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Review Articles:

Young S, Chaplin D. September 2004
Combretastatin A4 phosphate: background and current clinical status.
Expert Opin. Investig. Drugs. 13(9):1171-82

Siemann D, Chaplin D, Horsman MR. June 15, 2004
Vascular-Targeting Therapies for Treatment of Malignant Disease.
Cancer. 100(12):2491-9

West CML, Price P. March 2004.
Combretastatin A4 phosphate.
Anti-cancer Drugs. 15(3):179-87

Thorpe PE, Chaplin DJ, Blakeley DC. March 1, 2003
The First International Conference on Vascular Targeting: Meeting Overview.
Cancer Research. 63:1144-1147.

Chaplin DJ, Hill SA. Overview. 2002
Selective Induction of tumor ischemia; Development of vascular targeting agents for cancer therapy.
Current Opinion in Investigational Drugs. 3(9):1381-1384.

Chaplin DJ, Hill SA. December 1, 2002
The development of CA4P as a Vascular Targeting Agent.
Internation Journal of Radiation Oncology Biology Physics 54(5):1472.

Bibby MC. May 2002
Combretastatin anticancer drugs.
Drugs of the Future. 27(5):475-80.

Tozer GM, Kanthou C, Parkins CS, Hill SA. February 2002
The biology of combretastatins as tumour vascular targeting agents.
International Journal of Experimental Pathology 83(1):21-38

Griggs J. February 2001
Targeting tumour vasculature: the development of Combretastatin A-4.
The Lancent Oncology 2:82-7

POSTERS

D. Patterson et al.
OXi4503 Interim Phase I Results
AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics
October 2007

P. Nathan et al.
ZYBRESTAT™ + Bevacizumab Phase Ib Interim Results

European School of Haematology's International Conference on Vascular Targeted Therapies in Oncology, Mandelieu, France, October 2007

D. Brown & T. Wong

ZYBRESTAT™ (IV) Phase II in Myopic Macular Degeneration

Association for Research in Vision and Ophthalmology (ARVO) May 2007

CA4P / ZYBRESTAT

   Clinical Trial Research:

Bilenker JH, Flaherty KT, Rosen M, Davis L, Gallagher M, Stevenson JP, Sun W, Vaughn D, Giantonio B, Zimmer R, Schnall M, O'Dwyer PJ. February 15, 2005
Phase I Trial of Combretastatin A-4 Phosphate with Carboplatin.
Clinical Cancer Research 11:1527-33

Dowlatti A, Robertson K, Cooney M, Petros WP, Stratford M, Jesberger J, Rafie N, Overmoyer B, Makkar V, Stambler B, Taylor A, Waas J, Lewin JS, McCrae KR, Remick SC. June 15, 2002
A Phase I Pharmacokinetic and Translational Study of the novel Vascular Targeting Agent CA4P on a Single-Dose Intravenous Schedule in Patients with Advanced Cancer.
Cancer Research 62(12):3408-16

   Preclinical Research:

Vincent L, Kermani P, Young LM, Cheng J, Zhang F, Shido K, Lam G, Bompais-Vincent H, Zhu Z, Hicklin DJ, Bohlen P, Chaplin D, May C, Rafi S. November 2005.
Combretastatin A4 phosphate induces rapid regression of tumor neovessels and growth through interference with vascular endothelial-cadherin signaling.
J. Clin. Invest. 115:2992-3006.

Escalona-Benz E, Jockovich ME, Murray TG, Hayden B, Hernandez E, Feuer W, Windle JJ. January 2005
Combretastatin A-4 Prodrug in the Treatment of a Murine Model of Retinoblastoma.
IOVs. 46(1):8-11.

Kirwan IG, Loadman PM, Swaine DJ, Anthoney DA, Pettit GR, Lippert JW III, Shnyder SD, Cooper PA, Bibby MC. February 15, 2004.
Comparative Preclinical Pharmacokinetic and Metabolic Studies of the Combretastatin Prodrugs Combretastatin A4 Phosphate and A1 Phosphate.
Clinical Cancer Research. 10:1446-53.

Nambu H, Nambu R, Melia M, Campochiaro P. August, 2003.
Combretastatin A-4 Phosphate Suppresses Development and Induces Regression of Choroidal Neovascularization.
IOVS. 44(8):3650-5

Ahmed B, Ven Eijk LI, Bouma-Ter Steege JC, Van Der Schaft DW, Van Esch AM, Joosten-Achjanie SR, Lambin P, Landuyt W, Giffioen AW. May 20, 2003.
Vascular targeting effect of CA4P dominates the inherent angiogenesis inhibitory activity.
International Journal of Cancer 105(1):20-5.

