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509 dose escalation of therapeutic high capacity, gutless adenoviral vectors in the naã¯ve rat brain: pre clinical safety and toxicity evaluation as a prelude to a phase i clinical trial for glioma

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509 Dose Escalation of Therapeutic High Capacity, Gutless Adenoviral Vectors in the Naïve Rat Brain Pre Clinical Safety and Toxicity Evaluation as a Prelude to a Phase I Clinical Trial for Glioma Mol[.]

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Molecular Therapy Volume 19, Supplement 1, May 2011 Copyright © The American Society of Gene & Cell Therapy

S196

CANCER - IMMUNOTHERAPY II

Apoptosis was induced by upregulation of caspases 3, 8 and 9

Secondly, we compared the therapeutic effi cacy of anthocyanins

with a leukemia specifi c DNA vaccine to treat mice with minimal

residual disease (MRD) of syngeneic Ph+ ALL Non-viral minimalistic

immunogenically defi ned gene expression vectors (MIDGE) encoding

a BCR-ABL fusion specifi c peptide, GM-CSF and IL12 were used for

in vivo transfection of murine skin As TLR-9 agonist we used a

DNA-based double stem-loop immunomodulator (dSLIM), containing six

CpG-motifs Following a lethal leukemia challenge mice received

either daily oral applications of berry extract or intraperitoneal

applications of cyanidin from day 1 – 21 or were immunized with

the DNA vaccine on days 2 and 9 In addition, two groups received

a combination of the DNA vaccine and berry extract or cyanidin In

contrast to the anti-leukemia activity in vitro the anthocyanins were

not effi cient to treat mice with Ph+ ALL in vivo However, mice which

received the DNA vaccine showed a signifi cant longer tumor-free and

overall survival compared to the control and a survival rate of 56%

Intriguingly, the combined treatment with DNA vaccine and berry

extract but not with cyanidin further improved the outcome and lead

to a signifi cant longer tumor-free and overall survival compared to

the DNA vaccine alone and a survival rate of 90% In conclusion,

we provide data that a leukemia-specifi c DNA vaccine and berry

extract act synergistically in the treatment of mice with MRD This

approach may have implications to optimize maintenance therapy in

patients with Ph+ ALL

Cells during Activation

Vladimir Senyukov,1 Cecele J Denman,1 Laurence J N Cooper,1

Dean A Lee.1

1 Pediatrics, UT MD Anderson Cancer Center, Houston, TX.

Natural killer (NK) cells, as a key component of innate immunty,

have recently shown clinical potential for adoptive immunotherapy

against broad spectrum of oncological diseases One of the major

obstacles for adoptive NK cell immunotherapy is obtaining suffi cient

numbers of NK cells for effective therapy To address this hurdle, we

developed an artifi cial antigen presenting cells (aAPC) to expand

primary NK cells in vitro using K562 cells gene-modifi ed to express

membrane-bound cytokine, and showed that mIL21 promoted stronger

NK cells expansion than mIL15 To investigate this phenomenon we

compared NK cell proliferation kinetics (by SFCE dilution) in parallel

with daily assessment of apoptosis (by annexin V biding) in response

to mIL15 and mIL21 We fi nd that in the presence of mIL21 NK

cells proliferated much faster than in response to mIL15 (fi g.1a)

Moreover, in the presence of mIL15 as much as 90% of NK cells

(versus 15% in presence of mIL21) became able to bind annexin V

by the 3rd day after aAPC stimulation (fi g1b) Furthermore, we have

found that mIL21 up-regulated and supported CD160 expression by

NK cells during expansion time (42% in presence of mIL21 vs 6%

in response to mIL15 on day 3 and 83% vs 16% on day 7) CD160

is a GPI-anchored protein and its expression is down-modulated by

GPI-specifi c phospholipase D and synthesis of which, in turn, is

induced in NK cells in response to IL15 and IL2 It has been shown

that CD160 signaling mediates PI3K-dependent survival and growth

in CLL cells that was associated with up-regulation of Bcl-2, Bcl-xL,

and Mcl-1 In addition to the herpes virus entry mediator that is a

high affi nity ligand for CD160 it has been shown that classical and

nonclassical MHC class I molecules bind to CD160 with low affi nity

The K562 cell line used to generate the aAPC is characterized as

HLA-Cw3+/Cw5+,with low-level constitutive expression that can be

augmented by IFN-γ To verify if CD160 engagement with MHC class

I is important for NK cell survival in this system we applied w6/32

antibodies to block HLA-C recognition We stained fresh purifi ed NK

cells with CFSE and blocked Fc-receptors with human IgG to prevent

CD16 involvement in NK cell activation In parallel, irradiated

aAPC-mIL21 were incubated with w6/32 antibodies or with isotype-matched control antibodies and after washing cells were co-cultured with NK cells We found that blocking of HLA class I recognition did not affect NK cell proliferation in response to aAPC-mIL21 (fi g.2a) but increased apoptosis (fi g.2b) This data suggests that IL21might prevent activation-induced NK cell death through up-regulation of anti-apoptotic factors through a CD160–mediated mechanism Future experiments will focus on identifying the mechanisms of suppressing apoptosis in this system

