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50 years of preclinical anticancer drug screening: empirical to target-driven approaches.
  • M. Suggitt, M. Bibby
  • Medicine
    Clinical cancer research : an official journal of…
  • 1 February 2005
This review focuses on the major contributions of preclinical screening models to anticancer drug development over the past 50 years of the US National Cancer Institute (NCI), and Europe has played a key role in the development of new anticancer agents.
Differentiation and definition of vascular-targeted therapies.
A simple taxonomy and nomenclature is proposed in anticipation that the therapeutic potential of this novel class of vascular-targeted therapies can be realized as these approaches advance in clinical settings and a new anticancer strategy becomes available in the clinic.
Orthotopic models of cancer for preclinical drug evaluation: advantages and disadvantages.
  • M. Bibby
  • Medicine
    European journal of cancer
  • 1 April 2004
The use of orthotopic systems will strengthen the ability to select the most appropriate molecules for recommended use in clinical studies, given the expertise now being developed and some interesting observations being made on the role of the tumour site on response to therapeutic agents.
The delivery of antisense therapeutics.
Recent advances in the in vitro and in vivo delivery of antisense oligodeoxynucleotides and ribozymes look at recent advances in cellular targeting and intracellular delivery.
Antimicrobial activity of cecropins.
Through combination studies with hydrophobic antibiotics and electron microscopy, cecropin B was shown to disrupt the bacterial outer membrane, suggesting that the cytoplasmic membranes of Gram-positive organisms were inherently more resistant to the peptide.
Comparative Preclinical Pharmacokinetic and Metabolic Studies of the Combretastatin Prodrugs Combretastatin A4 Phosphate and A1 Phosphate
Although in vitro studies suggest that variable rates of tumor-specific prodrug dephosphorylation may explain differences in pharmacokinetics profiles, the improved antitumor activity and altered pharmacokinetic profile of CA1 may be due to the formation of a more reactive metabolite.
In vivo and in vitro evaluation of combretastatin A-4 and its sodium phosphate prodrug
It is concluded that combretastatin A-4 and its prodrug caused extensive necrosis in MAC 15A s.c. and orthotopic colon cancer and metastases, resulting in anti-tumour effects.
EO9: a novel bioreductive alkylating indoloquinone with preferential solid tumour activity and lack of bone marrow toxicity in preclinical models.
In vivo, EO9 was inactive against the P388 murine leukaemia, while exerting significant antiproliferative effects against several murine and human solid tumours, including the generally resistant MAC mouse colon tumours and gastric, ovarian and breast xenografts.
In vitro activity of the novel indoloquinone EO-9 and the influence of pH on cytotoxicity.
The results of this study demonstrate that EO-9 induces a broad spectrum of activity against a panel of human and murine tumour cell lines and suggest that if Eo-9 can be delivered to regions of low pH within solid tumours, a therapeutic advantage may be obtained.
Combination chemotherapy with combretastatin A-4 phosphate and 5-fluorouracil in an experimental murine colon adenocarcinoma.
This study demonstrates that extensive necrosis occurred in a treated refractory murine colon adenocarcinoma but the damage was not accompanied by any measurable effect on tumour growth, and suggests that if an antivascular mechanism can be demonstrated in humans, combination chemotherapy should be rapidly assessed in a clinical setting.