Table 1.
Drug Class | Medication | Dose/Administration | Mechanism of Action |
---|---|---|---|
SERM | Tamoxifen [17] | 20 mg PO once daily | Inhibitory effect on estrogen-regulated pathways through competitive mechanisms of ER-binding, leading to suppression of mammary tumor angiogenesis |
AI Non-Steroidal Steroidal |
Anastrozole [18] Letrozole [19] Exemestane [20] |
1 mg PO once daily 2.5 mg PO once daily 25 mg PO once daily |
By inhibiting the aromatase enzyme, it reduces the circulating estrogen levels by suppressing its conversion from androgens, predominantly in adipose tissues |
GnRHa | Goserelin [21] Leuprolide [22] Triptorelin [23] |
3.6 mg SubQ q28 days 3.75 mg IM q28 days 3.75 mg IM q28 days |
Chemical castration leading to lower secretion of FSH and LH, thereby suppressing estrogen levels |
CDK 4/6 Inhibitor | Abemaciclib [24] | 150 mg PO twice daily | Selective inhibition of CDK4 and CDK6, subsequently terminating the cell cycle at the G1 phase by interrupting pRb phosphorylation |
Bisphosphonate * | Zoledronic Acid [25] Clodronate [26] Ibandronate [27] |
4 mg IV q6 month 1600 mg PO daily 50 mg PO daily |
Inhibits osteoclasts by way of apoptosis, and thereby decreases bone resorption and increases bone mineralization |
* Dosing, mode of administration and total duration of the bisphosphonates recommended by ASCO guideline [28]: Zoledronic Acid 4 mg IV every 6 months for 3 years or at 4 mg once every 3 months for 2 years. Clodronate 1600 mg PO daily for 2 to 3 years. Ibandronate 50 mg PO daily for 3 years. SERM: Selective Estrogen Receptor Modulator, ER: Estrogen Receptor, PO: Per oral, AI: Aromatase Inhibitor, IV: Intravenous, SubQ: Subcutaneous, IM: Intramuscular, GnRHa: Gonadotropin-releasing hormone agonist, FSH: Follicle stimulating hormone, LH: Luteinizing hormone, CDK 4/6: Cyclin-Dependent Kinase 4/6 inhibitor, pRb: Retinoblastoma protein.