High-Capacity, Gutless Adenoviral Vectors in the Nạve Rat Brain: Pre-Clinical Safety and Toxicity Evaluation as a Prelude to a Phase I Clinical Trial for Glioma

A K M G Muhammad,1 Mariana Puntel,1 Weidong Xiong,1

Kyle Kelson,1 Alireza Salem,1 Kurt M Kroeger,1 Chunyan Liu,1

Catherine Farrokhi,1 Liliana Lacayo,1 Robert N Pechnick,1 Donna Palmer,2 Philip Ng,2 Pedro R Lowenstein,1 Maria G Castro.1

1 Cedars-Sinai Medical Center/UCLA, Los Angeles, CA; 2 Baylor College of Medicine, Houston, TX.

Glioblastoma multiforme (GBM) carries a dismal prognosis with

a median survival of 18-21 months post-diagnosis We have recently demonstrated the therapeutic effi cacy and high safety profi le of intratumoral delivery of a novel, combined gene therapy consisting

of fi rst generation, or high-capacity adenoviral vectors (HC-Ads) encoding either the conditionally cytotoxic gene herpes simplex type 1-thymidine kinase (TK) or the immunostimulatory gene fms-like tyrosine kinase 3 ligand (Flt3L) transgenes in a syngeneic, orthotopic rat model of GBM In anticipation of an upcoming dose

fi nding, Phase I clinical trial for primary GBM, we herein performed

a thorough assessment of the safety and toxicity of HC-Ads encoding

TK and Flt3L upon administration into the nạve rat brain Lewis rats were injected intracranially with escalating doses of HC-Ad-TK and HC-Ad-TetON-Flt3L (1x10^8, 1x10^9, or 1x10^10 vp of each) followed by systemic administration of gancyclovir and doxycycline Rats were evaluated at 5 days, 1 month, 6 months and 12 months for biodistribution of HC-Ad vector genomes, HC-Ad vector induced behavioral defi ciencies, neurotoxicity, peripheral blood cell counts and serum biochemistry, circulating levels of Flt3L, anti-adenovirus neutralizing antibodies, and anti-TK antibodies Even at the highest dose tested, real-time quantitative PCR did not detect evidence

of biodistribution of HC-Ad genomes to peripheral organs and a comprehensive panel of behavioral testing did not reveal any vector mediated abnormalities Peripheral blood cell counts and serum biochemistry were within normal ranges during all time points,

at all doses tested Flt3L expression was tightly regulated, with

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Molecular Therapy Volume 19, Supplement 1, May 2011

CANCER - IMMUNOTHERAPY II

expression dynamics that coincided with the administration of the

inducer doxycycline However, a comprehensive neuropathological

panel revealed evidence of neurotoxicity at the highest dose tested

(1x10^10 vp of each), i.e loss of brain tissue, and high levels of

infl ammation We did not detect any evidence of neurotoxicity or

long-term infl ammation at either lower dose tested Taken together,

these data indicate that 1x10^9 vp of each HC-Ad is the maximally

tolerated dose (MTD) that can be safely administered into the brains

of nạve Lewis rats These well controlled, non-clinical safety and

toxicity studies are required by the FDA in order to fi le of an IND

and constitute a major milestone in the path towards implementation

of the fi rst ever Phase I clinical trial for GBM using gutless, HC-Ad

vectors

Therapy Mediated Brain Tumor Regression

Hikmat H Assi,1,2 James Curtin,1 Chunyan Liu,1 Maria G Castro,1,2

Pedro R Lowenstein.1,2

1 Gene Therapy Research Institute, Cedars Sinai Medical Center,

Los Angeles, CA; 2 Molecular and Medical Pharmacology, UCLA,

Los Angeles, CA.

