Key point here!
* must be taken with a normal meal/snack or breakfast with some fat to ensure absorption
A meal or snack with a moderate amount of fat would be ideal when using Jatenzo or Kyzatrex and a meal/snack with some fat will suffice when using Tlando.
KYZATREX®
Absorption
The KYZATREX® self-emulsifying drug delivery system is well absorbed from the gastrointestinal tract. Both testosterone undecanoate and the newly formed 5-alpha-dihydrotestosterone undecanoate are absorbed via the lymphatic system, circumventing first passage through the liver.
Following oral administration an important part of the active substance testosterone undecanoate is co-absorbed with the lipophilic solvent from the intestine into the lymphatic system, thus partially circumventing the first-pass inactivation by the liver. KYZATREX® must be taken with a normal meal or breakfast to ensure absorption.
KYZATREX® is expected to produce testosterone concentrations that approximate normal concentrations seen in healthy men.
When KYZATREX® was given with breakfast containing 16%, 33%, and 45% fat, the exposure (AUC 0- 24 hr) of testosterone was increased by 37%, 87%, and 94%, respectively, compared to when given under fasted conditions. The primary efficacy and safety study was conducted under fed conditions regardless of the type of meals and the primary efficacy endpoint of achieving testosterone C avg in normal testosterone range was met.
There was no effect on testosterone PK when KYZATREX® was administered with 20% alcohol along with a high-fat meal versus a high-fat meal alone.
Figure 1: Mean (±SEM) Concentration-Time Profile for NaF-EDTA Plasma Total Testosterone in KYZATREX® -Treated Patients at Day 90 Visit
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JATENZO®
Absorption
JATENZO delivers physiologic amounts of testosterone, producing testosterone concentrations that approximate normal concentrations seen in healthy men.
The JATENZO self-emulsifying drug delivery system is well absorbed from the gastrointestinal tract. Testosterone undecanoate is absorbed via the lymphatic system, circumventing first passage through the liver.
Following oral administration an important part of the active substance testosterone undecanoate is co-absorbed with the lipophilic solvent from the intestine into the lymphatic system, thus partially circumventing the first-pass inactivation by the liver. JATENZO must be taken with a normal meal or breakfast to ensure absorption.
When JATENZO was dosed with different breakfasts containing various amounts of fat, the bioavailability with the 30 g fat, 45 g fat, and high-calorie high-fat breakfasts was comparable, but there was a food effect with the 15 g fat breakfast compared to the 30 g fat breakfast. The 15 g fat breakfast had a 25% decrease in testosterone exposure compared to the 30 g fat breakfast.
Figure 1. Mean (±SEM) Concentration-Time Profile for NaF-EDTA Plasma Total Testosterone in JATENZO Treated Subjects at Final PK Visit
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TLANDO®
Absorption
Testosterone undecanoate is a lipophilic molecule that is primarily absorbed into the lymph system after oral administration and then released into the general blood circulation by the thoracic duct, avoiding absorption into the portal vein thereby circumventing first-pass metabolism in the liver. Testosterone undecanoate is converted to testosterone following absorption.
Effect of Food
Administration of TLANDO with moderate fat containing food did not significantly impact the pharmacokinetic parameters of testosterone compared to high or low fat. However, there is decrease in exposure when administered without food compared to fed conditions.
In studies with 13 to 14 hypogonadal males, mean testosterone Cmax and AUC were comparable when TLANDO was administered with food containing low, moderate or high fat amounts. Administration in fasting conditions resulted in approximately 65 % and 38% lower Cmax and AUC, respectively, compared to administration with food (high fat).
Figure 1: Mean (±SEM) Serum Total Testosterone Concentrations (ng/dL)
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