Therapy Detail

Therapy Name Rucaparib
Therapy Description

Rubraca (rucaparib) binds to and inhibits PARP, which may result in accumulation of DNA damage and chemosensitization of tumor cells (PMID: 17363489). Rubraca (rucaparib) is FDA approved for use in ovarian cancer patients with deleterious somatic and/or germline BRCA mutations (FDA.gov).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Rucaparib Rubraca AG014699|PF-01367338|CO-388|AG14447 PARP Inhibitor (Pan) 17 Rubraca (rucaparib) binds to and inhibits PARP, which may result in accumulation of DNA damage and chemosensitization of tumor cells (PMID: 17363489). Rubraca (rucaparib) is FDA approved for use in ovarian cancer patients with deleterious somatic and/or germline BRCA mutations (FDA.gov).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PTEN del prostate cancer sensitive Rucaparib Preclinical - Cell culture Actionable In a preclinical study, Rubraca (rucaparib) induced senescence and increased radiosensitivity in PTEN null prostate cancer cells in culture (PMID: 23565244). 23565244
Unknown unknown ovarian carcinoma not applicable Rucaparib Phase II Actionable In a Phase II trial, Rubraca (rucaparib) demonstrated activity in patients with platinum-sensitive high-grade ovarian carcinoma, with patients in the BRCA mutant and BRCA wild-type with high genomic loss-of-heterozygosity subgroups demonstrating increased progression-free survival compared to the BRCA wild-type with low genomic loss-of-heterozygosity subgroup (PMID: 27908594). 27908594
MET dec exp triple-receptor negative breast cancer sensitive Rucaparib Preclinical - Cell culture Actionable In a preclinical study, triple-receptor negative breast cancer cell lines with decreased Met expression via shRNA knockdown demonstrated increased sensitivity to Rubraca (rucaparib) induced growth and colony formation inhibition in culture (PMID: 26779812). 26779812
BRCA1 N682* ovarian carcinoma sensitive Rucaparib Clinical Study Actionable In a clinical study, an ovarian carcinoma patient harboring a BRCA1 N682* germline mutation demonstrated a partial response when treated with Rubraca (rucaparib) (PMID: 28588062). 28588062
ARID1A dec exp breast cancer sensitive Rucaparib Preclinical - Cell culture Actionable In a preclinical study, Rubraca (rucaparib) inhibited colony formation of human mammary epithelial cells and inhibited proliferation of a human breast cancer cell line after knockdown of ARID1A in culture (PMID: 26069190). 26069190
BRCA1 E23Vfs*17 invasive ductal carcinoma resistant Rucaparib Preclinical - Cell line xenograft Actionable In a preclinical study, breast invasive ductal carcinoma cells harboring BRCA1 E23Vfs*17 (also referred to as BRCA1 185delAG) acquired resistance to Rubraca (rucaparib) both in culture and in cell line xenograft models through the expression of a RING-less Brca1 protein utilizing an in-frame translation start site downstream of the mutation (PMID: 27454289). 27454289
BRCA1 dec exp MET dec exp triple-receptor negative breast cancer sensitive Rucaparib Preclinical - Cell culture Actionable In a preclinical study, decreasing Brca1 expression via shRNA knockdown sensitized triple-receptor negative breast cancer cells with low expression of Met to Rubraca (rucaparib) in culture (PMID: 26779812). 26779812
BRCA2 mutant ovarian cancer sensitive Rucaparib Guideline Actionable Rubraca (rucaparib) is included in the guidelines as recurrence therapy for ovarian cancer patients harboring BRCA1/2 germline mutations (NCCN.org). detail...
