Pharmacokinetics of estradiol
Estradiol can be administered in the form of a very long-lasting subcutaneous pellet implant. These implants are replaced once every 6 to 12 months, and can achieve high and very constant circulating levels of estradiol. They are surgically inserted by a trained physician in a medical office or clinic and can be placed into locations including the lower abdomen, lower back, buttocks, or hips. Subcutaneous implants containing 25, 50, and 100 mg estradiol for replacement usually once every 6 months are available as approved pharmaceutical medications. Up to 800 mg estradiol per implantation has been used. Pharmaceutical estradiol implants have been said to be used almost exclusively in the United Kingdom. An estradiol implant has not been approved by the FDA as a pharmaceutical medication in the United States, but hormone implants, including estradiol implants, are available as custom compounded products in this country.
Segesterone acetate
A combination of SGA and the estrogen estradiol is under development in a transdermal gel formulation for use as a contraceptive in women by the Population Council in conjunction with Antares Pharma in the United States and Europe. As of December 2017, it is in phase III clinical trials for this indication. The medication has the tentative brand name NestraGel. A combination of SGA and the estrogen ethinylestradiol is under development in a vaginal ring formulation for use as a one-year contraceptive by the Population Council in multiple regions including Latin America, Europe, and Australia. It has completed phase III clinical trials and efforts are underway to pursue regulatory approval. It was approved in the United States in August 2018.