U.S. court rules: Johnson & Johnson's patent on heavy drug abiraterone is invalid

Last Friday (2018On October 26, 2002), the U.S. District Court of New Jersey ruled that the U.S. patent US8822438 of Johnson's prostate cancer drug Zytiga(abiraterone acetate, Abiraterone acetate) was invalid. This result was consistent with the decision made by the U.S. Patent and Trademark Office (USPTO) earlier this year. Johnson's patent is scheduled to expire in 2027. Analysts pointed out that the patent was ruled invalid, will open the door to Zytiga's generic drug market.

But Johnson & Johnson is US8822438 about its patents.According to a previous statement, the company has once again submitted a request to the USPTO for reconsideration of the disputed patent, stressing that "the commercial launch of a generic Zytiga drug before the outcome of the appeal will be considered a dangerous action".

Abiraterone Introduction

Name: Tandoro, Abiraterone Acetate (abiraterone acetate)

Product: Abiraterone (ZYTIGA)®)

Chemical name: 17-(3-Pyridyl) androsten-5, 16-dien-3 β-ol.

Time to market: 2011.04.28 (FDA)/ 2015.05.22 (CFDA)

Original research company: Johnson & Johnson Group (Johnson & Johnson)Janssen Company (Janssen Biotech)

Primary indications: Metastatic high-risk castration-sensitive prostate cancer (CSPC)

Dosage form: Tablet

Chemical structure: C₂₄H₃₁NO(Molecular Weight 349.509)

Zytiga is a blockbuster product of Johnson & Johnson and one of Johnson & Johnson's best-selling products. Since 2011It has dominated the field of prostate cancer treatment since its listing in 2017, with global sales reaching US $2.51 billion in 2017, of which the US market contributed US $1.228 billion. In the first nine months of this year, Zytiga's revenue in the US market further increased to as much as US $1.4 billion.

Most fully, ZytigaSales have been steadily rising, in part because of the drug's positive results in a LATITUDE study of metastatic, high-risk, castration-sensitive prostate cancer, cementing its rival to Pfizer's prostate cancer blockbuster, Xtandi. Some analysts pointed out that this new indication may increase Zytiga's sales by $1 billion and is expected to increase its global sales by more than $4 billion in 2020.

Mechanism of action of abaterone

Abiraterone is an oral CYP17The inhibitor, CYP17, catalyzes two reactions:1 by 17α-Hydroxylase activity pregnenolone (pregnenolone) and progesterone (progesterone) inted 17α-hydroxy derivatives;2 followed by the formation of dehydroepiandrogens (Steroid) ketone (dehydroepiandrosterone,DHEA) and C17 and C20 lyase activities Androstenedione (androstenedione) ,DHEA and androstenedione are androgens and precursors of testosterone. They effectively reduce prostate specific antigen (PSA) levels in prostate cancer patients by inhibiting the activities of C17, C20-lyase and 17α-hydroxylase in CYP17, a key enzyme in androgen synthesis. Abiraterone inhibits male hormones in the testis, prostate, and adrenal glands, although inhibition of CYP17 by abiraterone may also lead to increased mineralocorticoid production by the adrenal glands. Other studies have shown that abiraterone's direct antagonism to androgen receptors is also one of the main mechanisms for the treatment of CRPC. Androgenic castration of abiraterone is more effective than surgical castration or GnRH analogs. Abiraterone common adverse reactions are joint swelling, low serum potassium levels, fluid retention, muscle discomfort and so on.

The situation of generic drugs at home and abroad

In the U.S. market, there are currently several generic drug companies to the U.S. FDA.Submitted an application for a generic version of Zytiga. Yonsa (Abiraterone acetate), a generic drug from Indian pharmaceutical company Sun Pharmaceuticals, was approved by FDA in May this year. Yonsa is developed using SoluMatrix particle technology and can be absorbed more effectively in the body than Zytiga.

In China, because abiraterone has not entered the medical insurance list at present, the expensive drug price cannot solve the accessibility of clinical medication for most prostate cancer patients in China. It is worth mentioning that domestic enterprises pay high attention to this product. Before the original research company obtained import approval, there were 24 domestic companies including Zhengda Tianqing Pharmaceutical, Chongqing Pharmaceutical Industry Research Institute, Zhejiang Xianju and Shandong New Era.However, only the raw materials (CXHL12000754) and tablets (acceptance number: CXHL1200075) developed by Zhengda Tianqing Pharmaceutical Company obtained clinical approval before the original research company obtained import approval. Currently, Zhengda Tianqing Pharmaceutical Company is currently carrying out BE tests on this product (clinical test registration numbers: CTR20160307 and CTR20140915), while the evaluation conclusions of the remaining 23 enterprises on this product are not approved.

However, Johnson & Johnson has already begun to work for Zytiga.In preparation for losing market exclusivity, the company has launched a new prostate cancer drug Erleada, which was approved by the US FDA for non-metastatic prostate cancer in February this year.

Reference: http://med.sina.com/article_detail_100_2_55005.html
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