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Babiker HM, Milhem M, Aisner J, et al. Evaluation of the bioequivalence and food effect on the bioavailability of CC-486 (oral azacitidine) tablets in adult patients with cancer. Cancer Chemother Pharmacol. 2020;85(3):621-626doi: 10.1007/s00280-020-04037-9.
Babiker, H. M., Milhem, M., Aisner, J., Edenfield, W., Shepard, D., Savona, M., Iyer, S., Abdelrahim, M., Beach, C. L., Skikne, B., Laille, E., Tsai, K. T., & Ho, T. (2020). Evaluation of the bioequivalence and food effect on the bioavailability of CC-486 (oral azacitidine) tablets in adult patients with cancer. Cancer chemotherapy and pharmacology, 85(3), 621-626. https://doi.org/10.1007/s00280-020-04037-9
Babiker, Hani M, et al. "Evaluation of the bioequivalence and food effect on the bioavailability of CC-486 (oral azacitidine) tablets in adult patients with cancer." Cancer chemotherapy and pharmacology vol. 85,3 (2020): 621-626. doi: https://doi.org/10.1007/s00280-020-04037-9
Babiker HM, Milhem M, Aisner J, Edenfield W, Shepard D, Savona M, Iyer S, Abdelrahim M, Beach CL, Skikne B, Laille E, Tsai KT, Ho T. Evaluation of the bioequivalence and food effect on the bioavailability of CC-486 (oral azacitidine) tablets in adult patients with cancer. Cancer Chemother Pharmacol. 2020 Mar;85(3):621-626. doi: 10.1007/s00280-020-04037-9. Epub 2020 Feb 08. PMID: 32036412; PMCID: PMC7036073.
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Cancer Chemother Pharmacol. 2020 Mar;85(3):621-626. doi: 10.1007/s00280-020-04037-9. Epub 2020 Feb 08.

Evaluation of the bioequivalence and food effect on the bioavailability of CC-486 (oral azacitidine) tablets in adult patients with cancer.

Cancer chemotherapy and pharmacology

Hani M Babiker, Mohammed Milhem, Joseph Aisner, William Edenfield, Dale Shepard, Michael Savona, Swaminathan Iyer, Maen Abdelrahim, C L Beach, Barry Skikne, Eric Laille, Kao-Tai Tsai, Thai Ho

Affiliations

  1. University of Arizona Comprehensive Cancer Center, Tucson, AZ, USA. [email protected].
  2. University of Iowa Hospital, Iowa City, IA, USA.
  3. Rutgers Cancer Institute of New Jersey, New Brunswick, NJ, USA.
  4. Greenville Health System, Greenville, SC, USA.
  5. Cleveland Clinic, Cleveland, OH, USA.
  6. Vanderbilt University Medical Center, Nashville, TN, USA.
  7. MD Anderson Cancer Center, Houston, TX, USA.
  8. Houston Methodist Hospital, Houston, TX, USA.
  9. Celgene Corporation, Summit, NJ, USA.
  10. University of Kansas Medical Center, Kansas City, KS, USA.
  11. Mayo Clinic, Phoenix, AZ, USA.

PMID: 32036412 PMCID: PMC7036073 DOI: 10.1007/s00280-020-04037-9

Abstract

PURPOSE: CC-486 is an oral formulation of azacitidine that allows for extended dosing schedules to prolong azacitidine exposure to malignant cells and maximize clinical activity. CC-486 300 mg daily, administered for 14 or 21 days of 28-day treatment cycles, is currently under investigation in two ongoing phase III trials. The 300-mg daily dose in these studies is administered as two 150-mg tablets (Formulation A).

METHODS: We evaluated the bioequivalence of one 300-mg CC-486 tablet (Formulation B) with Formulation A and food effect on Formulation B, in adult patients with cancer in a 2-stage crossover design study.

RESULTS: The ratios of the geometric means of the maximum azacitidine plasma concentration (C

CONCLUSION: The single 300-mg CC-486 tablet was bioequivalent to two 150-mg tablets, which have shown to be efficacious and generally well-tolerated in clinical trials, and can be taken with or without food.

Keywords: Bioequivalence; CC-486; Oral azacitidine; Pharmacokinetics

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