Novel Substituted Steroid Hormones

新型替代类固醇激素

• 批准号: 10908181
• 负责人: Diana Blithe
• 金额: $ 8.63万
• 依托单位: EUNICE KENNEDY SHRIVER NATIONAL INSTITUTE OF CHILD HEALTH & HUMAN DEVELOPMENT
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/10908181
• 关键词: Aerosols; Androgens; Biological Availability; Dose; Employee; Formulation; Gel; Goals; Hormonal; Hour; Implant; Injections; Legal patent; Male Contraceptive Agents; Methods; Modification; National Institute of Child Health and Human Development; Needles; Oral; Pharmaceutical Preparations; Process; Prodrugs; Production; Property; Publications; Reporting; Research Project Grants; Serum; Spermatogenesis; Steroids; Testis; Testosterone; Transactivation; androgen sensitive; androgenic; drug candidate; hormone therapy; hypothalamic pituitary axis; interest; invention; lead candidate; new chemical entity; novel; receptor binding; sperm cell; steroid hormone

The research project has a goal to develop novel male contraceptive agents. Candidate drugs have been developed and have been submitted for patents through an employee invention report. After review of the report, it was determined that a provisional patent application would be submitted by NICHD. This class of steroid core molecules could be a first-in-class male contraceptive agent that possesses all necessary hormonal properties for which serum testosterone is responsible. Lead candidates are derivitized to prepare pro-drugs that can sustain the androgenic activity for 24 hours for oral or transdermal gel, patch or aerosol formulations or could provide extended activity over several months when administered as an injection, implant, microneedle array or other delivery method for the purpose of male contraception or potential endocrine therapies. As a male contraceptive agent, this invention takes advantage of molecules with demonstrated androgenic activity, oral bioavailability and combines modifications that maintain drug levels over a sustained period so that oral dosing is limited to one dose per day. Thus, one molecule contains multiple hormonal activities that fulfill all necessary hormonal activities for which serum testosterone is required but does not support testicular function that would lead to spermatogenesis. Several lead candidates are being evaluated for receptor binding and transactivation properties that demonstrate the desired functional activities of the drug. Since the products, if successful in achieving the desired functions, would have commercial utility, publications cannot be issued until after patent applications have been filed through appropriate channels.

该研究项目的目标是开发新型男性避孕药。候选药物已经开发出来，并已通过员工发明报告提交专利。经审查报告后，决定由NICHD提交临时专利申请。这类类固醇核心分子可能是一流的男性避孕药，它具有血清睾酮负责的所有必要的激素特性。主要候选药物被衍生化以制备前药，这些前药可以在口服或透皮凝胶、贴剂或气雾剂制剂中维持雄激素活性24小时，或者当以注射、植入物、微针阵列或其他递送方法施用时可以提供几个月的延长活性，用于男性避孕或潜在的内分泌治疗。 作为男性避孕剂，本发明利用了具有已证实的雄激素活性、口服生物利用度的分子，并结合了在持续时间内维持药物水平的修饰，从而将口服剂量限制为每天一剂。因此，一种分子含有多种激素活性，可以满足血清睾酮所需的所有必要的激素活性，但不支持导致精子发生的睾丸功能。 正在评估几种主要候选药物的受体结合和反式激活特性，以证明药物所需的功能活性。 由于产品如果成功实现所需功能，将具有商业实用性，因此只有在通过适当渠道提交专利申请后才能发布出版物。