TLANDO & TLANDO XR - novel oral prodrugs of testosterone

[Systemlord]

It seems wasteful to have those levels while you are sleeping, not to mention potentially disruptive to sleep.

I have never had any sleep problems on Jatenzo and if anything high testosterone helps me sleep.

I still wake up at the appropriate time, just before the sun is starting to come out over the horizon.

Remember, the oral TRT formulations more closely mimic the circadian rhythm.

 

[Nelson Vergel]

I am going to try Tlando this week.

 

[Fortunate]

I am going to try Tlando this week.

That is great @Nelson Vergel. Will you report back here? I have a prescription of Jatenzo, which I’m going to trial for at least a minimum of one week and possibly longer. I am also getting some samples of Tlando later today. I’ll have it at the ready in the event that Jatenzo doesn’t seem to be providing therapeutic benefit.

 

[Nelson Vergel]

Hey @Fortunate. Please remind me the dose and number of capsules per day of Jatenzo you were prescribed.
Walgreens is telling me now that my insurance does not want to pay for Tlando. These pharma companies have to make deals with insurance plans and probably Lipocine has not been successful doing so yet.

 

[Systemlord]

Walgreens is telling me now that my insurance does not want to pay for Tlando.

Do you know if Tlando is cheaper than Jatenzo @Nelson Vergel?

I understand why the prices are high right now on oral T, if oral T is going to go mainstream, the price needs to be more affordable.

 

[Fortunate]

Hey @Fortunate. Please remind me the dose and number of capsules per day of Jatenzo you were prescribed.
Walgreens is telling me now that my insurance does not want to pay for Tlando. These pharma companies have to make deals with insurance plans and probably Lipocine has not been successful doing so yet.

237 mg tablets. One tablet twice a day.

 

[Nelson Vergel]

According to GoodRX

The lowest GoodRx price for the most common version of Jatenzo is around $954.17, 16% off the average retail price of $1,141.74.


The lowest GoodRx price for the most common version of Tlando is around $691.15, 16% off the average retail price of $831.51.

 

[Fortunate]

According to GoodRX

The lowest GoodRx price for the most common version of Jatenzo is around $954.17, 16% off the average retail price of $1,141.74.


The lowest GoodRx price for the most common version of Tlando is around $691.15, 16% off the average retail price of $831.51.

Somehow, I qualified for a patient assistance program. Local pharmacy helped me with it. As of now, it cost me $0. No idea how this works.

 

[madman]

I have never had any sleep problems on Jatenzo and if anything high testosterone helps me sleep.

I still wake up at the appropriate time, just before the sun is starting to come out over the horizon.

Remember, the oral TRT formulations more closely mimic the circadian rhythm.

Dosed twice daily.....not a chance!

As I have stated in previous threads that title would go to the transdermal T-patch.

*Only Androderm®, an evening PA transdermal patch, closely replicates the normal T circadian rhythmicity



Comparison of Testosterone Blood Concentrations from Different TRT Products Versus Normal Diurnal Variations


3. PK Profiles of Approved Exogenous T Formulations

3.4 Transdermal T patch

The FDA originally approved ANDRODERM®, 51 a non-scrotal transdermal T patch, in 1995, with the 2.5 mg/day and 5.0 mg/day systems. This method of delivery allows T to be continually absorbed without dose accumulations for 24 hours. 52-56 In a 24-week, multicenter, randomized 1:1, parallel-group study comparing the PK, efficacy, and safety of a transdermal T system with IM TE injections in 66 men with TD, daily application of 2 transdermal T patches (5.0 mg/day total) resulted in morning T levels within the defined normal physiologic range (10.6–35.7 nmol/L, or 306–1,031 ng/dL) in 96% of patients over weeks 2 to 24. 54 At week 16, T Cavg was 17.9 ± 6.1 nmol/L (517 ± 176 ng/dL) compared with 1.9 ± 2.2 nmol/L (55.4 ± 62.8 ng/dL) at baseline. Peak T levels were reached approximately 8.2 hours after application, with a Cmax of 26.5 ± 9.6 nmol/L (765 ± 277 ng/dL). In 34 men from a multicenter, phase 3 study of a transdermal T patch system for TD, nightly applications of 2 patches (5.0 mg/day) resulted in peak levels occurring in the morning after application and decreasing slowly until system removal, mimicking the circadian patterns reported in healthy, young men.52

A reduced dosing regimen for either 2.0 mg/day or 4.0 mg/day systems applied nightly was evaluated in an interventional study enrolling 40 men with TD for 4 weeks (Clinicaltrials.gov identifier: NCT01104246). This reduced dosing regimen was approved in 2011, and manufacturer data show that following 28 days of transdermal T application, 97% (34/35) men with TD were able to achieve Cavg within 10.4 to 35.7 nmol/L (300–1,030 ng/dL). 51 Mean Cmax values with 2.0 mg/day and 4.0 mg/day treatment were 22.5 ± 5.0 nmol/L (648 ± 145 ng/dL) and 24.1 ± 5.5 nmol/L (696 ± 158 ng/dL), respectively. Similar to the 2.5 mg/day and 5.0 mg/day systems, peak T levels occurred 8 hours post-application, mimicking diurnal variation when the patch is applied at night.




