Preclinical Antitumor Activity and Pharmacokinetics of Methyl-2-Benzimidazolecarbamate (FB642)

@article{Hao2004PreclinicalAA,
  title={Preclinical Antitumor Activity and Pharmacokinetics of Methyl-2-Benzimidazolecarbamate (FB642)},
  author={Desir{\'e}e Hao and Jinee D. Rizzo and Stephanie Stringer and Rodney V. Moore and Jennifer Marty and Daniel L. Dexter and G L Mangold and James Berger Camden and Daniel D. Von Hoff and Steven D. Weitman},
  journal={Investigational New Drugs},
  year={2004},
  volume={20},
  pages={261-270}
}
Methyl-2-benzimidazolecarbamate(carbendazim, FB642) is an anticancer agentthat induces apoptosis of cancer cells. [] Key Result In the murineB16 melanoma model, T/C values > 200 wereobserved. In the human tumor xenograft,FB642 produced tumor growth inhibition ofgreater than 58% in five of the sevenxenograft models evaluated. Partial andcomplete tumor shrinkage was noted withFB642 against the MCF-7 breast tumor model.
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References

SHOWING 1-10 OF 25 REFERENCES
Preclinical antitumor activity of 6-hydroxymethylacylfulvene, a semisynthetic derivative of the mushroom toxin illudin S.
TLDR
The excellent activity of HMAF in several human solid tumor xenografts, including the more refractory MV522 and HT-29 models, warrants the further investigation of this novel agent in clinical trials.
The new dioxolane, (-)-2'-deoxy-3'-oxacytidine (BCH-4556, troxacitabine), has activity against pancreatic human tumor xenografts.
TLDR
The new dioxolane analogue troxacitabine was evaluated in two human pancreatic cancer xenograft models and was more efficacious against Panc-01 and was equally active against MiaPaCa.
R17934-NSC 238159: a new antitumor drug--I. Effect on experimental tumors and factors influencing effectiveness.
The fate of 14C-carbendazim in rat.
TLDR
The disappearance of 14C-carbendazim in rat (i.v. 12 mg/kg) followed the kinetics of a two-compartment open-system model, and the concentration of unchanged carbendzim in blood and of 5-HBC in urine may be of diagnostic value in acute poisoning with carbendazIM.
Structure-activity relationships of benzimidazole carbamates as inhibitors of mammalian tubulin, in vitro.
The pharmacokinetics and bioavailability of a tracer dose of [3H]-mebendazole in man.
TLDR
Comparison of metabolite area under the plasma concentration vs time data from each route of administration indicates that absorption of mebendazole from the gastrointestinal tract at this dose level is almost complete, and the low bioavailability observed following oral administration at this doses level is postulated to be due to high first pass elimination.
A new culture model facilitating rapid quantitative testing of mitotic spindle inhibition in mammalian cells.
TLDR
A new culture model, which facilitated both mass screening of potential anticancer drugs acting on microtubules and quantitative experiments with known "antitubulins," was found to have the following advantages: use of mammalian cells, simplicity of the techniques, and ease with which it lent itself to quantification.
Microtubule-active drugs taxol, vinblastine, and nocodazole increase the levels of transcriptionally active p53.
TLDR
The ability of three microtubule-active agents, taxol, vinblastine, and nocodazole, to increase p53 levels and activate p53-dependent processes is examined to suggest there is an additional pathway for activating p53 and subsequent p53 -dependent processes.
...
...