Claims for Patent: 11,559,530

Summary for Patent: 11,559,530

Title:	Oral testosterone undecanoate therapy
Abstract:	The present disclosure provides methods and compositions for testosterone replacement therapy. The methods and compositions employ a fixed dose dosing regimen that does not require titration or dose adjustments and that can provide a therapeutically effective amount of a testosterone ester while avoiding unacceptably high testosterone levels.
Inventor(s):	Nachiappan Chidambaram, Satish Kumar Nachaegari, Mahesh V. Patel, Kilyoung Kim
Assignee:	Lipocine Inc
Application Number:	US15/825,019
Patent Claims:	1. A method of restoring serum testosterone levels to a normal eugonadal range in a male having a condition associated with a deficiency or absence of endogenous testosterone, comprising orally administering a pharmaceutical composition comprising a therapeutically effective amount of testosterone undecanoate (TU) and an additive as a hard or soft capsule in a unit dosage form providing 112.5 mg or 225 mg of TU in a fixed dose administration regimen of twice daily administration with food to provide a total daily dose of TU of from 420-500 mg, said method further comprising discontinuing said orally administering when said male consistently has serum testosterone concentrations above about 1040-1100 ng/dl measured about 8-9 hours after a single dose administration of said pharmaceutical composition, wherein said serum testosterone concentrations are measured on at least two or more separate occasions with a gap of at least 24 hours. 2. A method of restoring daily average serum testosterone (Cavg) to a normal eugonadal range in at least 75% of males in a population having a condition associated with a deficiency or absence of endogenous testosterone, comprising oral administration of an oral dosage form comprising a therapeutically effective amount of testosterone undecanoate (TU) and an additive as a hard or soft capsule in a unit dosage form providing 112.5 mg or 225 mg of TU in a fixed dose administration regimen of twice daily with food to provide a total daily dose of TU of from 420-500 mg, said method further comprising discontinuing said oral administration when said male consistently has serum testosterone concentrations above about 1040-1100 ng/dl measured about 8-9 hours after a single dose administration of said pharmaceutical composition, wherein said serum testosterone concentrations are measured on at least two or more separate occasions with a gap of at least 24 hours. 3. A method of treating a condition associated with a deficiency or absence of endogenous testosterone in a male patient, comprising: orally administering a composition comprising testosterone undecanoate (TU) and an additive as a hard or soft capsule in a unit dosage form providing 112.5 or 225 mg of TU in a in a fixed dose dosing regimen of twice daily with food to provide a total daily dose of TU of from 420-500 mg TU, said method further comprising discontinuing said orally administering when said male consistently has serum testosterone concentrations above about 1040-1100 ng/dl measured about 8-9 hours after a single dose administration of said pharmaceutical composition, wherein said serum testosterone concentrations are measured on at least two or more separate occasions with a gap of at least 24 hours. 4. The method of claim 3, further comprising determining a serum testosterone level of said male patient after initiation of administration of TU. 5. The method of claim 3, further comprising determining a serum testosterone level of said male after initiation of TU administration, wherein unacceptably low serum testosterone levels after reaching a steady state indicates an advised discontinuation of therapy. 6. The method of claim 3, wherein the fixed dose provides about 450 mg testosterone undecanoate per day. 7. The method of claim 3, wherein the fixed dose provides safe and efficacious testosterone replacement therapy. 8. The method of claim 3, wherein the fixed dose provides about 225 mg testosterone undecanoate per dose. 9. The method of claim 3, further comprising determining a total serum testosterone concentration, wherein a total serum testosterone concentration that is consistently below 300 ng/dL indicates an advised discontinuation of therapy. 10. The method of claim 3, further comprising assessing discontinuation criteria at steady state. 11. The method of claim 3, further comprising assessing discontinuation criteria at steady state by measuring serum testosterone concentrations. 12. The method of claim 3, further comprising determining a hematocrit or PSA level for the patient, wherein an unacceptably high hematocrit level or an unacceptably high PSA level indicates an advised discontinuation of therapy. 13. The method of claim 3, wherein administration of the fixed dose of TU in the fixed dose dosing regimen provides ≥75% of patients in a population with an average serum T (Cavg) within a normal range, wherein the population comprises a group of at least 20 individuals. 14. The method of claim 3, wherein administration of the fixed dose of TU in the fixed dose dosing regimen provides ≥65% of patients in a population with an average serum T (Cavg) within a normal range, wherein the population comprises a group of at least 20 individuals. 15. The method of claim 3, wherein administration of the fixed dose of TU in the fixed dose dosing regimen provides ≥75% of patients in a population with a Cmax<1500 ng/dL, wherein the population comprises a group of at least 20 individuals. 16. The method of claim 3, wherein administration of the fixed dose of TU in the fixed dose dosing regimen provides ≥90% of patients in a population with a Cmax<1800 ng/dL, wherein the population comprises a group of at least 20 individuals. 17. The method of claim 3, wherein administration of the fixed dose of TU in the fixed dose dosing regimen provides ≥95% of patients in a population with a Cmax<2500 ng/dL, wherein the population comprises a group of at least 20 individuals.