BRCA2 mutant ovarian cancer sensitive Rucaparib Phase II Actionable In a Phase II clinical trial, treatment with Rubraca (rucaparib) was tolerated and demonstrated activity in ovarian cancer patients with germline BRCA1/2 mutations (PMID: 27002934). 27002934
BRCA2 mutant ovarian cancer sensitive Rucaparib FDA approved Actionable In a retrospective analysis of two Phase II trials (ARIEL 2 and Study 10) that supported FDA approval, Rubraca (rucaparib) treatment resulted in an objective response rate of 54% (21/39) in high-grade ovarian cancer patients harboring BRCA2 mutations (PMID: 28751443). 28751443
BRCA2 mutant ovarian cancer sensitive Rucaparib Phase III Actionable In a Phase III trial (ARIEL3), Rubraca (rucaparib) treatment resulted in significantly improved progression-free survival compared to placebo (16.6 vs 5.4 months, HR=0.23, p=0.0001) in patients with BRCA-mutant, platinum-sensitive ovarian cancer (PMID: 28916367; NCT01968213). 28916367
ARID1A Q456* colorectal cancer sensitive Rucaparib Preclinical - Cell culture Actionable In a preclinical study, Rubraca (rucaparib) treatment resulted in increased apoptosis of colorectal cancer cells harboring ARID1A Q456* in culture (PMID: 26069190). 26069190
BRCA2 dec exp MET over exp triple-receptor negative breast cancer no benefit Rucaparib Preclinical - Cell culture Actionable In a preclinical study, decreasing Brca2 expression via shRNA knockdown did not sensitize triple-receptor negative breast cancer cells with Met overexpression to Rubraca (rucaparib) in culture (PMID: 26779812). 26779812
BRCA1 mutant pancreatic cancer predicted - sensitive Rucaparib Phase II Actionable In a Phase II trial, Rubraca (rucaparib) treatment resulted in an objective response rate of 11% (2/19) and a disease control rate of 32% (6/19) in advanced pancreatic cancer patients with a known deleterious BRCA mutation, of whom 79% harbored a BRCA2 mutation (J Clin Oncol 34, 2016 (suppl; abstr 4110)). detail...
BRCA1 mutant ovarian cancer sensitive Rucaparib Phase II Actionable In a Phase II clinical trial, treatment with Rubraca (rucaparib) was tolerated and demonstrated activity in ovarian cancer patients with germline BRCA1/2 mutations (PMID: 27002934). 27002934
BRCA1 mutant ovarian cancer sensitive Rucaparib Guideline Actionable Rubraca (rucaparib) is included in the guidelines as recurrence therapy for ovarian cancer patients harboring BRCA1/2 germline mutations (NCCN.org). detail...
BRCA1 mutant ovarian cancer sensitive Rucaparib FDA approved Actionable In a retrospective analysis of two Phase II trials (ARIEL2 and Study 10) that supported FDA approval, Rubraca (rucaparib) treatment resulted in an objective response rate of 54% (36/67) in high-grade ovarian cancer patients harboring BRCA1 mutations (PMID: 28751443). 28751443
BRCA1 mutant ovarian cancer sensitive Rucaparib Phase III Actionable In a Phase III trial (ARIEL3), Rubraca (rucaparib) treatment resulted in significantly improved progression-free survival compared to placebo (16.6 vs 5.4 months, HR=0.23, p=0.0001) in patients with BRCA-mutant, platinum-sensitive ovarian cancer (PMID: 28916367; NCT01968213). 28916367
Unknown unknown Advanced Solid Tumor not applicable Rucaparib Phase I Actionable In a Phase I trial, Rubraca (rucaparib) was well-tolerated and demonstrated preliminary efficacy, with a disease control rate of 86% (6/7), in patients with advanced solid tumors (J Clin Oncol 31, 2013 (suppl; abstr 2585)). detail...
BRCA1 dec exp MET over exp triple-receptor negative breast cancer no benefit Rucaparib Preclinical - Cell culture Actionable In a preclinical study, decreasing Brca1 expression via shRNA knockdown did not sensitize triple-receptor negative breast cancer cells with Met over expression to Rubraca (rucaparib) in culture (PMID: 26779812). 26779812
STAG2 N357fs glioblastoma multiforme sensitive Rucaparib Preclinical - Cell culture Actionable In a preclinical study, a glioblastoma cell line harboring a STAG2 mutation (reported as STAG2 N357fs, PMID: 21852505), demonstrated increased sensitivity to treatment with Rubraca (rucaparib) in culture compared to isogenic cells with wild-type STAG2 (PMID: 24356817). 21852505 24356817
BRCA2 mutant pancreatic cancer predicted - sensitive Rucaparib Phase II Actionable In a Phase II trial, Rubraca (rucaparib) treatment resulted in an objective response rate of 11% (2/19) and a disease control rate of 32% (6/19) in advanced pancreatic cancer patients with a known deleterious BRCA mutation, of whom 79% harbored a BRCA2 mutation (J Clin Oncol 34, 2016 (suppl; abstr 4110)). detail...
