Cyclotriol Explained

Cyclotriol (developmental code name ZK-136295; also known as 14α,17α-ethanoestriol) is a synthetic estrogen which was studied in the 1990s and was never marketed.^{[1] [2] [3] [4]} It is a derivative of estriol with a bridge between the C14α and C17α positions.^[5] The drug has 40% of the relative binding affinity of estradiol for the human ERα. It showed an absolute bioavailability of 40% with high interindividual variability and an elimination half-life of 12.3 hours in pharmacokinetic studies in women.

See also

• List of estrogens § Estriol derivatives
• Cyclodiol

Notes and References

1. Book: Oettel M, Schillinger E . Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen. 6 December 2012. Springer Science & Business Media. 978-3-642-60107-1. 10,15,76,331–332.
2. Baumann A, Fuhrmeister A, Brudny-Klöppel M, Draeger C, Bunte T, Kuhnz W . Comparative pharmacokinetics of two new steroidal estrogens and ethinylestradiol in postmenopausal women . Contraception . 54 . 4 . 235–242 . October 1996 . 8922877 . 10.1016/S0010-7824(96)00194-1 .
3. Lang R, Reimann R . Studies for a genotoxic potential of some endogenous and exogenous sex steroids. I. Communication: examination for the induction of gene mutations using the Ames Salmonella/microsome test and the HGPRT test in V79 cells . Environmental and Molecular Mutagenesis . 21 . 3 . 272–304 . 1993 . 8462531 . 10.1002/em.2850210311 . 39049586 .
4. Reimann R, Kalweit S, Lang R . Studies for a genotoxic potential of some endogenous and exogenous sex steroids. II. Communication: examination for the induction of cytogenetic damage using the chromosomal aberration assay on human lymphocytes in vitro and the mouse bone marrow micronucleus test in vivo . Environmental and Molecular Mutagenesis . 28 . 2 . 133–144 . 1996 . 8844995 . 10.1002/(SICI)1098-2280(1996)28:2<133::AID-EM10>3.0.CO;2-G . 10326219 .
5. Hundal BS, Dhillon VS, Sidhu IS . Genotoxic potential of estrogens . Mutation Research . 389 . 2–3 . 173–181 . March 1997 . 9093381 . 10.1016/S1383-5718(96)00144-1 .