2010年5月,Amgen公司开发的狄诺塞麦(Denosumab/prolia)获得欧盟委员会批准,用于治疗肿瘤和肿瘤转移导致的骨相关事件(SRE)。同年6月,狄诺塞麦获得美国FDA的批准,获准的适应证为:①用于增加因患有乳腺癌正在接受芳香酶抑制剂治疗而处在骨折高风险的妇女的骨质;②用于增加因患有前列腺癌正在接受趋势疗法而处在骨折高风险的男性的骨质。狄诺塞麦是一种人源化的单克隆抗体类生物制剂。
PROLIA
Generic Name for PROLIA
Denosumab 60mg/mL; soln for SC injection; preservative-free.
Legal Classification:
Rx
Pharmacological Class for PROLIA
Osteoclast inhibitor (RANKL inhibitor).
Manufacturer of PROLIA
Amgen, Inc.
Indications for PROLIA
In postmenopausal women with osteoporosis: at high risk for fracture, defined as a history of osteoporotic fracture, or multiple risk factors for fracture; or patients who have failed or are intolerant to other therapy; to reduce incidence of vertebral, nonvertebral, and hip fractures. To increase bone mass in men at high risk for fracture receiving androgen deprivation therapy for nonmetastatic prostate cancer; to reduce incidence of vertebral fractures. To increase bone mass in women at high risk for fracture receiving adjuvant aromatase inhibitor therapy for breast cancer.
Adult dose for PROLIA
Should be administered by a healthcare professional. 60mg SC once every 6 months; inject into upper arm, upper thigh, or abdomen.
Children's dosing for PROLIA
Not recommended.
Contraindications for PROLIA
Hypocalcemia. Pregnancy (Cat.X).
Warnings/Precautions for PROLIA
Correct hypocalcemia before starting; ensure adequate daily calcium (≥1000mg) and Vit. D (≥400IU) intake, esp. in renal impairment (CrCl<30mL/min). Monitor calcium, phosphorus, magnesium levels in susceptible patients (hypoparathyroidism, thyroid or parathyroid surgery, malabsorption, excision of small intestine, severe renal impairment, on dialysis). Monitor for infections, jaw osteonecrosis, bone oversuppression. Do baseline oral exam and preventive dentistry if risks for jaw osteonecrosis exist (eg, tooth extraction, dental implants, oral surgery, poor oral hygiene, periodontal disease and/or other pre-existing dental disease, ill-fitting dentures, cancer, anemia, coagulopathy, infection). Maintain good oral hygiene. Immunosuppressed. Latex allergy (prefilled syringe). Nursing mothers: avoid (may impair mammary glands/lactation).
Interactions for PROLIA
Concomitant other denosumab-containing products (eg, Xgeva): not recommended. Concomitant immunosuppressants (increased infection risk). Corticosteroids, chemotherapy (increased jaw osteonecrosis risk).
Adverse Reactions for PROLIA
Pain (back, lower extremities or musculoskeletal), arthralgia, hypercholesterolemia, cystitis; infections (may be serious; eg, cellulitis, UTI, otic, abdominal), dermatitis, rash, eczema, osteonecrosis of jaw, suppression of bone turnover, exacerbation of hypocalcemia, pancreatitis.
How is PROLIA supplied?
Single-use vial (1mL)—1; Single-dose prefilled syr (1mL)—1
Related Disease:
Bone disorders
Osteoporosis~bone metabolism 
Prolia (denosumab)
1. Prolia 曾獲選為美國時代雜誌(Time) 10 大醫療突破之一 (10 medical breakthroughs in 2009)。
2. 因為Prolia 是第一個且唯一的RANK Ligand Ihibitor，以模仿OPG(保骨素)的作用有效抑制蝕骨細胞的生成、作用與存活。不同於雙磷酸鹽的作用機轉，Prolia 也有與雙磷酸鹽不同的療效/安全性優勢。
3. 根據NEJM發表的FREEDOM study:
(1)可顯著降低68%的新脊椎骨折、40%的髖骨骨折與20%的非脊椎骨折的風險。(2)Prolia發生一般與嚴重不良反應的比例與Placebo相當。
4. 根據DECIDE及STAND study:
(1) Prolia 對骨骼強度與結構影響優於alendronate。(2) Prolia 對增加骨骼扭轉的承受力(PMI) 顯著優於alendronate。(3)而Prolia在緻密骨(cortical bone) 的骨密度、厚度都優於alendronate。
5. 任何時間皆可注射，不用考慮用餐時間，不用補充水分。
6. 對腎功能受損的患者並不需要調整劑量。
7. Prolia通過網狀內皮系統由血清排除，不經由肝臟的細胞色素P450系統代謝。
8. 每6個月皮下注射一次，簡單方便；不用躺著輸注或站著吃藥
Product Name : XGEVA SOLUTION FOR INJECTION 120MG
Ingredients : DENOSUMAB。