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 | 5.2Â nM/2.9Â 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 | 1.2Â nM/0.9Â 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 | |
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) | |
Sought FDA approval for second time on October 10, 2017 | For maintenance treatment settings | PO | ________ | ______ | ≥ 3 lines of therapy | [40] | |
Niraparib (Zejulaâ„¢) | 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 | 3.2Â nM/4Â nM (PARP1/2) | - CR or PR to previous (at least two) platinum-based chemotherapy. |