Evaluation of in vitro absorption, distribution, metabolism, and excretion and assessment of drug-drug interaction of rucaparib, an orally potent poly(ADP-ribose) polymerase inhibitor

References

• Rubraca (rucaparib) tablets [prescribing information]. Boulder (CO): Clovis Oncology, Inc., 2018.
   Google Scholar
• Rubraca (rucaparib) tablets [summary of product characteristics]. Swords: Clovis Oncology Ireland Ltd., 2019.
   Google Scholar
• Abida W, Campbell D, Patnaik A, et al. (2019). Preliminary results from the TRITON2 study of rucaparib in patients (pts) with DNA damage repair (DDR)-deficient metastatic castration-resistant prostate cancer (mCRPC): updated analyses. Ann Oncol 30:abst 846PD.
   Google Scholar
• Abida W, Campbell D, Patnaik A, et al. (2020). Non-BRCA DNA damage repair gene alterations and response to the PARP inhibitor rucaparib in metastatic castration-resistant prostate cancer: analysis from the phase 2 TRITON2 study. Clin Cancer Res. doi: 10.1158/1078-0432.CCR-20-0394.
   PubMed Web of Science ®Google Scholar
• Acharya P, Engel JC, Correia MA. (2009). Hepatic CYP3A suppression by high concentrations of proteasomal inhibitors: a consequence of endoplasmic reticulum (ER) stress induction, activation of RNA-dependent protein kinase-like ER-bound eukaryotic initiation factor 2α (eIF2α)-kinase (PERK) and general control nonderepressible-2 eIF2α kinase (GCN2), and global translational shutoff. Mol Pharmacol 76:503–15.
   PubMed Web of Science ®Google Scholar
• Chappell JC, Turner PK, Pak YA, et al. (2019). Abemaciclib inhibits renal tubular secretion without changing glomerular filtration rate. Clin Pharmacol Ther 105:1187–95.
   PubMed Web of Science ®Google Scholar
• Chu V, Einolf HJ, Evers R, et al. (2009). In vitro and in vivo induction of cytochrome p450: a survey of the current practices and recommendations: a pharmaceutical research and manufacturers of america perspective. Drug Metab Dispos 37:1339–54.
   PubMed Web of Science ®Google Scholar
• Chu X, Bleasby K, Chan GH, et al. (2016). The complexities of interpreting reversible elevated serum creatinine levels in drug development: does a correlation with inhibition of renal transporters exist? Drug Metab Dispos 44:1498–509.
   PubMedGoogle Scholar
• Chu X, Liao M, Shen H, et al. (2018). Clinical probes and endogenous biomarkers as substrates for transporter drug-drug interaction evaluation: perspectives from the International Transporter Consortium. Clin Pharmacol Ther 104:836–64.
   PubMed Web of Science ®Google Scholar
• Coleman RL, Oza AM, Lorusso D, et al. (2017). Rucaparib maintenance treatment for recurrent ovarian carcinoma after response to platinum therapy (ARIEL3): a randomised, double-blind, placebo-controlled, phase 3 trial. Lancet 390:1949–61.
   PubMed Web of Science ®Google Scholar
• Dierks EA, Stams KR, Lim H-K, et al. (2001). A method for the simultaneous evaluation of the activities of seven major human drug-metabolizing cytochrome P450s using an in vitro cocktail of probe substrates and fast gradient liquid chromatography tandem mass spectrometry. Drug Metab Dispos 29:23–9.
   PubMed Web of Science ®Google Scholar
• European Medicines Agency. (2012). Guideline on the investigation of drug interactions. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2012/07/WC500129606.pdf [last accessed 4 Mar 2019].
   Google Scholar
• Evers R, de Haas M, Sparidans R, et al. (2000). Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer 83:375–83.
   PubMed Web of Science ®Google Scholar
• Fahmi OA, Hurst S, Plowchalk D, et al. (2009). Comparison of different algorithms for predicting clinical drug-drug interactions, based on the use of CYP3A4 in vitro data: predictions of compounds as precipitants of interaction. Drug Metab Dispos 37:1658–66.
   PubMed Web of Science ®Google Scholar
• Food and Drug Administration. (2012). Draft guidance for industry: drug interaction studies – study design, data analysis, implications for dosing, and labeling recommendations. Available from: https://www.fda.gov/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm528107.htm [accessed 4 Mar 2019].
   Google Scholar
• Food and Drug Administration. (2017a). Draft guidance for industry: clinical drug interaction studies – study design, data analysis, and clinical implications. Available from: https://www.fda.gov/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm064982.htm [accessed 4 Mar 2019].
   Google Scholar
• Food and Drug Administration. (2017b). NDA/BLA multi-disciplinary review and evaluation NDA 208716 (VERZENIO (abemaciclib)). Available from: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208716Orig1s000MultidisciplineR.pdf [accessed 4 Mar 2019].
   Google Scholar
• Gilibili R, Kurawattimath V, Murali B, et al. (2018). In vitro stimulation of multidrug resistance-associated protein 2 function is not reproduced in vivo in rats. Pharmaceutics 10:125.
   Web of Science ®Google Scholar
• Gilibili RR, Chatterjee S, Bagul P, et al. (2017). Coproporphyrin-I: a fluorescent, endogenous optimal probe substrate for ABCC2 (MRP2) suitable for vesicle-based MRP2 inhibition assay. Drug Metab Dispos 45:604–11.
