Ethinylestradiol, also ethinyl estradiol (EE), is a synthetic derivative of estradiol. Ethinyl estradiol is orally bio-active and the estrogen in most formulations of oral contraceptives (the Pill). It is one of the most commonly used medications.

While estradiol is readily absorbed when taken orally, it is also quickly inactivated by the liver. Substitution at C17 of the estrane steroid with a ethinyl group proved to provide an estrogen that is much more resistant to degradation and paved the way for the development of oral contraceptives.

EE is absorbed in the small intestine and reaches a serum peak about 2 hours later. It undergoes extensive metabolism in the liver involving the cytochrome P450 3A4 isoenzyme. EE and its metabolites are in excreted with the bile. Due to the effect of enterohepatic circulation as second peak is seen several hours later. Individually, wide variations exist in the overall absorption process, and can be further modified by drug (i.e. antibiotics) that affect the enterohepatic circulation or liver enzymes. In circulation EE is almost fully bound to plasma albumin. It is metabolized by hydroxylation of the aromatic ring and excreted in both, feces and urine, in part as glucuronide and sulfate conjugate.

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