全球医药市场预测机构eva luate Pharma对今年销售前10位的药品作了估计。曾经叱咤风云的立普妥(阿托伐他汀，Lipitor, Atorvastatin)，完成了它作为销售额龙头老大的历史使命，预计2012年排名跌落至第十位。在前10名药品中，小分子药物日渐式微，而生物技术产品全面崛起，占据半壁江山。生物仿制药的注册审批在各国都有专门的法规。一些公司藉此补充产品线，保持销售竞争力。以下为预估全球销售额前10位治疗药2012年的业绩及市场发展趋势。
1. 修美乐(阿达木单抗, Humira, Adalimumab）销售额：94.8亿美元
生物药问鼎榜首已无悬念。2011年修美乐的销售额为79亿美元，较2009年的55亿美元、2010年的65亿美元均有大幅增长。修美乐于2003年获准 用于类风湿关节炎治疗，鉴于后续拓展的一系列新适应症：银屑病关节炎、强直性脊椎炎、斑块型银屑病、克罗恩病，今年10月初，FDA又批准了它的第7个适 应症——溃疡性结肠炎。预计这一新适应症可为修美乐创造5亿美元收入。
雅培(Abbott Laboratories)正全力以赴保护修美乐免受生物仿制药的袭扰，为此该公司向FDA提交了一份公民请愿书，阻止仿制产品上市。
2. 恩利(依那西普, Enbrel, Etanercept）销售额：83.7亿美元
恩利将在本月失去美国专利保护，不过生产商安进公司(Amgen)已获得了一项新的专利，为恩利赢得另外17年的保护期。这给安进及其合作伙伴辉瑞充分的时间，直至2028年以前都可联合销售该药，用于治疗获准的5种不同适应症。
2011年恩利的销售额为74亿美元，37亿美元为安进的销售收益，另外37亿美元为辉瑞所创造。
3. 舒利迭(沙美特罗-氟替卡松, Advair, Seretide）销售额：80亿美元
尽管已在几个国家失去专利保护，葛兰素史克(GlaxoSmithKline)的舒利迭其销售依然处于高位。这是因为该药的两种活性成分组合放在同一个吸入器内的生产工艺，让竞争者难以模仿复制。
2011年舒利迭的销售额为87亿美元。除了仿制药的竞争，舒利迭的销售还受另一些因素影响。葛兰素史克最近刚刚解决了司法部门的一系列指控，其中包括公司将该药推广给轻度哮喘患者，而FDA批准的适用人群是重度患者。
葛兰素史克需要关注该药在美国的仿制药竞争。Mylan公司2011年为获取传输送技术向辉瑞支付了1750万美元，作为仿制舒利迭的铺垫。
4. 类克(英利昔单抗, Remicade, Infliximab）销售额：76.7亿美元
强 生和默沙东一直分享类克的销售业绩。根据一项营销谈判结果，目前强生已拥有该药的最大份额，成为该公司最大的产品。今年上半年强生的类克销售额增长了 9.1％，达17.7亿美元。自去年7月新的合作协议生效以来，默沙东类克的销售下降至26.7亿美元，今年第一季度的销售又下降了28％。
5. 美罗华(利妥昔单抗, Rituxan ）销售额：69.4亿美元
罗氏(Roche) 的“超级重磅炸弹”美罗华将在明年底失去专利保护。预计直至专利保护期终止，该药也不会受到生物仿制药的竞争威胁。事实上，梯瓦(Teva Pharmaceutical Industries) 刚刚停止了利妥昔单抗的一项试验，到2015年之前不会有任何直接的竞争。美罗华在市场已经叱咤风云了14年，至今继续保持不凡的销售业绩。2011年该药销售额同比增长7％，占罗氏当年总销售收入的15％，超过抗癌药中销售名列前茅的安维汀(Avastin) 和赫赛汀(Herceptin, trastuzumab)。
6. 可定(瑞舒伐他汀钙, Crestor, Rosuvastatin）销售额：66.5亿美元
阿斯利康(AstraZeneca)有足够的能力确保其降胆固醇药可定强劲的销售势头。去年该药的销售额达到66.2亿美元，目前还没有受到仿制药的冲击。今年上半年，可定的销售减少约2％，为30.87亿美元。
阿斯利康希望一项长期研究结果能证实可定有超过阿托伐他汀(Lipitor, Atorvastatin)的优势。但这项SATURN研究表明，虽然可定在降胆固醇方面优于阿托伐他汀，但对保持动脉畅通并没有胜出一筹。
7. 来得时(甘精胰岛素, Lantus）销售额：61.2亿美元
赛诺菲(Sanofi)的降糖药来得时尽管遭遇一些新的竞争，但世界范围内糖尿病的高发病率将使该药在未来几年销售稳定，有数十亿美元的收入。2011年来得时的销售额为 39.16亿欧元（50.7亿美元），同比增长12％。今年上半年，该药销售额增长了16.5％，达23.46亿欧元（30.4亿美元），占据了长效胰岛 素市场80％的份额。
8. 赫赛汀(曲妥珠单抗, Herceptin）销售额：60.8亿美元
长期以来，赫赛汀在乳腺癌治疗药市场占主导地位。罗氏已在世界各地广泛建立了销售队伍。乳腺癌治疗药物的销售额在未来6年将呈上升趋势。由于赫赛汀的专利即将到期（在欧洲为2014年，美国为2018年或2019年），这将为目前已经着手开发的一些生物仿制药开辟新道路。
9. 安维汀（贝伐珠单抗, Avastin）销售额：59.8亿美元
