Antagonists

• Antioestrogens:

1. By: weak oestrogen occupies oestrogen receptors => blocking the negative
feedback mechanism => results in increased gonadotropin secretion, which may induce
ovulation.
Suffix:
(fen pronunciation)
-phene
-fen-

1. Clomiphene
2. Cyclofenil
3. Tamoxifen (Non-steroidal competitive oestrogen antagonist)- has little or no
estrogenic activity.
4. Toremifen (in postmenopausal metastatic beast cancer)

2. By: GnRh antagonist. (luteinising hormone-releasing hormone antagonists which

inhibit the release of gonadotrophins (LH and FSH)).
Suffix: -relix

1. Cetrorelix
2. Ganerelix
avoid in pregnancy and breast-feeding.

3. by: Aromatase (estrogen synthetase) inhibitors (non steroidal). Prevents

conversion of androgen to oestrogen.
Suffix:
-trozole

1. Anastrozole
2. Letrozole
Others: Exemestane, given after 2-3 years of tamoxifen therapy.

• Selective oestrogen receptor modulators

Combines oestrogeneic and antioestrogenic properties.

⁃ Raloxifene : antioestrogenic effects on the breast and endometrium but oestrogenic

effects on bone.
⁃ Tibolone: for short-term treatment of osteoporosis.

Fluvestrant and Toremifen: in postmenopausal metastatic beast cancer.

Progesterone derivatives => -progesterone

Testosterone derivatives => -gest, -sterone.
Antiprogestogens:

1. Mifepristone: is a pure
competitive antagonist at progesterone and glucocorticoid receptors. => Effective orally for
terminating pregnancies.

2. Danazol => inhibitor of gonadotrophins (LH, FSH). partial androgenic activity with
antioestrogenic and antiprogestogenic activity.