Table 1 List of FDA-approved small molecules for targeted therapy of breast cancer
From: Advancements in clinical aspects of targeted therapy and immunotherapy in breast cancer
S. no | Drugs (Year of regular approval) | Structures | Breast cancer subtypes | Conditions | Comments | References |
|---|---|---|---|---|---|---|
PARP inhibitors | ||||||
1 | Olaparib (2018) |
| gBRCA-mutated HER2 − metastatic BC | Combination with chemotherapy in the adjuvant and neoadjuvant setting | Approval was based on the phase III OlympiAD trial (NCT02000622) | [129] |
2 | Talazoparib (2018) |
| gBRCA-mutated HER2 − locally advanced or metastatic BC | - | Approval was based on the phase III EMBRACA trial (NCT01945775) | [52] |
PI3K inhibitor | ||||||
3 | Alpelisib (2019) |
| HR + /HER2 − , PIK3CA-mutated, advanced or metastatic BC | Combination with an ER antagonist, fulvestrant | Approval was based on the phase III SOLAR-1 trial (NCT02437318) | [139] |
mTOR inhibitor | ||||||
4 | Everolimus (2012) |
| Postmenopausal women with advanced HR + /HER2 − BC patients who have relapsed/ progressed following treatment with a non-steroidal aromatase inhibitor | Combination with a steroidal aromatase inhibitor, exemestane | Approval was based on the phase III BOLERO-2 trial (NCT00863655) | [140] |
CDK4/6 inhibitors | ||||||
5 | Abemaciclib (2017, 2023) |
| Refractory HR + /HER2 − metastatic BC | Monotherapy | Approval was based on the phase II MONARCH-1 trial (NCT02747004) | |
|  |  |  | HR + /HER2 − advanced or metastatic BC | Combination with fulvestrant | Approval was based on the phase III MONARCH-2 trial (NCT02107703) |  |
|  |  |  | Postmenopausal BC | Combination with a nonsteroidal aromatase inhibitor, letrozole or anastrozole | Approval was based on the phase III MONARCH-3 trial (NCT02246621) |  |
|  |  |  | HR + /HER2 − , LN + adult patients with early breast cancer at high risk of recurrence | Combination with an adjuvant aromatase inhibitor, tamoxifen | Approval was based on the phase III monarchE trial (NCT03155997) |  |
6 | Palbociclib (2017) |
| Postmenopausal ER + /HER2 − advanced BC | Combination with letrozole | Approval was based on the phase III PALOMA-2 trial (NCT01740427) | |
|  |  |  | HR + /HER2 − metastatic BC after endocrine failure | Combination with fulvestrant | Approval was based on the phase III PALOMA-3 trial (NCT01942135) |  |
7 | Ribociclib (2017) |
| Postmenopausal advanced BC | Combination with letrozole | Approval was based on the phase III MONALEESA-2 trial (NCT01958021) | |
|  |  |  | Postmenopausal advanced BC | Combination with fulvestrant | Approval was based on the phase III MONALEESA-3 trial (NCT02422615) |  |
|  |  |  | Premenopausal HR + /HER2 − advanced BC | Combination with non-steroidal aromatase inhibitor and goserelin | Approval was based on the phase III MONALEESA-7 trial (NCT02278120) |  |
Angiogenesis inhibitors | ||||||
8 | Lapatinib (2018) |
| Postmenopausal HR + , HER2 overexpressing advanced or metastatic BC | Combination with letrozole | Approval was based on the phase III trial (NCT00073528) | [145] |
9 | Tucatinib (2020) |
| HER2 + advanced BC | Combination with trastuzumab and capecitabine | Approval was based on the phase III HER2CLIMB trial (NCT02614794) | [146] |
10 | Neratinib (2020) |
| HER2 + metastatic BC | Combination with capecitabine | Approval was based on the phase III NALA trial (NCT01808573) | [147] |
