. 2021 Dec 6;14(12):1270. doi: 10.3390/ph14121270

Table 1.

Clinical trials with PARP inhibitors as monotherapy in the metastatic setting.

First Author Study Name	Year of Study	No. of Participants (BC Patients)	Type of Study	Median/Mean No. of Prior Chemotherapy Regimens (Range)	Comparative Arms		Patient Population	Outcome (Objective Response Rate, Progression Free Survival)
First Author Study Name	Year of Study	No. of Participants (BC Patients)	Type of Study	Median/Mean No. of Prior Chemotherapy Regimens (Range)	PARPi	Comparative Agent/ Standard Chemotherapy	Patient Population
Fong, P.C. et al. [42]	2009	60 (9 BC)	Phase I	28% ≤ 2 lines * 18%—3 lines * 53% ≥ 4 lines *	Olaparib Cohort 1: 10 mg/day to 600 mg twice daily Cohort 2: 200 mg twice daily	None	BRCA^MUT: N = 22 BRCA^WT: N = 38	ORR in all BRCA^MUT: 47.4% No objective response in BRCA^WT
de Bono, J. et al. [43]	2017	110 (20 BC)	Phase I	2.5 (0–13)	Talazoparib Part 1: 0.025 to 1.1 mg/day Part 2: 1.0 mg/day	None	Part 1: DNA repair deficiency; Part 2: gBRCA^MUT	ORR in BRCA^MUT in breast cancer: 50% PFS in breast cancer: 34.6 weeks
Puhalla S et al. [44] Pahuja S et al. [45]	2014	98 (40 BC)	Phase I	gBRCA^MUT: 6 (1–14) * BRCA^WT: 4 (1–12) *	Veliparib 50–500 mg twice daily	None	gBRCA^MUT: N = 70 BRCA^WT: N = 28	ORR in all BRCA^MUT: 23%, breast BRCAMUT: 29% ORR in all BRCA^WT: 4%, breast BRCAMUT: 5%
Tutt, A. et al. [46]	2010	54 (54 BC)	Phase II, non-randomized sequential-cohort	Cohort 1: 3 (1–5) Cohort 2: 3 (2–4)	Olaparib Cohort 1: 400 mg twice daily Cohort 2: 100 mg twice daily	None	gBRCA^MUT	ORR in cohort 1: 41%, cohort 2: 22% PFS in cohort 1: 5.7 months; PFS in cohort 2: 3.8 months
Gelmon, K.A. et al. [47]	2011	91 (26 BC)	Phase II, non-randomized	3 (1–7)	Olaparib capsule 400 mg twice daily	None	BRCA^MUT: N = 27 BRCA^WT: N = 63	ORR in ovarian cancer: BRCA^MUT 41%, BRCA^WT 24%; breast cancer: BRCA^MUT 0% BRCA^WT 0% PFS in ovarian cancer: BRCA^MUT 7.4 months, BRCA^WT: 6.4 months; breast cancer: BRCA^MUT 3.6 months, BRCA^WT: 1.8 months
Kaufman, B. et al. [48]	2015	298 (62 BC)	Phase II, single-arm, non-randomized	BC cohort: 4.6 (3–11)	Olaparib capsule 400 mg twice daily	None	gBRCA^MUT	Response rate for all: 26.2%; breast cancer 12.9% PFS in breast cancer 3.7 months
Robson, M.E. et al. [26,49] OlympiAD	2017	302 (302 BC)	Phase III, randomized	≤2 lines	Olaparib tablet 300 mg twice daily	Capecitabine, eribulin, or vinorelbine	gBRCA^MUT HER2-negative	ORR 59.9% vs. 28.8% (olaparib versus standard chemotherapy) PFS 7.0 months vs. 4.2 months (olaparib versus standard chemotherapy)
Litton J.K. et al. [27] EMBRACA	2018	431 (431 BC)	Phase III, randomized	≤3 lines	Talazoparib 1 mg once daily	Capecitabine, eribulin, gemcitabine, or vinorelbine	gBRCA^MUT HER2-negative	ORR 62.2% vs. 27.2% (olaparib versus standard chemotherapy) PFS 8.6 months vs. 5.6 months (olaparib versus standard chemotherapy)
Tung N.M. et al. [50] TBCRC 048	2020	54 (54 BC)	Phase II, non-randomized	1 (0–4)	Olaparib tablet 300 mg twice daily	None	Cohort 1: Germline mutation in HR-related gene (not gBRCA1/2) Cohort 2: Somatic mutations in same genes (including BRCA1/2)	ORR in all cohort 1, 33%; gPALB2^MUT 82%; all cohort 2, 31%; sBRCA^MUT 50% PFS for gPALB2^MUT, 13.3 months; sBRCA^MUT 6.3 months

Abbreviations: BC, breast cancer. * Previous treatment regimen.