Oral paclitaxel with encequidar compared to intravenous paclitaxel in patients with advanced cancer: A randomised crossover pharmacokinetic study.
HM30181A
cancer
encequidar
oral chemotherapy
p-glycoprotein
paclitaxel
taxanes
Journal
British journal of clinical pharmacology
ISSN: 1365-2125
Titre abrégé: Br J Clin Pharmacol
Pays: England
ID NLM: 7503323
Informations de publication
Date de publication:
12 2021
12 2021
Historique:
revised:
20
04
2021
received:
19
12
2020
accepted:
24
04
2021
pubmed:
8
5
2021
medline:
11
3
2022
entrez:
7
5
2021
Statut:
ppublish
Résumé
Paclitaxel is a widely used anti-neoplastic agent but has low oral bioavailability due to gut extrusion by P-glycoprotein (P-gp). Oral paclitaxel could be more convenient, less resource intensive, and more tolerable than intravenous administration. Encequidar (HM30181A) is a novel, minimally absorbed gut-specific P-gp inhibitor. We tested whether administration of oral paclitaxel with encequidar (oPac+E) achieved comparable AUC to intravenous paclitaxel (IVP) 80 mg/m We conducted a multi-centre randomised crossover study with two treatment periods. Patients (pts) with advanced cancer received either oral paclitaxel 615 mg/m Forty-two patients were enrolled; 35 completed both treatment periods. AUC GMR for AUC was within the predefined acceptable range of 80-125% for demonstrating equivalence. oPac+E is tolerable and there is no evidence of P-gp induction with repeat administration. With further study, oPac+E could be an alternative to IVP.
Substances chimiques
ATP Binding Cassette Transporter, Subfamily B, Member 1
0
Paclitaxel
P88XT4IS4D
Types de publication
Journal Article
Multicenter Study
Randomized Controlled Trial
Langues
eng
Sous-ensembles de citation
IM
Pagination
4670-4680Informations de copyright
© 2021 British Pharmacological Society.
Références
Ghersi D, Willson ML, Chan MMK, Simes J, Donoghue E, Wilcken N. Taxane-containing regimens for metastatic breast cancer. Cochrane Database Syst Rev. 2015;2015(6):CD003366. https://doi.org/10.1002/14651858.CD003366.pub3
Clamp AR, James EC, McNeish IA, et al. Weekly dose-dense chemotherapy in first-line epithelial ovarian, fallopian tube, or primary peritoneal carcinoma treatment (ICON8): primary progression free survival analysis results from a GCIG phase 3 randomised controlled trial. Lancet. 2019;394(10214):2084-2095. https://doi.org/10.1016/s0140-6736(19)32259-7
Masters GA, Temin S, Azzoli CG, et al. Systemic therapy for stage IV non-small-cell lung cancer: American Society of Clinical Oncology clinical practice guideline update. J Clin Oncol. 2015;33(30):3488-3515. https://doi.org/10.1200/jco.2015.62.1342
Lu Z, Zhang X, Liu W, et al. A multicenter, randomized trial comparing efficacy and safety of paclitaxel/capecitabine and cisplatin/capecitabine in advanced gastric cancer. Gastric Cancer. 2018;21(5):782-791. https://doi.org/10.1007/s10120-018-0809-y
Rowinsky EK. Paclitaxel pharmacology and other tumor types. Semin Oncol. 1997;24(6 Suppl 19):S19-1-s19-12.
World Health Organization. World Health Organization Model List of Essential Medicines, 21st List, 2019. https://www.who.int/groups/expert-committee-on-selection-and-use-of-essential-medicines/essential-medicines-lists
De Bono JS, Oudard S, Ozguroglu M, et al. Prednisone plus cabazitaxel or mitoxantrone for metastatic castration-resistant prostate cancer progressing after docetaxel treatment: a randomised open-label trial. Lancet. 2010;376(9747):1147-1154. https://doi.org/10.1016/s0140-6736(10)61389-x
Lee H, Park S, Kang JE, Lee HM, Kim SA, Rhie SJ. Efficacy and safety of nanoparticle-albumin-bound paclitaxel compared with solvent-based taxanes for metastatic breast cancer: a meta-analysis. Sci Rep. 2020;10(1):530. https://doi.org/10.1038/s41598-019-57380-0
O'Shaughnessy J, Schwartzberg L, Piccart M, et al. Results from CONTESSA: A phase 3 study of tesetaxel plus a reduced dose of capecitabine versus capecitabine alone in patients with HER2-, hormone receptor+ (HR+) metastatic breast cancer (MBC) who have previously received a taxane. San Antonio Breast Cancer Symposium. 2020;(Abstr GS4-01).