3.8 Oral testosterone undecanoate (TU)

Historically, oral TTh with non-esterified T has been unsuccessful in delivering physiological T due to first-pass hepatic metabolism; to overcome this, high doses were needed to achieve measurable serum T levels.86 A new, oral TU formulation delivered via a self-emulsifying drug delivery system was developed to promote solubilization and absorption of the lipophilic TU in the gastrointestinal tract, and in March 2019, became the first oral TTh approved by the FDA. In a phase 2 study, 200 mg oral TU administered twice a day resulted in 87% of men achieving average serum T levels within the physiological range (10.4–34.7 nmol/L, or 300–1,000 ng/dL), and none of the men had serum T levels >52 nmol/L (1,500 ng/dL). 87 Peak T levels were reached 4 to 5 hours after administration, and levels steadily decreased to baseline at approximately 12 hours unless a second dose was administered. As oral TU capsules are recommended to be taken with a meal, serum T levels appear to be modulated by dietary fat content. 88 Cavg and mean Cmax serum T levels were approximately 2-fold higher when 200 mg oral TU was administered with food compared with fasting. 87 Dietary fat was found to affect mean serum T levels achieved with oral TU; meals with higher fat content increased serum T concentrations. In a phase 3 study comparing the efficacy and safety of 237 mg oral TU given twice daily with a once-daily 60 mg topical T solution, 87% (145/166) of men with TD treated with oral TU were able to achieve a mean Cavg within 8.7 to 31.4 nmol/L (252–907 ng/dL), meeting the primary objective.89 At the final study visit on day 105, the mean Cavg was 14.0 nmol/L (403 ng/dL) and Cmax was 34.9 nmol/L (1,008 ng/dL). As oral TU is given twice daily, there were 2 serum T peaks between 20.8 and 24.3 nmol/L (600 and 700 ng/dL) approximately 4 hours after administration, and 2 sub-therapeutic troughs (<6.9 nmol/L or <200 ng/dL) 12 hours after administration, and a peak-to-trough ratio approaching 4.

*Daily transdermal gels and solutions, and nasal and oral T products, provide a consistent serum T level within the physiologic range in most patients. The daily dosing frequency of the topical gel products results in a PK profile with a resemblance to that of endogenous T in younger males

*Men using nasal and oral T products are able to achieve mean serum T levels that are within the normal range, but they experience several T peaks and troughs throughout the day because of the multiple daily dosing regimens required (2 or 3 times/day). This results in a PK profile that significantly deviates from the endogenous PK profiles of both younger and older patients

 

[eli]

Tlando appears to be an advantage over Jatenzo in that it does not require dose titration (not sure how this is the case) and fat content has less impact on absorption.

However, when looking at the pharmacokinetic curves, it appears that Tlando reaches peak levels around 6 hours after dosing, compared with two hours for Jatenzo. If you take Tlando at 6AM and 6PM, this would mean you would get a surge around midnight.

It seems wasteful to have those levels while you are sleeping, not to mention potentially disruptive to sleep.

Take at 6AM and then 1-2PM then

 

[Fortunate]

Take at 6AM and then 1-2PM then

This is what you are recommending or you are doing? And? How is it going?

 

[Systemlord]

View attachment 12808
View attachment 12809
View attachment 12811
View attachment 12812
View attachment 12813

Hay madman, what is the recommended starting dosage for Tlando?

 

[madman]

View attachment 12861

​

​

PIONEERING FOR NEXT GENERATION ORAL TRT​

TLANDO XR is a next-generation, novel ester prodrug of testosterone that uses the patent-protected Lip'ral technology to enhance solubility and improve systemic absorption. Lipocine completed a Phase 2b dose-finding study in hypogonadal men in 2016. The primary objectives of the Phase 2b clinical study were to determine the starting Phase 3 dose of TLANDO XR along with the safety and tolerability of TLANDO XR and its metabolites following oral administration of single and multiple doses in hypogonadal men. The Phase 2b clinical trial was a randomized, open-label, two-period, multi-dose PK study. Results suggested that the primary objectives were met, including identifying the dose expected to be tested in the planned Phase 3 study. A good dose-response relationship was observed over the tested dose range. Additionally, the target Phase 3 dose met primary and secondary endpoints. TLANDO XR was well tolerated with no drug-related severe or serious adverse events reported in the Phase 2b study.

Lipocine Corporate Presentation

www.excelmale.com

 

[Mastodont]

Take at 6AM and then 1-2PM then

Why not take just before bed if it actually takes 6 hours to reach peak, this would be pretty close to natural. Of course it might be tricky if it has to be taken with a meal.

 

[Systemlord]

I prefer a shorter half-life of Jatenzo. I take my Jatenzo without meals on occasion and notice no difference.

 

[madman]

License Agreement for TLANDO® Franchise in the U.S. and Canada

https://www.prnewswire.com/news-releases/lipocine-and-verity-pharma-enter-into-license-agreement-for-tlando-franchise-in-the-us-and-canada-302037718.html SALT LAKE CITY, Jan. 18, 2024 /PRNewswire/ -- Lipocine Inc. (NASDAQ: LPCN), a biopharmaceutical company focused on treating Central Nervous...

www.excelmale.com