KYZATREX (oral testosterone undecanoate) Updates


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KYZATREX (testosterone undecanoate) is an oral testosterone replacement therapy specifically designed for adult males with conditions associated with a deficiency or absence of endogenous testosterone, such as primary hypogonadism and hypogonadotropic hypogonadism 1112. Here is detailed information regarding its dosage, usage, side effects, price, and efficacy:

Dosage​

KYZATREX is available in capsule form in three dosage strengths: 100 mg, 150 mg, and 200 mg. The recommended starting dose is 200 mg taken orally twice daily, once in the morning and once in the evening, with food to enhance absorption 2412. Dosage adjustments are made based on serum testosterone levels measured 3 to 5 hours after the morning dose, at least 7 days after starting treatment or following a dose adjustment 45.

Usage​

KYZATREX capsules should be taken with food. The therapy is initiated only after confirming hypogonadism through appropriate tests that show serum testosterone concentrations below the normal range. It is important to monitor blood pressure regularly due to the risk of hypertension associated with its use 1012.

Side Effects​

Common side effects include increased blood pressure, which may necessitate the use of antihypertensive medications. Other potential side effects are acne, pain at the injection site, increased red blood cell count, and mood changes. Serious side effects may include major adverse cardiovascular events such as heart attacks and strokes11517.

Price​

The price of KYZATREX can vary depending on the pharmacy, insurance coverage, and dosage. It is advisable to consult with a healthcare provider or pharmacist for the most accurate pricing information.

Efficacy​

KYZATREX has shown high efficacy in clinical trials, with up to 96% of patients achieving normal testosterone levels within 90 days of treatment. The therapy effectively manages symptoms associated with testosterone deficiency, such as fatigue, low libido, and muscle loss 367. The formulation is designed to be absorbed through the lymphatic system, reducing the risk of liver toxicity commonly associated with oral testosterone treatments 18.

Additional Considerations​

KYZATREX carries a boxed warning regarding the potential for blood pressure increases and the associated risk of cardiovascular events. It is classified as a Schedule III controlled substance due to potential for misuse and abuse 1017. It is not indicated for use in women, particularly those who are pregnant, and it is not approved for treating low testosterone due to aging19.In summary, KYZATREX offers a significant advancement in the treatment of male hypogonadism, providing a convenient oral formulation that avoids the complications of other testosterone delivery methods like injections and gels. However, careful monitoring for side effects, particularly hypertension, is crucial.

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If there are studies or case reports on kyzatrex plus clomid, and guys get their T up plus keep their LH functioning, why aren’t more people doing this? Sounds like best of both worlds
 
If there are studies or case reports on kyzatrex plus clomid, and guys get their T up plus keep their LH functioning, why aren’t more people doing this? Sounds like best of both worlds

As you would know lots of men do not fare well on clomid,

Combining clomid with once daily dosing oral TU would be worth trialing to see how you respond but keep in mind the high peak TT and more importantly FT level achieved is short-lived due to the PK.

Nothing to fret over here seeing as the case reports/small pilot studies have shown that most men seen a big improvement in low-T symptoms and experienced minimal sides (elevated hematocrit, testicular atrophy) and some preservation HPG-axis.

Injections will always be king here especially seeing as many men want to take advantage of the anabolic properties of having T levels elevated 24/7 as in steady-state which can easily be achieved depending on the weekly dose of T.

Injections allow one to. achieve high/very high or in some cases absurdly high trough/steady-state FT levels.

Injections will always reign king when it comes to building muscle/increasing strength.

Downfall here is one can easily run into sides (elevated hematocrit/sexual dysfunction) when running too high a. trough/steady-state FT level as you are hammering the s**t out of your dopamine and CNS 24/7.

Throw in the strong suppression of the HPG-axis and the negative impact on fertility and testicular atrophy mind you many men are using hCG with exogenous T in order to maintain fertility and minimize/prevent testicular atrophy..

Even then the HPG-axis still remains high suppressed.




 
As you would know lots of men do not fare well on clomid,

Combining clomid with once daily dosing oral TU would be worth trialing to see how you respond but keep in mind the high peak TT and more importantly FT level achieved is short-lived due to the PK.

Nothing to fret over here seeing as the case reports/small pilot studies have shown that most men seen a big improvement in low-T symptoms and experienced minimal sides (elevated hematocrit, testicular atrophy) and some preservation HPG-axis.

Injections will always be king here especially seeing as many men want to take advantage of the anabolic properties of having T levels elevated 24/7 as in steady-state which can easily be achieved depending on the weekly dose of T.

Injections allow one to. achieve high/very high or in some cases absurdly high trough/steady-state FT levels.

Injections will always reign king when it comes to building muscle/increasing strength.

Downfall here is one can easily run into sides (elevated hematocrit/sexual dysfunction) when running too high a. trough/steady-state FT level as you are hammering the s**t out of your dopamine and CNS 24/7.

Throw in the strong suppression of the HPG-axis and the negative impact on fertility and testicular atrophy mind you many men are using hCG with exogenous T in order to maintain fertility and minimize/prevent testicular atrophy..

