TABLE 2

Published plasma pharmacokinetic parameters of BEL in humans after a single intravenous dose

Human Subjects with Cancer TypeDosage of BELCmax (µM)Tmax (h)t1/2 (h)AUC(0–t) (µM/h)Reference
Prostate adenocarcinoma, thymus, urothelial carcinoma, and uterine leiomyosarcoma1000 mg/m2131 ± 31.60.482.9 ± 4.5186.8 ± 21.7 (0–24 h)Bailey et al. (2016)
Uterine carcinosarcoma, urothelial bladder carcinoma, pancreatic adenocarcinoma, lung adenocarcinoma, gastroesophageal junction, and colorectal carcinoma1500 mg175.59 ± 41.46a0.481.58103.03 ± 19.41 (0–12 h)aCalvo et al. (2016)
Hepatocellular carcinoma900 mg/m298.34 ± 29.66a0.424.07 ± 0.3969.94 ± 17.22 (0–24 h)aYeo et al. (2012)
1200 mg/m2153.29 ± 50.33a0.424.14 ± 0.42122.46 ± 37 (0–24 h)aYeo et al. (2012)
1400 mg/m2182.92 ± 56.11a0.453.49 ± 0.73149.21 ± 44.11 (0–24 h)aYeo et al. (2012)
Pancreatic carcinoma, osteosarcoma/chondrosarcoma, soft tissue sarcoma, rectal carcinoma, gastric carcinoma, unknown carcinoma, ovarian carcinoma, malignant melanoma, mesothelioma, bladder carcinoma, hepatocellular carcinoma, and cholangiocarcinoma800 mg/m2b70.8 ± 18.9N/AN/A35.5 ± 8.7 (0–24 h)Lassen et al. (2010)
1000 mg/m2b127.6 ± 43.5N/AN/A102 ± 58.3 (0–24 h)Lassen et al. (2010)
Colorectal, melanoma, renal, esophagogastric, breast, cervix, diffuse large B-cell lymphoma, germ cell, lung (non–small cell), mesothelioma, ovary, prostate, pseudomyxoma peritonei, sarcoma, and thymoma900 mg/m2145.36 ± 56.20aN/AN/A47.66 ± 11.78 (0–24 h)aSteele et al. (2008)
1000 mg/m2100.90 ± 28.67aN/AN/A31.39 ± 10.47 (0–24 h)aSteele et al. (2008)
1200 mg/m2168.97 ± 36.04aN/AN/A60.34 ± 27.93 (0–24 h)aSteele et al. (2008)
  • AUC(0–t), area under the curve for time 0 to present; N/A, not applicable; Tmax, time to plasma Cmax.

  • a Micromolar concentration was calculated based on the provided nanogram per milliliter concentration.

  • b BEL was administered in combination chemotherapy.