Claims for Patent: 11,426,416

Summary for Patent: 11,426,416

Title:	Oral testosterone ester formulations and methods of treating testosterone deficiency comprising same
Abstract:	A pharmaceutical formulation of testosterone undecanoate is provided. Methods of treating a testosterone deficiency or its symptoms with the inventive formulations are also provided.
Inventor(s):	Dudley; Robert E. (Murfreesboro, TN), Constantinides; Panayiotis P. (Gurnee, IL)
Assignee:	Clarus Therapeutics, Inc. (Northbrook, IL)
Application Number:	16/656,169
Patent Claims:	1. A method for treating a hypogonadal male comprising orally administering to the male twice-daily a composition comprising a capsule and a liquid formulation encased within the capsule, the formulation being a self-emulsifying drug delivery system comprising a) 18-22 percent by weight of testosterone undecanoate (TU), h) 12-18 percent by weight of hydrophilic surfactant, and c) 50-65 percent by weight of lipophilic surfactant, wherein the weight ratio of the total amount of lipophilic surfactant to the total amount of hydrophilic surfactant is about 6:1 to about 3.5:1, wherein the total TU administered per day ranges from about 316 mg TU to about 948 mg TU, and wherein the composition, when orally administered to a plurality of hypogonadal males, provides, at steady state, an average serum testosterone concentration Cave of from about 300 to about 1100 ng/dl in at least 75% of the males, a serum testosterone Cmax value of from 1800 to 2500 ng/dl in less than 5% of the males, a serum testosterone Cmax value that does not exceed 1500 ng/dl in at least 85% of the males, and a serum testosterone Cmax value that does not exceed 2500 ng/dl in any of the males. 2. The method according to claim 1, wherein administration of the composition provides a serum Tmax at 3 to 7 hours. 3. The method according to claim 1, wherein the Cave in the plurality of hypogonadal males is proportional to the amount of testosterone undecanoate orally administered to the males. 4. The method according to claim 1, wherein the formulation further comprises a 5-alpha reductase inhibitor. 5. The method according to claim 1, wherein the formulation further comprises a P450 isozyme CYP3A4 inhibitor. 6. The method according to claim 1, wherein the formulation further comprises a digestible oil. 7. The method according to claim 6, wherein the digestible oil comprises 10-15 percent by weight of the formulation. 8. The method according to claim 7, wherein the hydrophilic surfactant is polyoxyethylene (40) hydrogenated castor oil and the lipophilic surfactant is oleic acid. 9. The method according to claim 1, wherein the composition releases about 40 wt. % TU within the first 30 minutes and about 60 wt. % TU after 4 hours when evaluated in Fed State Simulated Intestinal Fluid medium containing sodium hydroxide, glacial acetic acid, potassium chloride, lecithin, and sodium taurocholate at a pH of 5.