation criteria.
The therapy is further characterized by serum testosterone-based criteria, including a therapy discontinuation criterion advising discontinuation when serum testosterone (T) levels are consistently greater than 2500 ng/dl. The document also characterizes outcomes where administration to eugonadal and hypogonadal subjects results in daily average serum testosterone (Cavg) in a normal eugonadal range in at least 75% of subjects in a population having the condition.
The pharmaceutical composition portion of the invention includes a therapeutically effective amount of a non-undecanoate testosterone ester, at least one pharmaceutically acceptable carrier, and at least one additive, where the non-undecanoate testosterone ester is about 15%-45% w/w of the composition. Additives include pharmaceutically acceptable additives such as surfactants and solidifying agents, and the administration is described as improving or preventing further worsening of at least one of the stated conditions and/or reductions.
Claims Coverage
The independent claims cover three inventive features: oral untitrated dosing of a non-undecanoate testosterone ester, defined untitrated oral dose thresholds, and a pharmaceutical composition with specified ester content plus carrier and additive system.
Oral untitrated dose regimen with a non-undecanoate testosterone ester
A method comprising orally administering a pharmaceutical composition comprising a therapeutically effective amount of a non-undecanoate testosterone ester in an untitrated dose administration regimen to treat a subject having a condition associated with depression, insomnia, obesity, fatigue, reductions in muscle characteristics, and reductions in bone characteristics.
Defined untitrated oral dosing thresholds for non-undecanoate testosterone ester
A method of treatment comprising orally administering an untitrated dose of about 100-500 mg of a non-undecanoate testosterone ester in an untitrated dose dosing regimen, and/or a total daily dose of at least about 500 mg of a non-undecanoate testosterone ester in an untitrated dose dosing regimen.
Pharmaceutical composition with non-undecanoate testosterone ester content and additive system
A pharmaceutical composition comprising a therapeutically effective amount of a non-undecanoate testosterone ester, at least one pharmaceutically acceptable carrier, and at least one additive, wherein the non-undecanoate testosterone ester comprises about 15%-45% w/w of the composition, and wherein administration results in improving or preventing further worsening of at least one of depression, insomnia, obesity, fatigue, reductions in muscle characteristics, and reductions in bone characteristics.
Collectively, the independent claims require oral administration of a therapeutically effective non-undecanoate testosterone ester in an untitrated dose regimen, including specified dose thresholds, and in the composition claim, a formulation with a specified ester weight fraction plus pharmaceutically acceptable carrier(s) and additive(s).
Stated Advantages
Achieves oral treatment using an untitrated dose administration regimen of a non-undecanoate testosterone ester.
Administration results in improving or preventing further worsening of at least one of the recited conditions or reductions.
Daily average serum testosterone (Cavg) is maintained in a normal eugonadal range in at least 75% of subjects.
Therapy discontinuation is advised based on serum testosterone (T) levels consistently greater than 2500 ng/dl.
Documented Applications
Treatment of subjects having conditions associated with depression, insomnia, obesity, fatigue, reductions in muscle size/mass/strength/endurance, and reductions in bone size/mass/density using an oral pharmaceutical composition with a non-undecanoate testosterone ester in an untitrated dosing regimen.
Interested in licensing this patent?