Wani MC, Taylor HL, Wall ME, Coggon P, McPhail AT. Plant antitumor agents. VI. Isolation and structure of taxol, a novel antileukemic and antitumor agent from Taxus brevifolia. J Am Chem Soc. 1971;93(9):2325-2327. https://doi.org/10.1021/ja00738a045
Walsh V, Goodman J. The billion dollar molecule: Taxol in historical and theoretical perspective. Clio Med. 2002;66:245-267. https://doi.org/10.1163/9789004333499_013
Picard M, Castells MC. Re-visiting hypersensitivity reactions to taxanes: a comprehensive review. Clin Rev Allergy Immunol. 2015;49(2):177-191. https://doi.org/10.1007/s12016-014-8416-0
Joerger M. Treatment regimens of classical and newer taxanes. Cancer Chemother Pharmacol. 2016;77(2):221-233. https://doi.org/10.1007/s00280-015-2893-6
Schrag D, Hershman DL, Basch E. Oncology practice during the COVID-19 pandemic. JAMA. 2020;323(20):2005-2006. https://doi.org/10.1001/jama.2020.6236
Gosain R, Abdou Y, Singh A, Rana N, Puzanov I, Ernstoff MS. COVID-19 and cancer: a comprehensive review. Curr Oncol Rep. 2020;22(5):53. https://doi.org/10.1007/s11912-020-00934-7
Jibodh RA, Lagas JS, Nuijen B, Beijnen JH, Schellens JH. Taxanes: old drugs, new oral formulations. Eur J Pharmacol. 2013;717(1-3):40-46. https://doi.org/10.1016/j.ejphar.2013.02.058
Schellens JHM, Malingré MM, Kruijtzer CMF, et al. Modulation of oral bioavailability of anticancer drugs: from mouse to man. Eur J Pharm Sci. 2000;12(2):103-110. https://doi.org/10.1016/s0928-0987(00)00153-6
Kartner N, Riordan JR, Ling V. Cell surface P-glycoprotein associated with multidrug resistance in mammalian cell lines. Science. 1983;221(4617):1285-1288. https://doi.org/10.1126/science.6137059
Helgason HH, Kruijtzer CMF, Huitema ADR, et al. Phase II and pharmacological study of oral paclitaxel (Paxoral) plus ciclosporin in anthracycline-pretreated metastatic breast cancer. Br J Cancer. 2006;95(7):794-800. https://doi.org/10.1038/sj.bjc.6603332
Hendrikx JJ, Lagas JS, Rosing H, Schellens JH, Beijnen JH, Schinkel AH. P-glycoprotein and cytochrome P450 3A act together in restricting the oral bioavailability of paclitaxel. Int J Cancer. 2013;132(10):2439-2447. https://doi.org/10.1002/ijc.27912
van Asperen J, van Tellingen O, van der Valk MA, Rozenhart M, Beijnen JH. Enhanced oral absorption and decreased elimination of paclitaxel in mice cotreated with cyclosporin A. Clin Cancer Res. 1998;4(10):2293-2297.
Malingré MM, Terwogt JM, Beijnen JH, et al. Phase I and pharmacokinetic study of oral paclitaxel. J Clin Oncol. 2000;18(12):2468-2475. https://doi.org/10.1200/jco.2000.18.12.2468
Grossman RM, Chevret S, Abi-Rached J, Blanchet F, Dubertret L. Long-term safety of cyclosporine in the treatment of psoriasis. Arch Dermatol. 1996;132(6):623-629.