Dziba JM, Marcinek R, Venkataraman G, Robinson JA, Ain KB. December 2002.
Combretastatin A-4 Phosphate has primary antineoplastic activity against human anaplastic thyroid carcinoma cell lines and xenograft tumors.
Thyroid 12(12):1063-70.

Horsman MR, Murata R. December 1, 2002.
Combination of vascular targeting agents with thermal or radiation therapy.
International Journal of Radiation Oncology Biology and Physics 54(5):1518-23.

Pedley RB, El-Emir E, Flynn AA, Boxer GM, Dearling J, Raleigh JA, Hill SA, Stuart S, Motha R, Begent RH. December 1, 2002
Synergy between vascular targeting agents and antibody-directed therapy.
International Journal of Radiation Oncology Biology Physics 54(5):1524-1531.

Hill SA, Chaplin DJ, Lewis G, Tozer GM. November 1, 2002
Schedule dependence of Combretastatin A-4 Phosphate in transplanted and spontaneous tumor models.
International Journal of Cancer 102(1):70-4.

Prise VE, Honess DJ, Stratford MR, Wilson J, Tozer GM. October 2002
The vascular response of tumor and normal tissues in the rat to the vascular targeting agent, Combretastatin A-4 Phosphate, at clinically relevant doses.
International Journal of Cancer. 21(4):717-26.

Nabha SM, Mohammad RM, Dandashi MH, Coupaye-Gerard B, Aboukameel A, Pettit GR, Al-Katib AM. August 2002
Combretastatin-A4 Prodrug induces mitotic catastophe in Chronic Lymphocytic Leukemia cell line independent of Caspase activation and Poly(ADP-ribose) Polymerase Cleavage.
Clinical Cancer Research 8:2735-41

Eikesdal HP, Landuyt W, Dahl O. April 25, 2002
The influence of CA4P and vinblastine on interstitial fluid pressure in BT(4)An rat gliomas.
Cancer Letter 178(2):209-17

Beauregard DA, Pedley RB, Hill SA, Brindle KM. April 2002
Differential sensitivity of two andenocarcinoma xenografts to the anti-vascular drugs CA4P and DMXAA, assessed using MRI and MRS.
NMR Biomedicine 15(2):99-105

Maxwell RJ, Wilson J, Prise VE, Vojnovic B, Rustin GJ, Lodge MA, Tozer GM. April 2002
Evaluation of the anti-vascular effects of combretastatin in rodent tumours by dynamic contrast enhanced MRI.
NMR Biomedicine 15(2):89-98

Kanthou C, Tozer GM. March 15, 2002
The tumor vascular targeting agent CA4P induces reorganization of the actin cytoskeleton and early membrane blebbing in human endothelial cells.
Blood 99(6):2060-9

Griggs J, Skepper JN, Smith GA, Brindle KM, Metcalfe JC, Hesketh R. March 2002
Inhibition of proliferative retinopathy by the anti-vascular agent Combretastatin A-4.
American Journal of Pathology 160(3):1097-103

Li Ly, Rojiani A, Siemann DW. 2002
Preclinical evaluations of therapies combining the vascular targeting agent CA4DP and conventional cancer therapies in the treatment of Kaposi's sarcoma.
Acta Oncologica 41(1):91-7

Rojiani A, Li Ly, Rise L, Siemann DW. 2002
Activity of the vascular targeting agent CA4DP in a xenograft model of AIDS-associated Kaposi's sarcoma.
Acta Oncologica 41(1):98-105

Eikesdal HP, Bjerkvig R, Raleigh JA, Mello O, Dahl O. December 2001
Tumor vasculature is targeted by the combination of CA4P and hyperthermia.
Radiotherapy and Oncology 61(3):313-20

Griggs J, Brindle KM, Metcalfe JC, Hill SA, Smith GA, Beauregard DA, Hesketh R. October 2001
Potent anti-metastatic activity of Combretastatin-A4.
International Journal of Oncology 19(4):821-5

Beauregard DA, Hill SA, Chaplin DJ, Brindle KM. September 15, 2001
The susceptibility of tumor to the antivascular drug CA4P correlates with vascular permeability.
Cancer Research 61(18):6811-15

