SPL Set ID: b78d1919-9dee-44fa-90f9-e0a26d32481d

ELIGARD ® is a sterile polymeric matrix formulation of leuprolide acetate, a GnRH agonist, for subcutaneous injection. It is designed to deliver leuprolide acetate at a controlled rate over a one-, three-, four- or six-month therapeutic period. Leuprolide acetate is a synthetic nonapeptide analog of naturally occurring gonadotropin releasing hormone (GnRH) that, when given continuously, inhibits pituitary gonadotropin secretion and suppresses testicular and ovarian steroidogenesis. The analog possesses greater potency than the natural hormone. The chemical name is 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-leucyl-L-arginyl-N-ethyl-L-prolinamide acetate (salt) with the following structural formula: ELIGARD ® is prefilled and supplied in two separate, sterile syringes whose contents are mixed immediately prior to administration. The two syringes are joined and the single dose product is mixed until it is homogenous. ELIGARD ® is administered subcutaneously, where it forms a solid drug delivery depot. One syringe contains the ATRIGEL ® Delivery System and the other contains leuprolide acetate. ATRIGEL ® is a polymeric (non-gelatin containing) delivery system consisting of a biodegradable poly (DL-lactide-co-glycolide) (PLGH or PLG) polymer formulation dissolved in a biocompatible solvent, N-methyl-2-pyrrolidone (NMP). Refer to Table 6 for the delivery system composition and reconstituted product formulation for each ELIGARD ® product. Table 6. ELIGARD ® Delivery System Composition and Reconstituted Product Formulation ELIGARD ® 7.5 mg 22.5 mg 30 mg 45 mg ATRIGEL ® Delivery System syringe Polymer PLGH PLG PLG PLG Polymer description Copolymer containing carboxyl endgroups Copolymer with hexanediol Copolymer with hexanediol Copolymer with hexanediol Polymer DL-lactide to glycolide molar ratio 50:50 75:25 75:25 85:15 Reconstituted product Polymer delivered 82.5 mg 158.6 mg 211.5 mg 165 mg NMP delivered 160.0 mg 193.9 mg 258.5 mg 165 mg Leuprolide acetate delivered 7.5 mg 22.5 mg 30 mg 45 mg Approximate Leuprolide free base equivalent 7.0 mg 21 mg 28 mg 42 mg Approximate administered formulation weight 250 mg 375 mg 500 mg 375 mg Approximate injection volume 0.25 mL 0.375 mL 0.5 mL 0.375 mL 153d1272-figure-12