Course Content
Module 1 — Principles of Hormone Therapy in Oncology
Mechanism and Dosing Overview Aromatase Inhibitors (AIs): block the enzyme aromatase (CYP19A1), which converts androgens to estrogens in adipose and peripheral tissues. Examples: Anastrozole 1 mg orally daily, Letrozole 2.5 mg orally daily, Exemestane 25 mg orally daily. These are the preferred agents in postmenopausal women with estrogen receptor–positive breast cancer. Selective Estrogen Receptor Modulators (SERMs): such as Tamoxifen 20 mg orally daily — bind the estrogen receptor and act as antagonists in breast tissue but partial agonists in bone and endometrium. Selective Estrogen Receptor Degraders (SERDs): such as Fulvestrant 500 mg intramuscularly on days 0, 14, 28, then every 28 days thereafter — promote estrogen receptor degradation. CYP17 Inhibitors: Abiraterone acetate 1000 mg orally daily on an empty stomach plus Prednisone 5 mg orally twice daily — block the CYP17A1 enzyme, suppressing androgen synthesis in adrenal glands and tumors. Gonadotropin-Releasing Hormone (GnRH) Agonists and Antagonists: Leuprolide 7.5 mg subcutaneously every 4 weeks or depot every 3–6 months; Degarelix 240 mg subcutaneously loading dose, then 80 mg every 4 weeks; Relugolix 120 mg orally daily — suppress testosterone or estrogen production by downregulating or directly blocking pituitary gonadotropin release.
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Hormone Therapy for Cancer Patients: Mechanisms, Indications, and Clinical Practice

1️⃣ Next-generation endocrine agents

  • Oral SERDs (elacestrant, camizestrant) → better bioavailability, ER mutant activity.

  • PROTAC degraders (target ER or AR for ubiquitin destruction).

  • Selective AR degraders (SARDs) for castration-resistant prostate cancer.

2️⃣ Combination innovations

  • Radioligand therapy (177Lu-PSMA) + ADT or AR blockers → synergistic in mCRPC.

  • PARP inhibitors + AR blockade for BRCA-mutated cases.

  • Endocrine + Immunotherapy being explored in ER-positive MSI-H tumors.

3️⃣ Personalization via biomarkers

  • ESR1, PIK3CA, AR-V7 testing guides drug choice.

  • Liquid biopsy for ctDNA mutation tracking.

  • Machine-learning models predicting AI response under trial.

4️⃣ Patient-centric models

  • Long-acting oral formulations → home adherence programs.

  • Telemonitoring of BP, weight, mood, DEXA reminders.

(ESMO Innovation Summit 2025)