Denosumab

Denosumab is a human monoclonal antibody (IgG2) that targets and binds with high affinity and specificity to RANKL, preventing RANKL from activating its receptor, RANK, on the surface of osteoclasts and their precursors. Prevention of the RANKL/RANK interaction inhibits osteoclast formation, function and survival. Denosumab therefore reduces bone resorption and increases bone mass and strength in both cortical and trabecular bone.

• Postmenopausal osteoporosis at high risk for fracture
• Bone mass increase in men with osteoporosis
• Glucocorticoid-induced osteoporosis
• Bone loss in men receiving androgen deprivation therapy for prostate cancer
• Bone loss in women receiving adjuvant aromatase inhibitor therapy for breast cancer
• Prevention of skeletal-related events in multiple myeloma and bone metastases from solid tumors
• Giant cell tumor of bone
• Hypercalcemia of malignancy refractory to bisphosphonate therapy

Denosumab is a human IgG2 monoclonal antibody with affinity and specificity for human RANKL. Denosumab binds to RANKL, a transmembrane or soluble protein essential for the formation, function, and survival of osteoclasts. Prevention of the RANKL/RANK interaction inhibits osteoclast formation, function, and survival, thereby decreasing bone resorption and increasing bone mass and strength.

Denosumab binds to RANKL, preventing RANK receptor activation, inhibiting osteoclast formation and function, reducing bone resorption and increasing bone mass and strength.

Osteoporosis and Bone Loss: 60 mg SC every 6 months.
Multiple Myeloma and Bone Metastasis: 120 mg SC every 4 weeks.
Giant Cell Tumor: 120 mg SC every 4 weeks (with additional 120 mg on Days 8 and 15 of the first month).
Hypercalcemia of Malignancy: 120 mg SC every 4 weeks (with additional 120 mg on Days 8 and 15 of the first month).

This medicine is given as a subcutaneous injection (upper arm, upper thigh, or abdomen) by a healthcare professional. Kindly do not self administer.

If you miss a dose of Denosumab, please consult your doctor.

Postmenopausal osteoporosis: Back pain, pain in extremity, hypercholesterolemia, musculoskeletal pain, cystitis.
Male osteoporosis: Back pain, arthralgia, nasopharyngitis.
Bone metastasis: Fatigue, hypophosphatemia, nausea.
Multiple myeloma: Diarrhea, nausea, anemia, thrombocytopenia.

Hypocalcemia: Correct before initiating therapy; Osteonecrosis of the jaw; Atypical femoral fractures; Multiple vertebral fractures following discontinuation; Serious infections including skin infections; Severe pain; Suppression of bone turnover; Embryo-fetal toxicity.

Hypocalcemia; Pregnancy; Hypersensitivity.

Immunosuppressive agents: Increased risk of serious infections.
Denosumab must not be mixed with other medicinal products.

Caution is advised when consuming alcohol with Denosumab. Please consult your doctor.

Pregnancy Category X. Denosumab is highly unsafe during pregnancy. May cause fetal harm. Females of reproductive potential should use effective contraception during therapy and for at least 5 months after the last dose.

Denosumab is probably safe during breastfeeding. Limited human data suggests that the drug does not represent any significant risk to the baby.

Denosumab is not approved for use in pediatric patients (except for skeletally mature adolescents with giant cell tumor of bone).

No overall differences in safety or efficacy were observed between elderly and younger patients.

Renal impairment: No dose adjustment necessary. Patients with CrCl <30 mL/min or on dialysis are at risk for hypocalcemia; calcium and vitamin D supplementation is important.
Hepatic impairment: No clinical studies have been conducted.

Treatment of overdose should consist of observation and general supportive measures.

Store in a refrigerator at 2°C to 8°C in the original carton. Do not freeze. Once removed from the refrigerator, use within 14 days.

Denosumab