Table 2.
Targeted agent | Phase | Dosing schedule | Participants (n) | Results | Adverse effects | Ref. |
---|---|---|---|---|---|---|
Olaparib | 1 | Olaparib 400 mg b.i.d, 21-day cycles | 59 | RR of 41 and 43% among patients with BRCA1/2 mutation | Neutropenia, lekopenia, anemia | [47] |
Olaparib | Olaparib 400 mg b.i.d, 28-day cycles | 19 | Partial response of 37%, one patient remains on olaparib monotherapy without progression | Diarrhea, nausea, neutropenia | [48] | |
Olaparib | I | Olaparib 400 mg b.i.d, 28-day cycles | 28 | RR of 44%, clinical benefit rate of 61%, 2 patients had stable disease for >24 weeks | Hypertension, fatigue | [49] |
Olaparib | I | Olaparib 400 mg b.i.d, 28-day cycles | 298 | RR of 31.1%, stable disease ≥8 weeks observed in 42% of patients | Fatigue, nausea, vomiting, anemia | [52] |
Olaparib + cediranib | II | Cediranib 20 mg/day + olaparib 100 mg b.i.d (standard 3 + 3 dose escalation design) → cediranib 20 mg/day + olaparib 200 mg b.i.d → cediranib 30 mg/day + olaparib 400 mg b.i.d | 46 | Median PFS of 17.7 months RR of 44%, clinical benefit rate of 61 %, 2 patients had stable disease for >24 weeks, median PFS of 17.7 months | Fatigue, diarrhea, hypertension | [50] |
Veliparib | I | Veliparib 60 mg/day, 21-day cycles | 35 | Seven patients had partial responses, additional six patients had disease stabilization for at least six cycles | Myelosuppression | [60] |
Veliparib | I | Veliparib 70 mg/day, 21-day cycles | 68 | RR of 23%, clinical benefit rate of 58% | Neutropenia, thrombocytopenia, peripheral neuropathy | [61] |
Rucaparib | I | Rucaparib 12 mg/m2 iv. every 28 days | 40 | RR of 17.4%, median time to progression 3.5 months, median OS 9.9 months, 36% of patients progression-free at 6 months | Thrombocytopenia, neutropenia, anemia | [62] |
Rucaparib | I | Rucaparib 12 mg/m2 iv. every 28 days | 32 | RR of 20%, median time to progression 5.5 months, median OS 9 months, 30% of patients progression-free at 6 months | Thrombocytopenia, anemia, neutropenia | [63] |
(Talazoparib) NCT02326844) | I | Talazoparib 1 mg/day, 28-day cycles until disease progression | − | Ongoing | − | [64] |
b.i.d: Two-times a day; iv.: Intravenous; OS: Overall survival; PFS: Progression-free survival; RR: Response rate.