Novel Substituted Steroid Hormones

该研究项目的目标是开发新型男性避孕药。候选药物已被开发，并已通过员工发明报告提交专利。这类类固醇核心分子可能是一种一流的男性避孕药，具有血清睾酮所负责的所有必要的激素特性。先导候选药物被衍生制成可维持24小时雄激素活性的前药，用于口服或透皮凝胶、贴片或气雾剂制剂，或可作为注射、植入、微针阵列或其他用于男性避孕或潜在内分泌治疗的给药方式，提供长达数月的活性。

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.