BRCA1 W1782* ovarian carcinoma sensitive Rucaparib Clinical Study Actionable In a clinical study, an ovarian carcinoma patient harboring a BRCA1 W1782* germline mutation demonstrated stable disease when treated with Rubraca (rucaparib) (PMID: 28588062). 28588062
MET over exp triple-receptor negative breast cancer decreased response Rucaparib Preclinical - Cell culture Actionable In a preclinical study, triple-receptor negative breast cancer cell lines overexpressing Met demonstrated decreased sensitivity to Rubraca (rucaparib) induced growth and colony formation inhibition in culture (PMID: 26779812). 26779812
BRCA1 L631Qfs*4 ovarian carcinoma sensitive Rucaparib Clinical Study Actionable In a clinical study, an ovarian carcinoma patient harboring a BRCA1 L631Qfs*4 germline mutation demonstrated a partial response when treated with Rubraca (rucaparib) (PMID: 28588062). 28588062
IDH1 R132H Advanced Solid Tumor sensitive Rucaparib Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing IDH1 R132H demonstrated increased sensitivity to Rubraca (rucaparib)-induced growth inhibition in culture (PMID: 28148839). 28148839
BRCA1 L392Qfs*5 ovarian carcinoma sensitive Rucaparib Clinical Study Actionable In a clinical study, an ovarian carcinoma patient harboring a BRCA1 L392Qfs*5 germline mutation demonstrated a partial response when treated with Rubraca (rucaparib) (PMID: 28588062). 28588062
BRCA2 dec exp MET dec exp triple-receptor negative breast cancer sensitive Rucaparib Preclinical - Cell culture Actionable In a preclinical study, decreasing Brca2 expression via shRNA knockdown sensitized triple-receptor negative breast cancer cells with low expression of Met to Rubraca (rucaparib) in culture (PMID: 26779812). 26779812
Clinical Trial Phase Therapies Title Recruitment Status
NCT03542175 Phase I Rucaparib A Study of Rucaparib Administered With Radiation in Patients With Triple Negative Breast Cancer With an Incomplete Response Following Chemotherapy Recruiting
NCT02975934 Phase III Rucaparib A Study of Rucaparib Verses Physician's Choice of Therapy in Patients With Metastatic Castration-resistant Prostate Cancer and Homologous Recombination Gene Deficiency Recruiting
NCT01891344 Phase II Rucaparib A Study of Rucaparib in Patients With Platinum-Sensitive, Relapsed, High-Grade Epithelial Ovarian, Fallopian Tube, or Primary Peritoneal Cancer (ARIEL2) Active, not recruiting
NCT03572478 Phase Ib/II Nivolumab + Rucaparib Nivolumab Rucaparib Rucaparib and Nivolumab in Patients With Prostate or Endometrial Cancer Recruiting
NCT02042378 Phase II Rucaparib A Study of Rucaparib in Patients With Pancreatic Cancer and a Known Deleterious BRCA Mutation Completed
NCT01968213 Phase III Rucaparib A Study of Rucaparib as Switch Maintenance Following Platinum-Based Chemotherapy in Patients With Platinum-Sensitive, High-Grade Serous or Endometrioid Epithelial Ovarian, Primary Peritoneal or Fallopian Tube Cancer Active, not recruiting
NCT02952534 Phase II Rucaparib A Study of Rucaparib in Patients With MetA Study of Rucaparib in Patients With Metastatic Castration-resistant Prostate Cancer and Homologous Recombination Gene Deficiency (TRITON2) Recruiting
NCT02855944 Phase III Cisplatin Rucaparib Carboplatin Gemcitabine Paclitaxel ARIEL4: A Study of Rucaparib Versus Chemotherapy BRCA Mutant Ovarian, Fallopian Tube, or Primary Peritoneal Cancer Patients Recruiting
NCT01482715 Rucaparib A Study of Oral Rucaparib in Patients With a Solid Tumor (Phase I) or With gBRCA Mutation Ovarian Cancer (Phase II) Active, not recruiting
NCT03413995 Phase II Rucaparib Trial of Rucaparib in Patients With Metastatic Hormone-Sensitive Prostate Cancer Harboring Germline DNA Repair Gene Mutations (TRIUMPH) Recruiting
NCT03617679 Phase I Rucaparib Rucaparib vs Placebo Maintenance Therapy in Metastatic and Recurrent Endometrial Cancer Not yet recruiting
NCT03397394 Phase II Rucaparib Rucaparib in Patients With Locally Advanced or Metastatic Urothelial Carcinoma (ATLAS) Recruiting
NCT03318445 Phase I Rucaparib Irinotecan + Rucaparib Rucaparib and Irinotecan in Cancers With Mutations in DNA Repair Recruiting
NCT03522246 Phase III Rucaparib Nivolumab Nivolumab + Rucaparib A Study in Ovarian Cancer Patients Evaluating Rucaparib and Nivolumab as Maintenance Treatment Following Response to Front-Line Platinum-Based Chemotherapy (ATHENA) Recruiting
NCT03533946 Phase II Rucaparib Rucaparib in Nonmetastatic prOstAte With BRCAness (ROAR) Recruiting
NCT03140670 Phase II Rucaparib Rucaparib in BRCA1/2 or PALB2 Mutated Pancreatic Cancer Recruiting