Testing a male oral contraceptive targeting Eppin

2011年，全球避孕药市场价值160亿美元，预计2013年至2018年的复合年增长率为5.9%，2018年将达到233亿美元的估计价值。避孕市场包括避孕套和口服避孕等短期方法，包括植入物和宫内节育器在内的长期方法，以及输卵管结扎和输精管切除术等永久性方法。Eppin Pharma的产品具有一系列独特的特点，即易于使用、高效、可逆性和无副作用，这使其有别于所有其他男性避孕药竞争对手。这一市场的一个重要的高影响驱动因素是意外怀孕的流行。在美国，每年有310万人因不一致或不使用避孕措施而意外怀孕。Eppin Pharma将在短期避孕市场上展开竞争。Eppin Pharma Inc.的目标是开发一种非荷尔蒙男性避孕药，针对存在于人类精子表面的Eppin蛋白。与荷尔蒙避孕抑制精子生成不同，我们的治疗剂EP055存在于附睾液中，并与精子表面的Eppin结合。靶标Eppin只存在于男性中，存在于睾丸、附睾和精子上，从而减少了非特异性结合的担忧。这项STTR2期提案的具体目标是在STTR1期数据的基础上，将我们的先导化合物EP055作为针对Eppin的口服男性避孕药。我们在STTR第二阶段应用中的目标是收集足够的药理学数据，以便与FDA进行IND前会议。特定目标1将扩大纯化EP055的生产，以支持更多的临床前研究，并优化配方产品的AlphaScreen分析。特定目标2将完成EP055的配方研究，并为临床前药理学研究创建一批测试批次的片剂。具体目标3将进行猴子避孕/生育研究，以证明原则。具体目标4将在大鼠和猴子身上进行口服药代动力学研究，使用大鼠口服灌胃，猴子口服片剂，并进行剂量范围研究，以进行PK/PD评估。

The global contraceptives market was valued at $16.0 billion in 2011 and is expected to grow at a CAGR of 5.9% from 2013 to 2018, to reach an estimated value of $23.3 billion in 2018. The contraceptive market consists of short-term methods such as condoms and oral contraception, long-term methods including implants and IUDs, and permanent methods such as tubal ligations and vasectomies. Eppin Pharma's product has a unique set of characteristics, namely ease-of use, high efficacy, reversibility and no side-effects, that differentiates it favorably from all the other male contraceptive competitors. An important high impact driver of this market is the prevalence of unintended pregnancies. In the US, there are 3.1 million unintended pregnancies annually through inconsistent or non-use of contraception. Eppin Pharma will be competing in the short-term contraception market. The goal of EPPIN PHARMA INC is to develop a non- hormonal male contraceptive drug that targets the protein EPPIN, which is present on the human sperm surface. Unlike hormonal contraception which inhibits spermatogenesis our therapeutic agent, EP055, is present in epididymal fluid and binds to EPPIN on the surface of sperm. The target EPPIN is only present in the male; in testis, epididymis, and on sperm, thereby reducing non-specific binding concerns. The Specific Aims of this STTR Phase 2 proposal are designed to build on STTR phase 1 data and formulate our lead compound, EP055, as an oral male contraceptive that targets EPPIN. Our goal in this STTR phase II application is to collect sufficient pharmacology data to conduct a pre-IND meeting with the FDA. Specific aim 1 will scale up production of purified EP055 to support additional preclinical studies and optimize AlphaScreen assays for formulation products. Specific aim 2 will complete formulation studies with EP055 and create a test batch of tablets for preclinical pharmacology studies. Specific aim 3 will conduct a monkey contraception/fertility study for proof of principle. Specific aim 4 will conduct oral pharmacokinetics studies in rats and monkeys, using oral gavage in rats, oral dosing of tablets in monkeys and conduct dose-range studies for PK/PD assessment.