Table of Contents

2012年4月20日，阿斯利康及施贵宝公司2型糖尿病治疗新药达格列净（dapagliflozin，Forxiga）上市许可获欧洲药品管理局（EMA）推荐。

EMA在一份声明中指出，达格列净是一种口服药物，通过抑制钠-葡萄糖转运蛋白2（SGLT2）——肾内的一种使葡萄糖被重新吸收到血液中的蛋白质——而发挥作用。这使得多余的葡萄糖通过尿液被排除体外，从而在不增加胰岛素分泌的情况下改善血糖控制。使用这种药物要求患者的肾功能正常，中至重度肾功能不全患者禁用该药。

达格列净的疗效与二肽基肽酶抑制剂等数种新型降糖药物相当，而且可轻度降低血压和体重。该药有5 mg和10 mg两种片剂可供选择，可单独使用或与包括胰岛素在内的其他糖尿病药物联用。

美国食品药物管理局（FDA）内分泌药物顾问委员会于2011年7月因安全性顾虑而反对批准达格列净上市。临床试验显示，达格列净膀胱癌和乳腺癌风险增加有关：治疗组和对照组的膀胱癌发病率分别为0.16％和0.03％，乳腺癌发病率分别为0.4％和0.22％。EMA则认为，达格列净的收益超过其风险，但已要求生产商进行上市后流行病学研究，以澄清与使用达格列净相关的癌症和其他风险。

1. Name of the medicinal product

2. Qualitative and quantitative composition

3. Pharmaceutical form

4. Clinical particulars

4.1 Therapeutic indications

4.2 Posology and method of administration

4.3 Contraindications

4.4 Special warnings and precautions for use

4.5 Interaction with other medicinal products and other forms of interaction

4.6 Fertility, pregnancy and lactation

4.7 Effects on ability to drive and use machines

4.8 Undesirable effects

4.9 Overdose

5. Pharmacological properties

5.1 Pharmacodynamic properties

5.2 Pharmacokinetic properties

5.3 Preclinical safety data

6. Pharmaceutical particulars

6.1 List of excipients

6.2 Incompatibilities

6.3 Shelf life

6.4 Special precautions for storage

6.5 Nature and contents of container

6.6 Special precautions for disposal and other handling

7. Marketing authorisation holder

8. Marketing authorisation number(s)

9. Date of first authorisation/renewal of the authorisation

10. Date of revision of the text

This medicinal product is subject to additional monitoring. This will allow quick identification of new safety information. Healthcare professionals are asked to report any suspected adverse reactions. See section 4.8 for how to report adverse reactions

 

  1. Name of the medicinal product

 Forxiga▼ 5 mg film-coated tablets

 

Forxiga▼ 10 mg film-coated tablets

 

 2. Qualitative and quantitative composition

 5 mg:

 

Each tablet contains dapagliflozin propanediol monohydrate equivalent to 5 mg dapagliflozin.

 

Excipient with known effect:

 

Each tablet contains 25 mg of lactose anhydrous.

 

For the full list of excipients, see section 6.1.

 

10 mg:

 

Each tablet contains dapagliflozin propanediol monohydrate equivalent to 10 mg dapagliflozin.

 

Excipient with known effect:

 

Each tablet contains 50 mg of lactose anhydrous.

 

For the full list of excipients, see section 6.1.

 

 3. Pharmaceutical form

 Film-coated tablet (tablet).

 

5 mg:

 

Yellow, biconvex, 0.7 cm diameter round, film-coated tablets with “5” engraved on one side and “1427” engraved on the other side.

 

10 mg:

 

Yellow, biconvex, approximately 1.1 x 0.8 cm diagonally diamond-shaped, film-coated tablets with “10” engraved on one side and “1428” engraved on the other side.

 

4. Clinical particulars

   

4.1 Therapeutic indications

 Forxiga is indicated in adults aged 18 years and older with type 2 diabetes mellitus to improve glycaemic control as:

 

Monotherapy

 

When diet and exercise alone do not provide adequate glycaemic control in patients for whom use of metformin is considered inappropriate due to intolerance.

 

Add-on combination therapy 

 

In combination with other glucose-lowering medicinal products including insulin, when these, together with diet and exercise, do not provide adequate glycaemic control (see sections 4.4, 4.5 and 5.1 for available data on different combinations).

 

 4.2 Posology and method of administration

 Posology

 

Monotherapy and add-on combination therapy