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Astellas和小野公司的口服二膦酸盐Bonoteo／Recalbon（minodronate）已在日本获批准用于治疗骨质疏松。对于每日服用一次的该药来说，此次批准在全球尚属首次。当地的Ⅲ期临床试验显示，与安慰剂相比，该药在脊柱骨折发生率方面有显著获益。同时公司还强调了1mg本品在肠胃副作用方面有很大的减少和高度有效。
ボノテオ錠1mg
商標名
Bonoteo Tablets 1mg
一般名
ミノドロン酸水和物（Minodronic Acid Hydrate）
化学名
［1-Hydroxy-2-（imidazo［1,2-a］pyridin-3-yl）ethylidene］ bisphosphonic acid monohydrate
構造式
分子式
C9H12N2O7P2・H2O
分子量
340.16
融点
約250℃（分解）
性状
ミノドロン酸水和物は白色～微帯赤白色の結晶又は結晶性の粉末である。水に極めて溶けにくく、エタノール（99.5）にほとんど溶けない。水酸化ナトリウム試液に溶ける。
製造販売
アステラス製薬株式会社
原处方附附件：http://www.info.pmda.go.jp/go/pack/3999026F1026_1_10/3999026F1026_1_10?view=body
Osteoporosis is a systemic bone disease characterized by decreased bone strength leading to an increased risk of bone fractures. It is estimated that over 10 million people, including potential patients, are suffering from the condition in Japan but that the number of patients continues to increase as aging population grows. Elderly osteoporosis patients in particular are liable to vertebral or femoral neck fracture keeping some of them in bed, and therefore measures to tackle the disease by not only therapeutic but social means have been an important issue.
Minodronic acid hydrate is an orally taken bisphosphonate that was first discovered in Japan and exhibits extremely potent inhibition of bone resorption* in the class. It is the first drug that demonstrated significant effect in prevention of bone fractures superior to placebo in Japanese osteoporosis patients in Phase III double blind comparative study.
It is expected that the drug, once launched, can contribute to the improvement of the patients' quality of life by offering an additional therapeutic option for the treatment of osteoporosis.
The drug will be available under the brand name of RECALBON® Tablets 1mg by Ono and Bonoteo® Tablets 1mg by Astellas respectively.
Bone resorption: The process by which osteoclasts break down old bone losing elasticity and hardness.
Dosage and administration:
Normally in adults, 1 mg of minodronic acid hydrate is taken orally together with enough amount of water (180 mL) (or lukewarm water) once a day at the time of awakening. The drug must be taken without lying down at least for 30 minutes before the first food, beverage (other than plain water), and other oral medication.
Distinctive features:
1. Minodronic acid hydrate is a bisphosphonate that was first discovered in Japan.
2. It is also the first bisphosphonate that demonstrated significant effect in prevention of bone fractures superior to placebo in Japanese osteoporosis patients.
3. It shows an excellent effect in increment of bone mineral density (BMD).
4. It also exhibits potent reduction of a bone resorption marker from the beginning of the treatment with the drug.
5. It exhibits extremely potent inhibition of bone resorption (in vitro and in rats).
6. The drug is in an easy-to-administrated small film coated tablet (6.6 mm in diameter, 3.0 mm thick.)
7. Incidence of adverse reactions (side effects) was observed in 18.6% (206 out of 1,108 patients) including abnormal laboratory test values, and those include stomach and abdominal discomfort in 35 patients (3.2%), abdominal pain in 27 patients (2.4%), decrease in blood calcium level in 22 patients (2.0%), and gastritis in 15 patients (1.4%). Disorders in upper gastrointestinal tract such as duodenal ulcer and gastric ulcer were reported as clinically significant adverse reactions.
Packaging:
RECALBON® Tablets 1mg: 100 tablets (blister packaging and bottle)
Bonoteo® Tablets 1mg: 100 tablets (blister packaging) and 500 tablets (bottle)
Source: Ono Pharmaceutical Co., Ltd |
