Jet Injector
Pharmacokinetic Profile of 50 Mg and 100 Mg Doses of Subcutaneous Testosterone Enanthate Administered with the Novel Jet-InjectorTM
http://press.endocrine.org/doi/abs/10.1210/endo-meetings.2014.RE.12.SUN-0056
Topical treatments for males with hypogonadism (HGM) result in physiologic testosterone (T) concentrations but require daily administration, dose titration, and carry risk of transfer to women and children, leading to abnormal development of male sexual characteristics. T for IM injection (IMT) does not carry this risk, but may be painful, inconvenient, and typically cannot be self-administered. IMT may also be associated with T level peaks and troughs leading to mood swings. The pharmacokinetic (PK) profile of subcutaneous T enanthate (TE) administered with the Jet-Injector™ (JT), a novel, pre-filled, self-administration system for T, were studied.
Twenty adults (age 31-69) with HGM (T <300 mg/dL at two screening visits with documented clinical symptoms received 50 mg (n=10) or 100 mg (n=10) JT weekly for 6 weeks in clinic administered by a healthcare professional. Mean baseline T was 301 ng/dL for patients in the 50 mg group and 214 ng/dL in the 100 mg group. At week 1, both doses produced normal mean total T concentrations 24 h post-dose (433 ng/dL in the 50 mg group [range 197-821 ng/dL] and 545 ng/dL in the 100 mg group [range 388-833 ng/dL]). Pre- and post-dose T levels rose with successive doses and plateaued at week 5. At week 6, 24 h post-dose mean T was 421 ng/dL in the 50 mg group (range 263-640) and 1042 ng/dL in the 100 mg group (range 526-1420). In the 50 mg group, T C[SUB]min[/SUB] was generally unchanged. In the 100 mg group, T C[SUB]min[/SUB]increased through week 5.
Steady state Cavg[SUB][0-168h][/SUB] T levels at week 6 were higher in the 100 mg group vs. the 50 mg group (927 vs. 420 ng/dL; 2.21-fold higher). In the 50 mg group at week 6, C[SUB]max[/SUB] was 624 ng/dL (range 388-825 ng/dL) and T[SUB]max[/SUB] was 46.2 h; C[SUB]min[/SUB] was 286 ng/dL (range 211-372 ng/dL). In the 100 mg dose at week 6, C[SUB]max[/SUB] was 1427 ng/dL (range 662-2120 ng/dL) and T[SUB]max[/SUB] was 33.9 h; C[SUB]min[/SUB] was 584 ng/dL (range 236-860 ng/dL). Mean AUC[SUB](0-168h) [/SUB]at week 6 was 704.96 and 1556.94 ng*h/ml for the 50 and 100 mg doses, respectively. Serum estradiol and dihydrotesterone rose proportionately with T levels. JT injection took 3-4 seconds per patient and consistently provided the precise dose.
JT rapidly restored and maintained steady, physiologic Cavg[SUB][0-168h][/SUB] levels of T with attenuated peak to trough fluctuations relative to that seen with higher doses of TE administered on a 1-2 times per month schedule. This may be clinically important in avoiding treatment-related mood swings observed with IM TE. These PK data suggest that JT may represent an alternative to daily topical T that decreases risks associated with secondary exposure while delivering T replacement weekly via a self-administration option.