Nelson Vergel
Founder, ExcelMale.com
Nelson, have you considered cjc-1295 mpa at all?
Hi Cjc
No, I have not but I am curious after reading this paper:
"This report describes the safety, pharmacokinetic profile, and pharmacodynamic effects of CJC-1295, a synthetic analog of GHRH that permanently and covalently binds to serum albumin after administration. Results of the single-dose and multiple-dose studies demonstrate a prolonged half-life of CJC-1295 (∼6–8 d) after sc administration, with measurable drug concentrations for 10–13 d after single or multiple doses. In addition, there was clear evidence of a dose-responsive and sustained biological effect, with elevated GH and IGF-I serum concentrations persisting for at least 6 and 14 d, respectively, after single doses of CJC-1295. In the multiple-dose study, there was a cumulative effect after two or three injections of CJC-1295 administered weekly or biweekly, with elevated levels of both GH and IGF-I above baseline on d 14 in most subjects. CJC-1295 was safe and generally well tolerated, particularly at doses of 30 and 60 μg/kg.Treatment with human GH typically consists of a single daily injection of the hormone, resulting in transient supraphysiological levels, followed by a decline to baseline. However, failure to mimic the physiological pulsatile nature of GH secretion may preclude optimal therapeutic effects and may contribute to some of the adverse effects that have been observed even in the presence of normal serum IGF-I levels. In contrast, injections or infusions of GHRH stimulate the pulsatile release of GH (9, 10), but the short plasma half-life (7 min) (5) renders GHRH impractical for therapeutic use. Therefore, the availability of a GHRH preparation with sustained effect has important therapeutic potential.
The half-life of CJC-1295, as predicted from preclinical animal studies (8), was substantially prolonged compared with that of native GHRH, ranging from 5.8–8.1 d in the single-dose study and from 5.4–9.2 d in the multiple-dose study. Maximum concentrations were typically reached within 2 h after injection and exhibited a slow exponential decrease over several days. The disappearance rates were not dose dependent, although serum CJC-1295 concentrations were proportional to the dose injected. In the multiple-dose study, C[SUB]max[/SUB] and AUC[SUB]0–24 h[/SUB] were 17% greater on d 7 than on d 0 and from 30–70% greater on d 14 than on d 0.
Administration of single doses of CJC-1295 resulted in a 2- to 10-fold increase in mean serum GH levels in all dosing groups, which was dose incremental and persisted for up to 6 d. Similarly, a dose-related increase in mean serum IGF-I levels was observed at all dose levels, ranging from 1.5- to 3-fold and persisting for up to 14 d.
Administration of ascending multiple doses of CJC-1295 resulted in elevated levels of GH, similar to those observed after a single dose.
In contrast, elevations in IGF-I levels showed a progressive effect over time, particularly in subjects receiving CJC-1295 every 7 d. Results of the multiple-dose study suggest both a cumulative pharmacokinetic effect [i.e. persistence of elevated predose levels of IGF-I in all dosing groups except group 1 (i.e. two injections of 30 μg/kg)] and a pituitary priming effect (i.e. progressively greater C[SUB]max[/SUB] and progressively shorter T[SUB]max[/SUB] after serial dosing). The data indicate that a minimum dosing interval of 7 d appears reasonable. The most appropriate dosing interval will be determined based on actual efficacy and safety data from longer-term therapeutic studies in patients with various clinical conditions.
No serious adverse reactions were reported in either study.
http://press.endocrine.org/doi/full/10.1210/jc.2005-1536