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Developmental therapeutics

1384 - An open-label, randomized cross-over bioavailability study of oral paclitaxel and HM30181 compared with weekly intravenous (IV) paclitaxel in patients with advanced solid tumours (133O)


18 Nov 2017


Developmental therapeutics


Cytotoxic Therapy;  Clinical Research


Christopher Jackson


Annals of Oncology (2017) 28 (suppl_10): x39-x41. 10.1093/annonc/mdx658


C.G.C.A. Jackson1, S. Deva2, K. Bayston3, P. Barlow2, K. Eden4, N. Hung5, G. Fetterly6, D. Cutler6, R. Kwan6, D. Kramer6, W. Chan6, T. Hung7

Author affiliations

  • 1 Department Of Medicine, University of Otago, 9016 - Dunedin/NZ
  • 2 Regional Cancer And Blood Service, Auckland District Health Board, Auckland/NZ
  • 3 Southern Blood And Cancer, Southern District Health Board, Invercargill/NZ
  • 4 Southern Blood And Cancer, Southern District Health Board, 9016 - Dunedin/NZ
  • 5 Department Of Pathology, University of Otago, 9016 - Dunedin/NZ
  • 6 -, Athenex, Buffalo/US
  • 7 -, Zenith Technologies, Dunedin/NZ


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Abstract 1384


Paclitaxel has poor oral bioavailability due to active excretion by p-glycoprotein (Pgp) on intestinal epithelial cells. Oral administration is preferable to IV administration to minimize IV access, avoid allergic reactions to cremaphor, obviate steroid pre-medication, reduce day stay, provide cost-savings, and improve patient convenience. Oraxol (Athenex, USA) is a combination of oral paclitaxel and HM30181, a novel oral non-absorbed specific inhibitor of intestinal Pgp. Following a previously reported phase 1 dose-escalation study, we report the preliminary bio-equivalence results of a three-day schedule of Oraxol compared to IV paclitaxel.


We conducted a randomized crossover study recruiting patients from 2 sites in New Zealand. HM30181 15mg plus oral paclitaxel 205mg/m2 (®Oraxol) were administered orally once daily for 3 consecutive days and compared to a single dose of IV paclitaxel (80 mg/m2) in patients with advanced solid tumours. PK blood samples were taken up to day 9 for Oraxol and day 5 for IV paclitaxel.


A scheduled interim analysis of the first 6 patents’ Oraxol PK (AUC0-∞) compared to IV paclitaxel showed: - Geometric mean ratios (GMR) = 87.09%, (90% CI 74.61-101.66%) - Intra-subject coefficients of variation (CV) = 12.62% - Time over minimum effective concentration was approximately 6 hours for IV paclitaxel, and 30 hours for Oraxol. Further results will be presented. The safety profile of Oraxol was acceptable without grade 3-4 toxicities. A total sample size of 30 subjects is required to demonstrate bioequivalence between Oraxol and IV paclitaxel (90% CI of the GMR is within the limits of 80% – 125%), with 80% power.


Oraxol 615mg/m2 orally over three days achieved paclitaxel AUC comparable to IV paclitaxel 80mg/m2. A three-day schedule of Oraxol is within predicted range needed to demonstrate bioequivalence, and further patients are being enrolled to achieve adequate power. A phase 3 study is now underway.

Clinical trial indentification

ACTRN 12615000894594.

Clinical trial identification

ACTRN 12615000894594.

Legal entity responsible for the study





G. Fetterly, R. Kwan, W-K. Chan: Employee of Athenex, D. Cutler: Employee and shareholder in Athenex, D. Kramer: Employee of Athenex; Shareholder in Athenex, All other authors have declared no conflicts of interest.

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