From: Recent advances in targeted strategies for triple-negative breast cancer
Target | Drug name | Com | Num | Regiments | Phase | Status | Object | POM | NCT number |
---|---|---|---|---|---|---|---|---|---|
PI3K inhibitor | Alpelisib (BYL719) | nab-paclitaxel | 137 | Alpelisib: 300Â mg qd po nab-paclitaxel: 100Â mg/m2 iv on Days 1, 8 and 15 of a 28-day cycle | III | Active, not recruiting | TNBC | PFS, ORR | NCT04251533 |
 | Alpelisib (BYL719) | nab-paclitaxel | 8 | Alpelisib: qd po on days 1–21 Nab-paclitaxel: iv over 30 min on days 1, 8, and 15 | II | Active, not recruiting | TNBC | pCR | NCT04216472 |
 | AZD8186 |  | 147 | A single dose on day 1 followed by ongoing multiple dosing | I | Completed | TNBC | Safety and tolerability | NCT01884285 |
 | BKM120 (Buparlisib) |  | 50 | 100 mg/d po in cycles of 28 days | II | Completed | TNBC | CBR | NCT01790932 |
 | BKM120 |  | 50 | 100 mg/d po in cycles of 28 days, until disease progression | II | Completed | TNBC | CBR | NCT01629615 |
 | BKM120 | Capecitabine | 10 | BKM120: 100 mg/d po Capecitabine: 500 mg bid po, 14 days on and 7 days off | II | Completed | mBC | CBR | NCT02000882 |
 | BKM120/BYL719 | Olaparib | 118 | BKM120: 40 mg/d po Olaparib: 50 mg bid po BYL719: 250 mg/d po | I | Completed | TNBC | MTD | NCT01623349 |
 | CUDC-907 |  | 43 | 60 mg/d po 5 days on 2 days off until disease progression | I | Completed | TNBC | Safety and tolerability | NCT02307240 |
 | GDC-0941 | Cisplatin | 11 | GDC-0941: 260 mg po, days 2–6, 9–13, 16–20, 23–27. 28 days cycle Cisplatin: 25 mg/m2 iv day 1, 8, 15 | I/II | Terminated | TNBC | Safety and tolerability, ORR | NCT01918306 |
 | SF1126 |  | 44 | Dose Escalating with 3 + patients in each cohort | I | Completed | Solid cancer | DLTs | NCT00907205 |
Akt inhibitor | GSK2141795 | Trametinib (GSK1120212) | 37 | GSK2141795: po qd on days 1–28 Trametinib: po qd on days 1–28 | II | Completed | TNBC | ORR | NCT01964924 |
 | GSK2141795 | Trametinib | 240 | Po qd | I | Completed | TNBC | Safety and tolerability | NCT01138085 |
 | GSK2141795 | Trametinib | 37 | Po qd on days 1–28 | II | Completed | TNBC | ORR | NCT01964924 |
 | ONC201 (TIC10) |  | 4 | Po on days 3, 10, and 17 | II | Terminated | TNBC | ORR | NCT03733119 |
 | Ipatasertib (GDC-0068) | Paclitaxel | 151 | Ipatasertib: 400 mg/d po on days 1–21 of each 28-day cycle for 3 cycles Paclitaxel: 80 mg/m2 iv q1w | II | Completed | TNBC | pCR | NCT02301988 |
 | Ipatasertib | Paclitaxel | 124 | Ipatasertib: 400 mg/d po days 1–21 in each cycle of 28 days Paclitaxel: 80 mg/m2 iv on days 1, 8, and 15 | II | Completed | TNBC | PFS | NCT02162719 |
PI3K /mTOR inhibitor | PF-05212384 (Gedatolisib) | Docetaxel/ Cisplatin | 110 | 90Â mg/m2 iv as a 3Â weeks cycle Docetaxel/Cisplatin: 75Â mg/m2 iv once q3w | I | Completed | TNBC | DLTs, ORR | NCT01920061 |
 | BEZ235 | MEK162 | 29 | NA | I | Completed | TNBC | DLTs | NCT01337765 |
 | PQR309 | Eribulin (Halaven®) | 41 | PQR309: after eribulin Eribulin: 1.4 mg/m2 iv on day 1, 8 in a period of 21 days | I | Completed | TNBC | AEs, SAEs | NCT02723877 |
EGFR inhibitor | Cetuximab (Erbitux) | Ixabepilone (Ixempra ®) | 40 | Cetuximab: 400 mg/m2 iv over 120 min on day 1 of the first of four 21 days cycles Ixabepilone: 40 mg/m2 iv over 180 min on day 1 of each of four 21 days cycles | II | Completed | TNBC | CRR | NCT01097642 |
 | Lapatinib (Tykerb ®) | Veliparib (ABT-888) | 23 | Lapatinib:1250 mg/d for 28 days Veliparib: 200 mg/bid for 28 days | NA | Active, not recruiting | TNBC | Safety and toxicity | NCT02158507 |
 | Lapatinib | Everolimus (mTOR inhibitor) | 5 | Lapatinib: 1250 mg by mouth daily Everolimus: 5 mg by mouth daily | II | Terminated | TNBC | Safety and toxicity, ORR | NCT01272141 |
 | Erlotinib (Tarceva ®) | Cisplatin plus temsirolimus | 9 | Erlotinib: 100 mg by mouth daily Cisplatin: 30 mg/m2 iv weekly on days 1 and 8 of a 3 weeks cycle Temsirolimus: dosing level, 15 mg, 25 mg | I | Completed | TNBC | MTD | NCT00998036 |
 | Erlotinib | Metformin | 8 | Erlotinib: 150 mg/d Metformin: 850 mg bid | I | Completed | TNBC | MTD | NCT01650506 |
 | Erlotinib | Bendamustine | 11 | Erlotinib: 100 or 150 mg po on days 5—21 of each 28 days cycle Bendamustine: 100 or 120 mg/m2 iv on days 1 and 2 | I/II | Completed | Breast Cancer | MTD, DLTs, PFS | NCT00834678 |
 | Gefitinib (Irresa ®) |  | 50 | 250 mg/d by mouth until disease progression | II | Unknown | TNBC | CBR | NCT01732276 |
Notch inhibitor | AL101 | Â | 67 | NA | II | Active, not recruiting | TNBC | ORR | NCT04461600 |
 | RO4929097 (R4733) |  | 6 | Po qd on days 1–3, 8–10, and 15–17 | II | Terminated | TNBC | ORR, PFS | NCT01151449 |
 | RO4929097 | Carboplatin plus Paclitaxel | 14 | RO4929097: po qd on days 1–3, 8–10, and 15–17 Paclitaxel: iv over 60 min on days 1, 8, and 15 Carboplatin: iv over 60 min on day 1 | I | Terminated | TNBC | AEs, MTD | NCT01238133 |
TGF-β inhibitor | Bintrafusp Alfa (M7824) |  | 11 | 1200 mg once q2w | II | Completed | TNBC | ORR | NCT04489940 |