Even then the HPG-axis still remains high suppressed.




I tried switching to kyzatrex but felt so bad, tired, brain fog etc.

I’m wondering if doing like 50 mg a week of injectible T plus kyzatrex in am , enclomiphene at night would yield an increase in LH
 
I tried switching to kyzatrex but felt so bad, tired, brain fog etc.

I’m wondering if doing like 50 mg a week of injectible T plus kyzatrex in am , enclomiphene at night would yield an increase in LH

Doubtful as the injectable T even at that dose would be suppressive.

Hard to say where your peak/trough would land on such dose especially IM.

Look over the Phase II Xyosted study from 2015 by Kaminetsky (pdf) in post #2 of this thread.



Pharmacokinetic Profile of Subcutaneous Testosterone Enanthate Delivered via a Novel, Prefilled Single-Use Autoinjector: A Phase II Study (2015)

Jed Kaminetsky, MD,* Jonathan S. Jaffe, MD,† and Ronald S. Swerdloff, MD‡




PK Profile for T

Figure 2 shows pre-dose and 24 hours post-dose TT levels collected during the dosing interval.
Patients achieved mean TT levels within the pre-determined reference range (300–1,100 ng/dL) within 24 hours following the first dose with either 50 or 100 mg of TE delivered via the self- administration system. The 50 mg dose of SC TE provided a temporary increase to T levels, which fell to baseline between doses (Figure 2). PK curves in the 50 mg SC group were similar between weeks 1, 5, and 6 (Figure 3A). Unlike the 50-mg group, T levels rose following the first three doses of 100 mg SC TE. Pre-dose and 24 hours post-dose concentration ranges overlapped at week 4 and beyond, which is consistent with having approached steady-state exposure (Figure 2). At weeks 5 and 6, PK curves for the 100-mg group overlapped and provided greater T exposure than the exposure observed at week 1 (Figure 3B).

Table 2 summarizes PK parameters by treatment. Both doses of SC TE produced average steady-state concentrations of T within the normal range over the dosing interval of 168 hours (7 days). In contrast, 200 mg IM TE produced supra-physiologic levels the first week after dosing. At week 6, the 50 mg SC TE treatment group achieved a Cavg0–168 h (standard deviation [SD] ) of 422.4 ng/dL (123.9), while the 100 mg SC TE treatment group achieved a Cavg0–168 h (SD) of 895.5 ng/dL (279.8). The IM TE treatment group achieved a Cavg0–168 h (SD) of 1658.7 ng/dL (1001.8). Because of rising T levels at later time points in the 50 mg arm, reliable estimation of half-life (T1/2) of this dose was not possible. The apparent T1/2 (SD) was 239.63 hours (59.93) for 100 mg SC TE and 172.57 hours (34.74) for 200 mg IM TE.

SC TE demonstrated dose proportionality as AUC0–168 h, Cavg0–168 h, Cmax, and minimum observed plasma concentration (Cmin) of the 100 mg dose of SC TE were approximately twice those of the 50 mg dose (Table 2). Relative to 200 mg IM TE, the two doses of 100 mg SC TE (week 5 and week 6 combined) demonstrated similar AUC0-inf, suggesting that the bioavailability of TE is similar whether administered SC or IM.





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Discussion

Although there have been only a few reports in the literature, these previous studies suggest that the SC route of administration achieves therapeutic T levels and is a viable alternative to IM administration [30–32]. Our article reports the results from a multicenter, multiple-dose, phase II PK study and demonstrates that TE in oil-administered SC via a prefilled single-use disposable autoinjector was able to achieve serum T reliably within reference ranges over a 1-week dosing interval. Normal T levels were achieved within hours after first dose and steady-state was approached after the third dose. SC TE minimized variation in exposure relative to a chronic 200 mg IM TE dosing cohort. Mean steady-state Cavg and Cmax T levels were in the reference range with both doses of SC TE. In the IM TE cohort, Cavg and Cmax were higher than normal in the week after dosing. The supra- physiologic levels of T following 200 mg IM TE is consistent with prior reports [21,22].

The 50-mg dose exhibited no accumulation between doses. A similar result at this dose was demonstrated in healthy men, suggesting that clearance exceeds exposure by the end of the dosing interval [33]. The 100 mg SC TE dose achieved approximately twice the T exposure as the 50 mg dose; thus demonstrating dose proportionality. Accordingly, DHT and E2 levels increased with TE dose. The ratio of DHT to T was similar across the groups, suggesting a similar rate of metabolism. Overall, the results presented here suggest that an intermediate dose of 75 mg weekly will provide optimal T exposure in most patients.










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CONCLUSIONS

In our population of patients on stable IM T dose, there was a wide mean variation in both Tp (23%) and Tt (17.5%). In addition to that, 25% of patients had a maximum Tp change greater than 50% and a maximum Tt change greater than 35%.
Clinicians should be aware of this high variability in levels when deciding on dose adjustment.
 

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