   PubMed Web of Science ®Google Scholar
• Herédi-Szabó K, Glavinas H, Kis E, et al. (2009). Multidrug resistance protein 2-mediated estradiol-17β-D-glucuronide transport potentiation: in vitro-in vivo correlation and species specificity. Drug Metab Dispos 37:794–801.
   PubMed Web of Science ®Google Scholar
• Kristeleit R, Shapiro GI, Burris HA, et al. (2017). A phase I-II study of the oral PARP inhibitor rucaparib in patients with germline BRCA1/2-mutated ovarian carcinoma or other solid tumors. Clin Cancer Res 23:4095–106.
   PubMed Web of Science ®Google Scholar
• Lagas JS, van der Kruijssen CMM, van de Wetering K, et al. (2009). Transport of diclofenac by breast cancer resistance protein (ABCG2) and stimulation of multidrug resistance protein 2 (ABCC2)-mediated drug transport by diclofenac and benzbromarone. Drug Metab Dispos 37:129–36.
   PubMed Web of Science ®Google Scholar
• Liao M, Watkins S, Nash E, et al. (2019). Evaluation of absorption, distribution, metabolism, and excretion of [14C]-rucaparib, a poly(ADP-ribose) polymerase inhibitor, in patients with advanced solid tumors. Invest New Drugs. doi: 10.1007/s10637-019-00815-2.
   Web of Science ®Google Scholar
• Lv X, Xia Y, Finel M, et al. (2019). Recent progress and challenges in screening and characterization of UGT1A1 inhibitors. Acta Pharm Sin B 9:258–78.
   PubMed Web of Science ®Google Scholar
• Mathialagan S, Rodrigues AD, Feng B. (2017). Evaluation of renal transporter inhibition using creatinine as a substrate in vitro to assess the clinical risk of elevated serum creatinine. J Pharm Sci 106:2535–41.
   PubMed Web of Science ®Google Scholar
• Murai J, Huang SY, Renaud A, et al. (2014). Stereospecific PARP trapping by BMN 673 and comparison with olaparib and rucaparib. Mol Cancer Ther 13:433–43.
   PubMed Web of Science ®Google Scholar
• Oza AM, Tinker AV, Oaknin A, et al. (2017). Antitumor activity and safety of the PARP inhibitor rucaparib in patients with high-grade ovarian carcinoma and a germline or somatic BRCA1 or BRCA2 mutation: integrated analysis of data from Study 10 and ARIEL2. Gynecol Oncol 147:267–75.
   PubMed Web of Science ®Google Scholar
• Polyak K, Garber J. (2011). Targeting the missing links for cancer therapy. Nat Med 17:283–4.
   PubMed Web of Science ®Google Scholar
• Robillard L, Nguyen M, Harding TC, Simmons AD. (2017). In vitro and in vivo assessment of the mechanism of action of the PARP inhibitor rucaparib. Cancer Res 77:abstr 2475.
   Web of Science ®Google Scholar
• Shapiro GI, Kristeleit R, Burris HA, et al. (2019). Pharmacokinetic study of rucaparib in patients with advanced solid tumors. Clin Pharmacol Drug Dev 8:107–18.
   PubMed Web of Science ®Google Scholar
• Swisher EM, Lin KK, Oza AM, et al. (2017). Rucaparib in relapsed, platinum-sensitive high-grade ovarian carcinoma (ARIEL2 Part 1): an international, multicentre, open-label, phase 2 trial. Lancet Oncol 18:75–87.
   PubMed Web of Science ®Google Scholar
• Thomas HD, Calabrese CR, Batey MA, et al. (2007). Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther 6:945–56.
   PubMed Web of Science ®Google Scholar
• Wahlberg E, Karlberg T, Kouznetsova E, et al. (2012). Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors. Nat Biotechnol 30:283–8.
   PubMed Web of Science ®Google Scholar
• Waikar SS, Betensky RA, Emerson SC, Bonventre JV. (2012). Imperfect gold standards for kidney injury biomarker evaluation. J Am Soc Nephrol 23:13–21.
   PubMed Web of Science ®Google Scholar
• Xiao JJ, Nowak D, Ramlau R, et al. (2019). Evaluation of drug-drug interactions of rucaparib and CYP1A2, CYP2C9, CYP2C19, CYP3A, and P-gp substrates in patients with an advanced solid tumor. Clin Transl Sci 12:58–65.
   PubMed Web of Science ®Google Scholar
• Zamek-Gliszczynski MJ, Chu X, Cook JA, et al. (2018). ITC commentary on metformin clinical drug-drug interaction study design that enables an efficacy- and safety-based dose adjustment decision. Clin Pharmacol Ther 104:781–4.
   PubMed Web of Science ®Google Scholar
• Zelcer N, Huisman MT, Reid G, et al. (2003). Evidence for two interacting ligand binding sites in human multidrug resistance protein 2 (ATP binding cassette C2). J Biol Chem 278:23538–44.
   PubMed Web of Science ®Google Scholar
• Zibetti Dal Molin G, Westin SN, Msaouel P, et al. (2020). Discrepancy in calculated and measured glomerular filtration rates in patients treated with PARP inhibitors. Int J Gynecol Cancer 30:89–93.
   PubMed Web of Science ®Google Scholar