1-Hydroxy pregnacalciferol derivatives of formula (I) and their corresponding 5,6-trans isomers wherein R1 is hydroxyl or lower alkoxy and R2 is optionally hydroxylated or lower alkoxylated lower alkynyl or R1 is C(RA) (RB)CH3 where RA is optionally hydroxylated or lower alkoxylated lower alkynyl and RB is hydroxyl or lower alkoxy or RA and RB together represent oxo and R2 is hydrogen, hydroxyl or lower alkoxy, and R3 and R4 represent hydrogen atoms, exhibit anti-progesterone activity and may be useful as antineoplastic, antifertility, antiproliferative, immunosuppressive and/or antiinflammatory agents.
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