This study evaluated the growth performance, testicular and semen characteristics, and hormonal profile of Markhoz (Iranian Angora) bucklings injected with letrozole (LTZ). Twenty-eight 4–4.5 month old bucks were randomly assigned into four groups and received either 0.25 mg/kg body weight (BW) LTZ subcutaneously (sc LTZ) or intramuscularly (im LTZ), and also sc (sc CONT) or im (im CONT) controls every week for 3 months. The study was performed at the beginning of the breeding season in Sanandaj Animal Husbandry Research Station (46.99 °E, 35.31 °N). The results showed that LTZ causes increased final body weight (25.78 ± 1.61 kg), higher average daily gain (104 ± 0.03 g/days), and decreased feed conversion ratio (7.81 ± 2.57) (P < 0.05). The pre-slaughter, hot, and cold carcass weights (27.56 ± 2.40, 11.45 ± 1.07 and 11.11 ± 1.05 kg, respectively) were (P < 0.05) heavier in LTZ groups while other carcass characteristics did not differ between groups. No differences occurred between the groups in biochemical parameters, except high-density lipoprotein levels (35.47 ± 2.43 mg/dL) which was higher in LTZ treatments (P < 0.05). LTZ-treated bucks had larger scrotal circumference (20.12 ± 5.75 cm), higher relative testicular weight (560.91 ± 78.59 mg/100 g BW) and volume (175.5 ± 29.71 cm3), greater diameter of seminiferous tubules (224.5 ± 5.21 μm), and number of Sertoli cells (8.39 ± 0.77) (P < 0.05). Semen volume (0.74 ± 0.16 mL), sperm concentration (2.64 ± 0.19 × 10−9/mL), total sperm per ejaculate (1.95 ± 0.49 × 10−9), and semen index (1248 ± 323) increased (P < 0.05) by LTZ treatments, while semen pH (6.77), motility (80.91%), progressive motility (76.75%), viability (83.35%), abnormality (13.70%), acrosome integrity (78.06%), and membrane integrity (80.05%) of sperm remained unaffected. Intratesticular and serum testosterone (T) levels (7.97 ± 0.89 ng/mg protein and 2.47 ± 0.59 ng/mL, respectively), serum luteinizing hormone (LH), growth hormone (GH) levels (1.71 ± 0.24 and 3.62 ± 0.33 ng/mL, respectively) of LTZ groups were elevated, whereas intratesticular and serum estradiol (E2) levels (84.14 ± 8.15 pg/mg protein and 32.33 ± 2.16 pg/mL, respectively) decreased (P < 0.05). No differences were recorded between the sc and im routes of LTZ administration in the measured parameters. To conclude, we have found that LTZ treatment improves growth and reproductive functions of goat bucklings associated with increased serum LH and GH, elevated T and reduced E2 levels in both serum and testis.