Novel Substituted Steroid Hormones

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，并通过员工发明报告提交专利申请。这类类固醇核心分子可能是一流的男性避孕药，具有血清睾酮负责的所有必要的激素特性。先导候选物被衍生化以制备前药，所述前药可以维持雄激素活性24小时用于口服或透皮凝胶、贴剂或气雾剂制剂，或者当作为注射剂、植入剂、微针阵列或用于男性避孕或潜在内分泌治疗的其他递送方法施用时可以提供延长的活性数月。 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，使得口服给药限于每天一剂。因此，一个分子包含多种激素活性，这些激素活性满足血清睾酮所需的所有必要激素活性，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，以证明药物的预期功能活性。 由于这些产品如果成功地实现了预期的功能，将具有商业用途，因此在通过适当渠道提交专利申请之前，不能发布出版物。

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. 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.