Murata R, Horsman MR, Overgaard J, Siemann DW. August 2001
Interaction between combretastatin A-4 disodium phosphate and radiation in murine tumors.
Radiotherapy and Oncology 60:155-161

Pedley BR. June 15, 2001
Eradication of colorectal xenografts by combined radioimmunotherapy and Combretastatin A-4 3-O-phosphate.
Cancer Research 6:4716-22

Malcontenti-Wilson C, Muralidharan V, Skinner S, Christophi C, Sherris D, O'Brien PE. April 2001
Combretastatin A4 prodrug study of the effect on the growth and microvasculature of colorectal liver metastases in a murine model.
Clinical Cancer Research 7(4):1052-60

Griggs J, Brindle KM, Metcalfe JC, Hill SA, Smith GA, Beauregard DA, Hesketh R. March 23, 2001
CA4 disrupts neovascular development in anon-neoplastic tissue.
British Journal of Cancer 84(6):832-5

Nabha SM, Mohammad RM, Wall NR, Dutcher JA, Salkini BM, Pettit GR, Al-Katib AM. January 2001
Evaluation of CA4P in a non-Hodgkin's lymphoma xenograft model: preclinical efficacy.
Anticancer Drugs 12(1):57-63

Eikesdal HP, Bjerkvig R, Dahl O, Mella O. 2001
Combretastatin A-4 and hyperthermia; a potent combination for the treatment of solid tumors.
Radiotherapy and Oncology 60:147-154

Landuyt W, De Beeck MO, Van Oosterom A, Ahmed B, Anne J, Lambin P. 2001
In vivo antitumor effect of vascular targeting combined with either ionizing radiation or anti-angiogenesis treatment.
International Journal of Radiation Oncology Biology and Physics 49:443-450

Galbraith SM, Chaplin DJ, Lee F. 2001
Effects of combretastatin A4 phosphate on endothelial cell morphology in vitro and relationship to tumour vascular targeting activity in vivo.
Anticancer Research 21:93-102

Murata R, Horsman MR, Overgaard J. 2001
Comparative effects of combretastatin A-4 disodium phophate and 5, 6-dimethylxanthenone-4-acetic acid on blood perfusion in a murine tumour and normal tissues.
International Journal of Radiation Biology Biology Physics 77:195-204

Murata R, Horsman MR, Overgaard J. 2001
Combretastatin A-4 disodium phosphate: A vascular targeting agent that improves the anti-tumor effects of hyperthermia, radiation, and mild thermoradiotherapy.
International Journal of Radiation Oncology 51:1018-1024

Nelkin BD, Ball DW. 2001
Combretastatin A-4 and doxorubicin combination treatment is effective in a preclinical model of human medullary thyroid carcinoma.
Oncology Reports 8:157-160

Grosios K, Loadman PM, Swaine DJ. 2000
Combination chemotherapy with combretastatin A-4 phophate and 5-flourouracil in an experimental murine colon adenocarcinama.
Anticancer Research 20:229-234

Landuyt W, Van Oosterom A, Anne J, Darius DO, Drijkoningen M, Fowler JF. 2000
Vascular targeting of solid tumours; A major 'inverse' volume-response relationship following combretastatin A-4 phosphate treatment of rat rhabdomyosarcomas.
European Journal of Cancer 36:1833-1843.

Boehle AS, Henne-Bruns D, Kalthoff H, Leuschner I. 2000
Combretastatin A-4 Prodrug: A potent inhibitor of malignant hemangioendothelioma cell proliferation.
International Journal of Cancer 87:838-843

Chaplin DJ, Pettit GR, Hill SA. 1999
Anti-vascular approaches to solid tumor therapy: Evaluation of combretastatin A4 phosphate.
Anticancer Research 19:189-196

Grosios K, Holwell Se, McGown AT. 1999
In vivo and in vitro evaluation of combretastatin A-4 and its sodium phosphate Prodrug.
British Journal of Cancer 81(8):1318-1327

Tozer GM, Prise VE, Wilson J, Locke RJ, Vojnovic B, Stratford MRL, Dennis MF Chaplin DJ. 1999
Combretastatin A-4 Phosphate as a Tumor Vascular-Targeting Agent: Early Effects in Tumors and Normal Tissues.
Cancer Research. 59:1625-1634.

