A Novel Inexpensive Process for Preparation of Polymeric Microspheres

SpheriTech的专利技术和本申请中描述的技术不仅新颖，而且提供了一种廉价和有效的方法来制造聚合物微球。确定具体的协议和技术诀窍是这项工作取得成功的关键。在生物催化中，竞争技术的全球市场在250亿美元左右（Biocombinatorial Approaches for DrugFinding，Springer柏林海德堡）。ISBN 978-3-540-22092-3）。在全球8000亿美元的商品、特种和精细化学品市场中，有500亿美元可以通过生物过程轻松解决。另外2000亿美元已被确定为在未来10至20年内可由生物应用程序潜在地解决（Chemical & Engineering News，第79卷，第21号）。基于肽的药物已经是药物组合的主要部分。前十名肽类药物的年销售额超过2000美元，其中前五名处于专利保护的后期阶段。肽类药物中价值最高的市场领域是前列腺癌治疗领域，由于这些药物几乎是由大型制药公司同时开发的，因此它们都接近其专利寿命的终点。亮丙瑞林（拜耳公司，赛诺菲安万特和其他）在2005年结束了专利，已经有5-6个仿制药制造商表示兴趣。SpheriTech的创始人兼首席执行官Don Wellings博士曾为三家公司提供亮丙瑞林的合成咨询，出于保密原因，这些公司的名字不能透露。用于生物药物纯化的亲和色谱法是生产成本的最高贡献者。例如，固定化蛋白A（能够与各种类型的免疫球蛋白[Ig]分子结合的天然蛋白，由各种细菌菌株分泌）用于纯化单克隆抗体。2007年蛋白A培养基的市场规模估计为4900万美元，2013年的市场规模估计为7000万美元，基于抗体生产的平均年增长率为6%。更详细的市场研究包括在本申请的C部分。SpheriTech计划在3-4年内在每个市场领域获得显著的市场份额。

The technology patented by SpheriTech and described in this application isnot only novel but provides an inexpensive and efficient means formanufacture of polymeric microspheres.Page 3 of44The most important objective is to identify a range of polymers and linkagetechnologies for the three target markets. Identification of specific protocolsand technical know how is essential for the success of this work. Ultimatelythis will lead to large scale production of specialist polymeric microspheres foreach chosen market sector.In biocatalysis the worldwide market for the competing technology ismeasured in the region of $25 billion (Biocombinatorial Approaches for DrugFinding, Springer Berlin Heidelberg. ISBN 978-3-540-22092-3). $50 billion ofthe $800 billion global commodity, specialty, and fine chemicals markets arereadily addressable by bioprocesses. Another $200 billion has been identifiedas potentially addressable by biological app~oaches in the next 1 0 to 20 years(Chemical & Engineering News, Volume 79, Number 21).Peptide based drugs are already a major section of the pharmaceuticalportfolio. Sales of the top ten peptide based drugs total over $2000mannually and the top five of these are in the late stages of patent protection.The highest value market sector in peptides is in the area of prostate cancertherapy and since these were developed almost concurrently by majorpharmaceutical companies they are all nearing the end of their patent life.Leuprolide (Bayer AG, Sanofi-Aventis and others) came off patent in 2005and already there are 5-6 generic drug manufacturers showing interest. DrDon Wellings, the founder and CEO of SpheriTech has consulted on thesynthesis of Leuprolide for three individual companies that cannot be namedfor reasons of confidentiality.Affinity chromatography, used in the purification of biopharmaceuticals is thehighest contributor to the cost of manufacture. lmmobilised Protein A (anatural protein capable of binding to various classes of immunoglobulin [lg]molecules, excreted by various bacterial strains) for example is used for thepurification of monoclonal antibodies. The market size for Protein A media in2007 was estimated to be $49 million and the market size in 2013 isestimated to be $70 million based on an average annual growth rate of 6% inantibody production.More detailed market research is covered in Part C of this application.SpheriTech plans to obtain a significant market share within each marketsector in 3-4 years.