安维汀占据抗癌药市场顶级销售额的席位已经多年。广泛的争议使FDA于2011年11月18日撤销了该药用于乳腺癌治疗的批准。而安维汀治疗湿性年龄相关黄斑变性，令专门用于此症的Lucentis销售受到严重影响。
该药最近在欧洲被建议用于治疗卵巢癌。由于专利保护期终止问题被延长至2019年（美国）和2022年（欧洲），罗氏有相当长一段时间继续从该药销售中获益。
10. 立普妥(阿托伐他汀钙, Lipitor, Atorvastatin)销售额：55.5亿美元
去年，立普妥还雄踞销售额榜首，收入达125亿美元。今年销售额估计下降一半。随着立普妥光环的消退，大公司正在寻找未来的降胆固醇“超级重磅炸弹”。赛诺菲、Regeneron公司和罗氏纷纷在PCSK9抑制剂（高胆固醇血症药理作用新靶点）下功夫。对这些数百万美元的开发投资是否结出硕果，人们将拭目以 待。
此外，销售排名第11~15位的产品及今年全年预测销售额为：安律凡（阿立哌唑, Abilify,Apriprazole，53.8亿美元）、波立维(硫酸氢氯吡格雷，Plavix, Clopidogrel, 51.1亿美元)、欣百达（盐酸度洛西汀，Cymbalta , Duloxetine, 50.1亿美元）、格列卫（甲磺酸伊马替尼，Gleevec , imatinib, 47.2亿美元）、思力华（噻托溴铵, Spiriva , 44.9亿美元）。
The 15 Best Selling Blockbuster Drugs for 2012
Three biologic medicines initially developed to treat rheumatoid arthritis—a joint disorder that afflicts just 1% of the population worldwide—are on track to top the sales charts this year. Humira (adalimumab) and two comparable — Amgen and Pfizer’s Enbrel and Johnson & Johnson and Merck & Co’s Remicade — are set to take second and fourth place behind Humira this year.
Lipitor, once the world’s biggest-selling medications ($12.5 billion) until its patent expired November last year, tumbles from its top-selling spot to the 10th place.
1. Humira – Abbott Laboratories/Eisai – $9.48 billion
Humira was pproved by FDA for treatment of rheumatoid arthritis on Dec 2002 – human monoclonal antibody – Adalimumab (HUMIRA, Abbott) is the third TNF inhibitor, after infliximab and etanercept, to be approved in the United States.
US patent expires December 2016
2. Enbrel – Amgen/Pfizer/Takeda – $8.37 billion
Etanercept (trade name Enbrel) is a fusion protein produced through expression of recombinant DNA. Etanercept, an anti-inflammatory drug, was developed by researchers at Immunex, and was released for commercial use in late 1998.
US patent expiry 2028
3. Advair/Seretide – GlaxoSmithKline – $8 billion
Advair is an inhaled combination of fluticasone and salmeterol for the management of chronic asthma. Advair’s patent expires in March, 2012, but Generic industry veterans Teva (TEVA) and Sandoz (a unit of Novartis) have both been running into problems perfecting GSK’s manufacturing technique.
