Hormonal Therapies

These drugs are used to inhibit certain cancers which are characterized by the presence of oestrogen receptors on target cells.

For breast cancer, they will only be given if the cancer is oestrogen receptor or progesterone receptor positive.

Selective estrogen receptor modulators (SERMS) – Tamoxifen, raloxifene

These are drugs that act by modulating activity of the oestrogen receptor

They can have both oestrogenic and anti-oestrogen effects depending on the tissue on which they are acting.

In the breast, SERMs inhibit oestrogen receptors, so inhibit proliferation of oestrogen-dependent cancers. Therefore, they are used in pre-menopausal women with metastatic breast cancer or those who are high risk

In the uterus, bone and liver, SERMs activate oestrogen receptors and so have oestrogenic effect

Side Effects

Menopausal symptoms (fatigue, hot flushes, night sweats, mood swings)

Abnormal vaginal bleeding or discharge

Increased risk of VTE

 Increased risk of endometrial cancer (due to oestrogenic effects on endometrium)

Fulvestrant

This is an oestrogen receptor antagonist used to treat ER+ breast cancer

It is given once the breast cancer has spread to lymph nodes and breastbone

Aromatase inhibitors – Anastrozole, letrozole

These inhibit the aromatase enzyme which converts testosterone to oestrogen

They are used in postmenopausal women with ER-positive breast cancer.

Side Effects

Hot flushes

Osteoporosis

GnRH Analogs – Leoprolide, Goserelin

These are analogs that bind the GnRH receptor but over time inhibit LH and FSH secretion

This has downstream effects to decrease levels of testosterone and oestrogen

They are useful for treating prostate cancer (in men) and breast/ovarian cancer (women)

They are only given in pre-menopausal women who have ER+ or PR+ breast cancer

Side Effects

Gynaecomastia

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