阿仑膦酸钠已证实可降低髋关节和脊柱骨折危险性
瑞士FREIENBACH--(美国商业资讯)--EffRx Pharmaceuticals SA今日宣布，美国食品药品监督管理局（FDA）已批准BINOSTO（阿仑膦酸钠）泡腾片，该药品以前称为EX101，用于治疗绝经后女性的骨质疏松症，并且还可用于提高男性骨质疏松症患者的骨量。EffRx预期 BINOSTO将于2012年第三季度在美国上市。
EffRx董事长兼首席执行官Christer Rosén表示：“收到FDA的这项批准，我们非常高兴。BINOSTO®是用于骨质疏松治疗的突破性创新产品，以美味和易于吞咽的缓冲液给药方式，为那些服用片剂困难的患者提供阿仑膦酸钠，该制剂已被证实可降低骨折风险。”
骨质疏松症在全球7大市场上影响超过2亿人，预估的全球市场高达100亿美元，并且仍在持续增长，特别是在新兴市场这种增长趋势更加显著。BINOSTO是一种创新的治疗选择方案，可向医生确保为那些服用片剂困难的患者提供已经证实有效的治疗。一项美国哈里斯互动民意调查（Harris Interactive Poll）总结显示，高达40%的美国成年人存在吞咽片剂困难的问题。
关于BINOSTO：
BINOSTO是一种含有70mg阿仑膦酸钠的泡腾片，它带有草莓香味，可快速溶解于半杯（4盎司）室温纯水中并形成缓冲溶液，每周仅需给药一次。BINOSTO现有包装为4片和12片。
在与默克公司（Merck & Co, Inc.）达成授权EffRx世界范围所有FOSAMAX（阿仑膦酸钠）泡腾片及相关专利协议的基础上，EffRx开发了BINOSTO。这些专利已被授予EffRx，直到2023年2月BINOSTO®由EffRx独家所有。其他相关专利已申请，仍在审查待批。
关于EffRx：
EffRx Pharmaceuticals SA是一家从事药物释放的公司，总部位于瑞士Freienbach。该公司利用其不同的泡腾实施创新技术，专长于改进现有的高容量药物产品。EffRx的主要工作重心放在代谢性骨病、肿瘤支持治疗、儿童用药领域，并为大型生命周期管理（Life Cycle Management）公司提供支持。
EffRx已与Takeda旗下的奈科明公司（Nycomed）达成授权协议。
FDA已批准BINOSTO——全球首个也是唯一的用于治疗骨质疏松的可缓冲液给药的泡腾片剂
MANUFACTURER:
Mission Pharmacal Company
PHARMACOLOGICAL CLASS:
Bisphosphonate.
ACTIVE INGREDIENT(S):
Alendronate (as sodium) 70mg; effervescent tabs for oral soln; strawberry-flavor; contains 650mg sodium/tab.
INDICATION(S):
Treatment of postmenopausal osteoporosis. To increase bone mass in men with osteoporosis.
PHARMACOLOGY:
Alendronate binds to bone hydroxyapatite and specifically inhibits the activity of osteoclasts, the bone-resorbing cells. It reduces bone resorption with no direct effect on bone formation, although the latter process is ultimately reduced because bone resorption and formation are coupled during bone turnover.
CLINICAL TRIALS:
Binosto (alendronate sodium) effervescent tablet 70mg is bioequivalent to alendronate sodium tablet 70mg. The fracture reduction efficacy and bone mineral density changes attributed to Binosto are based on clinical trial data of alendronate sodium 10mg daily and alendronate sodium 70mg weekly.
LEGAL CLASSIFICATION:
Rx
ADULTS:
Dissolve one tab in 4oz plain (not mineral) water only; after effervescence stops, wait 5mins and stir soln for 10secs. Take in the AM at least 30 minutes before the first food, drink, or medication of the day. Do not lie down for at least 30 minutes and until after the first food of the day. 70mg once weekly.
CHILDREN:
Not recommended.
CONTRAINDICATION(S):
Esophagus abnormalities which delay esophageal emptying (eg, stricture, achalasia). Inability to stand or sit upright for at least 30 minutes. Increased risk of aspiration. Hypocalcemia.
WARNINGS/PRECAUTIONS:
Active upper GI disease; discontinue and reeva luate if signs/symptoms of esophageal reaction occur. Severe renal impairment (CrCl <35mL/min): not recommended. Correct preexisting hypocalcemia or other mineral metabolism disorders (eg, Vit. D deficiency) before starting. Monitor for hypocalcemia during therapy. Ensure adequate Vit. D and calcium intake. Sodium restriction (including heart failure, hypertension, or other cardiovascular diseases). Consider discontinuing therapy during invasive dental procedures (eg, tooth extraction, implants, boney surgery). History of bisphosphonate exposure: eva luate for atypical fractures if thigh/groin pain develops; consider withholding therapy until risk/benefit assessment. Reeva luate periodically. Pregnancy (Cat.C). Nursing mothers.
INTERACTION(S):
Calcium supplements, antacids, other multivalent cations reduce absorption (separate dosing by at least 30min). Increased upper GI events with aspirin-containing products and alendronate >10mg/day; caution with NSAIDs.
ADVERSE REACTION(S):
Abdominal pain, acid regurgitation, constipation, diarrhea, dyspepsia, musculoskeletal pain (may be severe), nausea; esophagitis, esophageal ulcers or erosions; jaw osteonecrosis, atypical femur fractures; rarely: gastric or duodenal ulcer.
HOW SUPPLIED:
Tabs—4, 12
LAST UPDATED:
10/29/2012
BINOSTO® (alendronate sodium) Dosing
Dosing Instructions
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BINOSTO should only be taken upon arising for the day and must be taken at least 30 minutes before the first food, beverage, or medication of the day
Click on the arrow to see how to prepare BINOSTO.
Patients should not lie down for at least 30 minutes after taking BINOSTO and until after their first food of the day
BINOSTO should not be taken at bedtime or before arising for the day
Waiting less than 30 minutes, or taking BINOSTO with food, beverages (other than plain water) or other medications will lessen the effect of BINOSTO by decreasing its absorption into the body
Failure to follow these instructions may increase the risk of esophageal adverse reactions
Recommendations for Calcium and Vitamin D Supplementation
Patients should receive supplemental calcium and vitamin D, if dietary intake is inadequate. Patients at increased risk for vitamin D insufficiency (e.g., over the age of 70 years, nursing home-bound, or chronically ill) may need vitamin D supplementation. Patients with gastrointestinal malabsorption syndromes may require higher doses of vitamin D supplementation and measurement of 25-hydroxyvitamin D should be considered.
完整说明书附件：http://www.drugs.com/pro/binosto.html