Approved August, 2000. US patent expired March, 2012.
4. Remicade – Johnson & Johnson/Merck/Mitsubishi Tanabe Pharma – $7.67 billion
Arthritis drug Infliximab (trade name Remicade), J&J’s biggest drug, is a combination of mouse and human antibody, it is called a chimeric monoclonal antibody. Infliximab was developed by Junming Le and Jan Vilcek at New York University School of Medicine and developed by Centocor, (now Jannsen Biotech, Inc.) Other monoclonal antibodies targeting TNF-α are golimumab (Simponi), adalimumab (Humira), and certolizumab pegol (Cimzia). Like all of the TNF inhibitors, infliximab is an expensive medication, costing about US$900 for a 100 mg dose, and is covered by almost every medical insurance plan.
5. Rituxan – Roche – $6.94 billion -
Rituxan (rituximab) is used in combination with other cancer medicines to treat non-Hodgkin’s lymphoma. The megablockbuster moves off patent at the end of next year. While Teva Pharmaceutical Industries just stopped a trial of its Rituxan version, as Boehringer Ingelheim said it was trying to design a clinical trial that would satisfy both U.S. and European regulators at the same time.
US patent expires end of 2013.
6. Crestor – AstraZeneca/Shionogi – $6.65 billion
Crestor (rosuvastatin) is used to reduce cholesterol prevent heart disease. It is manufactured by IPR Pharmaceuticals and is marketed and distributed by AstraZeneca Pharmaceuticals. With Lipitor going generic, Crestor sales are going to feel the impact.
Approved December, 1996. US patent expires November, 2016.
7. Lantus – Sanofi – $6.12 billion
Insulin glargine, marketed by Sanofi-Aventis under the name Lantus, is a long-acting basal insulin analogue, given once daily to help control the blood sugar level of those with diabetes.
8. Herceptin – Roche – $6.08 billion
Herceptin (trastuzumab) is a HER2+ breast cancer therapy designed to treat aggressive HER positive metastatic and adjuvant breast cancer.
US patent expires 2018 or 2019
9. Avastin – Genentech/Roche – $5.98 billion
Avastin (Bevacizumab) is used with chemotherapy to treat various cancers, including colorectal, lung, breast (outside the USA), glioblastoma (USA only), kidney and ovarian. At one point bevacizumab was approved for breast cancer by the FDA, but the approval was revoked on 18 November 2011.
10. Lipitor – Pfizer/Astellas Pharma/Jeil Pharmaceutical – $5.55 billion ($12.5 billion last year)
Lipitor (atorvastatin) lowers LDLs or “bad cholesterol”, reducing the risk of heart attack and stroke.
Approved December, 1996. US patent expired November, 2011.
11. Abilify – Bristol-Myers Squibb/Otsuka Holdings – $5.38 billion
Abilify (apriprazole) is an antipsychotic and antidepressant.
Approved November, 2002. US patent expires October, 2014.
12. Plavix – Sanofi/Bristol-Myers Squibb – $5.11 billion
Plavix (clopidogrel) is an anti platelet agent used to prevent clots, helping prevent heart attacks and strokes.
Approved November, 1997. US patent expired May, 2012.
13. Cymbalta – Eli Lilly/Shionogi – $5.01 billion
Cymbalta (duloxetine) is a drug used to treat depression and anxiety. Lilly recently lost exclusivity with its another anti-psychotic Zyprexa which is facing several genetic competitors. The loss of Cymbalta will further pressure revenues.
Approved in August 2004, US patent expires in June, 2013.
14. Gleevec – Novartis – $4.72 billion
Gleevec (Imatinib) is used to treat certain types of leukemia (cancer that begins in the white blood cells) and other cancers of the blood cells.
FDA approval in May 2001, US patent expires 2015.
15. Spiriva – Boehringer Ingelheim – $4.49 billion
Spiriva (tiotropium Bromide) is used to prevent bronchospasm in people with bronchitis, emphysema, o chronic obstructive pulmonary disease (COPD). Spiriva holds promise as a treatment for asthma, 11 final-stage clinical trials are being conducted.
US patent expires 2014.
