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年全球避孕药市场的价值为240亿美元，预计将增长 从2019年到2027年的复合年增长率为6.9％。避孕市场由短期方法组成 例如避孕套，口服避孕药，补丁和环，包括植入物在内的长期方法 和宫内节育器，以及诸如输卵管结扎和输精管切除术等永久方法。全球避孕套 预计市场将在2018年获得120亿美元的收入，预计将以复合年增长率 在2019 - 2024年期间9％。避孕套在2018年在美国的$ 200毫米 从2017 - 2020年起，以3.5％的复合年增长率生长。目前尚无市售 非荷尔蒙男性避孕技术类别的产品涉及口服药丸 和/或将在短期市场竞争的可植入设备。 Eppin Pharma's 药物将为雄性避孕套提供重要的药物替代品，应命令 避孕市场很大一部分。一旦市售，这个新男性 避孕技术有可能破坏传统的男性避孕药 避孕套市场以及避孕市场。 Eppin Pharma的市场评论 新的男性避孕技术参赛者可以捕获8-10％的项目 传统的短期男性避孕市场至少为550毫米。 Eppin Pharma's 产品具有独特的特征，即易于使用，可逆性和最小的侧面 - 影响它与所有其他男性避孕竞争者有利的影响。一个 这个市场的重要高影响力驱动力是意外怀孕的普遍存在。在 美国，由于不一致或不使用，每年有310万例意外怀孕 避孕。 Eppin Pharma是一家新兴制药公司 开发可以口服的安全，非荷尔蒙男性避孕药。这 公司的避孕产品候选者是一种与Eppin结合的小有机化合物 （附子蛋白酶抑制剂），一种在人类精子表面的蛋白质，导致丧失 精子运动。该SBIR 2阶段提案的具体目的旨在建立 SBIR 1阶段数据并证明我们的铅化合物EP055是安全的，可以准备 第1阶段临床试验是针对Eppin的口服男性避孕药。具体目的是： 1）安全药理学；此目标旨在评估EP055引起的潜力 对器官系统对生命至关重要的影响：中枢神经系统，呼吸道和心血管。 2） 毒理学;重复剂量GLP毒理学研究。 3）生产2公斤EP055。