STAT3 signaling is constitutively active in high-grade tumors and

its transcriptional activity is required by malignant cells for their

proliferation well as promotion of an immunosuppressive tumor

microenvironment Recently pre-clinical models have investigated

whether STAT3 antagonists can be used in combination with the

immunotherapy to induce tumor cell death and enhance immune

responses against GBM antigens Owing to the multiple roles

of STAT3 in both tumor cells and immune cells, we wished to

investigate whether STAT3 signaling is involved in Ad-TK/Ad-Flt3L

gene therapy-mediated T cell dependent brain tumor regression We

used adenovirus expressing STAT3 shRNA as well small molecule

inhibitors to silence STAT3 and assessed its role in tumor cell

proliferation as well as dendritic cell (DC) activity We report that

expression of STAT3 is up regulated in various syngeneic glioma

mouse models Treating Gl26 or SMA560 glioma cells with the novel

small molecule inhibitor CPA-7 blocks STAT3 in vitro and leads to

cell death through a loss of Cyclin D, Bcl-xl and survivin expression

We also show that STAT3 mediates the activation and maturation of

DCs Using bone marrow cells with GM-CSF we generated immature

mouse DCs and examined the effects on DC maturation elicited by

the TLR ligand CpG and the STAT3 inhibitor CPA7 Treatment of

DCs with CPA-7 induced their maturation evidenced by increased

expression of co-stimulatory molecules CD80, CD86 and CD40

as well as decreased antigen uptake indicative of a more mature

phenotype CPA-7 treatment enhanced the maturation activity of

CpG DCs treated with CPA7 in combination with CpG were able

to better stimulate the proliferation of T cells in an allogeneic MLR

when compared to DCs treated with CpG alone We have previously

demonstrated that intra-tumoral delivery of Flt3L and TK using

adenoviral vectors drives T cell dependent tumor regression in

intra-cranial syngeneic glioma (GBM) models in rodents (Ali et al, 2005;

Curtin et al 2009; Candolfi et al, 2009) Intra-tumoral delivery of

STAT3 shRNA, however, completely blocks Flt3L and TK mediated

tumor regression compared with a scrambled non-specifi c shRNA

This was confi rmed using the small molecule inhibitor CPA-7 Our

data suggest that STAT3 signaling is involved in tumor cells’ survival

and DCs’ functions, thus constituting an attractive therapeutic target

for brain cancer

Improved Responses in Immunogene Cancer Treatment over Standard Plasmid Vectors

Patrick F Forde,1 Lindsay J Hall,1 Marcel de Kruijf,1 Gerald C O’Sullivan,1 Declan M Soden.1

1 Cork Cancer Research Centre, University College Cork, Cork, Ireland.

We compared the effi cacy of an enhanced expression vector (EEV) with CMV standard plasmid vector for non viral immunogenetherapy

of solid tumours The EEV contains its own RNA replicase and transcribes mRNA cytoplasmically The transgenes LacZ and GM-CSF/B71 were under the control of the CMV promoter Comparison of the EEV with the standard vector in normal and growing tumours used quantitative RT-PCR, histological tools and in vivo murine tumour growth and survival curves In all normal tissues (liver, spleen, and colon and oesophageal epithelium) there were signifi cant increased RNA/DNA ratios for the EEV over the standard plasmid The EEV gives superior results than standard vector in non viral immunogene therapy of solid growing tumours The EEV was curative in two tumour models and has potential for clinical development Antitumor responses of the EEV vector were both from immune cell recruitment

to the tumour environment and the unrestrained RNA production in the cytoplasm

the Effi cacy of DNA Cancer Vaccine by Activating Dendritic Cells

Chi-Chen Lin,1 Chia-Chiao Shih,1 Ching-Liang Chu.2

1 Institute of Biomedical Sciences, National Chung Hsin University, Taichung, Taiwan; 2 Yeastern Biotechnology Inc, Taipei, Taiwan.

DNA vaccine has been applied in cancer therapy, but the effi cacy remains to be improved The immunostimulatory effect of a fungal immunomodulatory protein Ling Zhi-8 (LZ-8) isolated from

Ganoderma lucidum has been reported on human dendritic cells

(DCs) In this study, we tested the adjuvanticity of LZ-8 for HER-2/ neu DNA vaccine against p185neu expressing tumor MBT-2 in mice

We found that recombinant LZ-8 activated mouse bone marrow-derived DCs via TLR4 and this stimulation was not due to any microbe contaminant In addition, LZ-8 enhanced the ability of DCs to induce

antigen-specifi c T cell activation in vitro and in a subunit vaccine model in vivo Surprisingly, LZ-8 co-treatment strongly improved

the therapeutic effect of DNA vaccine against MBT-2 tumor in mice This increase of anti-tumor activity was attributed to the enhancement

of vaccine-induced Th1 and CTL responses Consistent with the results from DCs, the promoting effect of LZ-8 on DNA vaccine was diminished when the MBT-2 tumor cells were grown in TLR4 mutant mice Thus, we concluded that LZ-8 may be a promising adjuvant to enhance the effi cacy of DNA vaccine by activating DCs

Bi-Specifi c Tumor-Reactive T Cells

Robert C Chan,1 Ceidy Sanchez,1 Anna Worth,1 Ann M Leen,1

Malcolm K Brenner,1 Ganesh Palapattu,2 Juan F Vera.1

1 Baylor College of Medicine, Texas Children’s Hospital, The Methodist Hospital, Houston; 2 Department of Urology, The Methodist Hospital, Houston.

Although localized prostate cancer (PC) can often be cured by surgery and/or radiation therapy, the therapeutic options for castrate-resistant disease (CRPC) are largely palliative, underscoring the need for alternative therapies Like many other tumors, CRPC expresses tumor-associated antigens (TAAs), which are potential targets for immune destruction However, tumors use multiple mechanisms

of immune evasion including downregulation of target antigen

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