Triptorelin Acetate

Triptorelin is a GnRH agonist analog with a D-Trp substitution at position 6 that confers resistance to enzymatic degradation and increases receptor affinity. Initial administration causes a transient surge in LH, FSH, and sex steroids (flare effect). Continuous or depot administration leads to GnRH receptor downregulation and desensitization, resulting in profound suppression of the gonadal axis (medical castration). This reversible chemical castration suppresses testosterone (males) and estrogen (females) to near-zero levels.