Indications
Prolia. Treatment of osteoporosis in postmenopausal
women who are at high risk for fracture or those who
have failed/are intolerant of conventional osteoporosis
therapy. To increase bone mass in men with osteoporosis
who are at high risk for fracture or those who have
failed/are intolerant of conventional osteoporosis therapy.
To increase bone mass in men receiving androgen
deprivation therapy for nonmetastatic prostate cancer
who are at high risk for fracture. To increase bone
mass in women receiving adjuvant aromatase inhibitor
therapy for breast cancer who are at high risk for fracture.
Xgeva. Prevention of skeletal-related events in patients
with bone metastases from solid tumors. Giant
cell tumor of bone that is unresectable or where surgical
resection is likely to result in severe morbidity.
Treatment of hypercalcemia of malignancy that is refractory
to bisphosphonate therapy.
Action
A monoclonal antibody that binds specifically to the human
receptor activator of nuclear factor kappa-B-ligand
(RANKL), which is required for formation, function,
and survival of osteoclasts. Binding inhibits
osteoclast formation, function, and survival. Therapeutic
Effects:pbone resorption withpoccurrence
of fractures (vertebral, nonvertebral, hip) or other
skeletal-related events (e.g., radiation therapy to bone,
surgery to bone, spinal cord compression).qbone
mass.
Pharmacokinetics
Absorption: Well absorbed following subcutaneous
administration.
Distribution: Unknown.
Metabolism and Excretion: Unknown.
Half-life: 25.4 days.
TIME/ACTION PROFILE (effects on bone
resorption)
ROUTE ONSET PEAK DURATION
Subcut 1 mo unknown† 12 mo‡
†Maximumpin serum calcium occurs at 10 days.
‡Following discontinuation.
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Hypocalcemia
(correct before administering); adequate supplemental
calcium and vitamin D required; OB: May
cause fetal harm; Lactation: Avoid use;pmammary
gland development and lactation.
Use Cautiously in: Conditions associated with hypocalcemia
including hypoparathyroidism, previous
thyroid/parathyroid surgery, malabsorption syndromes,
history of small intestinal excision, inadequate/no calcium
supplementation, renal impairment/hemodialysis
(CCr 30 mL/min and/or on dialysis); monitoring of
calcium levels and calcium and vitamin D intake recommended;
Invasive dental procedures, cancer, receiving
chemotherapy, corticosteroids, or angiogenesis inhibitors,
poor oral hygiene, diabetes. gingival
infections, periodontal disease, dental disease, anemia,
coagulopathy, infection, or poorly-fitting dentures (may
qrisk of jaw osteonecrosis); Concurrent use of immunosuppressants
or diseases resulting in immunosuppression
(qrisk of infection); Geri: May be more sensitive
to drug effects; Rep: Women of reproductive
potential (use effective contraception) (for Xgeva only);
Pedi: Safety and effectiveness not established.
Adverse Reactions/Side Effects
CNS: headache. GI: PANCREATITIS, diarrhea, nausea.
GU: cystitis. Derm: dermatitis, eczema, rashes. F
and E: hypocalcemia, hypophosphatemia, hypercalcemia.
Metab: hypercholesterolemia. MS: back pain,
extremity pain, musculoskeletal pain, atypical femoral
fracture, osteonecrosis of the jaw, suppression of bone
turnover. Resp: dyspnea, cough. Misc: hypersensitivity
reactions including ANAPHYLAXIS, infection.
Interactions
Drug-Drug: Concurrent use of immunosuppressantsqrisk
of infection.
Route/Dosage
Prolia
Subcut (Adults): 60 mg every 6 mo.
Xgeva
Subcut (Adults ): Bone metastasis from solid tumors—
120 mg every 4 weeks; Giant cell tumor of
bone—120 mg every 4 weeks, with additional doses of
120 mg given on Days 8 and 15 of first mo of therapy;
Hypercalcemia of malignancy—120 mg every 4
weeks, with additional doses of 120 mg given on Days 8
and 15 of first mo of therapy.
Availability
Solution for subcutaneous injection (Prolia)
(prefilled syringe): 60 mg/mL. Solution for subcutaneous
injection (Xgeva): 120 mg/1.7 mL.
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