Table 2.
Summary of steady‐state pharmacokinetic parameters by treatment
| PK parameters at week 6 | 50 mg SC TE (n = 14) | 100 mg SC TE (n = 15) | 200 mg IM TE (n = 10) | Ratio of SC TE 100/SC TE 50 | Ratio of 200 mg IM TE/100 mg SC TE |
|---|---|---|---|---|---|
| Testosterone | |||||
| Mean AUC0–168h—ng × h/dL (SD) | 70955.7 (20815.2) | 150445.2 (46998.8) | 278657.9 (168295.5) | 2.13 | 1.85 |
| Cavg0–168h | |||||
| Mean—ng/dL (SD) | 422.4 (123.9) | 895.5 (279.8) | 1658.7 (1001.8) | 2.12 | 1.85 |
| Range—ng/dL | 257–673 | 406–1,368 | 681–3,758 | ||
| Number of patients with Cavg0–168h within 300–1,100 ng/dL | 12 | 10 | 3 | ||
| Cavg0–336h | |||||
| Mean—ng/dL (SD) | 409.6 (96.1) | 868.5 (256.5) | 1267.5 (724.5) | 1.4 † | |
| Number of patients with Cavg0–336h within 300–1,100 ng/dL | 12 | 11 | 5 | ||
| Cmax—ng/dL | |||||
| Mean (SD) | 622.4 (129.5) | 1345.6 (435.6) | 2261.9 (1310.3) | 2.17 | 1.7 |
| Range | 388–825 | 624–2,120 | 787–4,840 | ||
| Cmin—ng/dL | |||||
| Mean (SD) | 272.9 (54.7) | 568.3 (196.4) | 466.1 (199.1) | 2.08 | 0.82 |
| Range | 182–372 | 236–860 | 203–780 | ||
| Mean Tmax—h (SD) | 45.43 (33.60) | 35.54 (30.40) | 33.30 (24.52) | ||
| Mean T½—h (SD) | ND ‡ | 239.63 (59.93) | 172.57 (34.74) | ||
| DHT | |||||
| Mean AUC0–168h—ng × h/dL (SD) | 5173.8 (1641.4) | 8718.4 (2436.8) | 19668.6 (11145.0) | ||
| Mean DHT/T ratio § | 0.0750 | 0.0609 | 0.0732 | ||
| Mean Cavg0–168h—ng/dL (SD) ¶ | 30.8 (9.8) | 51.9 (14.5) | 117.1 (66.3) | ||
| E2 | |||||
| Mean AUC0–168h—ng × h/dL (SD) | 429.2 (139.4) | 811.0 (344.9) | 839.4 (478.1) | ||
| Mean E2/T ratio § | 0.0063 | 0.0055 | 0.0032 | ||
| Mean Cavg0–168h—pg/mL (SD) ¶ | 25.6 (8.3) | 48.3 (20.5) | 50.0 (28.5) |
| Testosterone PK parameters (combined weeks 5 and 6) | 50 mg SC TE | 100 mg SC TE | 200 mg IM TE | Ratio of SC TE 100/SC TE 50 | Ratio of 200 mg IM/100 mg SC TE |
|---|---|---|---|---|---|
| Mean AUC0–336h—ng × h/dL (SD) | 137620.1 (32282.2) | 291829.3 (86197.7) | 425879.5 (243433.7) | 2.13 | 1.45 |
| Mean AUC0‐inf—ng × h/dL (SD) | 376238.6 ‡ | 541221.9 (140895.3) | 517679.0 (193305.0) | 1.45 | 0.95 |
†Calculation for the 168‐h dosing interval for SC TE and 336‐h dosing interval for IM TE. ‡n = 1 due to rising T levels at later time points in 13/14 patients. §Ratio of AUC0–168h of metabolite to AUC0–168h of T. ¶Reference range was defined as 300–1,100 ng/dL for T, 4–57.5 ng/dL for DHT, and 10–50 pg/mL for E2. AUC = area under the concentration–time curve; DHT = dihydrotestosterone; E2 = estradiol; IM = intramuscular; ND = not determined; PK = pharmacokinetic; SC = subcutaneous; SD = standard deviation; T = testosterone; TE = testosterone enanthate