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项与 Peplin Ltd. 相关的药物

Ingenol Mebutate

巨大戟醇甲基丁烯酸酯

靶点

PKCα x PKCδ

作用机制

PKCα刺激剂 [+1]

在研机构

原研机构

在研适应症

非在研适应症

最高研发阶段批准上市

首次获批国家/地区

美国

首次获批日期2012-01-23

PEP-001

靶点-

作用机制-

在研机构-

原研机构

Peplin Ltd.

在研适应症-

非在研适应症

光化性角化病 [+1]

最高研发阶段终止

首次获批国家/地区-

首次获批日期-

100 项与 Peplin Ltd. 相关的临床结果

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0 项与 Peplin Ltd. 相关的专利（医药）

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项与 Peplin Ltd. 相关的文献（医药）

2013-01-01·Archives of Dermatological Research3区 · 医学

Effective treatment of squamous cell carcinomas with ingenol mebutate gel in immunologically intact SKH1 mice

3区 · 医学

Article

作者: Cozzi, Sarah-Jane ; Le, Thuy T ; Ogbourne, Steven M ; James, Cini ; Suhrbier, Andreas

Ingenol mebutate has recently been approved by the Federal Drug Administration (USA) as a topical treatment for actinic keratoses. Herein, we describe the efficacy of ingenol mebutate for the topical treatment of squamous cell carcinoma (SCC) using a wild-type mouse model (SKH1) and the UV-induced mouse SCC cell line, T7. Daily treatment for 2 days with 0.25 % ingenol mebutate gel produced a cure rate of 70 %, with 0 % for placebo gel. Electron microscopy revealed swelling of cancer cell mitochondria within 1 h, with disruption of the inner mitochondrial membranes evident at 6 h post treatment. Primary necrosis of cancer cells was clearly evident by 24 h. Treatment was associated with local haemorrhage and a prodigious neutrophil infiltrate, with anti-T7 antibodies also detected. This is the first report of the successful treatment of SCC tumours with ingenol mebutate gel in wild-type mice, and supports the view that ingenol mebutate induces primary necrosis and activates the immune system.

2007-03-01·Anti-Cancer Drugs4区 · 医学

Proceedings of the First International Conference on PEP005

4区 · 医学

作者: Hampson, Peter ; Lord, Janet M. ; De Witte, Peter A. ; Ogbourne, Steven M. ; Parsons, Peter ; Suhrbier, Andreas

The sap of Euphorbia peplus, commonly know as 'petty spurge', 'radium weed' or 'milkweed' has been used for centuries as a traditional treatment for skin conditions, including warts, corns and cancers of the skin. Documentation of its use by medical professionals to treat basal cell carcinoma (BCC) dates from the early 19 century. Individuals who participated in a 1988 survey of home treatments for cancer indicated the sap of E. peplus was an effective cure for actinic lesions leading the investigators to suggest that this potential utility should be further explored in controlled clinical trials. The fractionation of the sap E. peplus using solvents of varying polarity yielded several macrocyclic diterpenes, many of which were found to have cytotoxic activity or the ability to influence cellular differentiation. Ultimately, ingenol 3-angelate (I3A) of PEP005, emerged as a promising potential new anti-cancer treatment. Here we report the proceedings from the First International Conference on PEP005, covering the exciting potential of PEP005 as the therapeutic agent for the treatment of skin cancer, leukemia and bladder cancer.

2004-04-15·Cancer Research1区 · 医学

Antitumor Activity of 3-Ingenyl Angelate

1区 · 医学

Article

作者: Suhrbier, Andreas ; Ogbourne, Steven M. ; Johns, Jenny ; Parsons, Peter G. ; Cozzi, Sarah-Jane ; McAlpine, Devi ; Gardner, Joy M. ; Lenarczyk, Aleksandra ; Boyle, Glen M. ; Aylward, James H. ; Le, Thuy T. T. ; Jones, Brad ; Scott, Tania M. ; Sutherland, Kirsty P. ; Morris, Melanie

AbstractOptions for skin cancer treatment currently include surgery, radiotherapy, topical chemotherapy, cryosurgery, curettage, and electrodessication. Although effective, surgery is costly and unsuitable for certain patients. Radiotherapy can leave a poor cosmetic effect, and current chemotherapy is limited by low cure rates and extended treatment schedules. Here, we describe the preclinical activity of a novel topical chemotherapeutic agent for the treatment of skin cancer, 3-ingenyl angelate (PEP005), a hydrophobic diterpene ester isolated from the plant Euphorbia peplus. Three daily topical applications of 42 nmol (18 μg) of PEP005 cured a series of s.c. mouse tumors (B16 melanoma, LK2 UV-induced squamous cell carcinoma, and Lewis lung carcinoma; n = >14 tumors/group) and human tumors (DO4 melanoma, HeLa cervical carcinoma, and PC3 and DU145 prostate carcinoma; n = >4 tumors/group) previously established (5–10 mm3) on C57BL/6 or Foxn1nu mice. The treatment produced a mild, short-term erythema and eschar formation but, ultimately, resulted in excellent skin cosmesis. The LD90 for PEP005 for a panel of tumor cell lines was 180–220 μm. Electron microscopy showed that treatment with PEP005 both in vitro (230 μm) and in vivo (42 nmol) rapidly caused swelling of mitochondria and cell death by primary necrosis. 51Cr release, uptake of propidium iodide, and staining with the mitochondria dye JC1, revealed that PEP005 (230 μm) treatment of tumor cells in vitro resulted in a rapid plasma membrane perturbation and loss of mitochondrial membrane potential. PEP005 thus emerges as a new topical anti-skin cancer agent that has a novel mode of action involving plasma membrane and mitochondrial disruption and primary necrosis, ultimately resulting in an excellent cosmetic outcome.

100 项与 Peplin Ltd. 相关的药物交易

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100 项与 Peplin Ltd. 相关的转化医学

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