Skip to main content

Table 1 Overview of common FDA approved and investigational PARP inhibitors and their treatment profile

From: PARP inhibitors as potential therapeutic agents for various cancers: focus on niraparib and its first global approval for maintenance therapy of gynecologic cancers

Name of the drug Approval by FDA Clinical conditions for which the drug are approved or under investigation Route Targeted PARP enzyme(s) (Affinity) IC50 Line of previous chemotherapy References
Veliparib (ABT-888) Under investigation (its efficacy and safety have not been established yet) FDA grants orphan drug designation for advanced squamous non-small cell lung cancer (Phase III) PO PARP 1and PARP2 5.2 nM/2.9 nM (PARP1/2) _____ [63]
Fluzoparib (SHR3162) Under investigation (phase I) in combination with apatinib Recurrent ovarian cancer PO PARP 1 and PARP 2 ______ Two lines of platinum-based therapy (gynecologic cancers) and only one line of standard chemotherapy (TNBC) [64]
TNBC
Talazoparib (BMN 673) Investigational drug Under development for advanced breast cancer patients with gBRCA mutations PO PARP 1/2>>>>PARP3 1.2 nM/0.9 nM (PARP1/2) _____ [65]
Olaparib (Lynparza®) December 2014
(First FDA approval)
Patients with germline BRCA1/2-mutated advanced recurrent ovarian cancer PO PARP 1 > PARP2>>PARP3 5 nM/1 nM(PARP1/2) ≥ 3 prior lines of chemotherapy [9, 32, 33].
Approved again on Aug 17, 2017 For the maintenance treatment of adult patients with recurrent gynecologic cancers PO ______ ______ ≥ 2 lines of therapy [34]
Rucaparib (Rubraca®) December 2016
(Second approval)
Treatment of ovarian cancer patients with somatic and/or germline BRCA mutations PO PARP 1>>>>>PARP2/3 1.4 nM (PARP1) One line earlier than olaparib (patients who have received ≥2 prior lines of chemotherapy) [37, 38, 60]
Sought FDA approval for second time on October 10, 2017 For maintenance treatment settings PO ________ ______ ≥ 3 lines of therapy [40]
Niraparib (Zejula™) March 2017 (Third Approval) Maintenance therapy of adult patients with recurrent gynecologic cancers irrespective of the status of BRCA mutations and/or HRD status PO PARP1 and PARP2 3.2 nM/4 nM (PARP1/2) - CR or PR to previous (at least two) platinum-based chemotherapy. [42, 56]
  1. Abbreviations: IC intracellular concentrations, BRCA breast cancer genem, PO per oral, PARP Poly(ADP-ribose) polymerase, CR complete response, PR partial response, FDA Food and Drug Administration, HRD homologous recombination deficiency, TNBC triple negative breast cancer