EP055, a non-hormonal male contraceptive:IND-enabling studies

EP055，一种非激素男性避孕药：IND支持研究

• 批准号: 10396672
• 负责人: MICHAEL GENE ORAND
• 金额: $ 60.25万
• 依托单位: EPPIN PHARMA, INC.
• 依托单位国家: 美国
• 财政年份: 2021
• 资助国家: 美国
• 起止时间: 2021-04-19 至 2023-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/10396672
• 关键词: ABCG2 gene; Acute; Binding; Blood - brain barrier anatomy; Canis familiaris; Cardiovascular system; Categories; Characteristics; Chronic; Clinical Research; Clinical Trials; Conscious; Contraceptive Agents; Contraceptive methods; Cytochrome P450; Data; Developed Countries; Development; Dose; Electrocardiogram; Epididymis; Evaluation; Family Planning; Feedback; Formulation; Future; Goals; Grant; Heart Rate; Human; Implant; Intestines; Kidney; Kilogram; Lead; Life; Liquid substance; Liver; Lung; Male Condoms; Male Contraceptive Agents; Methods; Oral; Oral Contraceptives; Pharmaceutical Preparations; Pharmacologic Substance; Pharmacology; Pharmacology and Toxicology; Phase; Phase I Clinical Trials; Prevalence; Process; Production; Protease Inhibitor; Proteins; Public Health; Rattus; Recovery; Research Proposals; Safety; Small Business Innovation Research Grant; Small Business Technology Transfer Research; Source; Sperm Motility; Spermatogenesis; Surface; Technology; Testis; Therapeutic; Therapeutic Agents; Toxic effect; Toxicology; Tubal Ligation; United States; Vasectomy; Woman; body system; condoms; contraceptive target; design; drug candidate; electric impedance; hormonal contraception; implantable device; improved; in vivo; inhibitor; male; manufacturing process; meetings; men; neurobehavioral test; phase 1 study; pill; preclinical study; pressure; process optimization; programs; public health research; respiratory; scale up; side effect; sperm cell; telemetering; unintended pregnancy

The global contraceptives market was valued at $24BN in 2018 and is expected to grow at a CAGR of 6.9% from 2019 to 2027. The contraceptive market consists of short-term methods such as condoms, oral contraceptives, patches and rings, long-term methods including implants and IUDs, and permanent methods such as tubal ligations and vasectomies. The global condom market was expected to see $12BN in revenue in 2018 and is projected to grow at a CAGR of 9% over the period 2019-2024. Condoms accounted for $200MM in the United States in 2018 growing at a CAGR of 3.5% from 2017-2020. There are currently no commercially available products in the category of non-hormonal male contraceptive technologies involving oral pills and/or implantable devices which would compete in the short-term market. Eppin Pharma's drug will provide a significant pharmaceutical alternative to male condoms and should command a significant share of the contraceptive market. Once commercially available, this new male contraceptive technology has the potential to be disruptive to the traditional male contraceptive condom market as well as the contraceptive market generally. Eppin Pharma's market review projects that new male contraceptive technology entrants can feasibly capture 8-10% of the traditional short-term male contraceptive market which is at least $550MM. Eppin Pharma's product has a unique set of characteristics, namely ease-of use, reversibility and minimal 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 due to inconsistent or non-use of contraception. Eppin Pharma is an emerging pharmaceutical company focused on the development of a safe, non-hormonal male contraceptive that can be taken orally. The company's contraceptive product candidate is a small organic compound that binds to EPPIN (epididymal protease inhibitor), a protein on the surface of human sperm, resulting in the loss of sperm motility. The Specific Aims of this SBIR Phase 2 proposal are designed to build on SBIR phase 1 data and demonstrate that our lead compound, EP055, is safe and ready for a phase 1 clinical trial as an oral male contraceptive that targets EPPIN. The Specific aims are: 1) Safety pharmacology; this aim is intended to evaluate the potential for EP055 to cause effects on organ systems acutely critical for life: CNS, Respiratory and Cardiovascular. 2) Toxicology; repeat-dose GLP toxicology studies. 3) Manufacture of 2kg of EP055.

2018年全球避孕药市场价值240亿美元，预计将以 2019年至2027年的复合年增长率为6.9%。避孕药市场由短期方法组成 例如避孕套、口服避孕药、贴片和环、包括植入物在内的长期方法 和宫内节育器，以及永久性的方法，如输卵管结扎和输精管切除术。全球安全套 预计2018年市场收入将达到120亿美元，预计复合年增长率为 2019-2024年期间为9%。2018年，康宝莱在美国占2亿美元 2017-2020年的复合年增长率为3.5%。目前还没有商业上可用的 涉及口服药丸的非激素男性避孕技术类产品 和/或可植入设备，这些设备将在短期市场上竞争。Eppin Pharma的 药物将为男性避孕套提供重要的药物替代品，并且应该得到 占据避孕药市场的很大份额。一旦商业化，这种新的雄性 避孕技术有可能破坏传统的男性避孕方法， 避孕套市场以及一般避孕药市场。Eppin Pharma的市场评论 新的男性避孕技术进入者可以切实获得8%至10%的 传统的短期男性避孕药市场至少为5.5亿美元。Eppin Pharma的 产品具有一系列独特的特性，即易用性、可逆性和最小侧边， 这些效果使它与所有其他男性避孕药竞争者区别开来。一个 该市场的重要高影响力驱动因素是意外怀孕的普遍性; 美国每年有310万例意外怀孕，原因是不一致或不使用避孕药具。 避孕。Eppin Pharma是一家新兴的制药公司，专注于 开发一种可口服的安全、非激素男性避孕药。的 该公司的避孕产品候选人是一个小的有机化合物，结合到EPPIN （附睾蛋白酶抑制剂），人类精子表面的一种蛋白质，导致精子丢失。 精子活力SBIR第2阶段提案的具体目标旨在建立在 SBIR第一阶段的数据，并证明我们的铅化合物，EP 055，是安全的，并准备用于 1期临床试验作为口服男性避孕药的目标EPPIN。具体目标是： 1)安全药理学;该目的旨在评价EP 055引起 对生命至关重要的器官系统的影响：CNS、呼吸系统和心血管系统。（二） 毒理学;重复给药GLP毒理学研究。3)生产2kg EP 055。