Li Ly, Rojoano A, Siemann DW. 1998
Targeting the tumor vasculature with Combretastatin A-4 disodium phosphate: Effects on radiation therapy.
International Journal of Radiation Oncology 42:899-903

Pettit GR, Rhodes MR. 1998
Antineoplastic agents 389. New syntheses of the Combretastatin A-4 Prodrug.
Anticancer Drug Design 13:183-91

Beauregard DA, Thelwall PE, Chaplin DJ, Hill SA, Adams GE, Brindle KM. 1998
Magnetic resonance imaging and spectroscopy of Combretastatin A4 Prodrug-induced disruption of tumour perfusion and energetic status. 
British Journal of Cancer 77:1761-7

Horsman MR, Ehrnrooth E, Ladekarl M, Overgaard J. 1998
The effect of Combretastatin A-4 disodium phosphate in a C3H mouse mammary carcinoma and a variety of murine spontaneous tumours.
International Journal of Radiation Oncology 42:895-8

Iyer S, Chaplin DJ, Rosenthal DS, Hamid Boulares A, Li LY, Smulson ME. 1998
Induction of apoptosis in proliferating human endothelial cells by tumor-specific antiangiogenesis agent Combretastatin A-4.
Cancer Research 58:4510-14

Maxwell RJ, Nielsen FU, Breidahl T, Stedkilde-Jergensen H, Horsman MR. 1998
Effects of combretastatin on murine tumours monitored by 31P MRS, 1H MRS and 1H MRI.
International Journal of Radiation Oncology Biology and Physic 42:891-894

Dark GG, Hill SA, Prise VE, Tozer GM, Pettit GR, Chaplin DJ. 1997
Combretastatin A-4, an agent that displays potent and selective toxicity toward tumor vasculature.
Cancer Research 57:1829-34

O'Brien C. 1997
Combretastatin A-4 vascular damage to tumours [news].
Molecular Medicine Today 3:36

Chaplin DJ, Pettit GR, Parkins CS, Hill SA. 1996
Antivascular approaches to solid tumour therapy: evaluation of tubulin binding agents.
British Journal of Cancer 74:S86-8

Dorr T, Dvorakova K, Snead K, Alberts DS, Salmon SE, Pettit GR. 1996
Antitumor activity of combretastatin-A4 phosphate, a natural product tubulin inhibitor.
Investigational New Drugs 14:131-7

Hill SA, Sampson LE, Chaplin DJ. 1995
Anti-vascular approaches to solid tumour therapy: evaluation of vinblastine and flavone acetic acid.
International Journal of Cancer 63:119-23

Pettit GR, Singh SB, Boyd MR, Hamel E, Pettit RK, Schmidt JM, Hogan F. 1995
Antineoplastic agents. 291. Isolation and synthesis of Combretastatins A-4, A-5, and A-6.
Journal of Medicinal Chemistry 38:1666-72

Pettit GR, Singh SB, Boyd MR, Hamel E, Pettit RK, Schmidt JM, Hogan F. 1995
Antineoplastic agents. 291. Isolation and synthesis of Combretastatins A-4, A-5, and A-6(1a). [published erratum appears in Journal of Medicinal Chemistry 38:2994]
Journal of Medicinal Chemistry 38:1666-72

Pettit GR, Temple C Jr, Narayanan VL, Varma R, Simpson MJ, Boyd MR, Rener GA, Bansal N. 1995
Antineoplastic agents 322. synthesis of Combretastatin A-4 prod rugs.
Anticancer Drug Design 10:299-309

El-Zayat AA, Degen D, Drabek S, Clark GM, Pettit GR, Von Hoff DD. 1993
In vitro evaluation of the Antineoplastic activity of combretastatin A-4, a natural product from Combretum caffrum (arid shrub).
Anticancer Drugs 4:19-25

OXi4503:

Holwell SE, Cooper PA, Thompson MJ, Pettit GR, Lippert JW, Martin SW, Bibby MC. Nov-Dec 2002
Anti-tumor and anti-vascular effects of the novel tubulin-binding agent Combretastatin A-1 phosphate.
Anticancer Research. 22(6C):3933-40.

Hill SA, Tozer GM, Pettit GR, Chaplin DJ. May-June 2002
Preclinical evaluation of the antitumor activity of the novel vascular targeting agent OXi4503.
Anticancer Research 22(3):1453-8

Holwell SE, Cooper PA, Grosios K, Lippert JW, Pettit GR. March-April 2002
Combretastatin A-1 phosphate: A novel tubulin-binding agent with in vivo anti-vascular effects in experimental tumors.
Anticancer Research 22(2A):707-11

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