Hendrikx JJ, Lagas JS, Wagenaar E, et al. Oral co-administration of elacridar and ritonavir enhances plasma levels of oral paclitaxel and docetaxel without affecting relative brain accumulation. Br J Cancer. 2014;110(11):2669-2676. https://doi.org/10.1038/bjc.2014.222
Malingré MM, Beijnen JH, Rosing H, et al. Co-administration of GF120918 significantly increases the systemic exposure to oral paclitaxel in cancer patients. Br J Cancer. 2001;84(1):42-47. https://doi.org/10.1054/bjoc.2000.1543
Dash RP, Jayachandra Babu R, Srinivas NR. Therapeutic potential and utility of elacridar with respect to P-glycoprotein inhibition: an insight from the published in vitro, preclinical and clinical studies. Eur J Drug Metab Pharmacokinet. 2017;42(6):915-933. https://doi.org/10.1007/s13318-017-0411-4
Paek IB, Ji HY, Kim MS, Lee G, Lee HS. Metabolism of a new P-glycoprotein inhibitor HM-30181 in rats using liquid chromatography/electrospray mass spectrometry. Rapid Commun Mass Spectrom. 2006;20(9):1457-1462. https://doi.org/10.1002/rcm.2468
Paek IB, Ji HY, Kim MS, Lee GS, Lee HS. Simultaneous determination of paclitaxel and a new P-glycoprotein inhibitor HM-30181 in rat plasma by liquid chromatography with tandem mass spectrometry. J Sep Sci. 2006;29(5):628-634. https://doi.org/10.1002/jssc.200500368
Kim T-E, Gu N, Yoon SH, et al. Tolerability and pharmacokinetics of a new P-glycoprotein inhibitor, HM30181, in healthy Korean male volunteers: single- and multiple-dose randomized, placebo-controlled studies. Clin Ther. 2012;34(2):482-494. https://doi.org/10.1016/j.clinthera.2012.01.003
Lee HJ, Heo D-S, Cho J-Y, et al. A phase I study of oral paclitaxel with a novel P-glycoprotein inhibitor, HM30181A, in patients with advanced solid cancer. Cancer Res Treat. 2014;46(3):234-242. https://doi.org/10.4143/crt.2014.46.3.234
Lee KW, Lee KH, Zang DY, et al. Phase I/II study of weekly oraxol for the second-line treatment of patients with metastatic or recurrent gastric cancer. Oncologist. 2015;20(8):896-897. https://doi.org/10.1634/theoncologist.2015-0202
Jackson C, Bayston K, McLaren B, et al. An open label, randomised cross-over bioavailability study of oral paclitaxel (oraxol) compared to intravenous paclitaxel 80mg/m2. J Clin Oncol. 2016;34(15_suppl):2569. https://doi.org/10.1200/JCO.2016.34.15_suppl.2569
Alexander SPH, Fabbro D, Kelly E, et al. The Concise Guide to PHARMACOLOGY 2019/20: Enzymes. Br J Pharmacol. 2019;176(S1):S297-S396.
Alexander SPH, Kelly E, Mathie A, et al. The Concise Guide to PHARMACOLOGY 2019/20: Transporters. Br J Pharmacol. 2019;176(S1):S397-S493.
Lopes NM, Adams EG, Pitts TW, Bhuyan BK. Cell kill kinetics and cell cycle effects of taxol on human and hamster ovarian cell lines. Cancer Chemother Pharmacol. 1993;32(3):235-242. https://doi.org/10.1007/bf00685842
Moulder SL, Holmes FA, Tolcher AW, et al. A randomized phase 2 trial comparing 3-hour versus 96-hour infusion schedules of paclitaxel for the treatment of metastatic breast cancer. Cancer. 2010;116(4):814-821. https://doi.org/10.1002/cncr.24870
Seidman AD, Berry D, Cirrincione C, et al. Randomized phase III trial of weekly compared with every-3-weeks paclitaxel for metastatic breast cancer, with trastuzumab for all HER-2 overexpressors and random assignment to trastuzumab or not in HER-2 nonoverexpressors: final results of Cancer and Leukemia Group B protocol 9840. J Clin Oncol. 2008;26(10):1642-1649. https://doi.org/10.1200/jco.2007.11.6699
Lim HS, Bae KS, Jung JA, et al. Predicting the efficacy of an oral paclitaxel formulation (DHP107) through modeling and simulation. Clin Ther. 2015;37(2):402-417. https://doi.org/10.1016/j.clinthera.2014.12.009
Umanzor G, Cutler DL, Barrios FJ, et al. Abstract GS6-01: Oral paclitaxel with encequidar: the first orally administered paclitaxel shown to be superior to IV paclitaxel on confirmed response and survival with less neuropathy: a phase III clinical study in metastatic breast cancer. Cancer Res. 2020;80(4 Supplement):GS6-01. https://doi.org/10.1158/1538-7445.SABCS19-GS6-01