[(8R,9S,10R,13S,14S,17S)-10,13-dimethyl-3-oxo-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl] 2-(dimethylamino)acetate;hydrochloride

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: [(8R,9S,10R,13S,14S,17S)-10,13-dimethyl-3-oxo-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl] 2-(dimethylamino)acetate;hydrochloride
• 化学式: C23H36ClNO3
• 分子量: 410.0
• InChiKey: NNTUBVJUVXRBGE-HZIHITNPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.41
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  46.6
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] ONE-AND TWO-POINT TITRATION METHODS TO DETERMINE DAILY TREATMENT REGIMENS TO TREAT HYPOGONADISM OR MALE TESTOSTERONE DEFICIENCY WITH AN INTRANASAL TESTOSTERONE BIO-ADHESIVE GEL, AND PRIMARY AND SECONDARY EFFICACY AND SAFETY ENDPOINTS<br/>[FR] PROCÉDÉ DE TITRATION À UN ET DEUX POINTS POUR DÉTERMINER DES RÉGIMES DE TRAITEMENT QUOTIDIENS POUR TRAITER L'HYPOGONADISME OU UN DÉFICIT EN TESTOSTÉRONE MASCULINE PAR UN GEL BIOADHÉSIF DE TESTOSTÉRONE INTRANASAL, ET INDICATEURS DE RÉSULTAT D'EFFICACITÉ PRIMAIRE ET SECONDAIRE ET DE SÉCURITÉ
  申请人：TRIMEL BIOPHARMA SRL

  公开号：WO2014080282A2

  公开（公告）日：2014-05-30

  The present invention relates to 4.0% and 4.5% intranasal testosterone bio- adhesive gels for providing sustained intranasal delivery of testosterone to a male and intranasal treatment methods for safely providing sustained release testosterone to treat males with hypogonadism. In particular, the present invention relates to improved testosterone replacement therapy (TRT) and sustained intranasal testosterone gel formulations for treating male hypogonadism. The 4.0% and 4.5% intranasal testosterone bio-adhesive gels are effective, are statistically significant regarding improvement in effect on erectile function and mood, provide for favourable trends for effect on body composition and bone mineral density and have safety measures after 360 days of treatment that are consistent with currently marketed topical testosterone products. The present invention also relates to a system for dispensing intranasally a precise dosage amount of such gels in smaller volumes at an optimal anatomical location within each nostril of the male, so that an effective amount of testosterone is deposited within each nostril at the optimal anatomical location for TRT, including to effectively treat testosterone deficiency in male subjects, such as hypogonadism. The present invention is also concerned with a novel titration method to determine the appropriate daily treatment regimen, i.e., a BID or TID treatment regimen, to administer the intranasal gels of the present invention to treat hypogonadism or TRT. The present invention is also concerned with novel titrations method to determine the appropriate daily treatment regimen, i.e., a QD, BID or TID treatment regimen, to administer the intranasal gels of the present invention to treat hypogonadism or TRT in males. In particular, the present testosterone therapy remains effective for treating hypogonadism when an allergic rhinitis event occurs in the male or when the male subject uses a topical nasal vasoconstrictor or a topical intranasal decongestant during the hypogonadism treatment. Further, the present invention relates to a novel method of preventing the occurrence of an allergic rhinitis event in a male, who is undergoing a hypogonadism treatment with an intranasal testosterone bio-adhesive gel formulation. In certain embodiments, the intranasal testosterone bio-adhesive gel formulation according to the invention comprises 4.0% and 4.5% testosterone.
• [EN] MALE TESTOSTERONE TITRATION METHODS, MALE INTRANASAL TESTOSTERONE BIO-ADHESIVE GEL FORMULATIONS AND USE THEREOF FOR TREATING HYPOGONADISM AND TRT<br/>[FR] PROCÉDÉS DE TITRAGE DE TESTOSTÉRONE CHEZ L'HOMME, FORMULATIONS DE GEL BIOADHÉSIF DE TESTOSTÉRONE INTRANASAL ET LEUR UTILISATION POUR LE TRAITEMENT DE L'HYPOGONADISME ET DE LA THÉRAPIE DE REMPLACEMENT DE TESTOSTÉRONE (TRT)
  申请人：TRIMEL BIOPHARMA SRL

  公开号：WO2014080283A2

  公开（公告）日：2014-05-30

  The present invention relates to pernasal testosterone bio-adhesive gel formulations for intranasal administration and testosterone replacement treatment methods for using the pernasal testosterone bio-adhesive gel formulations for providing sustained intranasal delivery of testosterone to testosterone deficient males to treat, for example, male subjects diagnosed with hypogonadism. The present invention is also concerned with a novel titration method to determine the appropriate daily treatment regimen, i.e., a BID or TID treatment regimen, to administer the intranasal gels of the present invention to treat hypogonadism or TRT.