Pharmacokinetics of progesterone concentrations was around 4 hours and the elimination half-life was in the range of 30 to 40 hours. The venous blood levels observed were very low. Because progesterone is a lipophilic and hydrophobic compound, it is not absorbed efficiently by the skin. Moreover, because the body produces about 25 mg progesterone per day on average during the luteal phase, around 50% of the body would need to be used as a surface of absorption to deliver a similar quantity of progesterone. As such, the transdermal route cannot easily achieve adequate circulating progesterone levels, and this makes transdermal progesterone impractical for
Selective progesterone receptor modulator Selective progesterone receptor modulator A selective progesterone receptor modulator (SPRM) is an agent that acts on the progesterone receptor (PR), the biological target of progestogens like progesterone. A characteristic that distinguishes such substances from full receptor agonists (e.g., progesterone, progestins) and full antagonists (e.g., aglepristone) is that their action differs in different tissues, i.e. agonist in some tissues while antagonist in others. This mixed profile of action leads to stimulation or inhibition in tissue-specific manner, which further raises the possibility of dissociating undesirable adverse effects from the development of synthetic PR-modulator drug candidates. Ever since the discovery of the progesterone