OnCo
technologiesTechnologyStandard of care

Endocrine therapy (SERMs, AIs, SERDs)

Pills that block or remove oestrogen signalling, the mainstay of treatment for hormone-driven breast cancer for 50 years.

Tamoxifen (SERM), aromatase inhibitors (letrozole, anastrozole, exemestane), fulvestrant (injectable SERD), oral SERDs (elacestrant, imlunestrant approved 2025, camizestrant), and the PROTAC vepdegestrant (2026). Ovarian function suppression (goserelin) for premenopausal women. Five to ten years of adjuvant therapy halves recurrence; adherence is a major real-world problem.

Schematic · not to scale
Oestrogen receptor · Ligand pocket blocked / receptor degraded · Oestrogen kept out

How it works

Compete for ER (SERM), deplete oestrogen (AI), or degrade ER (SERD, PROTAC).

Strengths
  • Oral, effective, cheap (generics)
Limitations
  • ESR1 mutations; menopausal symptoms, bone loss, adherence
Since
1977

Products

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ApprovedOral SERD
Camizestrant · Etcamah

Camizestrant is an oral oestrogen-receptor degrader approved in September 2026 for a new kind of decision: switching treatment when a blood test shows resistance developing, before the cancer visibly grows.

ApprovedOral SERD
Elacestrant · Orserdu

Elacestrant was the first oral oestrogen-receptor degrader (2023), for ESR1-mutant breast cancer detected by blood test.

ApprovedSmall-molecule steroidal aromatase inactivator
Exemestane · Aromasin

Exemestane is a steroidal aromatase inhibitor, the partner of everolimus and the agent tested with ovarian suppression in young women.

ApprovedInjectable SERD
Fulvestrant · Faslodex

Fulvestrant is a monthly injection that destroys the oestrogen receptor; it is the standard partner for many targeted drugs after hormone therapy stops working.

Phase 3Oral SERD
Giredestrant

Giredestrant is Roche's oral SERD: it failed to beat an aromatase inhibitor in first-line metastatic disease but succeeded after surgery and after CDK4/6 failure.

ApprovedGnRH agonist
Goserelin / leuprolide (ovarian function suppression) · Zoladex; Lupron

Monthly or 3-monthly injections that switch off the ovaries, letting premenopausal women use aromatase inhibitors and lowering recurrence in higher-risk cases.

ApprovedOral SERD
Imlunestrant · Inluriyo

Imlunestrant is Lilly's oral oestrogen-receptor degrader, approved in 2025 for ESR1-mutant breast cancer and shown to work with abemaciclib regardless of mutation.

ApprovedSmall-molecule aromatase inhibitor
Letrozole (and other aromatase inhibitors) · Femara; anastrozole (Arimidex); exemestane (Aromasin)

Daily pills that stop the body making oestrogen after menopause, the backbone of hormone therapy for most breast cancers.

Not mapped hereGnRH agonist depot
Leuprolide (leuprorelin) and GnRH agonists · Lupron / Eligard / Camcevi

Leuprolide is the injectable that shuts off testosterone production, the foundation of hormone therapy for prostate cancer since the 1980s; it is also used for ovarian suppression in premenopausal breast cancer.

ApprovedHormonal therapy (progestin)
Progestins (megestrol acetate, medroxyprogesterone, levonorgestrel IUD) · Megace; Mirena (IUD)

Progesterone-like hormones that can reverse early endometrial cancer in women who want to keep their uterus, and control advanced hormone-sensitive disease.

ApprovedSmall-molecule SERM
Tamoxifen · Nolvadex

The original targeted cancer drug (1977): a pill that blocks oestrogen's effect on breast cancer and halves recurrence, still essential for premenopausal women.

ApprovedPROTAC oestrogen receptor degrader
Vepdegestrant · Veppanu

Vepdegestrant is the first PROTAC ever approved (2026): a pill that tags the oestrogen receptor for destruction, for breast cancers with ESR1 mutations.

Key papers

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rctNew England Journal of Medicine 2024changed practice
NATALEE: three years of ribociclib after surgery in a broad population of hormone-receptor-positive early breast cancer

Ribociclib is a second adjuvant CDK4/6 option, and the only one with data in node-negative stage II disease. Roughly 3 in 100 patients avoid a relapse or death at three years, so the decision depends heavily on individual risk, tolerance of a three-year oral drug, and cost. Whether the benefit persists after treatment ends, as it did with abemaciclib, needs longer follow-up.

rctJournal of Clinical Oncology 2020changed practice
monarchE: two years of abemaciclib after surgery in high-risk, hormone-receptor-positive early breast cancer

Women with hormone-receptor-positive, HER2-negative breast cancer that has spread to lymph nodes and has other high-risk features can now be offered two years of abemaciclib alongside their hormone therapy, with a durable reduction in relapse. It does not apply to node-negative or low-risk disease, and the diarrhoea and cost are real trade-offs to discuss.

rctNew England Journal of Medicine 2017changed practice
STAMPEDE: adding abiraterone to hormone therapy at diagnosis of advanced prostate cancer

Men diagnosed with prostate cancer that has already spread, or that is locally advanced and high risk, should start abiraterone (or another androgen-receptor pathway inhibitor) at the same time as testosterone suppression rather than waiting for resistance. This roughly halves the risk of death over several years. The same platform later showed that docetaxel chemotherapy and, in high-volume metastatic disease, triple therapy also help, and that abiraterone benefits men with high-risk disease treated with radiotherapy.

rctLancet Oncology 2015changed practice
IBIS-I: five years of tamoxifen keeps preventing breast cancer for at least 20 years

For women at raised risk, a 5-year course of tamoxifen offers long-lasting protection against the commonest kind of breast cancer. Uptake is low because of side effects and fear of rare serious harms; low-dose tamoxifen (TAM-01) is now being tested to improve the balance. It has not been shown to save lives.

Latest papers

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Literature trend1,292 papers in the last 12 months+20% vs prior 12How this is computed
Latest papers · live from Europe PMC
Open in Europe PMC

Query for this technology: (TITLE:"endocrine therapy" OR ABSTRACT:"endocrine therapy" OR TITLE:"aromatase inhibitor" OR ABSTRACT:"aromatase inhibitor" OR TITLE:"oral SERD" OR ABSTRACT:"oral SERD") AND breast. Results are unfiltered search hits about Endocrine therapy (SERMs, AIs, SERDs), not a curated reading list.

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